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Assay Detail

CHEMBL686322

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Binding
Inhibition of Glycogen synthase kinase-3 beta
12
Total Activities
12
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

Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.
Zhang HC, White KB, Ye H, McComsey DF, Derian CK, Addo MF, Andrade-Gordon P, Eckardt AJ, Conway BR, Westover L, Xu JZ, Look R, Demarest KT, Emanuel S, Maryanoff BE.
Bioorg Med Chem Lett (2003) 13 : 3049 -3053
PubMed 12941331 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.73 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL103506 1 8.40
CHEMBL321315 1 8.40
CHEMBL105477 1 8.22
CHEMBL102714 SB-216763 1 8.15
CHEMBL105620 1 8.10
CHEMBL103055 1 7.60
CHEMBL103421 1 7.51
CHEMBL106384 1 7.48
CHEMBL321529 1 7.40
CHEMBL103628 1 7.37
CHEMBL106061 1 7.15
CHEMBL319265 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL103506 IC50 = 4.0 nM 8.40
CHEMBL321315 IC50 = 4.0 nM 8.40
CHEMBL105477 IC50 = 6.0 nM 8.22
CHEMBL102714 SB-216763 IC50 = 7.0 nM 8.15
CHEMBL105620 IC50 = 8.0 nM 8.10
CHEMBL103055 IC50 = 25.0 nM 7.60
CHEMBL103421 IC50 = 31.0 nM 7.51
CHEMBL106384 IC50 = 33.0 nM 7.48
CHEMBL321529 IC50 = 40.0 nM 7.40
CHEMBL103628 IC50 = 43.0 nM 7.37
CHEMBL106061 IC50 = 71.0 nM 7.15
CHEMBL319265 IC50 = 110.0 nM 6.96