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Assay Detail

CHEMBL4768630

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Binding
Inhibition of CDK7/cyclin H (unknown origin)
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Cyclin-dependent kinase 7/ cyclin H (CHEMBL2111288)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors.
Shi C,Wang Q,Liao X,Ge H,Huo G,Zhang L,Chen N,Zhai X,Hong Y,Wang L,Wang Z,Shi W,Mao Y,Yu J,Ke Y,Xia G
Eur J Med Chem (2020) 193 : 112239 -112239
PubMed 32200202 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.50 7.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4778367 1 7.02
CHEMBL4776781 1 6.69
CHEMBL3301610 ABEMACICLIB 4.0 1 5.80
CHEMBL189963 PALBOCICLIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4778367 IC50 = 94.7 nM 7.02
CHEMBL4776781 IC50 = 204.0 nM 6.69
CHEMBL3301610 ABEMACICLIB IC50 = 1596.0 nM 5.80
CHEMBL189963 PALBOCICLIB IC50 > 3333.0 nM -