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Assay Detail

CHEMBL661129

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

Binding
In vitro inhibition of Cyclin-dependent kinase 2 was determined.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Anilinopyrazole as selective CDK2 inhibitors: design, synthesis, biological evaluation, and X-ray crystallographic analysis.
Tang J, Shewchuk LM, Sato H, Hasegawa M, Washio Y, Nishigaki N.
Bioorg Med Chem Lett (2003) 13 : 2985 -2988
PubMed 12941317 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.55 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL317703 1 9.48
CHEMBL321517 1 9.47
CHEMBL103104 GW831090X 1 8.04
CHEMBL319903 1 8.00
CHEMBL421578 1 7.97
CHEMBL319103 1 7.97
CHEMBL103115 GW831091X 1 7.90
CHEMBL103382 1 7.76
CHEMBL103285 1 7.63
CHEMBL319685 1 7.61
CHEMBL321939 1 7.21
CHEMBL319831 1 6.78
CHEMBL102241 1 6.39
CHEMBL103039 1 6.31
CHEMBL418985 1 6.22
CHEMBL329040 1 6.06
CHEMBL323326 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL317703 IC50 = 0.33 nM 9.48
CHEMBL321517 IC50 = 0.34 nM 9.47
CHEMBL103104 GW831090X IC50 = 9.1 nM 8.04
CHEMBL319903 IC50 = 10.0 nM 8.00
CHEMBL421578 IC50 = 10.7 nM 7.97
CHEMBL319103 IC50 = 10.7 nM 7.97
CHEMBL103115 GW831091X IC50 = 12.6 nM 7.90
CHEMBL103382 IC50 = 17.4 nM 7.76
CHEMBL103285 IC50 = 23.4 nM 7.63
CHEMBL319685 IC50 = 24.5 nM 7.61
CHEMBL321939 IC50 = 61.6 nM 7.21
CHEMBL319831 IC50 = 166.0 nM 6.78
CHEMBL102241 IC50 = 407.0 nM 6.39
CHEMBL103039 IC50 = 490.0 nM 6.31
CHEMBL418985 IC50 = 602.0 nM 6.22
CHEMBL329040 IC50 = 871.0 nM 6.06
CHEMBL323326 IC50 > 2000.0 nM -