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Assay Detail

CHEMBL952109

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Binding
Inhibition of CDK2
68
Total Activities
68
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Cyclin-dependent kinase 2 (CHEMBL301)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of kinase inhibitors by high-throughput docking and scoring based on a transferable linear interaction energy model.
Kolb P, Huang D, Dey F, Caflisch A.
J Med Chem (2008) 51 : 1179 -1188
PubMed 18271520 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 68 7.87 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL411224 1 8.92
CHEMBL445945 1 8.82
CHEMBL270544 GW396574X 1 8.82
CHEMBL409892 GW305178X 1 8.80
CHEMBL271136 1 8.77
CHEMBL429142 1 8.72
CHEMBL411887 1 8.70
CHEMBL409731 1 8.68
CHEMBL271953 1 8.68
CHEMBL269882 1 8.66
CHEMBL269827 GW276655X 1 8.64
CHEMBL411426 1 8.60
CHEMBL270132 1 8.60
CHEMBL271595 GW297361X 1 8.55
CHEMBL269883 GW416981X 1 8.52
CHEMBL271160 1 8.47
CHEMBL410883 1 8.35
CHEMBL314397 1 8.34
CHEMBL272667 1 8.34
CHEMBL410072 GW301784X 1 8.17
CHEMBL407709 1 8.15
CHEMBL411425 1 8.10
CHEMBL408210 1 8.05
CHEMBL272165 GW300657X 1 8.05
CHEMBL272380 1 8.03
CHEMBL271952 1 8.02
CHEMBL409690 1 8.00
CHEMBL273060 1 7.96
CHEMBL272028 GW300660X 1 7.92
CHEMBL411865 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL411224 IC50 = 1.2 nM 8.92
CHEMBL445945 IC50 = 1.5 nM 8.82
CHEMBL270544 GW396574X IC50 = 1.5 nM 8.82
CHEMBL409892 GW305178X IC50 = 1.6 nM 8.80
CHEMBL271136 IC50 = 1.7 nM 8.77
CHEMBL429142 IC50 = 1.9 nM 8.72
CHEMBL411887 IC50 = 2.0 nM 8.70
CHEMBL409731 IC50 = 2.1 nM 8.68
CHEMBL271953 IC50 = 2.1 nM 8.68
CHEMBL269882 IC50 = 2.2 nM 8.66
CHEMBL269827 GW276655X IC50 = 2.3 nM 8.64
CHEMBL411426 IC50 = 2.5 nM 8.60
CHEMBL270132 IC50 = 2.5 nM 8.60
CHEMBL271595 GW297361X IC50 = 2.8 nM 8.55
CHEMBL269883 GW416981X IC50 = 3.0 nM 8.52
CHEMBL271160 IC50 = 3.4 nM 8.47
CHEMBL410883 IC50 = 4.5 nM 8.35
CHEMBL314397 IC50 = 4.6 nM 8.34
CHEMBL272667 IC50 = 4.6 nM 8.34
CHEMBL410072 GW301784X IC50 = 6.8 nM 8.17
CHEMBL407709 IC50 = 7.1 nM 8.15
CHEMBL411425 IC50 = 7.9 nM 8.10
CHEMBL408210 IC50 = 8.9 nM 8.05
CHEMBL272165 GW300657X IC50 = 8.9 nM 8.05
CHEMBL272380 IC50 = 9.3 nM 8.03
CHEMBL271952 IC50 = 9.5 nM 8.02
CHEMBL409690 IC50 = 10.0 nM 8.00
CHEMBL273060 IC50 = 11.0 nM 7.96
CHEMBL272028 GW300660X IC50 = 12.0 nM 7.92
CHEMBL411865 IC50 = 12.0 nM 7.92
CHEMBL260103 IC50 = 12.0 nM 7.92
CHEMBL272833 IC50 = 13.0 nM 7.89
CHEMBL409104 IC50 = 13.0 nM 7.89
CHEMBL411490 IC50 = 13.0 nM 7.89
CHEMBL412091 IC50 = 15.0 nM 7.82
CHEMBL411886 IC50 = 15.0 nM 7.82
CHEMBL272389 IC50 = 16.0 nM 7.80
CHEMBL409868 IC50 = 17.0 nM 7.77
CHEMBL272684 IC50 = 19.0 nM 7.72
CHEMBL272217 IC50 = 21.0 nM 7.68
CHEMBL271182 IC50 = 21.0 nM 7.68
CHEMBL412097 IC50 = 22.0 nM 7.66
CHEMBL272026 GW290597X IC50 = 25.0 nM 7.60
CHEMBL272668 IC50 = 28.0 nM 7.55
CHEMBL273061 IC50 = 34.0 nM 7.47
CHEMBL272387 IC50 = 43.0 nM 7.37
CHEMBL271183 IC50 = 43.0 nM 7.37
CHEMBL270054 GW280670X IC50 = 43.0 nM 7.37
CHEMBL271843 GW275944X IC50 = 46.0 nM 7.34
CHEMBL271137 IC50 = 54.0 nM 7.27