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Assay Detail

CHEMBL4022686

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

Binding
Inhibition of human GSK3alpha using biotin-CREB peptide substrate after 1 hr by scintillation counting method
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glycogen synthase kinase-3 alpha (CHEMBL2850)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3.
Wagman AS, Boyce RS, Brown SP, Fang E, Goff D, Jansen JM, Le VP, Levine BH, Ng SC, Ni ZJ, Nuss JM, Pfister KB, Ramurthy S, Renhowe PA, Ring DB, Shu W, Subramanian S, Zhou XA, Shafer CM, Harrison SD, Johnson KW, Bussiere DE.
J Med Chem (2017) 60 : 8482 -8514
PubMed 29016121 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.94 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3185148 1 8.15
CHEMBL412142 LADUVIGLUSIB 1.0 1 8.11
CHEMBL1080901 1 7.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3185148 IC50 = 7.0 nM 8.15
CHEMBL412142 LADUVIGLUSIB IC50 = 7.8 nM 8.11
CHEMBL1080901 IC50 = 27.1 nM 7.57