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Assay Detail

CHEMBL1019786

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Binding
Inhibition of CDK9
12
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cyclin-dependent kinase 9 (CHEMBL3116)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery.
Menichincheri M, Bargiotti A, Berthelsen J, Bertrand JA, Bossi R, Ciavolella A, Cirla A, Cristiani C, Croci V, D'Alessio R, Fasolini M, Fiorentini F, Forte B, Isacchi A, Martina K, Molinari A, Montagnoli A, Orsini P, Orzi F, Pesenti E, Pezzetta D, Pillan A, Poggesi I, Roletto F, Scolaro A, Tatò M, Tibolla M, Valsasina B, Varasi M, Volpi D, Santocanale C, Vanotti E.
J Med Chem (2009) 52 : 293 -307
PubMed 19115845 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.19 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL526092 2 7.77
CHEMBL524266 1 7.55
CHEMBL402272 1 7.54
CHEMBL445340 2 7.51
CHEMBL225519 1 7.47
CHEMBL497995 2 7.08
CHEMBL451570 1 7.02
CHEMBL498200 2 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL526092 IC50 = 17.0 nM 7.77
CHEMBL524266 IC50 = 28.0 nM 7.55
CHEMBL402272 IC50 = 29.0 nM 7.54
CHEMBL445340 IC50 = 31.0 nM 7.51
CHEMBL225519 IC50 = 34.0 nM 7.47
CHEMBL526092 IC50 = 73.0 nM 7.14
CHEMBL445340 IC50 = 73.0 nM 7.14
CHEMBL497995 IC50 = 83.0 nM 7.08
CHEMBL451570 IC50 = 96.0 nM 7.02
CHEMBL497995 IC50 = 96.0 nM 7.02
CHEMBL498200 IC50 = 218.0 nM 6.66
CHEMBL498200 IC50 = 395.0 nM 6.40