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Assay Detail

CHEMBL840825

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

Functional
Effective concentration to increase glycogen deposition in rat skeletal muscle L6 myoblast cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type L6
Confidence 9 — Direct single protein target
Curated By Expert

Target

Glycogen synthase kinase-3 beta (CHEMBL3669)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

N-Phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amines as potent and selective inhibitors of glycogen synthase kinase 3 with good cellular efficacy.
Tavares FX, Boucheron JA, Dickerson SH, Griffin RJ, Preugschat F, Thomson SA, Wang TY, Zhou HQ.
J Med Chem (2004) 47 : 4716 -4730
PubMed 15341487 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 5.72 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361894 GW806290X 1 6.10
CHEMBL188665 1 6.00
CHEMBL184510 1 6.00
CHEMBL361697 1 6.00
CHEMBL360206 1 5.92
CHEMBL187081 PYRAZOLOPYRIDAZINE 1 1 5.89
CHEMBL186054 PYRAZOLOPYRIDAZINE 2 1 5.82
CHEMBL360408 1 5.80
CHEMBL186101 1 5.75
CHEMBL263448 1 5.68
CHEMBL189343 1 5.55
CHEMBL359554 1 5.54
CHEMBL364197 1 5.47
CHEMBL434158 1 5.44
CHEMBL439850 1 5.38
CHEMBL182493 1 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361894 GW806290X EC50 = 800.0 nM 6.10
CHEMBL188665 EC50 = 1000.0 nM 6.00
CHEMBL184510 EC50 = 1000.0 nM 6.00
CHEMBL361697 EC50 = 1000.0 nM 6.00
CHEMBL360206 EC50 = 1200.0 nM 5.92
CHEMBL187081 PYRAZOLOPYRIDAZINE 1 EC50 = 1300.0 nM 5.89
CHEMBL186054 PYRAZOLOPYRIDAZINE 2 EC50 = 1500.0 nM 5.82
CHEMBL360408 EC50 = 1600.0 nM 5.80
CHEMBL186101 EC50 = 1800.0 nM 5.75
CHEMBL263448 EC50 = 2100.0 nM 5.68
CHEMBL189343 EC50 = 2800.0 nM 5.55
CHEMBL359554 EC50 = 2900.0 nM 5.54
CHEMBL364197 EC50 = 3400.0 nM 5.47
CHEMBL434158 EC50 = 3600.0 nM 5.44
CHEMBL439850 EC50 = 4200.0 nM 5.38
CHEMBL182493 EC50 = 6800.0 nM 5.17