Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4023772

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

Binding
Inhibition of BTK T474I mutant (unknown origin) expressed in HEK293 cells
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 BTK (CHEMBL5251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
Crawford JJ, Johnson AR, Misner DL, Belmont LD, Castanedo G, Choy R, Coraggio M, Dong L, Eigenbrot C, Erickson R, Ghilardi N, Hau J, Katewa A, Kohli PB, Lee W, Lubach JW, McKenzie BS, Ortwine DF, Schutt L, Tay S, Wei B, Reif K, Liu L, Wong H, Young WB.
J Med Chem (2018) 61 : 2227 -2245
PubMed 29457982 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 7.90 7.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4065122 FENEBRUTINIB 3.0 1 7.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4065122 FENEBRUTINIB Ki = 12.6 nM 7.90