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Assay Detail

CHEMBL691184

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Functional
Increased glycogen synthase activity in HEK293 cells
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors.
Kuo GH, Prouty C, DeAngelis A, Shen L, O'Neill DJ, Shah C, Connolly PJ, Murray WV, Conway BR, Cheung P, Westover L, Xu JZ, Look RA, Demarest KT, Emanuel S, Middleton SA, Jolliffe L, Beavers MP, Chen X.
J Med Chem (2003) 46 : 4021 -4031
PubMed 12954055 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.82 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL340776 1 7.22
CHEMBL337642 1 6.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL340776 EC50 = 60.0 nM 7.22
CHEMBL337642 EC50 = 390.0 nM 6.41