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Assay Detail

CHEMBL665277

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

Binding
Inhibitory activity against Cyclin D1-cyclin-dependent kinase 4 in enzymatic assay by measuring phosphorylation of Rb21
64
Total Activities
64
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

Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles.
Engler TA, Furness K, Malhotra S, Sanchez-Martinez C, Shih C, Xie W, Zhu G, Zhou X, Conner S, Faul MM, Sullivan KA, Kolis SP, Brooks HB, Patel B, Schultz RM, DeHahn TB, Kirmani K, Spencer CD, Watkins SA, Considine EL, Dempsey JA, Ogg CA, Stamm NB, Anderson BD, Campbell RM, Vasudevan V, Lytle ML.
Bioorg Med Chem Lett (2003) 13 : 2261 -2267
PubMed 12824014 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 64 7.61 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307150 1 8.70
CHEMBL306856 1 8.40
CHEMBL312292 1 8.30
CHEMBL73764 1 8.30
CHEMBL306611 1 8.22
CHEMBL308541 1 8.22
CHEMBL73485 1 8.15
CHEMBL75368 1 8.10
CHEMBL76499 1 8.05
CHEMBL308099 1 8.05
CHEMBL76326 1 8.00
CHEMBL441258 1 8.00
CHEMBL307630 1 7.96
CHEMBL76390 1 7.96
CHEMBL73832 1 7.96
CHEMBL306748 1 7.92
CHEMBL73343 1 7.92
CHEMBL306501 1 7.89
CHEMBL72808 1 7.89
CHEMBL76464 1 7.85
CHEMBL306047 1 7.82
CHEMBL430606 1 7.82
CHEMBL72607 1 7.80
CHEMBL74637 1 7.77
CHEMBL74883 1 7.75
CHEMBL306114 1 7.75
CHEMBL307007 1 7.72
CHEMBL307152 1 7.72
CHEMBL76337 1 7.72
CHEMBL73718 1 7.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307150 IC50 = 2.0 nM 8.70
CHEMBL306856 IC50 = 4.0 nM 8.40
CHEMBL73764 IC50 = 5.0 nM 8.30
CHEMBL312292 IC50 = 5.0 nM 8.30
CHEMBL306611 IC50 = 6.0 nM 8.22
CHEMBL308541 IC50 = 6.0 nM 8.22
CHEMBL73485 IC50 = 7.0 nM 8.15
CHEMBL75368 IC50 = 8.0 nM 8.10
CHEMBL76499 IC50 = 9.0 nM 8.05
CHEMBL308099 IC50 = 9.0 nM 8.05
CHEMBL76326 IC50 = 10.0 nM 8.00
CHEMBL441258 IC50 = 10.0 nM 8.00
CHEMBL76390 IC50 = 11.0 nM 7.96
CHEMBL73832 IC50 = 11.0 nM 7.96
CHEMBL307630 IC50 = 11.0 nM 7.96
CHEMBL306748 IC50 = 12.0 nM 7.92
CHEMBL73343 IC50 = 12.0 nM 7.92
CHEMBL306501 IC50 = 13.0 nM 7.89
CHEMBL72808 IC50 = 13.0 nM 7.89
CHEMBL76464 IC50 = 14.0 nM 7.85
CHEMBL306047 IC50 = 15.0 nM 7.82
CHEMBL430606 IC50 = 15.0 nM 7.82
CHEMBL72607 IC50 = 16.0 nM 7.80
CHEMBL74637 IC50 = 17.0 nM 7.77
CHEMBL306114 IC50 = 18.0 nM 7.75
CHEMBL74883 IC50 = 18.0 nM 7.75
CHEMBL307007 IC50 = 19.0 nM 7.72
CHEMBL307152 IC50 = 19.0 nM 7.72
CHEMBL76337 IC50 = 19.0 nM 7.72
CHEMBL73718 IC50 = 21.0 nM 7.68
CHEMBL72077 IC50 = 21.0 nM 7.68
CHEMBL73751 IC50 = 22.0 nM 7.66
CHEMBL308479 IC50 = 22.0 nM 7.66
CHEMBL308116 IC50 = 22.0 nM 7.66
CHEMBL308979 IC50 = 23.0 nM 7.64
CHEMBL311851 IC50 = 23.0 nM 7.64
CHEMBL75952 IC50 = 23.0 nM 7.64
CHEMBL72076 IC50 = 24.0 nM 7.62
CHEMBL310491 IC50 = 24.0 nM 7.62
CHEMBL310260 IC50 = 24.0 nM 7.62
CHEMBL75953 IC50 = 25.0 nM 7.60
CHEMBL76332 IC50 = 25.0 nM 7.60
CHEMBL73781 IC50 = 28.0 nM 7.55
CHEMBL75610 IC50 = 33.0 nM 7.48
CHEMBL73794 IC50 = 35.0 nM 7.46
CHEMBL308252 IC50 = 36.0 nM 7.44
CHEMBL308994 IC50 = 39.0 nM 7.41
CHEMBL73413 IC50 = 40.0 nM 7.40
CHEMBL307219 IC50 = 40.0 nM 7.40
CHEMBL72754 IC50 = 42.0 nM 7.38