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Assay Detail

CHEMBL896714

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Binding
Inhibition of CDK2
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of a potent CDK2 inhibitor with a novel binding mode, using virtual screening and initial, structure-guided lead scoping.
Richardson CM, Nunns CL, Williamson DS, Parratt MJ, Dokurno P, Howes R, Borgognoni J, Drysdale MJ, Finch H, Hubbard RE, Jackson PS, Kierstan P, Lentzen G, Moore JD, Murray JB, Simmonite H, Surgenor AE, Torrance CJ.
Bioorg Med Chem Lett (2007) 17 : 3880 -3885
PubMed 17570665 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.82 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL231950 1 7.52
CHEMBL233553 1 6.92
CHEMBL233149 1 6.75
CHEMBL396614 1 6.24
CHEMBL233554 1 6.24
CHEMBL233970 1 6.21
CHEMBL391493 1 5.54
CHEMBL233765 1 5.03
CHEMBL396360 1 4.72
CHEMBL232148 1 4.57
CHEMBL233349 1 4.33
CHEMBL233763 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL231950 IC50 = 30.0 nM 7.52
CHEMBL233553 IC50 = 120.0 nM 6.92
CHEMBL233149 IC50 = 180.0 nM 6.75
CHEMBL396614 IC50 = 570.0 nM 6.24
CHEMBL233554 IC50 = 570.0 nM 6.24
CHEMBL233970 IC50 = 610.0 nM 6.21
CHEMBL391493 IC50 = 2900.0 nM 5.54
CHEMBL233765 IC50 = 9300.0 nM 5.03
CHEMBL396360 IC50 = 19000.0 nM 4.72
CHEMBL232148 IC50 = 27000.0 nM 4.57
CHEMBL233349 IC50 = 47000.0 nM 4.33
CHEMBL233763 IC50 = 150000.0 nM -