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Assay Detail

CHEMBL5227418

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

Binding
Inhibition of CDK1/Cyclin B (unknown origin) in presence of gamma32P-ATP by scintillation counter analysis
23
Total Activities
22
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 1/cyclin B (CHEMBL2094127)
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 23 6.22 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361708 HYMENIALDISINE 1 7.66
CHEMBL299756 PAULLONE 2 1 7.62
CHEMBL50894 ALSTERPAULLONE 1 7.46
CHEMBL1233473 1 6.66
CHEMBL255465 DEBROMOHYMENIALDISINE 2 6.60
CHEMBL296586 KENPAULLONE 1 6.40
CHEMBL259638 CAZPAULLONE 1 6.30
CHEMBL480350 1 6.28
CHEMBL5285766 1 6.26
CHEMBL323657 1 6.22
CHEMBL481333 1 6.10
CHEMBL5277152 1 6.00
CHEMBL5267995 1 5.82
CHEMBL5271328 1 5.82
CHEMBL336961 AZAKENPAULLONE 1 5.70
CHEMBL1782168 1 5.68
CHEMBL5281583 1 5.64
CHEMBL512682 SPONGIACIDIN D 1 5.40
CHEMBL1782169 1 5.24
CHEMBL134501 1 5.08
CHEMBL5272265 1 -
CHEMBL1782170 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361708 HYMENIALDISINE IC50 = 22.0 nM 7.66
CHEMBL299756 PAULLONE 2 IC50 = 24.0 nM 7.62
CHEMBL50894 ALSTERPAULLONE IC50 = 35.0 nM 7.46
CHEMBL1233473 IC50 = 220.0 nM 6.66
CHEMBL255465 DEBROMOHYMENIALDISINE IC50 = 250.0 nM 6.60
CHEMBL255465 DEBROMOHYMENIALDISINE IC50 = 250.0 nM 6.60
CHEMBL296586 KENPAULLONE IC50 = 400.0 nM 6.40
CHEMBL259638 CAZPAULLONE IC50 = 500.0 nM 6.30
CHEMBL480350 IC50 = 530.0 nM 6.28
CHEMBL5285766 IC50 = 550.0 nM 6.26
CHEMBL323657 IC50 = 600.0 nM 6.22
CHEMBL481333 IC50 = 800.0 nM 6.10
CHEMBL5277152 IC50 = 1000.0 nM 6.00
CHEMBL5267995 IC50 = 1500.0 nM 5.82
CHEMBL5271328 IC50 = 1500.0 nM 5.82
CHEMBL336961 AZAKENPAULLONE IC50 = 2000.0 nM 5.70
CHEMBL1782168 IC50 = 2100.0 nM 5.68
CHEMBL5281583 IC50 = 2300.0 nM 5.64
CHEMBL512682 SPONGIACIDIN D IC50 = 4000.0 nM 5.40
CHEMBL1782169 IC50 = 5700.0 nM 5.24
CHEMBL134501 IC50 = 8400.0 nM 5.08
CHEMBL5272265 IC50 > 10000.0 nM -
CHEMBL1782170 IC50 > 10000.0 nM -