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Assay Detail

CHEMBL1119481

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Binding
Inhibition of CDK2
16
Total Activities
16
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 N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.
Wang S, Midgley CA, Scaërou F, Grabarek JB, Griffiths G, Jackson W, Kontopidis G, McClue SJ, McInnes C, Meades C, Mezna M, Plater A, Stuart I, Thomas MP, Wood G, Clarke RG, Blake DG, Zheleva DI, Lane DP, Jackson RC, Glover DM, Fischer PM.
J Med Chem (2010) 53 : 4367 -4378
PubMed 20462263 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.64 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL298445 1 8.70
CHEMBL1084715 1 7.50
CHEMBL1084630 1 6.82
CHEMBL1084629 1 6.81
CHEMBL1084454 1 6.78
CHEMBL1083151 1 6.62
CHEMBL46817 1 6.60
CHEMBL1083152 1 6.59
CHEMBL1083150 1 6.54
CHEMBL1083785 1 6.53
CHEMBL482967 CYC-116 1.0 1 6.41
CHEMBL1083786 1 6.37
CHEMBL1086088 1 6.33
CHEMBL1084969 1 6.28
CHEMBL1085626 1 5.98
CHEMBL1083484 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL298445 Ki = 2.0 nM 8.70
CHEMBL1084715 Ki = 32.0 nM 7.50
CHEMBL1084630 Ki = 151.0 nM 6.82
CHEMBL1084629 Ki = 156.0 nM 6.81
CHEMBL1084454 Ki = 168.0 nM 6.78
CHEMBL1083151 Ki = 239.0 nM 6.62
CHEMBL46817 Ki = 251.0 nM 6.60
CHEMBL1083152 Ki = 256.0 nM 6.59
CHEMBL1083150 Ki = 286.0 nM 6.54
CHEMBL1083785 Ki = 297.0 nM 6.53
CHEMBL482967 CYC-116 Ki = 390.0 nM 6.41
CHEMBL1083786 Ki = 432.0 nM 6.37
CHEMBL1086088 Ki = 463.0 nM 6.33
CHEMBL1084969 Ki = 522.0 nM 6.28
CHEMBL1085626 Ki = 1039.0 nM 5.98
CHEMBL1083484 Ki = 3967.0 nM 5.40