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Assay Detail

CHEMBL5227427

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

Binding
Inhibition of rabbit muscle GSK3beta in presence of gamma32P-ATP
26
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 26 6.77 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50894 ALSTERPAULLONE 1 8.40
CHEMBL259638 CAZPAULLONE 1 8.10
CHEMBL361708 HYMENIALDISINE 1 8.00
CHEMBL336961 AZAKENPAULLONE 1 7.75
CHEMBL296586 KENPAULLONE 1 7.64
CHEMBL1233473 1 7.33
CHEMBL5277152 1 7.33
CHEMBL480350 1 7.29
CHEMBL5281583 1 7.29
CHEMBL5285766 1 7.28
CHEMBL481333 1 7.19
CHEMBL5272006 1 7.06
CHEMBL5271328 1 7.05
CHEMBL255465 DEBROMOHYMENIALDISINE 2 6.96
CHEMBL5267995 1 6.44
CHEMBL5265856 1 6.25
CHEMBL5280645 1 6.21
CHEMBL1782168 1 6.09
CHEMBL5272265 1 5.86
CHEMBL512682 SPONGIACIDIN D 1 5.52
CHEMBL1782169 1 5.47
CHEMBL323657 1 5.40
CHEMBL5267075 1 5.37
CHEMBL134501 1 4.92
CHEMBL1782170 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50894 ALSTERPAULLONE IC50 = 4.0 nM 8.40
CHEMBL259638 CAZPAULLONE IC50 = 8.0 nM 8.10
CHEMBL361708 HYMENIALDISINE IC50 = 10.0 nM 8.00
CHEMBL336961 AZAKENPAULLONE IC50 = 18.0 nM 7.75
CHEMBL296586 KENPAULLONE IC50 = 23.0 nM 7.64
CHEMBL1233473 IC50 = 47.0 nM 7.33
CHEMBL5277152 IC50 = 47.0 nM 7.33
CHEMBL480350 IC50 = 51.0 nM 7.29
CHEMBL5281583 IC50 = 51.0 nM 7.29
CHEMBL5285766 IC50 = 52.0 nM 7.28
CHEMBL481333 IC50 = 64.0 nM 7.19
CHEMBL5272006 IC50 = 88.0 nM 7.06
CHEMBL5271328 IC50 = 90.0 nM 7.05
CHEMBL255465 DEBROMOHYMENIALDISINE IC50 = 110.0 nM 6.96
CHEMBL255465 DEBROMOHYMENIALDISINE IC50 = 111.0 nM 6.96
CHEMBL5267995 IC50 = 363.0 nM 6.44
CHEMBL5265856 IC50 = 557.0 nM 6.25
CHEMBL5280645 IC50 = 613.0 nM 6.21
CHEMBL1782168 IC50 = 810.0 nM 6.09
CHEMBL5272265 IC50 = 1388.0 nM 5.86
CHEMBL512682 SPONGIACIDIN D IC50 = 3000.0 nM 5.52
CHEMBL1782169 IC50 = 3400.0 nM 5.47
CHEMBL323657 IC50 = 4000.0 nM 5.40
CHEMBL5267075 IC50 = 4280.0 nM 5.37
CHEMBL134501 IC50 = 12000.0 nM 4.92
CHEMBL1782170 IC50 > 10000.0 nM -