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Assay Detail

CHEMBL4382186

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

Binding
Inhibition of human recombinant FAK using poly[Glu:Tyr] (4:1) substrate in presence of 10 mM ATP and [gamma33P]-ATP
9
Total Activities
9
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

Focal adhesion kinase 1 (CHEMBL2695)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Bifunctional Pyrimidines as Modulators of Focal Adhesion Kinase.
Kargbo RB.
ACS Med Chem Lett (2020) 11 : 409 -411
PubMed 32292541 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.03 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3137331 DEFACTINIB 3.0 1 8.41
CHEMBL4586249 1 8.33
CHEMBL4541275 1 8.01
CHEMBL4449796 1 7.97
CHEMBL4567809 1 7.95
CHEMBL4560289 1 7.90
CHEMBL4558994 1 7.84
CHEMBL4464368 1 7.83
CHEMBL4447794 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3137331 DEFACTINIB IC50 = 3.9 nM 8.41
CHEMBL4586249 IC50 = 4.7 nM 8.33
CHEMBL4541275 IC50 = 9.7 nM 8.01
CHEMBL4449796 IC50 = 10.7 nM 7.97
CHEMBL4567809 IC50 = 11.3 nM 7.95
CHEMBL4560289 IC50 = 12.7 nM 7.90
CHEMBL4558994 IC50 = 14.5 nM 7.84
CHEMBL4464368 IC50 = 14.7 nM 7.83
CHEMBL4447794 IC50 = 6.5 nM -