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Assay Detail

CHEMBL660782

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Binding
Inhibition of Cyclin-dependent kinase 2
9
Total Activities
9
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

Imidazo[1,2-a]pyridines: a potent and selective class of cyclin-dependent kinase inhibitors identified through structure-based hybridisation.
Anderson M, Beattie JF, Breault GA, Breed J, Byth KF, Culshaw JD, Ellston RP, Green S, Minshull CA, Norman RA, Pauptit RA, Stanway J, Thomas AP, Jewsbury PJ.
Bioorg Med Chem Lett (2003) 13 : 3021 -3026
PubMed 12941325 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.09 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL103355 1 8.22
CHEMBL102926 1 7.50
CHEMBL72461 1 7.44
CHEMBL99842 1 5.54
CHEMBL100979 1 5.40
CHEMBL102047 1 4.50
CHEMBL102622 1 4.02
CHEMBL72510 1 -
CHEMBL317445 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL103355 IC50 = 6.0 nM 8.22
CHEMBL102926 IC50 = 32.0 nM 7.50
CHEMBL72461 IC50 = 36.0 nM 7.44
CHEMBL99842 IC50 = 2900.0 nM 5.54
CHEMBL100979 IC50 = 4000.0 nM 5.40
CHEMBL102047 IC50 = 32000.0 nM 4.50
CHEMBL102622 IC50 = 95000.0 nM 4.02
CHEMBL72510 IC50 < 3.0 nM -
CHEMBL317445 IC50 > 10000.0 nM -