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Assay Detail

CHEMBL666305

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

Binding
Inhibitory activity against Cyclin-dependent kinase 4-cyclin D1 using Rb21 as substrate
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Cyclin-dependent kinase 4/cyclin D1 (CHEMBL1907601)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors.
Zhu G, Conner SE, Zhou X, Shih C, Li T, Anderson BD, Brooks HB, Campbell RM, Considine E, Dempsey JA, Faul MM, Ogg C, Patel B, Schultz RM, Spencer CD, Teicher B, Watkins SA.
J Med Chem (2003) 46 : 2027 -2030
PubMed 12747775 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.55 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL62253 1 7.38
CHEMBL291402 1 7.14
CHEMBL293898 1 7.13
CHEMBL64758 1 7.12
CHEMBL59785 1 7.10
CHEMBL293157 1 6.99
CHEMBL64742 1 6.87
CHEMBL268368 STAUROSPORINE AGLYCON 1 6.80
CHEMBL292021 1 6.65
CHEMBL304428 1 6.27
CHEMBL302854 1 6.20
CHEMBL61790 1 5.95
CHEMBL60564 1 5.36
CHEMBL432715 1 4.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL62253 IC50 = 42.0 nM 7.38
CHEMBL291402 IC50 = 72.0 nM 7.14
CHEMBL293898 IC50 = 74.0 nM 7.13
CHEMBL64758 IC50 = 76.0 nM 7.12
CHEMBL59785 IC50 = 80.0 nM 7.10
CHEMBL293157 IC50 = 103.0 nM 6.99
CHEMBL64742 IC50 = 134.0 nM 6.87
CHEMBL268368 STAUROSPORINE AGLYCON IC50 = 160.0 nM 6.80
CHEMBL292021 IC50 = 226.0 nM 6.65
CHEMBL304428 IC50 = 540.0 nM 6.27
CHEMBL302854 IC50 = 630.0 nM 6.20
CHEMBL61790 IC50 = 1135.0 nM 5.95
CHEMBL60564 IC50 = 4400.0 nM 5.36
CHEMBL432715 IC50 = 16200.0 nM 4.79