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Assay Detail

CHEMBL1016197

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Binding
Inhibition of CDK4/Cyclin D1 assessed as inhibition of retinoblastoma susceptibility gene product phosphorylation
ChEMBL ↗
47
Total Activities
47
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

Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4.
Tsou HR, Liu X, Birnberg G, Kaplan J, Otteng M, Tran T, Kutterer K, Tang Z, Suayan R, Zask A, Ravi M, Bretz A, Grillo M, McGinnis JP, Rabindran SK, Ayral-Kaloustian S, Mansour TS.
J Med Chem (2009) 52 : 2289 -2310
PubMed 19317452 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 47 6.95 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL489646 — — 1 8.70
CHEMBL489853 — — 1 8.70
CHEMBL489445 — — 1 8.40
CHEMBL477860 — — 1 8.10
CHEMBL489245 — — 1 8.00
CHEMBL452447 — — 1 8.00
CHEMBL477063 — — 1 8.00
CHEMBL523780 — — 1 8.00
CHEMBL515631 — — 1 7.70
CHEMBL489629 — — 1 7.70
CHEMBL477863 — — 1 7.70
CHEMBL477861 — — 1 7.70
CHEMBL478487 — — 1 7.52
CHEMBL484274 — — 1 7.52
CHEMBL489244 — — 1 7.52
CHEMBL477064 — — 1 7.52
CHEMBL514678 — — 1 7.52
CHEMBL521922 — — 1 7.52
CHEMBL489246 — — 1 7.51
CHEMBL504547 — — 1 7.22
CHEMBL490451 — — 1 7.22
CHEMBL502651 — — 1 7.10
CHEMBL477877 — — 1 7.00
CHEMBL478488 — — 1 6.89
CHEMBL489432 — — 1 6.77
CHEMBL489430 — — 1 6.72
CHEMBL489631 — — 1 6.64
CHEMBL490251 — — 1 6.57
CHEMBL485502 — — 1 6.46
CHEMBL477862 — — 1 6.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL489646 — IC50 = 2.0 nM 8.70
CHEMBL489853 — IC50 = 2.0 nM 8.70
CHEMBL489445 — IC50 = 4.0 nM 8.40
CHEMBL477860 — IC50 = 8.0 nM 8.10
CHEMBL489245 — IC50 = 10.0 nM 8.00
CHEMBL452447 — IC50 = 10.0 nM 8.00
CHEMBL477063 — IC50 = 10.0 nM 8.00
CHEMBL523780 — IC50 = 10.0 nM 8.00
CHEMBL515631 — IC50 = 20.0 nM 7.70
CHEMBL489629 — IC50 = 20.0 nM 7.70
CHEMBL477863 — IC50 = 20.0 nM 7.70
CHEMBL477861 — IC50 = 20.0 nM 7.70
CHEMBL514678 — IC50 = 30.0 nM 7.52
CHEMBL484274 — IC50 = 30.0 nM 7.52
CHEMBL489244 — IC50 = 30.0 nM 7.52
CHEMBL478487 — IC50 = 30.0 nM 7.52
CHEMBL477064 — IC50 = 30.0 nM 7.52
CHEMBL521922 — IC50 = 30.0 nM 7.52
CHEMBL489246 — IC50 = 31.0 nM 7.51
CHEMBL504547 — IC50 = 60.0 nM 7.22
CHEMBL490451 — IC50 = 60.0 nM 7.22
CHEMBL502651 — IC50 = 80.0 nM 7.10
CHEMBL477877 — IC50 = 100.0 nM 7.00
CHEMBL478488 — IC50 = 130.0 nM 6.89
CHEMBL489432 — IC50 = 170.0 nM 6.77
CHEMBL489430 — IC50 = 190.0 nM 6.72
CHEMBL489631 — IC50 = 230.0 nM 6.64
CHEMBL490251 — IC50 = 270.0 nM 6.57
CHEMBL485502 — IC50 = 350.0 nM 6.46
CHEMBL477862 — IC50 = 440.0 nM 6.36
CHEMBL449818 — IC50 = 560.0 nM 6.25
CHEMBL447758 — IC50 = 780.0 nM 6.11
CHEMBL489039 — IC50 = 940.0 nM 6.03
CHEMBL450383 — IC50 = 1200.0 nM 5.92
CHEMBL489030 — IC50 = 1300.0 nM 5.89
CHEMBL489424 — IC50 = 7800.0 nM 5.11
CHEMBL489431 — IC50 = 16200.0 nM 4.79
CHEMBL451298 — IC50 = 19300.0 nM 4.71
CHEMBL490241 — IC50 = 31700.0 nM 4.50
CHEMBL490053 — IC50 = 50000.0 nM 4.30
CHEMBL490240 — IC50 < 5.0 nM -
CHEMBL477259 — IC50 < 5.0 nM -
CHEMBL484477 — IC50 < 7.0 nM -
CHEMBL485503 — IC50 < 40.0 nM -
CHEMBL489627 — IC50 < 50000.0 nM -
CHEMBL489854 — IC50 < 370.0 nM -
CHEMBL520020 — IC50 < 40.0 nM -