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Assay Detail

CHEMBL3112014

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

Binding
Inhibition of GSK-3beta (unknown origin) using (RREGGMSRPAS(p)VDG as substrate assessed as 32P[gamma-ATP] incorporation into substrate after 15 mins by autoradiography
12
Total Activities
12
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 beta (CHEMBL262)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of 1-phenylpyrazolo[3,4-e]pyrrolo[3,4-g]indolizine-4,6(1H,5H)-diones as new glycogen synthase kinase-3β inhibitors.
La Pietra V, La Regina G, Coluccia A, Famiglini V, Pelliccia S, Plotkin B, Eldar-Finkelman H, Brancale A, Ballatore C, Crowe A, Brunden KR, Marinelli L, Novellino E, Silvestri R.
J Med Chem (2013) 56 : 10066 -10078
PubMed 24295046 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.19 6.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL355496 1 6.76
CHEMBL3110144 1 6.62
CHEMBL3110142 1 6.36
CHEMBL3110140 1 6.16
CHEMBL3110135 1 6.09
CHEMBL3110143 1 6.03
CHEMBL3110139 1 6.00
CHEMBL3110138 1 5.92
CHEMBL3110134 1 5.77
CHEMBL3110141 1 -
CHEMBL3110137 1 -
CHEMBL3110136 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL355496 IC50 = 174.0 nM 6.76
CHEMBL3110144 IC50 = 240.0 nM 6.62
CHEMBL3110142 IC50 = 440.0 nM 6.36
CHEMBL3110140 IC50 = 690.0 nM 6.16
CHEMBL3110135 IC50 = 810.0 nM 6.09
CHEMBL3110143 IC50 = 940.0 nM 6.03
CHEMBL3110139 IC50 = 1000.0 nM 6.00
CHEMBL3110138 IC50 = 1210.0 nM 5.92
CHEMBL3110134 IC50 = 1690.0 nM 5.77
CHEMBL3110141 IC50 - -
CHEMBL3110137 IC50 - -
CHEMBL3110136 IC50 - -