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Assay Detail

CHEMBL686304

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

Binding
Inhibition of glycogen synthase kinase-3 (GSK3-beta)
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Glycogen synthase kinase-3 (CHEMBL2095188)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Novel GSK-3 inhibitors with improved cellular activity.
Peat AJ, Garrido D, Boucheron JA, Schweiker SL, Dickerson SH, Wilson JR, Wang TY, Thomson SA.
Bioorg Med Chem Lett (2004) 14 : 2127 -2130
PubMed 15080993 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.93 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL304533 PYRAZOLOPYRIMIDINE 1 1 8.80
CHEMBL66292 PYRAZOLOPYRIMIDINE 2 1 8.60
CHEMBL65944 1 8.40
CHEMBL69687 1 8.30
CHEMBL66072 1 8.30
CHEMBL66860 1 8.20
CHEMBL306865 GW784752X 1 8.20
CHEMBL65884 GW817396X 1 8.10
CHEMBL67374 1 7.80
CHEMBL66993 1 7.70
CHEMBL65988 1 7.50
CHEMBL63727 1 7.00
CHEMBL303926 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL304533 PYRAZOLOPYRIMIDINE 1 IC50 = 1.585 nM 8.80
CHEMBL66292 PYRAZOLOPYRIMIDINE 2 IC50 = 2.512 nM 8.60
CHEMBL65944 IC50 = 3.981 nM 8.40
CHEMBL69687 IC50 = 5.012 nM 8.30
CHEMBL66072 IC50 = 5.012 nM 8.30
CHEMBL66860 IC50 = 6.31 nM 8.20
CHEMBL306865 GW784752X IC50 = 6.31 nM 8.20
CHEMBL65884 GW817396X IC50 = 7.943 nM 8.10
CHEMBL67374 IC50 = 15.85 nM 7.80
CHEMBL66993 IC50 = 19.95 nM 7.70
CHEMBL65988 IC50 = 31.62 nM 7.50
CHEMBL63727 IC50 = 100.0 nM 7.00
CHEMBL303926 IC50 = 630.96 nM 6.20