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Assay Detail

CHEMBL839940

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Binding
Binding affinity for human glycogen synthase kinase 3 beta
ChEMBL ↗
92
Total Activities
92
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Glycogen synthase kinase-3 beta (CHEMBL262) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

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
Ki 92 6.88 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL186054 PYRAZOLOPYRIDAZINE 2 — 1 8.00
CHEMBL182326 — — 1 8.00
CHEMBL183064 — — 1 8.00
CHEMBL365297 GW827099X — 1 8.00
CHEMBL186476 — — 1 8.00
CHEMBL439850 — — 1 8.00
CHEMBL360408 — — 1 8.00
CHEMBL434337 — — 1 8.00
CHEMBL359554 — — 1 8.00
CHEMBL187750 — — 1 8.00
CHEMBL187081 PYRAZOLOPYRIDAZINE 1 — 1 8.00
CHEMBL359999 GW801372X — 1 8.00
CHEMBL186890 — — 1 8.00
CHEMBL364370 — — 1 8.00
CHEMBL263448 — — 1 8.00
CHEMBL186680 — — 1 8.00
CHEMBL189343 — — 1 7.70
CHEMBL182493 — — 1 7.70
CHEMBL186166 — — 1 7.70
CHEMBL189459 GW833373X — 1 7.70
CHEMBL186425 — — 1 7.70
CHEMBL365251 — — 1 7.70
CHEMBL361723 — — 1 7.52
CHEMBL364197 — — 1 7.52
CHEMBL188785 — — 1 7.52
CHEMBL359963 GW805758X — 1 7.52
CHEMBL434729 GW829906X — 1 7.40
CHEMBL189288 — — 1 7.40
CHEMBL361038 — — 1 7.30
CHEMBL434158 — — 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL186054 PYRAZOLOPYRIDAZINE 2 Ki = 10.0 nM 8.00
CHEMBL263448 — Ki = 10.0 nM 8.00
CHEMBL182326 — Ki = 10.0 nM 8.00
CHEMBL183064 — Ki = 10.0 nM 8.00
CHEMBL365297 GW827099X Ki = 10.0 nM 8.00
CHEMBL186476 — Ki = 10.0 nM 8.00
CHEMBL439850 — Ki = 10.0 nM 8.00
CHEMBL360408 — Ki = 10.0 nM 8.00
CHEMBL434337 — Ki = 10.0 nM 8.00
CHEMBL186680 — Ki = 10.0 nM 8.00
CHEMBL359554 — Ki = 10.0 nM 8.00
CHEMBL187750 — Ki = 10.0 nM 8.00
CHEMBL187081 PYRAZOLOPYRIDAZINE 1 Ki = 10.0 nM 8.00
CHEMBL359999 GW801372X Ki = 10.0 nM 8.00
CHEMBL186890 — Ki = 10.0 nM 8.00
CHEMBL364370 — Ki = 10.0 nM 8.00
CHEMBL365251 — Ki = 20.0 nM 7.70
CHEMBL186425 — Ki = 20.0 nM 7.70
CHEMBL189459 GW833373X Ki = 20.0 nM 7.70
CHEMBL189343 — Ki = 20.0 nM 7.70
CHEMBL186166 — Ki = 20.0 nM 7.70
CHEMBL182493 — Ki = 20.0 nM 7.70
CHEMBL359963 GW805758X Ki = 30.0 nM 7.52
CHEMBL188785 — Ki = 30.0 nM 7.52
CHEMBL361723 — Ki = 30.0 nM 7.52
CHEMBL364197 — Ki = 30.0 nM 7.52
CHEMBL434729 GW829906X Ki = 40.0 nM 7.40
CHEMBL189288 — Ki = 40.0 nM 7.40
CHEMBL361038 — Ki = 50.0 nM 7.30
CHEMBL434158 — Ki = 50.0 nM 7.30
CHEMBL365248 GW810372X Ki = 50.0 nM 7.30
CHEMBL362155 GW827102X Ki = 50.0 nM 7.30
CHEMBL189352 — Ki = 50.0 nM 7.30
CHEMBL189235 — Ki = 50.0 nM 7.30
CHEMBL364587 — Ki = 50.0 nM 7.30
CHEMBL188303 — Ki = 50.0 nM 7.30
CHEMBL186288 — Ki = 70.0 nM 7.16
CHEMBL180593 — Ki = 80.0 nM 7.10
CHEMBL188312 — Ki = 100.0 nM 7.00
CHEMBL186010 — Ki = 100.0 nM 7.00
CHEMBL188417 — Ki = 120.0 nM 6.92
CHEMBL186606 — Ki = 120.0 nM 6.92
CHEMBL185871 — Ki = 120.0 nM 6.92
CHEMBL189415 GW819077X Ki = 150.0 nM 6.82
CHEMBL185910 — Ki = 150.0 nM 6.82
CHEMBL189617 — Ki = 150.0 nM 6.82
CHEMBL183993 GW811761X Ki = 190.0 nM 6.72
CHEMBL187139 — Ki = 190.0 nM 6.72
CHEMBL184656 — Ki = 310.0 nM 6.51
CHEMBL184657 — Ki = 630.0 nM 6.20