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Assay Detail

CHEMBL4611596

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

Binding
Inhibition of GSK3 (unknown origin) using CREB peptide as substrate
23
Total Activities
23
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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
IC50 22 7.39 8.30
EC50 1 6.11 6.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4647324 1 8.30
CHEMBL1242830 1 8.10
CHEMBL4645243 1 7.96
CHEMBL4649659 1 7.96
CHEMBL4636986 1 7.92
CHEMBL4644060 1 7.89
CHEMBL4644888 1 7.89
CHEMBL4644014 1 7.89
CHEMBL4635530 1 7.82
CHEMBL4649593 1 7.75
CHEMBL4642372 1 7.54
CHEMBL4637210 1 7.44
CHEMBL4639648 1 7.36
CHEMBL4635592 1 7.28
CHEMBL4643626 1 7.24
CHEMBL4635565 1 7.18
CHEMBL4645239 1 7.16
CHEMBL4649815 1 7.13
CHEMBL4647951 1 6.70
CHEMBL4638891 1 6.68
CHEMBL412142 LADUVIGLUSIB 1.0 1 6.11
CHEMBL4636121 1 6.00
CHEMBL4637962 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4647324 IC50 = 5.0 nM 8.30
CHEMBL1242830 IC50 = 8.0 nM 8.10
CHEMBL4645243 IC50 = 11.0 nM 7.96
CHEMBL4649659 IC50 = 11.0 nM 7.96
CHEMBL4636986 IC50 = 12.0 nM 7.92
CHEMBL4644060 IC50 = 13.0 nM 7.89
CHEMBL4644888 IC50 = 13.0 nM 7.89
CHEMBL4644014 IC50 = 13.0 nM 7.89
CHEMBL4635530 IC50 = 15.0 nM 7.82
CHEMBL4649593 IC50 = 18.0 nM 7.75
CHEMBL4642372 IC50 = 29.0 nM 7.54
CHEMBL4637210 IC50 = 36.0 nM 7.44
CHEMBL4639648 IC50 = 44.0 nM 7.36
CHEMBL4635592 IC50 = 52.0 nM 7.28
CHEMBL4643626 IC50 = 57.0 nM 7.24
CHEMBL4635565 IC50 = 66.0 nM 7.18
CHEMBL4645239 IC50 = 69.0 nM 7.16
CHEMBL4649815 IC50 = 74.0 nM 7.13
CHEMBL4647951 IC50 = 202.0 nM 6.70
CHEMBL4638891 IC50 = 207.0 nM 6.68
CHEMBL412142 LADUVIGLUSIB EC50 = 770.0 nM 6.11
CHEMBL4636121 IC50 = 1012.0 nM 6.00
CHEMBL4637962 IC50 = 3700.0 nM 5.43