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Assay Detail

CHEMBL4050188

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

Binding
Inhibition of human FAK/PTK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-32P]ATP
3
Total Activities
3
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

Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.
Sugimoto Y, Sawant DB, Fisk HA, Mao L, Li C, Chettiar S, Li PK, Darby MV, Brueggemeier RW.
Bioorg Med Chem (2017) 25 : 2156 -2166
PubMed 28259529 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.88 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 7.70
CHEMBL4076767 1 6.05
CHEMBL573339 PI-103 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 20.0 nM 7.70
CHEMBL4076767 IC50 = 891.0 nM 6.05
CHEMBL573339 PI-103 IC50 - -