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selective ep2 antagonist pf-04418948  (Pfizer Inc)

 
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    Pfizer Inc selective ep2 antagonist pf-04418948
    Selective Ep2 Antagonist Pf 04418948, supplied by Pfizer Inc, 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/selective+ep2+antagonist+pf-04418948/pm40192484-17-11-7?v=Pfizer+Inc
    Average 90 stars, based on 1 article reviews
    selective ep2 antagonist pf-04418948 - by Bioz Stars, 2026-07
    90/100 stars

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    Selleck Chemicals selective ep2 receptor antagonist
    ( A ) Compound 1: lead compound from [29] with moderate dual inhibition; Compound 2. lead compound from [30] with potent <t>EP2</t> inhibition; Compound 3. lead compound from [31] with potent dual EP2/EP4 inhibition. The OKN4395 series is derived from [31]. Most of the diversity in the series comes from the exploration of the right hand aryl system bearing the carboxylic acid. Compound 3 is an example of that series. ( B ) cAMP production after stimulation with PGE2 (EC80, 2nM) measured on HEK293 stable clones expressing human EP2 (hEP2). Values represent mean of n=10 technical replicates ± SEM. ( C ) cAMP production after stimulation with PGE2 (EC80, 6nM) measured on HEK293 stable clones expressing human EP4 (hEP4). Values represent mean of n=10 technical replicates ± SEM. ( D ) cAMP production after stimulation with PGD2 (EC80, 300pM) measured on CHO-K1 cells stable clone transfected for human DP1 (hDP1). Values represent mean of n=4 technical replicates ± SEM. ( E ) Visualization of OKN4395 antagonist activity at 1µM screened with gpcrMAX GPCR LeadHunter Panel (Eurofins) obtained with the plotrender spatial data mapper tool developed by gpcrdb. ( F ) Summary table of OKN4395 IC50 on human prostanoid receptors. ( G ) Plausible binding mode of a representative of OKN4395 series in DP1 (DP1: orange, ligand: green). Hydrogen bonds are yellow dashed lines.
    Selective Ep2 Receptor Antagonist, supplied by Selleck Chemicals, used in various techniques. Bioz Stars score: 92/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    selective ep2 antagonist pf-04418948  (Pfizer Inc)
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    Pfizer Inc selective ep2 antagonist pf-04418948
    ( A ) Compound 1: lead compound from [29] with moderate dual inhibition; Compound 2. lead compound from [30] with potent <t>EP2</t> inhibition; Compound 3. lead compound from [31] with potent dual EP2/EP4 inhibition. The OKN4395 series is derived from [31]. Most of the diversity in the series comes from the exploration of the right hand aryl system bearing the carboxylic acid. Compound 3 is an example of that series. ( B ) cAMP production after stimulation with PGE2 (EC80, 2nM) measured on HEK293 stable clones expressing human EP2 (hEP2). Values represent mean of n=10 technical replicates ± SEM. ( C ) cAMP production after stimulation with PGE2 (EC80, 6nM) measured on HEK293 stable clones expressing human EP4 (hEP4). Values represent mean of n=10 technical replicates ± SEM. ( D ) cAMP production after stimulation with PGD2 (EC80, 300pM) measured on CHO-K1 cells stable clone transfected for human DP1 (hDP1). Values represent mean of n=4 technical replicates ± SEM. ( E ) Visualization of OKN4395 antagonist activity at 1µM screened with gpcrMAX GPCR LeadHunter Panel (Eurofins) obtained with the plotrender spatial data mapper tool developed by gpcrdb. ( F ) Summary table of OKN4395 IC50 on human prostanoid receptors. ( G ) Plausible binding mode of a representative of OKN4395 series in DP1 (DP1: orange, ligand: green). Hydrogen bonds are yellow dashed lines.
    Selective Ep2 Antagonist Pf 04418948, supplied by Pfizer Inc, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    ep2-selective antagonists pf-04418948  (Pfizer Inc)
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    Pfizer Inc ep2-selective antagonists pf-04418948
    ( A ) Compound 1: lead compound from [29] with moderate dual inhibition; Compound 2. lead compound from [30] with potent <t>EP2</t> inhibition; Compound 3. lead compound from [31] with potent dual EP2/EP4 inhibition. The OKN4395 series is derived from [31]. Most of the diversity in the series comes from the exploration of the right hand aryl system bearing the carboxylic acid. Compound 3 is an example of that series. ( B ) cAMP production after stimulation with PGE2 (EC80, 2nM) measured on HEK293 stable clones expressing human EP2 (hEP2). Values represent mean of n=10 technical replicates ± SEM. ( C ) cAMP production after stimulation with PGE2 (EC80, 6nM) measured on HEK293 stable clones expressing human EP4 (hEP4). Values represent mean of n=10 technical replicates ± SEM. ( D ) cAMP production after stimulation with PGD2 (EC80, 300pM) measured on CHO-K1 cells stable clone transfected for human DP1 (hDP1). Values represent mean of n=4 technical replicates ± SEM. ( E ) Visualization of OKN4395 antagonist activity at 1µM screened with gpcrMAX GPCR LeadHunter Panel (Eurofins) obtained with the plotrender spatial data mapper tool developed by gpcrdb. ( F ) Summary table of OKN4395 IC50 on human prostanoid receptors. ( G ) Plausible binding mode of a representative of OKN4395 series in DP1 (DP1: orange, ligand: green). Hydrogen bonds are yellow dashed lines.
    Ep2 Selective Antagonists Pf 04418948, supplied by Pfizer Inc, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    selective antagonist of the ep2 receptor pf-04418948  (Tocris)
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    ( A ) Compound 1: lead compound from [29] with moderate dual inhibition; Compound 2. lead compound from [30] with potent <t>EP2</t> inhibition; Compound 3. lead compound from [31] with potent dual EP2/EP4 inhibition. The OKN4395 series is derived from [31]. Most of the diversity in the series comes from the exploration of the right hand aryl system bearing the carboxylic acid. Compound 3 is an example of that series. ( B ) cAMP production after stimulation with PGE2 (EC80, 2nM) measured on HEK293 stable clones expressing human EP2 (hEP2). Values represent mean of n=10 technical replicates ± SEM. ( C ) cAMP production after stimulation with PGE2 (EC80, 6nM) measured on HEK293 stable clones expressing human EP4 (hEP4). Values represent mean of n=10 technical replicates ± SEM. ( D ) cAMP production after stimulation with PGD2 (EC80, 300pM) measured on CHO-K1 cells stable clone transfected for human DP1 (hDP1). Values represent mean of n=4 technical replicates ± SEM. ( E ) Visualization of OKN4395 antagonist activity at 1µM screened with gpcrMAX GPCR LeadHunter Panel (Eurofins) obtained with the plotrender spatial data mapper tool developed by gpcrdb. ( F ) Summary table of OKN4395 IC50 on human prostanoid receptors. ( G ) Plausible binding mode of a representative of OKN4395 series in DP1 (DP1: orange, ligand: green). Hydrogen bonds are yellow dashed lines.
    Selective Antagonist Of The Ep2 Receptor Pf 04418948, supplied by Tocris, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    selective ep2 antagonists pf-04418948  (Pfizer Inc)
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    Pfizer Inc selective ep2 antagonists pf-04418948
    ( A ) Compound 1: lead compound from [29] with moderate dual inhibition; Compound 2. lead compound from [30] with potent <t>EP2</t> inhibition; Compound 3. lead compound from [31] with potent dual EP2/EP4 inhibition. The OKN4395 series is derived from [31]. Most of the diversity in the series comes from the exploration of the right hand aryl system bearing the carboxylic acid. Compound 3 is an example of that series. ( B ) cAMP production after stimulation with PGE2 (EC80, 2nM) measured on HEK293 stable clones expressing human EP2 (hEP2). Values represent mean of n=10 technical replicates ± SEM. ( C ) cAMP production after stimulation with PGE2 (EC80, 6nM) measured on HEK293 stable clones expressing human EP4 (hEP4). Values represent mean of n=10 technical replicates ± SEM. ( D ) cAMP production after stimulation with PGD2 (EC80, 300pM) measured on CHO-K1 cells stable clone transfected for human DP1 (hDP1). Values represent mean of n=4 technical replicates ± SEM. ( E ) Visualization of OKN4395 antagonist activity at 1µM screened with gpcrMAX GPCR LeadHunter Panel (Eurofins) obtained with the plotrender spatial data mapper tool developed by gpcrdb. ( F ) Summary table of OKN4395 IC50 on human prostanoid receptors. ( G ) Plausible binding mode of a representative of OKN4395 series in DP1 (DP1: orange, ligand: green). Hydrogen bonds are yellow dashed lines.
    Selective Ep2 Antagonists Pf 04418948, supplied by Pfizer Inc, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    Average 90 stars, based on 1 article reviews
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    selective ep2 antagonist pf-04418948  (Cayman Chemical)
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    Cayman Chemical selective ep2 antagonist pf-04418948
    ( A ) Compound 1: lead compound from [29] with moderate dual inhibition; Compound 2. lead compound from [30] with potent <t>EP2</t> inhibition; Compound 3. lead compound from [31] with potent dual EP2/EP4 inhibition. The OKN4395 series is derived from [31]. Most of the diversity in the series comes from the exploration of the right hand aryl system bearing the carboxylic acid. Compound 3 is an example of that series. ( B ) cAMP production after stimulation with PGE2 (EC80, 2nM) measured on HEK293 stable clones expressing human EP2 (hEP2). Values represent mean of n=10 technical replicates ± SEM. ( C ) cAMP production after stimulation with PGE2 (EC80, 6nM) measured on HEK293 stable clones expressing human EP4 (hEP4). Values represent mean of n=10 technical replicates ± SEM. ( D ) cAMP production after stimulation with PGD2 (EC80, 300pM) measured on CHO-K1 cells stable clone transfected for human DP1 (hDP1). Values represent mean of n=4 technical replicates ± SEM. ( E ) Visualization of OKN4395 antagonist activity at 1µM screened with gpcrMAX GPCR LeadHunter Panel (Eurofins) obtained with the plotrender spatial data mapper tool developed by gpcrdb. ( F ) Summary table of OKN4395 IC50 on human prostanoid receptors. ( G ) Plausible binding mode of a representative of OKN4395 series in DP1 (DP1: orange, ligand: green). Hydrogen bonds are yellow dashed lines.
    Selective Ep2 Antagonist Pf 04418948, supplied by Cayman Chemical, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    selective ep2 antagonist pf 04418948  (Toronto Research Chemicals)
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    Toronto Research Chemicals selective ep2 antagonist pf 04418948
    ( A ) Compound 1: lead compound from [29] with moderate dual inhibition; Compound 2. lead compound from [30] with potent <t>EP2</t> inhibition; Compound 3. lead compound from [31] with potent dual EP2/EP4 inhibition. The OKN4395 series is derived from [31]. Most of the diversity in the series comes from the exploration of the right hand aryl system bearing the carboxylic acid. Compound 3 is an example of that series. ( B ) cAMP production after stimulation with PGE2 (EC80, 2nM) measured on HEK293 stable clones expressing human EP2 (hEP2). Values represent mean of n=10 technical replicates ± SEM. ( C ) cAMP production after stimulation with PGE2 (EC80, 6nM) measured on HEK293 stable clones expressing human EP4 (hEP4). Values represent mean of n=10 technical replicates ± SEM. ( D ) cAMP production after stimulation with PGD2 (EC80, 300pM) measured on CHO-K1 cells stable clone transfected for human DP1 (hDP1). Values represent mean of n=4 technical replicates ± SEM. ( E ) Visualization of OKN4395 antagonist activity at 1µM screened with gpcrMAX GPCR LeadHunter Panel (Eurofins) obtained with the plotrender spatial data mapper tool developed by gpcrdb. ( F ) Summary table of OKN4395 IC50 on human prostanoid receptors. ( G ) Plausible binding mode of a representative of OKN4395 series in DP1 (DP1: orange, ligand: green). Hydrogen bonds are yellow dashed lines.
    Selective Ep2 Antagonist Pf 04418948, supplied by Toronto Research Chemicals, 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/selective+ep2+antagonist+pf-04418948/pmc08161457-55-5-15?v=Toronto+Research+Chemicals
    Average 90 stars, based on 1 article reviews
    selective ep2 antagonist pf 04418948 - by Bioz Stars, 2026-07
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    pf-04418948, a selective ep2 antagonist  (Pfizer Inc)
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    Pfizer Inc pf-04418948, a selective ep2 antagonist
    ( A ) Compound 1: lead compound from [29] with moderate dual inhibition; Compound 2. lead compound from [30] with potent <t>EP2</t> inhibition; Compound 3. lead compound from [31] with potent dual EP2/EP4 inhibition. The OKN4395 series is derived from [31]. Most of the diversity in the series comes from the exploration of the right hand aryl system bearing the carboxylic acid. Compound 3 is an example of that series. ( B ) cAMP production after stimulation with PGE2 (EC80, 2nM) measured on HEK293 stable clones expressing human EP2 (hEP2). Values represent mean of n=10 technical replicates ± SEM. ( C ) cAMP production after stimulation with PGE2 (EC80, 6nM) measured on HEK293 stable clones expressing human EP4 (hEP4). Values represent mean of n=10 technical replicates ± SEM. ( D ) cAMP production after stimulation with PGD2 (EC80, 300pM) measured on CHO-K1 cells stable clone transfected for human DP1 (hDP1). Values represent mean of n=4 technical replicates ± SEM. ( E ) Visualization of OKN4395 antagonist activity at 1µM screened with gpcrMAX GPCR LeadHunter Panel (Eurofins) obtained with the plotrender spatial data mapper tool developed by gpcrdb. ( F ) Summary table of OKN4395 IC50 on human prostanoid receptors. ( G ) Plausible binding mode of a representative of OKN4395 series in DP1 (DP1: orange, ligand: green). Hydrogen bonds are yellow dashed lines.
    Pf 04418948, A Selective Ep2 Antagonist, supplied by Pfizer Inc, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    Average 90 stars, based on 1 article reviews
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    ep2 selective antagonist pf-04418948  (Cayman Chemical)
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    Cayman Chemical ep2 selective antagonist pf-04418948
    ( A ) Compound 1: lead compound from [29] with moderate dual inhibition; Compound 2. lead compound from [30] with potent <t>EP2</t> inhibition; Compound 3. lead compound from [31] with potent dual EP2/EP4 inhibition. The OKN4395 series is derived from [31]. Most of the diversity in the series comes from the exploration of the right hand aryl system bearing the carboxylic acid. Compound 3 is an example of that series. ( B ) cAMP production after stimulation with PGE2 (EC80, 2nM) measured on HEK293 stable clones expressing human EP2 (hEP2). Values represent mean of n=10 technical replicates ± SEM. ( C ) cAMP production after stimulation with PGE2 (EC80, 6nM) measured on HEK293 stable clones expressing human EP4 (hEP4). Values represent mean of n=10 technical replicates ± SEM. ( D ) cAMP production after stimulation with PGD2 (EC80, 300pM) measured on CHO-K1 cells stable clone transfected for human DP1 (hDP1). Values represent mean of n=4 technical replicates ± SEM. ( E ) Visualization of OKN4395 antagonist activity at 1µM screened with gpcrMAX GPCR LeadHunter Panel (Eurofins) obtained with the plotrender spatial data mapper tool developed by gpcrdb. ( F ) Summary table of OKN4395 IC50 on human prostanoid receptors. ( G ) Plausible binding mode of a representative of OKN4395 series in DP1 (DP1: orange, ligand: green). Hydrogen bonds are yellow dashed lines.
    Ep2 Selective Antagonist Pf 04418948, supplied by Cayman Chemical, 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/selective+ep2+antagonist+pf-04418948/pmc05409855-59-6-7?v=Cayman+Chemical
    Average 90 stars, based on 1 article reviews
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    ( A ) Compound 1: lead compound from [29] with moderate dual inhibition; Compound 2. lead compound from [30] with potent EP2 inhibition; Compound 3. lead compound from [31] with potent dual EP2/EP4 inhibition. The OKN4395 series is derived from [31]. Most of the diversity in the series comes from the exploration of the right hand aryl system bearing the carboxylic acid. Compound 3 is an example of that series. ( B ) cAMP production after stimulation with PGE2 (EC80, 2nM) measured on HEK293 stable clones expressing human EP2 (hEP2). Values represent mean of n=10 technical replicates ± SEM. ( C ) cAMP production after stimulation with PGE2 (EC80, 6nM) measured on HEK293 stable clones expressing human EP4 (hEP4). Values represent mean of n=10 technical replicates ± SEM. ( D ) cAMP production after stimulation with PGD2 (EC80, 300pM) measured on CHO-K1 cells stable clone transfected for human DP1 (hDP1). Values represent mean of n=4 technical replicates ± SEM. ( E ) Visualization of OKN4395 antagonist activity at 1µM screened with gpcrMAX GPCR LeadHunter Panel (Eurofins) obtained with the plotrender spatial data mapper tool developed by gpcrdb. ( F ) Summary table of OKN4395 IC50 on human prostanoid receptors. ( G ) Plausible binding mode of a representative of OKN4395 series in DP1 (DP1: orange, ligand: green). Hydrogen bonds are yellow dashed lines.

    Journal: bioRxiv

    Article Title: OKN4395, a first-in-class EP2/EP4/DP1 triple antagonist reprograms prostanoid-driven immunosuppression to restore antitumor immunity

    doi: 10.64898/2026.02.08.704632

    Figure Lengend Snippet: ( A ) Compound 1: lead compound from [29] with moderate dual inhibition; Compound 2. lead compound from [30] with potent EP2 inhibition; Compound 3. lead compound from [31] with potent dual EP2/EP4 inhibition. The OKN4395 series is derived from [31]. Most of the diversity in the series comes from the exploration of the right hand aryl system bearing the carboxylic acid. Compound 3 is an example of that series. ( B ) cAMP production after stimulation with PGE2 (EC80, 2nM) measured on HEK293 stable clones expressing human EP2 (hEP2). Values represent mean of n=10 technical replicates ± SEM. ( C ) cAMP production after stimulation with PGE2 (EC80, 6nM) measured on HEK293 stable clones expressing human EP4 (hEP4). Values represent mean of n=10 technical replicates ± SEM. ( D ) cAMP production after stimulation with PGD2 (EC80, 300pM) measured on CHO-K1 cells stable clone transfected for human DP1 (hDP1). Values represent mean of n=4 technical replicates ± SEM. ( E ) Visualization of OKN4395 antagonist activity at 1µM screened with gpcrMAX GPCR LeadHunter Panel (Eurofins) obtained with the plotrender spatial data mapper tool developed by gpcrdb. ( F ) Summary table of OKN4395 IC50 on human prostanoid receptors. ( G ) Plausible binding mode of a representative of OKN4395 series in DP1 (DP1: orange, ligand: green). Hydrogen bonds are yellow dashed lines.

    Article Snippet: For experiment controls, the following inhibitors were used across several experiments: PF-04418948 (S7211, Selleckchem) is a selective EP2 receptor antagonist .

    Techniques: Inhibition, Derivative Assay, Clone Assay, Expressing, Stable Transfection, Transfection, Activity Assay, Binding Assay

    ( A ) cAMP production after stimulation with PGE2 (EC80) measured on HEK293 stable clones expressing EP2 or EP4 from different species or stimulation with PGD2 (EC80) measured on transfected HEK293 cells transiently expressing DP1 from different species. EC80 PGE2 concentrations are mouse EP2 (mEP2) 300pM, mouse EP4 (mEP4) 200pM, rat EP2 (rEP2) 35-45pM, rat EP4 (rEP4) 5.8-7.8pM, monkey EP2 (mkEP2) 35-40pM, monkey EP4 (mkEP4) 4.2-7.8pM, dog EP2 (dEP2) 65-80pM and dog EP4 (dEP4) 17.8-22.7pM. EC80 PGD2 concentrations are mouse DP1 (mDP1) 2.5nM, rat DP1 (rDP1) 4.4nM and monkey DP1 (mkDP1) 0.75nM. Values represent mean of n=4 (mEP2), n=6 (mEP4), n=10 (rEP2, rEP4, mkEP2, mkEP4, dEP2, dEP4), n=2 (mDP1, rDP1, mkDP1) technical replicates ± SEM. ( B ) cAMP production after stimulation with different PGE2 concentrations measured on SF295 cells (left) or BT549 cells (right) naturally expressing EP2 and EP4 receptor respectively. Values represent mean of n=2 technical replicates ± SEM. ( C ) Activation of (left) hEP1 and (middle) hEP3 after stimulation with PGE2 (EC80, 45nM and 15nM respectively) was measurement on U2OS cells and CHO-K1 cells expressing human EP1 and human EP3 respectively. (Right) cAMP production after stimulation with iloprost (EC80, 60pM) measured on HEK293 stable clones expressing hIP. Values represent mean of n=8 (hEP1, hEP3) and n=4 (hIP) technical replicates ± SEM. ( D ) Selectivity of OKN4395 (top 1µM; bottom 10µM) across 166 G protein-coupled receptors. OKN4395 activity was quantified as the percentage of the natural ligand response, with reduced activity indicating inhibition. ( E ) Superimposition of EP4 (cyan), EP2 (purple) and DP1 (green) binding sites (left). Interactions made by a representative of OKN4395 series in DP1 (right). All the main residues essential for the interactions are conserved in the three proteins. ( F ) Evolution of the distance between the carboxylate of OKN4395 and the interacting arginine residue in EP3, EP4 and DP1, showing the gradual weakening of its strength through movement of the ligand in EP3 and the stability in EP4 and DP1 (solid line: averaged across the triplicates, shaded area: standard deviation).

    Journal: bioRxiv

    Article Title: OKN4395, a first-in-class EP2/EP4/DP1 triple antagonist reprograms prostanoid-driven immunosuppression to restore antitumor immunity

    doi: 10.64898/2026.02.08.704632

    Figure Lengend Snippet: ( A ) cAMP production after stimulation with PGE2 (EC80) measured on HEK293 stable clones expressing EP2 or EP4 from different species or stimulation with PGD2 (EC80) measured on transfected HEK293 cells transiently expressing DP1 from different species. EC80 PGE2 concentrations are mouse EP2 (mEP2) 300pM, mouse EP4 (mEP4) 200pM, rat EP2 (rEP2) 35-45pM, rat EP4 (rEP4) 5.8-7.8pM, monkey EP2 (mkEP2) 35-40pM, monkey EP4 (mkEP4) 4.2-7.8pM, dog EP2 (dEP2) 65-80pM and dog EP4 (dEP4) 17.8-22.7pM. EC80 PGD2 concentrations are mouse DP1 (mDP1) 2.5nM, rat DP1 (rDP1) 4.4nM and monkey DP1 (mkDP1) 0.75nM. Values represent mean of n=4 (mEP2), n=6 (mEP4), n=10 (rEP2, rEP4, mkEP2, mkEP4, dEP2, dEP4), n=2 (mDP1, rDP1, mkDP1) technical replicates ± SEM. ( B ) cAMP production after stimulation with different PGE2 concentrations measured on SF295 cells (left) or BT549 cells (right) naturally expressing EP2 and EP4 receptor respectively. Values represent mean of n=2 technical replicates ± SEM. ( C ) Activation of (left) hEP1 and (middle) hEP3 after stimulation with PGE2 (EC80, 45nM and 15nM respectively) was measurement on U2OS cells and CHO-K1 cells expressing human EP1 and human EP3 respectively. (Right) cAMP production after stimulation with iloprost (EC80, 60pM) measured on HEK293 stable clones expressing hIP. Values represent mean of n=8 (hEP1, hEP3) and n=4 (hIP) technical replicates ± SEM. ( D ) Selectivity of OKN4395 (top 1µM; bottom 10µM) across 166 G protein-coupled receptors. OKN4395 activity was quantified as the percentage of the natural ligand response, with reduced activity indicating inhibition. ( E ) Superimposition of EP4 (cyan), EP2 (purple) and DP1 (green) binding sites (left). Interactions made by a representative of OKN4395 series in DP1 (right). All the main residues essential for the interactions are conserved in the three proteins. ( F ) Evolution of the distance between the carboxylate of OKN4395 and the interacting arginine residue in EP3, EP4 and DP1, showing the gradual weakening of its strength through movement of the ligand in EP3 and the stability in EP4 and DP1 (solid line: averaged across the triplicates, shaded area: standard deviation).

    Article Snippet: For experiment controls, the following inhibitors were used across several experiments: PF-04418948 (S7211, Selleckchem) is a selective EP2 receptor antagonist .

    Techniques: Clone Assay, Expressing, Transfection, Activation Assay, Activity Assay, Inhibition, Binding Assay, Residue, Standard Deviation