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Assay Detail

CHEMBL4308764

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

Binding
Inhibition of CSK (unknown origin) using fluorescent labeled peptide as substrate in presence of ATP at Km concentration by caliper method
8
Total Activities
8
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 CSK (CHEMBL2634)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Pyridazinone and Pyrazolo[1,5-a]pyridine Inhibitors of C-Terminal Src Kinase.
O'Malley DP, Ahuja V, Fink B, Cao C, Wang C, Swanson J, Wee S, Gavai AV, Tokarski J, Critton D, Paiva AA, Johnson BM, Szapiel N, Xie D.
ACS Med Chem Lett (2019) 10 : 1486 -1491
PubMed 31620238 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.26 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4582324 1 8.70
CHEMBL4443654 1 8.40
CHEMBL4577049 1 8.40
CHEMBL4545269 1 8.40
CHEMBL4445994 1 8.40
CHEMBL4537527 1 8.22
CHEMBL4469360 1 7.89
CHEMBL4483095 1 7.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4582324 IC50 = 2.0 nM 8.70
CHEMBL4443654 IC50 = 4.0 nM 8.40
CHEMBL4577049 IC50 = 4.0 nM 8.40
CHEMBL4545269 IC50 = 4.0 nM 8.40
CHEMBL4445994 IC50 = 4.0 nM 8.40
CHEMBL4537527 IC50 = 6.0 nM 8.22
CHEMBL4469360 IC50 = 13.0 nM 7.89
CHEMBL4483095 IC50 = 21.0 nM 7.68