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Assay Detail

CHEMBL829439

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

Binding
Inhibition of Cyclin A-cyclin-dependent kinase 2
75
Total Activities
73
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Cyclin-dependent kinase 2/cyclin A (CHEMBL2094128)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Benzodipyrazoles: a new class of potent CDK2 inhibitors.
D'Alessio R, Bargiotti A, Metz S, Brasca MG, Cameron A, Ermoli A, Marsiglio A, Polucci P, Roletto F, Tibolla M, Vazquez ML, Vulpetti A, Pevarello P.
Bioorg Med Chem Lett (2005) 15 : 1315 -1319
PubMed 15713378 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 75 6.93 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL360520 1 9.52
CHEMBL361595 1 9.00
CHEMBL181036 1 8.70
CHEMBL181616 1 8.70
CHEMBL182209 1 8.70
CHEMBL361862 1 8.40
CHEMBL179588 1 8.30
CHEMBL178827 1 8.10
CHEMBL178190 1 8.10
CHEMBL178629 1 8.05
CHEMBL554716 1 8.05
CHEMBL178750 1 8.00
CHEMBL178478 1 7.89
CHEMBL360986 2 7.85
CHEMBL367798 1 7.82
CHEMBL360480 1 7.75
CHEMBL178572 1 7.70
CHEMBL181790 1 7.70
CHEMBL368043 1 7.55
CHEMBL369522 1 7.55
CHEMBL181223 1 7.54
CHEMBL359461 1 7.54
CHEMBL178408 1 7.52
CHEMBL362829 1 7.44
CHEMBL362656 1 7.43
CHEMBL180379 1 7.40
CHEMBL367363 1 7.21
CHEMBL179599 1 7.12
CHEMBL362004 1 7.11
CHEMBL426059 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL360520 IC50 = 0.3 nM 9.52
CHEMBL361595 IC50 = 1.0 nM 9.00
CHEMBL181616 IC50 = 2.0 nM 8.70
CHEMBL182209 IC50 = 2.0 nM 8.70
CHEMBL181036 IC50 = 2.0 nM 8.70
CHEMBL361862 IC50 = 4.0 nM 8.40
CHEMBL179588 IC50 = 5.0 nM 8.30
CHEMBL178827 IC50 = 8.0 nM 8.10
CHEMBL178190 IC50 = 8.0 nM 8.10
CHEMBL178629 IC50 = 9.0 nM 8.05
CHEMBL554716 IC50 = 9.0 nM 8.05
CHEMBL178750 IC50 = 10.0 nM 8.00
CHEMBL178478 IC50 = 13.0 nM 7.89
CHEMBL360986 IC50 = 14.0 nM 7.85
CHEMBL367798 IC50 = 15.0 nM 7.82
CHEMBL360480 IC50 = 18.0 nM 7.75
CHEMBL181790 IC50 = 20.0 nM 7.70
CHEMBL178572 IC50 = 20.0 nM 7.70
CHEMBL368043 IC50 = 28.0 nM 7.55
CHEMBL369522 IC50 = 28.0 nM 7.55
CHEMBL359461 IC50 = 29.0 nM 7.54
CHEMBL181223 IC50 = 29.0 nM 7.54
CHEMBL178408 IC50 = 30.0 nM 7.52
CHEMBL362829 IC50 = 36.0 nM 7.44
CHEMBL362656 IC50 = 37.0 nM 7.43
CHEMBL180379 IC50 = 40.0 nM 7.40
CHEMBL367363 IC50 = 62.0 nM 7.21
CHEMBL179599 IC50 = 75.0 nM 7.12
CHEMBL362004 IC50 = 78.0 nM 7.11
CHEMBL426059 IC50 = 80.0 nM 7.10
CHEMBL178452 IC50 = 87.0 nM 7.06
CHEMBL181828 IC50 = 140.0 nM 6.85
CHEMBL179548 IC50 = 140.0 nM 6.85
CHEMBL360986 IC50 = 140.0 nM 6.85
CHEMBL360695 IC50 = 150.0 nM 6.82
CHEMBL181462 IC50 = 150.0 nM 6.82
CHEMBL178505 IC50 = 160.0 nM 6.80
CHEMBL180265 IC50 = 160.0 nM 6.80
CHEMBL180715 IC50 = 180.0 nM 6.75
CHEMBL359737 IC50 = 190.0 nM 6.72
CHEMBL360312 IC50 = 200.0 nM 6.70
CHEMBL179921 IC50 = 210.0 nM 6.68
CHEMBL360149 IC50 = 210.0 nM 6.68
CHEMBL178107 IC50 = 210.0 nM 6.68
CHEMBL368433 IC50 = 210.0 nM 6.68
CHEMBL179511 IC50 = 250.0 nM 6.60
CHEMBL440379 IC50 = 260.0 nM 6.58
CHEMBL178183 IC50 = 270.0 nM 6.57
CHEMBL182256 IC50 = 290.0 nM 6.54
CHEMBL179112 IC50 = 310.0 nM 6.51