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Assay Detail

CHEMBL3858963

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of BMX (unknown origin)
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytoplasmic tyrosine-protein kinase BMX (CHEMBL3834)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers.
Watterson SH, De Lucca GV, Shi Q, Langevine CM, Liu Q, Batt DG, Beaudoin Bertrand M, Gong H, Dai J, Yip S, Li P, Sun D, Wu DR, Wang C, Zhang Y, Traeger SC, Pattoli MA, Skala S, Cheng L, Obermeier MT, Vickery R, Discenza LN, D'Arienzo CJ, Zhang Y, Heimrich E, Gillooly KM, Taylor TL, Pulicicchio C, McIntyre KW, Galella MA, Tebben AJ, Muckelbauer JK, Chang C, Rampulla R, Mathur A, Salter-Cid L, Barrish JC, Carter PH, Fura A, Burke JR, Tino JA.
J Med Chem (2016) 59 : 9173 -9200
PubMed 27583770 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.50 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3900554 BMS-986142 2.0 1 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3900554 BMS-986142 IC50 = 32.0 nM 7.50