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Assay Detail

CHEMBL5227420

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

Binding
Inhibition of CDK2/Cyclin A (unknown origin)
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Fused-azepinones: Emerging scaffolds of medicinal importance.
Akunuri R, Vadakattu M, Bujji S, Veerareddy V, Madhavi YV, Nanduri S.
Eur J Med Chem (2021) 220 : 113445 -113445
PubMed 33901899 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.46 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50894 ALSTERPAULLONE 1 7.82
CHEMBL299756 PAULLONE 2 1 7.62
CHEMBL361708 HYMENIALDISINE 1 7.16
CHEMBL259638 CAZPAULLONE 1 6.30
CHEMBL296586 KENPAULLONE 1 6.17
CHEMBL336961 AZAKENPAULLONE 1 5.70
CHEMBL1782168 1 5.68
CHEMBL1782169 1 5.21
CHEMBL1782170 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50894 ALSTERPAULLONE IC50 = 15.0 nM 7.82
CHEMBL299756 PAULLONE 2 IC50 = 24.0 nM 7.62
CHEMBL361708 HYMENIALDISINE IC50 = 70.0 nM 7.16
CHEMBL259638 CAZPAULLONE IC50 = 500.0 nM 6.30
CHEMBL296586 KENPAULLONE IC50 = 680.0 nM 6.17
CHEMBL336961 AZAKENPAULLONE IC50 = 2000.0 nM 5.70
CHEMBL1782168 IC50 = 2100.0 nM 5.68
CHEMBL1782169 IC50 = 6200.0 nM 5.21
CHEMBL1782170 IC50 > 10000.0 nM -