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Assay Detail

CHEMBL3240324

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

Binding
Inhibition of CDK4/cyclin D1 (unknown origin) using Rb as substrate after 60 mins by scintillation counting analysis in presence of [r-33P]ATP
30
Total Activities
30
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 4/cyclin D1 (CHEMBL1907601)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.
Li Z, Wang X, Eksterowicz J, Gribble MW, Alba GQ, Ayres M, Carlson TJ, Chen A, Chen X, Cho R, Connors RV, DeGraffenreid M, Deignan JT, Duquette J, Fan P, Fisher B, Fu J, Huard JN, Kaizerman J, Keegan KS, Li C, Li K, Li Y, Liang L, Liu W, Lively SE, Lo MC, Ma J, McMinn DL, Mihalic JT, Modi K, Ngo R, Pattabiraman K, Piper DE, Queva C, Ragains ML, Suchomel J, Thibault S, Walker N, Wang X, Wang Z, Wanska M, Wehn PM, Weidner MF, Zhang AJ, Zhao X, Kamb A, Wickramasinghe D, Dai K, McGee LR, Medina JC.
J Med Chem (2014) 57 : 3430 -3449
PubMed 24641103 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 8.39 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3237702 1 9.00
CHEMBL3237704 1 9.00
CHEMBL3237711 1 9.00
CHEMBL3237442 1 8.70
CHEMBL189963 PALBOCICLIB 4.0 1 8.70
CHEMBL3237710 1 8.70
CHEMBL3237709 1 8.70
CHEMBL3237708 1 8.70
CHEMBL3237707 1 8.70
CHEMBL3237706 1 8.52
CHEMBL3237450 1 8.52
CHEMBL3237705 1 8.52
CHEMBL3237712 1 8.52
CHEMBL3237714 1 8.52
CHEMBL3237717 1 8.52
CHEMBL3237719 1 8.52
CHEMBL3237443 1 8.52
CHEMBL3237713 1 8.52
CHEMBL3237716 1 8.40
CHEMBL3237444 1 8.40
CHEMBL3237446 1 8.30
CHEMBL3237451 1 8.30
CHEMBL3237703 1 8.15
CHEMBL3237715 1 8.05
CHEMBL3237718 1 7.89
CHEMBL3237445 1 7.70
CHEMBL3237447 1 7.57
CHEMBL3237449 1 7.40
CHEMBL3237448 1 7.29
CHEMBL1336 SORAFENIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3237702 IC50 = 1.0 nM 9.00
CHEMBL3237704 IC50 = 1.0 nM 9.00
CHEMBL3237711 IC50 = 1.0 nM 9.00
CHEMBL3237442 IC50 = 2.0 nM 8.70
CHEMBL189963 PALBOCICLIB IC50 = 2.0 nM 8.70
CHEMBL3237710 IC50 = 2.0 nM 8.70
CHEMBL3237709 IC50 = 2.0 nM 8.70
CHEMBL3237708 IC50 = 2.0 nM 8.70
CHEMBL3237707 IC50 = 2.0 nM 8.70
CHEMBL3237706 IC50 = 3.0 nM 8.52
CHEMBL3237450 IC50 = 3.0 nM 8.52
CHEMBL3237705 IC50 = 3.0 nM 8.52
CHEMBL3237712 IC50 = 3.0 nM 8.52
CHEMBL3237714 IC50 = 3.0 nM 8.52
CHEMBL3237717 IC50 = 3.0 nM 8.52
CHEMBL3237719 IC50 = 3.0 nM 8.52
CHEMBL3237443 IC50 = 3.0 nM 8.52
CHEMBL3237713 IC50 = 3.0 nM 8.52
CHEMBL3237716 IC50 = 4.0 nM 8.40
CHEMBL3237444 IC50 = 4.0 nM 8.40
CHEMBL3237446 IC50 = 5.0 nM 8.30
CHEMBL3237451 IC50 = 5.0 nM 8.30
CHEMBL3237703 IC50 = 7.0 nM 8.15
CHEMBL3237715 IC50 = 9.0 nM 8.05
CHEMBL3237718 IC50 = 13.0 nM 7.89
CHEMBL3237445 IC50 = 20.0 nM 7.70
CHEMBL3237447 IC50 = 27.0 nM 7.57
CHEMBL3237449 IC50 = 40.0 nM 7.40
CHEMBL3237448 IC50 = 51.0 nM 7.29
CHEMBL1336 SORAFENIB IC50 > 3000.0 nM -