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Assay Detail

CHEMBL832403

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

Binding
Inhibition of glycogen synthase kinase-3
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and structure-activity relationships of pyrazine-pyridine biheteroaryls as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors.
Kuo GH, Prouty C, Wang A, Emanuel S, Deangelis A, Zhang Y, Song F, Beall L, Connolly PJ, Karnachi P, Chen X, Gruninger RH, Sechler J, Fuentes-Pesquera A, Middleton SA, Jolliffe L, Murray WV.
J Med Chem (2005) 48 : 4892 -4909
PubMed 16033269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.23 6.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL372657 1 6.71
CHEMBL188502 1 6.50
CHEMBL177688 1 6.32
CHEMBL371169 1 6.22
CHEMBL188386 1 5.40
CHEMBL190984 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL372657 IC50 = 196.0 nM 6.71
CHEMBL188502 IC50 = 318.0 nM 6.50
CHEMBL177688 IC50 = 478.0 nM 6.32
CHEMBL371169 IC50 = 606.0 nM 6.22
CHEMBL188386 IC50 = 4020.0 nM 5.40
CHEMBL190984 IC50 > 10000.0 nM -