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DiscoverX corporation pathhunter™ β-arrestin recruitment assay
Pathhunter™ β Arrestin Recruitment Assay, supplied by DiscoverX corporation, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/%CE%B2-arrestin+recruitment+assay/pathhunter+%CE%B2+arrestin+assay/pm40460721-62-10-14
Average 90 stars, based on 1 article reviews
pathhunter™ β-arrestin recruitment assay - by Bioz Stars, 2026-09
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Functional Assay:

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP (Table 2) and the DiscoverX β-arrestin recruitment assay (Table 3), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D2R, D3R, or D4R.

Article Title: Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D 2 Dopamine Receptor
Article Snippet: GPCR Profiling To determine the GPCR selectivity profiles of ONC201 and haloperidol, these compounds were screened using the DiscoverX gpcrMAX GPCR panel, which measures the GPCR activation of β -arrestin recruitment to different GPCRs (see DiscoverX β -arrestin recruitment assay methods above).


Article Title: Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist
Article Snippet: These results confirm those obtained using the DiscoverX β-arrestin recruitment assay , although 20 exhibited ~30-fold greater potency using the BRET-based assay.

Article Title: Identification and Characterization of ML321: A Novel and Highly Selective D 2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity.
Article Snippet: For the DiscoverX β-arrestin recruitment assay, the LANCE cAMP assay, and the BRET curve-shift assays, the data were fit using non-linear regression analysis.

Article Title: Dopamine D 1 Agonists: First Potential Treatment for Late-Stage Parkinson's Disease.
Article Snippet: Studies performed in D1-transfected CHO cells using the GloSensor cAMP assay. β-arrestin recruitment assay performed using the DiscoverX Pathfinder kit.

Article Title: Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
Article Snippet: Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism.. Here, we designed twenty new analogs to investigate the structure–activity relationship effects for all three functional groups attached to the triazole core.. We identified specific groups that are critical for KOR potency and further extended the range of moieties explored.

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP ( Table ) and the DiscoverX β-arrestin recruitment assay ( Table ), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D R, D R, or D 4 R. In agonist mode, E max values for each compound are in comparison to dopamine and EC 50 values represent agonist potency.

Stable Transfection:

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP (Table 2) and the DiscoverX β-arrestin recruitment assay (Table 3), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D2R, D3R, or D4R.

Article Title: Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D 2 Dopamine Receptor
Article Snippet: GPCR Profiling To determine the GPCR selectivity profiles of ONC201 and haloperidol, these compounds were screened using the DiscoverX gpcrMAX GPCR panel, which measures the GPCR activation of β -arrestin recruitment to different GPCRs (see DiscoverX β -arrestin recruitment assay methods above).


Article Title: Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist
Article Snippet: These results confirm those obtained using the DiscoverX β-arrestin recruitment assay , although 20 exhibited ~30-fold greater potency using the BRET-based assay.

Article Title: Identification and Characterization of ML321: A Novel and Highly Selective D 2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity.
Article Snippet: For the DiscoverX β-arrestin recruitment assay, the LANCE cAMP assay, and the BRET curve-shift assays, the data were fit using non-linear regression analysis.

Article Title: Dopamine D 1 Agonists: First Potential Treatment for Late-Stage Parkinson's Disease.
Article Snippet: Studies performed in D1-transfected CHO cells using the GloSensor cAMP assay. β-arrestin recruitment assay performed using the DiscoverX Pathfinder kit.

Article Title: Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
Article Snippet: Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism.. Here, we designed twenty new analogs to investigate the structure–activity relationship effects for all three functional groups attached to the triazole core.. We identified specific groups that are critical for KOR potency and further extended the range of moieties explored.

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP ( Table ) and the DiscoverX β-arrestin recruitment assay ( Table ), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D R, D R, or D 4 R. In agonist mode, E max values for each compound are in comparison to dopamine and EC 50 values represent agonist potency.

Expressing:

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP (Table 2) and the DiscoverX β-arrestin recruitment assay (Table 3), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D2R, D3R, or D4R.

Article Title: Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D 2 Dopamine Receptor
Article Snippet: GPCR Profiling To determine the GPCR selectivity profiles of ONC201 and haloperidol, these compounds were screened using the DiscoverX gpcrMAX GPCR panel, which measures the GPCR activation of β -arrestin recruitment to different GPCRs (see DiscoverX β -arrestin recruitment assay methods above).


Article Title: Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist
Article Snippet: These results confirm those obtained using the DiscoverX β-arrestin recruitment assay , although 20 exhibited ~30-fold greater potency using the BRET-based assay.

Article Title: Identification and Characterization of ML321: A Novel and Highly Selective D 2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity.
Article Snippet: For the DiscoverX β-arrestin recruitment assay, the LANCE cAMP assay, and the BRET curve-shift assays, the data were fit using non-linear regression analysis.

Article Title: Dopamine D 1 Agonists: First Potential Treatment for Late-Stage Parkinson's Disease.
Article Snippet: Studies performed in D1-transfected CHO cells using the GloSensor cAMP assay. β-arrestin recruitment assay performed using the DiscoverX Pathfinder kit.

Article Title: Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
Article Snippet: Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism.. Here, we designed twenty new analogs to investigate the structure–activity relationship effects for all three functional groups attached to the triazole core.. We identified specific groups that are critical for KOR potency and further extended the range of moieties explored.

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP ( Table ) and the DiscoverX β-arrestin recruitment assay ( Table ), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D R, D R, or D 4 R. In agonist mode, E max values for each compound are in comparison to dopamine and EC 50 values represent agonist potency.

Comparison:

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP (Table 2) and the DiscoverX β-arrestin recruitment assay (Table 3), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D2R, D3R, or D4R.

Article Title: Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D 2 Dopamine Receptor
Article Snippet: GPCR Profiling To determine the GPCR selectivity profiles of ONC201 and haloperidol, these compounds were screened using the DiscoverX gpcrMAX GPCR panel, which measures the GPCR activation of β -arrestin recruitment to different GPCRs (see DiscoverX β -arrestin recruitment assay methods above).


Article Title: Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist
Article Snippet: These results confirm those obtained using the DiscoverX β-arrestin recruitment assay , although 20 exhibited ~30-fold greater potency using the BRET-based assay.

Article Title: Identification and Characterization of ML321: A Novel and Highly Selective D 2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity.
Article Snippet: For the DiscoverX β-arrestin recruitment assay, the LANCE cAMP assay, and the BRET curve-shift assays, the data were fit using non-linear regression analysis.

Article Title: Dopamine D 1 Agonists: First Potential Treatment for Late-Stage Parkinson's Disease.
Article Snippet: Studies performed in D1-transfected CHO cells using the GloSensor cAMP assay. β-arrestin recruitment assay performed using the DiscoverX Pathfinder kit.

Article Title: Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
Article Snippet: Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism.. Here, we designed twenty new analogs to investigate the structure–activity relationship effects for all three functional groups attached to the triazole core.. We identified specific groups that are critical for KOR potency and further extended the range of moieties explored.

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP ( Table ) and the DiscoverX β-arrestin recruitment assay ( Table ), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D R, D R, or D 4 R. In agonist mode, E max values for each compound are in comparison to dopamine and EC 50 values represent agonist potency.

Activity Assay:

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP (Table 2) and the DiscoverX β-arrestin recruitment assay (Table 3), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D2R, D3R, or D4R.

Article Title: Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D 2 Dopamine Receptor
Article Snippet: GPCR Profiling To determine the GPCR selectivity profiles of ONC201 and haloperidol, these compounds were screened using the DiscoverX gpcrMAX GPCR panel, which measures the GPCR activation of β -arrestin recruitment to different GPCRs (see DiscoverX β -arrestin recruitment assay methods above).


Article Title: Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist
Article Snippet: These results confirm those obtained using the DiscoverX β-arrestin recruitment assay , although 20 exhibited ~30-fold greater potency using the BRET-based assay.

Article Title: Identification and Characterization of ML321: A Novel and Highly Selective D 2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity.
Article Snippet: For the DiscoverX β-arrestin recruitment assay, the LANCE cAMP assay, and the BRET curve-shift assays, the data were fit using non-linear regression analysis.

Article Title: Dopamine D 1 Agonists: First Potential Treatment for Late-Stage Parkinson's Disease.
Article Snippet: Studies performed in D1-transfected CHO cells using the GloSensor cAMP assay. β-arrestin recruitment assay performed using the DiscoverX Pathfinder kit.

Article Title: Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
Article Snippet: Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism.. Here, we designed twenty new analogs to investigate the structure–activity relationship effects for all three functional groups attached to the triazole core.. We identified specific groups that are critical for KOR potency and further extended the range of moieties explored.

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP ( Table ) and the DiscoverX β-arrestin recruitment assay ( Table ), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D R, D R, or D 4 R. In agonist mode, E max values for each compound are in comparison to dopamine and EC 50 values represent agonist potency.

Inhibition:

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP (Table 2) and the DiscoverX β-arrestin recruitment assay (Table 3), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D2R, D3R, or D4R.

Article Title: Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D 2 Dopamine Receptor
Article Snippet: GPCR Profiling To determine the GPCR selectivity profiles of ONC201 and haloperidol, these compounds were screened using the DiscoverX gpcrMAX GPCR panel, which measures the GPCR activation of β -arrestin recruitment to different GPCRs (see DiscoverX β -arrestin recruitment assay methods above).


Article Title: Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist
Article Snippet: These results confirm those obtained using the DiscoverX β-arrestin recruitment assay , although 20 exhibited ~30-fold greater potency using the BRET-based assay.

Article Title: Identification and Characterization of ML321: A Novel and Highly Selective D 2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity.
Article Snippet: For the DiscoverX β-arrestin recruitment assay, the LANCE cAMP assay, and the BRET curve-shift assays, the data were fit using non-linear regression analysis.

Article Title: Dopamine D 1 Agonists: First Potential Treatment for Late-Stage Parkinson's Disease.
Article Snippet: Studies performed in D1-transfected CHO cells using the GloSensor cAMP assay. β-arrestin recruitment assay performed using the DiscoverX Pathfinder kit.

Article Title: Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
Article Snippet: Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism.. Here, we designed twenty new analogs to investigate the structure–activity relationship effects for all three functional groups attached to the triazole core.. We identified specific groups that are critical for KOR potency and further extended the range of moieties explored.

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP ( Table ) and the DiscoverX β-arrestin recruitment assay ( Table ), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D R, D R, or D 4 R. In agonist mode, E max values for each compound are in comparison to dopamine and EC 50 values represent agonist potency.

Concentration Assay:

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP (Table 2) and the DiscoverX β-arrestin recruitment assay (Table 3), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D2R, D3R, or D4R.

Article Title: Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D 2 Dopamine Receptor
Article Snippet: GPCR Profiling To determine the GPCR selectivity profiles of ONC201 and haloperidol, these compounds were screened using the DiscoverX gpcrMAX GPCR panel, which measures the GPCR activation of β -arrestin recruitment to different GPCRs (see DiscoverX β -arrestin recruitment assay methods above).


Article Title: Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist
Article Snippet: These results confirm those obtained using the DiscoverX β-arrestin recruitment assay , although 20 exhibited ~30-fold greater potency using the BRET-based assay.

Article Title: Identification and Characterization of ML321: A Novel and Highly Selective D 2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity.
Article Snippet: For the DiscoverX β-arrestin recruitment assay, the LANCE cAMP assay, and the BRET curve-shift assays, the data were fit using non-linear regression analysis.

Article Title: Dopamine D 1 Agonists: First Potential Treatment for Late-Stage Parkinson's Disease.
Article Snippet: Studies performed in D1-transfected CHO cells using the GloSensor cAMP assay. β-arrestin recruitment assay performed using the DiscoverX Pathfinder kit.

Article Title: Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
Article Snippet: Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism.. Here, we designed twenty new analogs to investigate the structure–activity relationship effects for all three functional groups attached to the triazole core.. We identified specific groups that are critical for KOR potency and further extended the range of moieties explored.

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP ( Table ) and the DiscoverX β-arrestin recruitment assay ( Table ), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D R, D R, or D 4 R. In agonist mode, E max values for each compound are in comparison to dopamine and EC 50 values represent agonist potency.

cAMP Assay:

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP (Table 2) and the DiscoverX β-arrestin recruitment assay (Table 3), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D2R, D3R, or D4R.

Article Title: Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D 2 Dopamine Receptor
Article Snippet: GPCR Profiling To determine the GPCR selectivity profiles of ONC201 and haloperidol, these compounds were screened using the DiscoverX gpcrMAX GPCR panel, which measures the GPCR activation of β -arrestin recruitment to different GPCRs (see DiscoverX β -arrestin recruitment assay methods above).


Article Title: Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist
Article Snippet: These results confirm those obtained using the DiscoverX β-arrestin recruitment assay , although 20 exhibited ~30-fold greater potency using the BRET-based assay.

Article Title: Identification and Characterization of ML321: A Novel and Highly Selective D 2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity.
Article Snippet: For the DiscoverX β-arrestin recruitment assay, the LANCE cAMP assay, and the BRET curve-shift assays, the data were fit using non-linear regression analysis.

Article Title: Dopamine D 1 Agonists: First Potential Treatment for Late-Stage Parkinson's Disease.
Article Snippet: Studies performed in D1-transfected CHO cells using the GloSensor cAMP assay. β-arrestin recruitment assay performed using the DiscoverX Pathfinder kit.

Article Title: Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
Article Snippet: Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism.. Here, we designed twenty new analogs to investigate the structure–activity relationship effects for all three functional groups attached to the triazole core.. We identified specific groups that are critical for KOR potency and further extended the range of moieties explored.

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP ( Table ) and the DiscoverX β-arrestin recruitment assay ( Table ), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D R, D R, or D 4 R. In agonist mode, E max values for each compound are in comparison to dopamine and EC 50 values represent agonist potency.

Bioluminescence Resonance Energy Transfer:

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP (Table 2) and the DiscoverX β-arrestin recruitment assay (Table 3), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D2R, D3R, or D4R.

Article Title: Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D 2 Dopamine Receptor
Article Snippet: GPCR Profiling To determine the GPCR selectivity profiles of ONC201 and haloperidol, these compounds were screened using the DiscoverX gpcrMAX GPCR panel, which measures the GPCR activation of β -arrestin recruitment to different GPCRs (see DiscoverX β -arrestin recruitment assay methods above).


Article Title: Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist
Article Snippet: These results confirm those obtained using the DiscoverX β-arrestin recruitment assay , although 20 exhibited ~30-fold greater potency using the BRET-based assay.

Article Title: Identification and Characterization of ML321: A Novel and Highly Selective D 2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity.
Article Snippet: For the DiscoverX β-arrestin recruitment assay, the LANCE cAMP assay, and the BRET curve-shift assays, the data were fit using non-linear regression analysis.

Article Title: Dopamine D 1 Agonists: First Potential Treatment for Late-Stage Parkinson's Disease.
Article Snippet: Studies performed in D1-transfected CHO cells using the GloSensor cAMP assay. β-arrestin recruitment assay performed using the DiscoverX Pathfinder kit.

Article Title: Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
Article Snippet: Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism.. Here, we designed twenty new analogs to investigate the structure–activity relationship effects for all three functional groups attached to the triazole core.. We identified specific groups that are critical for KOR potency and further extended the range of moieties explored.

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP ( Table ) and the DiscoverX β-arrestin recruitment assay ( Table ), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D R, D R, or D 4 R. In agonist mode, E max values for each compound are in comparison to dopamine and EC 50 values represent agonist potency.

Activation Assay:

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP (Table 2) and the DiscoverX β-arrestin recruitment assay (Table 3), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D2R, D3R, or D4R.

Article Title: Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D 2 Dopamine Receptor
Article Snippet: GPCR Profiling To determine the GPCR selectivity profiles of ONC201 and haloperidol, these compounds were screened using the DiscoverX gpcrMAX GPCR panel, which measures the GPCR activation of β -arrestin recruitment to different GPCRs (see DiscoverX β -arrestin recruitment assay methods above).


Article Title: Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist
Article Snippet: These results confirm those obtained using the DiscoverX β-arrestin recruitment assay , although 20 exhibited ~30-fold greater potency using the BRET-based assay.

Article Title: Identification and Characterization of ML321: A Novel and Highly Selective D 2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity.
Article Snippet: For the DiscoverX β-arrestin recruitment assay, the LANCE cAMP assay, and the BRET curve-shift assays, the data were fit using non-linear regression analysis.

Article Title: Dopamine D 1 Agonists: First Potential Treatment for Late-Stage Parkinson's Disease.
Article Snippet: Studies performed in D1-transfected CHO cells using the GloSensor cAMP assay. β-arrestin recruitment assay performed using the DiscoverX Pathfinder kit.

Article Title: Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
Article Snippet: Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism.. Here, we designed twenty new analogs to investigate the structure–activity relationship effects for all three functional groups attached to the triazole core.. We identified specific groups that are critical for KOR potency and further extended the range of moieties explored.

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP ( Table ) and the DiscoverX β-arrestin recruitment assay ( Table ), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D R, D R, or D 4 R. In agonist mode, E max values for each compound are in comparison to dopamine and EC 50 values represent agonist potency.

Detection Assay:

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP (Table 2) and the DiscoverX β-arrestin recruitment assay (Table 3), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D2R, D3R, or D4R.

Article Title: Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D 2 Dopamine Receptor
Article Snippet: GPCR Profiling To determine the GPCR selectivity profiles of ONC201 and haloperidol, these compounds were screened using the DiscoverX gpcrMAX GPCR panel, which measures the GPCR activation of β -arrestin recruitment to different GPCRs (see DiscoverX β -arrestin recruitment assay methods above).


Article Title: Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist
Article Snippet: These results confirm those obtained using the DiscoverX β-arrestin recruitment assay , although 20 exhibited ~30-fold greater potency using the BRET-based assay.

Article Title: Identification and Characterization of ML321: A Novel and Highly Selective D 2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity.
Article Snippet: For the DiscoverX β-arrestin recruitment assay, the LANCE cAMP assay, and the BRET curve-shift assays, the data were fit using non-linear regression analysis.

Article Title: Dopamine D 1 Agonists: First Potential Treatment for Late-Stage Parkinson's Disease.
Article Snippet: Studies performed in D1-transfected CHO cells using the GloSensor cAMP assay. β-arrestin recruitment assay performed using the DiscoverX Pathfinder kit.

Article Title: Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
Article Snippet: Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism.. Here, we designed twenty new analogs to investigate the structure–activity relationship effects for all three functional groups attached to the triazole core.. We identified specific groups that are critical for KOR potency and further extended the range of moieties explored.

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP ( Table ) and the DiscoverX β-arrestin recruitment assay ( Table ), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D R, D R, or D 4 R. In agonist mode, E max values for each compound are in comparison to dopamine and EC 50 values represent agonist potency.

Binding Assay:

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP (Table 2) and the DiscoverX β-arrestin recruitment assay (Table 3), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D2R, D3R, or D4R.

Article Title: Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D 2 Dopamine Receptor
Article Snippet: GPCR Profiling To determine the GPCR selectivity profiles of ONC201 and haloperidol, these compounds were screened using the DiscoverX gpcrMAX GPCR panel, which measures the GPCR activation of β -arrestin recruitment to different GPCRs (see DiscoverX β -arrestin recruitment assay methods above).


Article Title: Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist
Article Snippet: These results confirm those obtained using the DiscoverX β-arrestin recruitment assay , although 20 exhibited ~30-fold greater potency using the BRET-based assay.

Article Title: Identification and Characterization of ML321: A Novel and Highly Selective D 2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity.
Article Snippet: For the DiscoverX β-arrestin recruitment assay, the LANCE cAMP assay, and the BRET curve-shift assays, the data were fit using non-linear regression analysis.

Article Title: Dopamine D 1 Agonists: First Potential Treatment for Late-Stage Parkinson's Disease.
Article Snippet: Studies performed in D1-transfected CHO cells using the GloSensor cAMP assay. β-arrestin recruitment assay performed using the DiscoverX Pathfinder kit.

Article Title: Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
Article Snippet: Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism.. Here, we designed twenty new analogs to investigate the structure–activity relationship effects for all three functional groups attached to the triazole core.. We identified specific groups that are critical for KOR potency and further extended the range of moieties explored.

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP ( Table ) and the DiscoverX β-arrestin recruitment assay ( Table ), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D R, D R, or D 4 R. In agonist mode, E max values for each compound are in comparison to dopamine and EC 50 values represent agonist potency.

Imaging:

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP (Table 2) and the DiscoverX β-arrestin recruitment assay (Table 3), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D2R, D3R, or D4R.

Article Title: Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D 2 Dopamine Receptor
Article Snippet: GPCR Profiling To determine the GPCR selectivity profiles of ONC201 and haloperidol, these compounds were screened using the DiscoverX gpcrMAX GPCR panel, which measures the GPCR activation of β -arrestin recruitment to different GPCRs (see DiscoverX β -arrestin recruitment assay methods above).


Article Title: Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist
Article Snippet: These results confirm those obtained using the DiscoverX β-arrestin recruitment assay , although 20 exhibited ~30-fold greater potency using the BRET-based assay.

Article Title: Identification and Characterization of ML321: A Novel and Highly Selective D 2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity.
Article Snippet: For the DiscoverX β-arrestin recruitment assay, the LANCE cAMP assay, and the BRET curve-shift assays, the data were fit using non-linear regression analysis.

Article Title: Dopamine D 1 Agonists: First Potential Treatment for Late-Stage Parkinson's Disease.
Article Snippet: Studies performed in D1-transfected CHO cells using the GloSensor cAMP assay. β-arrestin recruitment assay performed using the DiscoverX Pathfinder kit.

Article Title: Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
Article Snippet: Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism.. Here, we designed twenty new analogs to investigate the structure–activity relationship effects for all three functional groups attached to the triazole core.. We identified specific groups that are critical for KOR potency and further extended the range of moieties explored.

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP ( Table ) and the DiscoverX β-arrestin recruitment assay ( Table ), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D R, D R, or D 4 R. In agonist mode, E max values for each compound are in comparison to dopamine and EC 50 values represent agonist potency.

Labeling:

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP (Table 2) and the DiscoverX β-arrestin recruitment assay (Table 3), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D2R, D3R, or D4R.

Article Title: Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D 2 Dopamine Receptor
Article Snippet: GPCR Profiling To determine the GPCR selectivity profiles of ONC201 and haloperidol, these compounds were screened using the DiscoverX gpcrMAX GPCR panel, which measures the GPCR activation of β -arrestin recruitment to different GPCRs (see DiscoverX β -arrestin recruitment assay methods above).


Article Title: Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist
Article Snippet: These results confirm those obtained using the DiscoverX β-arrestin recruitment assay , although 20 exhibited ~30-fold greater potency using the BRET-based assay.

Article Title: Identification and Characterization of ML321: A Novel and Highly Selective D 2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity.
Article Snippet: For the DiscoverX β-arrestin recruitment assay, the LANCE cAMP assay, and the BRET curve-shift assays, the data were fit using non-linear regression analysis.

Article Title: Dopamine D 1 Agonists: First Potential Treatment for Late-Stage Parkinson's Disease.
Article Snippet: Studies performed in D1-transfected CHO cells using the GloSensor cAMP assay. β-arrestin recruitment assay performed using the DiscoverX Pathfinder kit.

Article Title: Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
Article Snippet: Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism.. Here, we designed twenty new analogs to investigate the structure–activity relationship effects for all three functional groups attached to the triazole core.. We identified specific groups that are critical for KOR potency and further extended the range of moieties explored.

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP ( Table ) and the DiscoverX β-arrestin recruitment assay ( Table ), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D R, D R, or D 4 R. In agonist mode, E max values for each compound are in comparison to dopamine and EC 50 values represent agonist potency.

GTPγS Binding Assay:

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP (Table 2) and the DiscoverX β-arrestin recruitment assay (Table 3), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D2R, D3R, or D4R.

Article Title: Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D 2 Dopamine Receptor
Article Snippet: GPCR Profiling To determine the GPCR selectivity profiles of ONC201 and haloperidol, these compounds were screened using the DiscoverX gpcrMAX GPCR panel, which measures the GPCR activation of β -arrestin recruitment to different GPCRs (see DiscoverX β -arrestin recruitment assay methods above).


Article Title: Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist
Article Snippet: These results confirm those obtained using the DiscoverX β-arrestin recruitment assay , although 20 exhibited ~30-fold greater potency using the BRET-based assay.

Article Title: Identification and Characterization of ML321: A Novel and Highly Selective D 2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity.
Article Snippet: For the DiscoverX β-arrestin recruitment assay, the LANCE cAMP assay, and the BRET curve-shift assays, the data were fit using non-linear regression analysis.

Article Title: Dopamine D 1 Agonists: First Potential Treatment for Late-Stage Parkinson's Disease.
Article Snippet: Studies performed in D1-transfected CHO cells using the GloSensor cAMP assay. β-arrestin recruitment assay performed using the DiscoverX Pathfinder kit.

Article Title: Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
Article Snippet: Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism.. Here, we designed twenty new analogs to investigate the structure–activity relationship effects for all three functional groups attached to the triazole core.. We identified specific groups that are critical for KOR potency and further extended the range of moieties explored.

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP ( Table ) and the DiscoverX β-arrestin recruitment assay ( Table ), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D R, D R, or D 4 R. In agonist mode, E max values for each compound are in comparison to dopamine and EC 50 values represent agonist potency.

Incubation:

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP (Table 2) and the DiscoverX β-arrestin recruitment assay (Table 3), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D2R, D3R, or D4R.

Article Title: Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D 2 Dopamine Receptor
Article Snippet: GPCR Profiling To determine the GPCR selectivity profiles of ONC201 and haloperidol, these compounds were screened using the DiscoverX gpcrMAX GPCR panel, which measures the GPCR activation of β -arrestin recruitment to different GPCRs (see DiscoverX β -arrestin recruitment assay methods above).


Article Title: Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist
Article Snippet: These results confirm those obtained using the DiscoverX β-arrestin recruitment assay , although 20 exhibited ~30-fold greater potency using the BRET-based assay.

Article Title: Identification and Characterization of ML321: A Novel and Highly Selective D 2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity.
Article Snippet: For the DiscoverX β-arrestin recruitment assay, the LANCE cAMP assay, and the BRET curve-shift assays, the data were fit using non-linear regression analysis.

Article Title: Dopamine D 1 Agonists: First Potential Treatment for Late-Stage Parkinson's Disease.
Article Snippet: Studies performed in D1-transfected CHO cells using the GloSensor cAMP assay. β-arrestin recruitment assay performed using the DiscoverX Pathfinder kit.

Article Title: Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
Article Snippet: Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism.. Here, we designed twenty new analogs to investigate the structure–activity relationship effects for all three functional groups attached to the triazole core.. We identified specific groups that are critical for KOR potency and further extended the range of moieties explored.

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP ( Table ) and the DiscoverX β-arrestin recruitment assay ( Table ), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D R, D R, or D 4 R. In agonist mode, E max values for each compound are in comparison to dopamine and EC 50 values represent agonist potency.

Amplified Luminescent Proximity Homogenous Assay:

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP (Table 2) and the DiscoverX β-arrestin recruitment assay (Table 3), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D2R, D3R, or D4R.

Article Title: Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D 2 Dopamine Receptor
Article Snippet: GPCR Profiling To determine the GPCR selectivity profiles of ONC201 and haloperidol, these compounds were screened using the DiscoverX gpcrMAX GPCR panel, which measures the GPCR activation of β -arrestin recruitment to different GPCRs (see DiscoverX β -arrestin recruitment assay methods above).


Article Title: Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist
Article Snippet: These results confirm those obtained using the DiscoverX β-arrestin recruitment assay , although 20 exhibited ~30-fold greater potency using the BRET-based assay.

Article Title: Identification and Characterization of ML321: A Novel and Highly Selective D 2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity.
Article Snippet: For the DiscoverX β-arrestin recruitment assay, the LANCE cAMP assay, and the BRET curve-shift assays, the data were fit using non-linear regression analysis.

Article Title: Dopamine D 1 Agonists: First Potential Treatment for Late-Stage Parkinson's Disease.
Article Snippet: Studies performed in D1-transfected CHO cells using the GloSensor cAMP assay. β-arrestin recruitment assay performed using the DiscoverX Pathfinder kit.

Article Title: Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
Article Snippet: Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism.. Here, we designed twenty new analogs to investigate the structure–activity relationship effects for all three functional groups attached to the triazole core.. We identified specific groups that are critical for KOR potency and further extended the range of moieties explored.

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP ( Table ) and the DiscoverX β-arrestin recruitment assay ( Table ), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D R, D R, or D 4 R. In agonist mode, E max values for each compound are in comparison to dopamine and EC 50 values represent agonist potency.

Transfection:

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP (Table 2) and the DiscoverX β-arrestin recruitment assay (Table 3), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D2R, D3R, or D4R.

Article Title: Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D 2 Dopamine Receptor
Article Snippet: GPCR Profiling To determine the GPCR selectivity profiles of ONC201 and haloperidol, these compounds were screened using the DiscoverX gpcrMAX GPCR panel, which measures the GPCR activation of β -arrestin recruitment to different GPCRs (see DiscoverX β -arrestin recruitment assay methods above).


Article Title: Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist
Article Snippet: These results confirm those obtained using the DiscoverX β-arrestin recruitment assay , although 20 exhibited ~30-fold greater potency using the BRET-based assay.

Article Title: Identification and Characterization of ML321: A Novel and Highly Selective D 2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity.
Article Snippet: For the DiscoverX β-arrestin recruitment assay, the LANCE cAMP assay, and the BRET curve-shift assays, the data were fit using non-linear regression analysis.

Article Title: Dopamine D 1 Agonists: First Potential Treatment for Late-Stage Parkinson's Disease.
Article Snippet: Studies performed in D1-transfected CHO cells using the GloSensor cAMP assay. β-arrestin recruitment assay performed using the DiscoverX Pathfinder kit.

Article Title: Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
Article Snippet: Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism.. Here, we designed twenty new analogs to investigate the structure–activity relationship effects for all three functional groups attached to the triazole core.. We identified specific groups that are critical for KOR potency and further extended the range of moieties explored.

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP ( Table ) and the DiscoverX β-arrestin recruitment assay ( Table ), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D R, D R, or D 4 R. In agonist mode, E max values for each compound are in comparison to dopamine and EC 50 values represent agonist potency.

Construct:

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP (Table 2) and the DiscoverX β-arrestin recruitment assay (Table 3), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D2R, D3R, or D4R.

Article Title: Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D 2 Dopamine Receptor
Article Snippet: GPCR Profiling To determine the GPCR selectivity profiles of ONC201 and haloperidol, these compounds were screened using the DiscoverX gpcrMAX GPCR panel, which measures the GPCR activation of β -arrestin recruitment to different GPCRs (see DiscoverX β -arrestin recruitment assay methods above).


Article Title: Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist
Article Snippet: These results confirm those obtained using the DiscoverX β-arrestin recruitment assay , although 20 exhibited ~30-fold greater potency using the BRET-based assay.

Article Title: Identification and Characterization of ML321: A Novel and Highly Selective D 2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity.
Article Snippet: For the DiscoverX β-arrestin recruitment assay, the LANCE cAMP assay, and the BRET curve-shift assays, the data were fit using non-linear regression analysis.

Article Title: Dopamine D 1 Agonists: First Potential Treatment for Late-Stage Parkinson's Disease.
Article Snippet: Studies performed in D1-transfected CHO cells using the GloSensor cAMP assay. β-arrestin recruitment assay performed using the DiscoverX Pathfinder kit.

Article Title: Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
Article Snippet: Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism.. Here, we designed twenty new analogs to investigate the structure–activity relationship effects for all three functional groups attached to the triazole core.. We identified specific groups that are critical for KOR potency and further extended the range of moieties explored.

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP ( Table ) and the DiscoverX β-arrestin recruitment assay ( Table ), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D R, D R, or D 4 R. In agonist mode, E max values for each compound are in comparison to dopamine and EC 50 values represent agonist potency.

Mutagenesis:

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP (Table 2) and the DiscoverX β-arrestin recruitment assay (Table 3), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D2R, D3R, or D4R.

Article Title: Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D 2 Dopamine Receptor
Article Snippet: GPCR Profiling To determine the GPCR selectivity profiles of ONC201 and haloperidol, these compounds were screened using the DiscoverX gpcrMAX GPCR panel, which measures the GPCR activation of β -arrestin recruitment to different GPCRs (see DiscoverX β -arrestin recruitment assay methods above).


Article Title: Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist
Article Snippet: These results confirm those obtained using the DiscoverX β-arrestin recruitment assay , although 20 exhibited ~30-fold greater potency using the BRET-based assay.

Article Title: Identification and Characterization of ML321: A Novel and Highly Selective D 2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity.
Article Snippet: For the DiscoverX β-arrestin recruitment assay, the LANCE cAMP assay, and the BRET curve-shift assays, the data were fit using non-linear regression analysis.

Article Title: Dopamine D 1 Agonists: First Potential Treatment for Late-Stage Parkinson's Disease.
Article Snippet: Studies performed in D1-transfected CHO cells using the GloSensor cAMP assay. β-arrestin recruitment assay performed using the DiscoverX Pathfinder kit.

Article Title: Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
Article Snippet: Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism.. Here, we designed twenty new analogs to investigate the structure–activity relationship effects for all three functional groups attached to the triazole core.. We identified specific groups that are critical for KOR potency and further extended the range of moieties explored.

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP ( Table ) and the DiscoverX β-arrestin recruitment assay ( Table ), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D R, D R, or D 4 R. In agonist mode, E max values for each compound are in comparison to dopamine and EC 50 values represent agonist potency.

Two Tailed Test:

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP (Table 2) and the DiscoverX β-arrestin recruitment assay (Table 3), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D2R, D3R, or D4R.

Article Title: Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D 2 Dopamine Receptor
Article Snippet: GPCR Profiling To determine the GPCR selectivity profiles of ONC201 and haloperidol, these compounds were screened using the DiscoverX gpcrMAX GPCR panel, which measures the GPCR activation of β -arrestin recruitment to different GPCRs (see DiscoverX β -arrestin recruitment assay methods above).


Article Title: Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist
Article Snippet: These results confirm those obtained using the DiscoverX β-arrestin recruitment assay , although 20 exhibited ~30-fold greater potency using the BRET-based assay.

Article Title: Identification and Characterization of ML321: A Novel and Highly Selective D 2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity.
Article Snippet: For the DiscoverX β-arrestin recruitment assay, the LANCE cAMP assay, and the BRET curve-shift assays, the data were fit using non-linear regression analysis.

Article Title: Dopamine D 1 Agonists: First Potential Treatment for Late-Stage Parkinson's Disease.
Article Snippet: Studies performed in D1-transfected CHO cells using the GloSensor cAMP assay. β-arrestin recruitment assay performed using the DiscoverX Pathfinder kit.

Article Title: Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists
Article Snippet: Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism.. Here, we designed twenty new analogs to investigate the structure–activity relationship effects for all three functional groups attached to the triazole core.. We identified specific groups that are critical for KOR potency and further extended the range of moieties explored.

Article Title: Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder
Article Snippet: Functional analyses of each compound were completed using the LANCE assay for cAMP ( Table ) and the DiscoverX β-arrestin recruitment assay ( Table ), in both agonist and antagonist modes, using Chinese hamster ovary (CHO) cells stably expressing D R, D R, or D 4 R. In agonist mode, E max values for each compound are in comparison to dopamine and EC 50 values represent agonist potency.



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