Assay Detail

CHEMBL3858931

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Binding

Inhibition of BTK in human peripheral B cells assessed as suppression of BCR/anti-IgM/IgG-stimulated CD86 surface expression

ChEMBL ↗

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Target

Tyrosine-protein kinase BTK (CHEMBL5251) ↗

Open DB target context

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Tyrosine-protein kinase BTK (CHEMBL5251) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Tyrosine-protein kinase BTK

CHEMBL5251

Anchored from Assay target.

Protein identity Tyrosine-protein kinase BTK

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

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

Target

Tyrosine-protein kinase BTK (CHEMBL5251) ↗

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	2	7.90	8.40

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3900554	BMS-986142	2.0	1	8.40
CHEMBL3918580	—	—	1	7.40

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3900554	BMS-986142	IC50	=	4.0	nM	8.40
CHEMBL3918580	—	IC50	=	40.0	nM	7.40