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Assay Detail

CHEMBL4611597

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

Binding
Inhibition of GSK3 in CHO cells expressing insulin receptor assessed as activation of glycogen synthase measured after 30 mins in presence of glucose-6-phosphate by filter paper assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cricetulus griseus
Cell Type CHO
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery and optimization of novel pyridines as highly potent and selective glycogen synthase kinase 3 inhibitors.
Ramurthy S, Pfister KB, Boyce RS, Brown SP, Costales AQ, Desai MC, Fang E, Levine BH, Ng SC, Nuss JM, Ring DB, Shafer CM, Shu W, Subramanian S, Wagman AS, Wang H, Bussiere DE.
Bioorg Med Chem Lett (2020) 30 : 126930 -126930
PubMed 31926786 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 6.34 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4644888 1 7.40
CHEMBL4644014 1 7.16
CHEMBL412142 LADUVIGLUSIB 1.0 1 6.89
CHEMBL1242830 1 6.89
CHEMBL4645243 1 6.85
CHEMBL4635530 1 6.66
CHEMBL4635592 1 6.54
CHEMBL4637210 1 6.51
CHEMBL4649659 1 6.29
CHEMBL4647324 1 6.28
CHEMBL4639648 1 6.12
CHEMBL4643626 1 6.12
CHEMBL4635565 1 5.98
CHEMBL4645239 1 5.97
CHEMBL4642372 1 5.87
CHEMBL4644060 1 5.85
CHEMBL4636986 1 5.80
CHEMBL4649593 1 5.75
CHEMBL4649815 1 5.52
CHEMBL4637962 1 -
CHEMBL4647951 1 -
CHEMBL4638891 1 -
CHEMBL4636121 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4644888 EC50 = 40.0 nM 7.40
CHEMBL4644014 EC50 = 70.0 nM 7.16
CHEMBL412142 LADUVIGLUSIB EC50 = 130.0 nM 6.89
CHEMBL1242830 EC50 = 130.0 nM 6.89
CHEMBL4645243 EC50 = 140.0 nM 6.85
CHEMBL4635530 EC50 = 220.0 nM 6.66
CHEMBL4635592 EC50 = 290.0 nM 6.54
CHEMBL4637210 EC50 = 310.0 nM 6.51
CHEMBL4649659 EC50 = 510.0 nM 6.29
CHEMBL4647324 EC50 = 530.0 nM 6.28
CHEMBL4639648 EC50 = 760.0 nM 6.12
CHEMBL4643626 EC50 = 760.0 nM 6.12
CHEMBL4635565 EC50 = 1050.0 nM 5.98
CHEMBL4645239 EC50 = 1080.0 nM 5.97
CHEMBL4642372 EC50 = 1350.0 nM 5.87
CHEMBL4644060 EC50 = 1400.0 nM 5.85
CHEMBL4636986 EC50 = 1600.0 nM 5.80
CHEMBL4649593 EC50 = 1800.0 nM 5.75
CHEMBL4649815 EC50 = 3000.0 nM 5.52
CHEMBL4637962 EC50 - -
CHEMBL4647951 EC50 - -
CHEMBL4638891 EC50 - -
CHEMBL4636121 EC50 - -