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Assay Detail

CHEMBL5227478

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

Binding
Inhibition of recombinant Plasmodium falciparum GSK3 using GS-1 peptide as substrate in presence of [gamma-32P]ATP measured after 30 mins incubation by scintillation counting analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Plasmodium falciparum
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 7 6.43 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 8.00
CHEMBL361708 HYMENIALDISINE 1 7.64
CHEMBL216543 1 7.19
CHEMBL50894 ALSTERPAULLONE 1 6.50
CHEMBL5280328 1 5.82
CHEMBL296586 KENPAULLONE 1 5.10
CHEMBL430574 PAULLONE 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 10.0 nM 8.00
CHEMBL361708 HYMENIALDISINE IC50 = 23.0 nM 7.64
CHEMBL216543 IC50 = 65.0 nM 7.19
CHEMBL50894 ALSTERPAULLONE IC50 = 320.0 nM 6.50
CHEMBL5280328 IC50 = 1500.0 nM 5.82
CHEMBL296586 KENPAULLONE IC50 = 8000.0 nM 5.10
CHEMBL430574 PAULLONE IC50 = 18000.0 nM 4.75