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Assay Detail

CHEMBL683005

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

Binding
Inhibition of porcine GSK-3-alpha/beta kinase
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Glycogen synthase kinase-3 (CHEMBL2095188)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Generation of new protein kinase inhibitors utilizing cytochrome p450 mutant enzymes for indigoid synthesis.
Guengerich FP, Sorrells JL, Schmitt S, Krauser JA, Aryal P, Meijer L.
J Med Chem (2004) 47 : 3236 -3241
PubMed 15163202 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.03 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL321194 1 6.70
CHEMBL326919 1 6.26
CHEMBL321192 1 6.22
CHEMBL111624 1 6.10
CHEMBL111433 1 6.10
CHEMBL1276127 INDIRUBIN 2.0 1 5.60
CHEMBL114396 1 5.22
CHEMBL109622 1 -
CHEMBL599552 INDIGO 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL321194 IC50 = 200.0 nM 6.70
CHEMBL326919 IC50 = 550.0 nM 6.26
CHEMBL321192 IC50 = 600.0 nM 6.22
CHEMBL111624 IC50 = 800.0 nM 6.10
CHEMBL111433 IC50 = 800.0 nM 6.10
CHEMBL1276127 INDIRUBIN IC50 = 2500.0 nM 5.60
CHEMBL114396 IC50 = 6000.0 nM 5.22
CHEMBL109622 IC50 > 100000.0 nM -
CHEMBL599552 INDIGO IC50 > 100000.0 nM -