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Assay Detail

CHEMBL4616780

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

Binding
Inhibition of TXK (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

Tyrosine-protein kinase TXK (CHEMBL4367)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK).
Watterson SH, Liu Q, Beaudoin Bertrand M, Batt DG, Li L, Pattoli MA, Skala S, Cheng L, Obermeier MT, Moore R, Yang Z, Vickery R, Elzinga PA, Discenza L, D'Arienzo C, Gillooly KM, Taylor TL, Pulicicchio C, Zhang Y, Heimrich E, McIntyre KW, Ruan Q, Westhouse RA, Catlett IM, Zheng N, Chaudhry C, Dai J, Galella MA, Tebben AJ, Pokross M, Li J, Zhao R, Smith D, Rampulla R, Allentoff A, Wallace MA, Mathur A, Salter-Cid L, Macor JE, Carter PH, Fura A, Burke JR, Tino JA.
J Med Chem (2019) 62 : 3228 -3250
PubMed 30893553 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.30 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4297674 BRANEBRUTINIB 2.0 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4297674 BRANEBRUTINIB IC50 = 5.0 nM 8.30