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Assay Detail

CHEMBL665279

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Binding
Inhibitory activity against Cyclin D1-cyclin-dependent kinase 4 in enzymatic assay by measuring phosphorylation of RbING
ChEMBL ↗
72
Total Activities
72
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 72 7.15 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307150 — — 1 7.55
CHEMBL76390 — — 1 7.54
CHEMBL74883 — — 1 7.50
CHEMBL308099 — — 1 7.48
CHEMBL76326 — — 1 7.48
CHEMBL72076 — — 1 7.47
CHEMBL73718 — — 1 7.46
CHEMBL73751 — — 1 7.44
CHEMBL74637 — — 1 7.43
CHEMBL73832 — — 1 7.42
CHEMBL74289 — — 1 7.42
CHEMBL308979 — — 1 7.41
CHEMBL76337 — — 1 7.40
CHEMBL73485 — — 1 7.38
CHEMBL441258 — — 1 7.36
CHEMBL307630 — — 1 7.35
CHEMBL75368 — — 1 7.35
CHEMBL72808 — — 1 7.33
CHEMBL310260 — — 1 7.33
CHEMBL308116 — — 1 7.33
CHEMBL306114 — — 1 7.32
CHEMBL306856 — — 1 7.32
CHEMBL307152 — — 1 7.31
CHEMBL430606 — — 1 7.31
CHEMBL308541 — — 1 7.30
CHEMBL312292 — — 1 7.29
CHEMBL73764 — — 1 7.28
CHEMBL306611 — — 1 7.28
CHEMBL73794 — — 1 7.28
CHEMBL73343 — — 1 7.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307150 — IC50 = 28.0 nM 7.55
CHEMBL76390 — IC50 = 29.0 nM 7.54
CHEMBL74883 — IC50 = 32.0 nM 7.50
CHEMBL308099 — IC50 = 33.0 nM 7.48
CHEMBL76326 — IC50 = 33.0 nM 7.48
CHEMBL72076 — IC50 = 34.0 nM 7.47
CHEMBL73718 — IC50 = 35.0 nM 7.46
CHEMBL73751 — IC50 = 36.0 nM 7.44
CHEMBL74637 — IC50 = 37.0 nM 7.43
CHEMBL73832 — IC50 = 38.0 nM 7.42
CHEMBL74289 — IC50 = 38.0 nM 7.42
CHEMBL308979 — IC50 = 39.0 nM 7.41
CHEMBL76337 — IC50 = 40.0 nM 7.40
CHEMBL73485 — IC50 = 42.0 nM 7.38
CHEMBL441258 — IC50 = 44.0 nM 7.36
CHEMBL307630 — IC50 = 45.0 nM 7.35
CHEMBL75368 — IC50 = 45.0 nM 7.35
CHEMBL72808 — IC50 = 47.0 nM 7.33
CHEMBL310260 — IC50 = 47.0 nM 7.33
CHEMBL308116 — IC50 = 47.0 nM 7.33
CHEMBL306114 — IC50 = 48.0 nM 7.32
CHEMBL306856 — IC50 = 48.0 nM 7.32
CHEMBL307152 — IC50 = 49.0 nM 7.31
CHEMBL430606 — IC50 = 49.0 nM 7.31
CHEMBL308541 — IC50 = 50.0 nM 7.30
CHEMBL312292 — IC50 = 51.0 nM 7.29
CHEMBL306611 — IC50 = 53.0 nM 7.28
CHEMBL73794 — IC50 = 52.0 nM 7.28
CHEMBL73764 — IC50 = 53.0 nM 7.28
CHEMBL73343 — IC50 = 54.0 nM 7.27
CHEMBL72069 — IC50 = 54.0 nM 7.27
CHEMBL306047 — IC50 = 54.0 nM 7.27
CHEMBL73772 — IC50 = 56.0 nM 7.25
CHEMBL388978 STAUROSPORINE IC50 = 59.0 nM 7.23
CHEMBL307007 — IC50 = 59.0 nM 7.23
CHEMBL307219 — IC50 = 62.0 nM 7.21
CHEMBL311851 — IC50 = 63.0 nM 7.20
CHEMBL306748 — IC50 = 66.0 nM 7.18
CHEMBL308252 — IC50 = 67.0 nM 7.17
CHEMBL72607 — IC50 = 67.0 nM 7.17
CHEMBL72077 — IC50 = 69.0 nM 7.16
CHEMBL73499 — IC50 = 71.0 nM 7.15
CHEMBL73781 — IC50 = 72.0 nM 7.14
CHEMBL76499 — IC50 = 76.0 nM 7.12
CHEMBL306501 — IC50 = 77.0 nM 7.11
CHEMBL308594 — IC50 = 82.0 nM 7.09
CHEMBL310491 — IC50 = 82.0 nM 7.09
CHEMBL308994 — IC50 = 84.0 nM 7.08
CHEMBL75952 — IC50 = 84.0 nM 7.08
CHEMBL306367 — IC50 = 92.0 nM 7.04