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Assay Detail

CHEMBL833485

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Binding
Inhibitory concentration against the Glycogen synthase kinase-3
ChEMBL ↗
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

The development of potent and selective bisarylmaleimide GSK3 inhibitors.
Engler TA, Malhotra S, Burkholder TP, Henry JR, Mendel D, Porter WJ, Furness K, Diefenbacher C, Marquart A, Reel JK, Li Y, Clayton J, Cunningham B, McLean J, O'toole JC, Brozinick J, Hawkins E, Misener E, Briere D, Brier RA, Wagner JR, Campbell RM, Anderson BD, Vaughn R, Bennett DB, Meier TI, Cook JA.
Bioorg Med Chem Lett (2005) 15 : 899 -903
PubMed 15686883 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 8.17 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL181339 — — 1 9.10
CHEMBL178766 BISARYLMALEIMIDE 2 — 1 9.10
CHEMBL181371 — — 1 9.05
CHEMBL181518 — — 1 9.00
CHEMBL359871 — — 1 8.96
CHEMBL180779 — — 1 8.92
CHEMBL369090 — — 1 8.89
CHEMBL178737 — — 1 8.89
CHEMBL361765 — — 1 8.82
CHEMBL362814 — — 1 8.80
CHEMBL181031 BISARYLMALEIMIDE 1 — 1 8.80
CHEMBL369316 — — 1 8.77
CHEMBL368246 — — 1 8.74
CHEMBL361948 — — 1 8.72
CHEMBL369572 — — 1 8.72
CHEMBL362588 — — 1 8.70
CHEMBL178646 — — 1 8.68
CHEMBL178851 — — 1 8.68
CHEMBL181296 — — 1 8.60
CHEMBL178850 — — 1 8.57
CHEMBL445649 — — 1 8.49
CHEMBL361635 — — 1 8.49
CHEMBL361007 — — 1 8.49
CHEMBL178820 — — 1 8.48
CHEMBL361996 — — 1 8.47
CHEMBL179725 — — 1 8.46
CHEMBL181464 — — 1 8.33
CHEMBL359537 — — 1 8.32
CHEMBL426243 — — 1 7.92
CHEMBL181774 — — 1 7.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL181339 — IC50 = 0.8 nM 9.10
CHEMBL178766 BISARYLMALEIMIDE 2 IC50 = 0.8 nM 9.10
CHEMBL181371 — IC50 = 0.9 nM 9.05
CHEMBL181518 — IC50 = 1.0 nM 9.00
CHEMBL359871 — IC50 = 1.1 nM 8.96
CHEMBL180779 — IC50 = 1.2 nM 8.92
CHEMBL369090 — IC50 = 1.3 nM 8.89
CHEMBL178737 — IC50 = 1.3 nM 8.89
CHEMBL361765 — IC50 = 1.5 nM 8.82
CHEMBL362814 — IC50 = 1.6 nM 8.80
CHEMBL181031 BISARYLMALEIMIDE 1 IC50 = 1.6 nM 8.80
CHEMBL369316 — IC50 = 1.7 nM 8.77
CHEMBL368246 — IC50 = 1.8 nM 8.74
CHEMBL361948 — IC50 = 1.9 nM 8.72
CHEMBL369572 — IC50 = 1.9 nM 8.72
CHEMBL362588 — IC50 = 2.0 nM 8.70
CHEMBL178646 — IC50 = 2.1 nM 8.68
CHEMBL178851 — IC50 = 2.1 nM 8.68
CHEMBL181296 — IC50 = 2.5 nM 8.60
CHEMBL178850 — IC50 = 2.7 nM 8.57
CHEMBL445649 — IC50 = 3.2 nM 8.49
CHEMBL361635 — IC50 = 3.2 nM 8.49
CHEMBL361007 — IC50 = 3.2 nM 8.49
CHEMBL178820 — IC50 = 3.3 nM 8.48
CHEMBL361996 — IC50 = 3.4 nM 8.47
CHEMBL179725 — IC50 = 3.5 nM 8.46
CHEMBL181464 — IC50 = 4.7 nM 8.33
CHEMBL359537 — IC50 = 4.8 nM 8.32
CHEMBL426243 — IC50 = 12.0 nM 7.92
CHEMBL181774 — IC50 = 13.0 nM 7.89
CHEMBL369108 — IC50 = 19.0 nM 7.72
CHEMBL361125 — IC50 = 27.0 nM 7.57
CHEMBL182048 — IC50 = 27.0 nM 7.57
CHEMBL362221 — IC50 = 30.0 nM 7.52
CHEMBL362587 — IC50 = 33.0 nM 7.48
CHEMBL178645 — IC50 = 34.0 nM 7.47
CHEMBL181015 — IC50 = 41.0 nM 7.39
CHEMBL369099 — IC50 = 45.0 nM 7.35
CHEMBL181112 — IC50 = 60.0 nM 7.22
CHEMBL368248 — IC50 = 64.0 nM 7.19
CHEMBL361204 — IC50 = 71.0 nM 7.15
CHEMBL362259 — IC50 = 83.0 nM 7.08
CHEMBL361746 — IC50 = 120.0 nM 6.92
CHEMBL368426 — IC50 = 130.0 nM 6.89
CHEMBL362830 — IC50 = 150.0 nM 6.82
CHEMBL178237 — IC50 = 330.0 nM 6.48