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Assay Detail

CHEMBL996963

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

Binding
Inhibition of c-Src
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Proto-oncogene tyrosine-protein kinase Src (CHEMBL267)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of N-6 substituted analogues of 9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of Wee1 and Chk1 checkpoint kinases.
Smaill JB, Baker EN, Booth RJ, Bridges AJ, Dickson JM, Dobrusin EM, Ivanovic I, Kraker AJ, Lee HH, Lunney EA, Ortwine DF, Palmer BD, Quin J, Squire CJ, Thompson AM, Denny WA.
Eur J Med Chem (2008) 43 : 1276 -1296
PubMed 17869387 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 4.85 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL520904 1 5.60
CHEMBL508515 1 5.25
CHEMBL462170 1 4.89
CHEMBL453347 1 4.77
CHEMBL488899 1 4.57
CHEMBL519891 1 4.51
CHEMBL510668 1 4.34
CHEMBL379975 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL520904 IC50 = 2500.0 nM 5.60
CHEMBL508515 IC50 = 5600.0 nM 5.25
CHEMBL462170 IC50 = 13000.0 nM 4.89
CHEMBL453347 IC50 = 17000.0 nM 4.77
CHEMBL488899 IC50 = 27000.0 nM 4.57
CHEMBL519891 IC50 = 31000.0 nM 4.51
CHEMBL510668 IC50 = 46000.0 nM 4.34
CHEMBL379975 IC50 > 50000.0 nM -