inhibitor of egfr kinase and brd4 (MultiTarget Pharmaceuticals)
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Inhibitor Of Egfr Kinase And Brd4, supplied by MultiTarget Pharmaceuticals, 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/result/inhibitor of egfr kinase and brd4/product/MultiTarget Pharmaceuticals
Average 90 stars, based on 1 article reviews
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1) Product Images from "Large-Scale Computational Screening Identifies First in Class Multitarget Inhibitor of EGFR Kinase and BRD4"
Article Title: Large-Scale Computational Screening Identifies First in Class Multitarget Inhibitor of EGFR Kinase and BRD4
Journal: Scientific Reports
doi: 10.1038/srep16924
Figure Legend Snippet: High-throughput computational screening pipeline to identify dual inhibitors of EGFR kinase and BRD4(1).
Techniques Used: High Throughput Screening Assay
Figure Legend Snippet: Evaluation and characterization of the BRD4 docking data fusion model.
Techniques Used:
Figure Legend Snippet: Docking scores versus reported BRD4 pActivities (pIC 50 /pK d /pK i ) and Pearson correlation results of representative BRD4 inhibitors by chemotypes.
Techniques Used:
Figure Legend Snippet: Circles represent purchased compounds tested in the BRD4(1) assay, categorized by their activity against BRD4 and EGFR. Only compounds that were confirmed active against BRD4 were further tested for activity against EGFR; any of the black circles therefore could also be EGFR actives.
Techniques Used: Activity Assay
Figure Legend Snippet: ( A ) Average concentration-response profile of compound 2870 and known BRD4 inhibitor I-BET151 using the BRD4(1) biochemical alpha screen assay (n = 3). Emission data was normalized using DMSO and is reported as % response. Average IC 50 of 2870 was found to be 9.02 μ M against BRD4(1). ( B ) The EGFR kinase radioisotope filter binding assay was performed at a substrate concentration of 10 μ M against 2870 and Staurosporine (n = 3). Average IC 50 of 2870 was found to be 0.044 μ M against EGFR kinase.
Techniques Used: Concentration Assay, Filter-binding Assay
Figure Legend Snippet: Activity from the alphascreen assay against BRD4(1) and closest topological similarity to known BRD4(1) binders is also shown. Five other compounds comprising the same sulfonamide scaffold as 8302 were also confirmed actives but are not displayed.
Techniques Used: Activity Assay, Amplified Luminescent Proximity Homogenous Assay
Figure Legend Snippet: Binding affinity of 2870.
Techniques Used: Binding Assay