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Assay Detail

CHEMBL683004

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

Binding
Inhibition of glycogen synthase kinase-3-alpha/beta (GSK-3-alpha/beta) in porcine brain relative to indirubin
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases.
Polychronopoulos P, Magiatis P, Skaltsounis AL, Myrianthopoulos V, Mikros E, Tarricone A, Musacchio A, Roe SM, Pearl L, Leost M, Greengard P, Meijer L.
J Med Chem (2004) 47 : 935 -946
PubMed 14761195 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.17 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL337300 1 8.05
CHEMBL174025 1 7.38
CHEMBL367113 1 7.30
CHEMBL173682 1 7.26
CHEMBL111433 1 7.21
CHEMBL173445 1 7.17
CHEMBL367345 1 7.11
CHEMBL176676 1 6.60
CHEMBL173690 1 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL337300 IC50 = 9.0 nM 8.05
CHEMBL174025 IC50 = 42.0 nM 7.38
CHEMBL367113 IC50 = 50.0 nM 7.30
CHEMBL173682 IC50 = 55.0 nM 7.26
CHEMBL111433 IC50 = 62.0 nM 7.21
CHEMBL173445 IC50 = 68.0 nM 7.17
CHEMBL367345 IC50 = 78.0 nM 7.11
CHEMBL176676 IC50 = 250.0 nM 6.60
CHEMBL173690 IC50 = 350.0 nM 6.46