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Assay Detail

CHEMBL4334914

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

ADMET
Inhibition of human GSK-3beta H350L mutant (2 to end residues) at 10 uM using phospho GS2 peptide as substrate after 40 mins by [gamma-33ATP] radiometric assay
ChEMBL ↗
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of novel glycogen synthase kinase-3α inhibitors: Structure-based virtual screening, preliminary SAR and biological evaluation for treatment of acute myeloid leukemia.
Wang Y, Dou X, Jiang L, Jin H, Zhang L, Zhang L, Liu Z.
Eur J Med Chem (2019) 171 : 221 -234
PubMed 30925338 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 48 6.25 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL362558 LY-2090314 2.0 1 8.89
CHEMBL4455512 — — 1 6.96
CHEMBL4568120 — — 1 6.66
CHEMBL4572532 — — 1 6.51
CHEMBL4561377 — — 1 6.50
CHEMBL4526685 — — 1 6.47
CHEMBL4452888 — — 1 6.39
CHEMBL4537545 — — 1 6.25
CHEMBL4592453 — — 1 6.24
CHEMBL4536515 — — 1 6.24
CHEMBL4566633 — — 1 6.23
CHEMBL4436862 — — 1 6.17
CHEMBL4452978 — — 1 6.13
CHEMBL4558089 — — 1 6.12
CHEMBL4467604 — — 1 6.06
CHEMBL4456469 — — 1 6.04
CHEMBL4444495 — — 1 5.92
CHEMBL4444620 — — 1 5.92
CHEMBL4519757 — — 1 5.89
CHEMBL4519366 — — 1 5.84
CHEMBL4459001 — — 1 5.75
CHEMBL3437678 — — 1 5.72
CHEMBL1878704 — — 1 5.60
CHEMBL4442366 — — 1 5.43
CHEMBL1408125 — — 1 -
CHEMBL4541565 — — 1 -
CHEMBL4535203 — — 1 -
CHEMBL4541734 — — 1 -
CHEMBL4584696 — — 1 -
CHEMBL4555724 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL362558 LY-2090314 IC50 = 1.29 nM 8.89
CHEMBL4455512 — IC50 = 110.0 nM 6.96
CHEMBL4568120 — IC50 = 218.0 nM 6.66
CHEMBL4572532 — IC50 = 308.0 nM 6.51
CHEMBL4561377 — IC50 = 320.0 nM 6.50
CHEMBL4526685 — IC50 = 338.0 nM 6.47
CHEMBL4452888 — IC50 = 405.0 nM 6.39
CHEMBL4537545 — IC50 = 565.0 nM 6.25
CHEMBL4592453 — IC50 = 576.0 nM 6.24
CHEMBL4536515 — IC50 = 571.0 nM 6.24
CHEMBL4566633 — IC50 = 584.0 nM 6.23
CHEMBL4436862 — IC50 = 678.0 nM 6.17
CHEMBL4452978 — IC50 = 743.0 nM 6.13
CHEMBL4558089 — IC50 = 767.0 nM 6.12
CHEMBL4467604 — IC50 = 862.0 nM 6.06
CHEMBL4456469 — IC50 = 917.0 nM 6.04
CHEMBL4444495 — IC50 = 1193.0 nM 5.92
CHEMBL4444620 — IC50 = 1196.0 nM 5.92
CHEMBL4519757 — IC50 = 1291.0 nM 5.89
CHEMBL4519366 — IC50 = 1429.0 nM 5.84
CHEMBL4459001 — IC50 = 1758.0 nM 5.75
CHEMBL3437678 — IC50 = 1895.0 nM 5.72
CHEMBL1878704 — IC50 = 2495.0 nM 5.60
CHEMBL4442366 — IC50 = 3724.0 nM 5.43
CHEMBL4579205 — IC50 - — -
CHEMBL4575432 — IC50 - — -
CHEMBL3437676 — IC50 - — -
CHEMBL4577014 — IC50 - — -
CHEMBL4465279 — IC50 - — -
CHEMBL4515342 — IC50 - — -
CHEMBL4467699 — IC50 - — -
CHEMBL4468449 — IC50 - — -
CHEMBL4593954 — IC50 - — -
CHEMBL4463806 — IC50 - — -
CHEMBL4443667 — IC50 - — -
CHEMBL4459906 — IC50 - — -
CHEMBL4437351 — IC50 - — -
CHEMBL4589530 — IC50 - — -
CHEMBL4539454 — IC50 - — -
CHEMBL4443427 — IC50 - — -
CHEMBL4469930 — IC50 - — -
CHEMBL4535815 — IC50 - — -
CHEMBL4555724 — IC50 - — -
CHEMBL4584696 — IC50 - — -
CHEMBL4541734 — IC50 - — -
CHEMBL4535203 — IC50 - — -
CHEMBL4541565 — IC50 - — -
CHEMBL1408125 — IC50 - — -