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Assay Detail

CHEMBL925067

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Binding
Inhibition of GSK3
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Structure based de novo design of novel glycogen synthase kinase 3 inhibitors.
Dessalew N, Bharatam PV.
Bioorg Med Chem (2007) 15 : 3728 -3736
PubMed 17399989 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 8.09 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL181031 BISARYLMALEIMIDE 1 1 9.15
CHEMBL178766 BISARYLMALEIMIDE 2 1 9.10
CHEMBL304533 PYRAZOLOPYRIMIDINE 1 1 8.80
CHEMBL66292 PYRAZOLOPYRIMIDINE 2 1 8.60
CHEMBL427882 1 8.40
CHEMBL253769 INDIRUBIN 1 1 8.40
CHEMBL50894 ALSTERPAULLONE 1 8.40
CHEMBL253770 INDIRUBIN 2 1 8.30
CHEMBL187081 PYRAZOLOPYRIDAZINE 1 1 8.00
CHEMBL361708 HYMENIALDISINE 1 8.00
CHEMBL299756 PAULLONE 2 1 8.00
CHEMBL186054 PYRAZOLOPYRIDAZINE 2 1 7.92
CHEMBL340935 INDOLYLYLMALEIMIDE 1 1 7.77
CHEMBL340259 INDOLYLYLMALEIMIDE 2 1 7.66
CHEMBL102714 SB-216763 1 7.47
CHEMBL398498 HYMENIALDISINE 2 1 6.89
CHEMBL7463 GF-109203 1 6.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL181031 BISARYLMALEIMIDE 1 IC50 = 0.7 nM 9.15
CHEMBL178766 BISARYLMALEIMIDE 2 IC50 = 0.8 nM 9.10
CHEMBL304533 PYRAZOLOPYRIMIDINE 1 IC50 = 1.585 nM 8.80
CHEMBL66292 PYRAZOLOPYRIMIDINE 2 IC50 = 2.512 nM 8.60
CHEMBL427882 IC50 = 4.0 nM 8.40
CHEMBL253769 INDIRUBIN 1 IC50 = 4.0 nM 8.40
CHEMBL50894 ALSTERPAULLONE IC50 = 4.0 nM 8.40
CHEMBL253770 INDIRUBIN 2 IC50 = 5.0 nM 8.30
CHEMBL187081 PYRAZOLOPYRIDAZINE 1 IC50 = 10.0 nM 8.00
CHEMBL361708 HYMENIALDISINE IC50 = 10.0 nM 8.00
CHEMBL299756 PAULLONE 2 IC50 = 10.0 nM 8.00
CHEMBL186054 PYRAZOLOPYRIDAZINE 2 IC50 = 12.0 nM 7.92
CHEMBL340935 INDOLYLYLMALEIMIDE 1 IC50 = 17.0 nM 7.77
CHEMBL340259 INDOLYLYLMALEIMIDE 2 IC50 = 22.0 nM 7.66
CHEMBL102714 SB-216763 IC50 = 34.0 nM 7.47
CHEMBL398498 HYMENIALDISINE 2 IC50 = 130.0 nM 6.89
CHEMBL7463 GF-109203 IC50 = 190.0 nM 6.72