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Assay Detail

CHEMBL4353542

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

Binding
Inhibition of recombinant FAK (410 to 689 residues) (unknown origin) using Poly (4:1 Glu, Tyr) peptide as substrate enzyme pretreated with substrate for 15 mins prior to compound addition by ELISA
2
Total Activities
2
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

Discovery of 2,4-diarylaminopyrimidine derivatives bearing dithiocarbamate moiety as novel FAK inhibitors with antitumor and anti-angiogenesis activities.
Su Y, Li R, Ning X, Lin Z, Zhao X, Zhou J, Liu J, Jin Y, Yin Y.
Eur J Med Chem (2019) 177 : 32 -46
PubMed 31129452 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.61 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1084546 PF-00562271 1.0 1 8.82
CHEMBL514554 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1084546 PF-00562271 IC50 = 1.5 nM 8.82
CHEMBL514554 IC50 = 4.0 nM 8.40