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Assay Detail

CHEMBL4393036

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

Binding
Inhibition of recombinant human GSK3beta using YRRAAVPPSPSLSRHSSPHQ(pS)EDEEE as substrate measured after 60 mins by ADP-Glo luminescence assay
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Synthesis and biological evaluation of 3-substituted 2-oxindole derivatives as new glycogen synthase kinase 3β inhibitors.
Lozinskaya NA, Babkov DA, Zaryanova EV, Bezsonova EN, Efremov AM, Tsymlyakov MD, Anikina LV, Zakharyascheva OY, Borisov AV, Perfilova VN, Tyurenkov IN, Proskurnina MV, Spasov AA.
Bioorg Med Chem (2019) 27 : 1804 -1817
PubMed 30902399 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 6.30 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2094331 1 8.38
CHEMBL102714 SB-216763 1 8.08
CHEMBL4474153 1 6.81
CHEMBL4450851 1 6.63
CHEMBL4514599 1 6.46
CHEMBL4440139 1 5.91
CHEMBL4529655 1 5.76
CHEMBL4454916 1 5.36
CHEMBL4436958 1 4.89
CHEMBL4465183 1 4.70
CHEMBL4101711 1 -
CHEMBL4545169 1 -
CHEMBL4520227 1 -
CHEMBL4585682 1 -
CHEMBL4537467 1 -
CHEMBL4451858 1 -
CHEMBL4517715 1 -
CHEMBL4467292 1 -
CHEMBL4469665 1 -
CHEMBL4578156 1 -
CHEMBL4085946 1 -
CHEMBL4544396 1 -
CHEMBL4464997 1 -
CHEMBL4452454 1 -
CHEMBL4442846 1 -
CHEMBL3360387 1 -
CHEMBL4586793 1 -
CHEMBL4577668 1 -
CHEMBL4549051 1 -
CHEMBL4449604 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2094331 IC50 = 4.19 nM 8.38
CHEMBL102714 SB-216763 IC50 = 8.35 nM 8.08
CHEMBL4474153 IC50 = 155.4 nM 6.81
CHEMBL4450851 IC50 = 232.9 nM 6.63
CHEMBL4514599 IC50 = 347.9 nM 6.46
CHEMBL4440139 IC50 = 1231.0 nM 5.91
CHEMBL4529655 IC50 = 1717.0 nM 5.76
CHEMBL4454916 IC50 = 4343.0 nM 5.36
CHEMBL4436958 IC50 = 12750.0 nM 4.89
CHEMBL4465183 IC50 = 20000.0 nM 4.70
CHEMBL4537467 IC50 > 10000.0 nM -
CHEMBL4438406 IC50 > 10000.0 nM -
CHEMBL4451858 IC50 > 10000.0 nM -
CHEMBL4517715 IC50 > 10000.0 nM -
CHEMBL4467292 IC50 > 10000.0 nM -
CHEMBL4469665 IC50 > 10000.0 nM -
CHEMBL4578156 IC50 > 10000.0 nM -
CHEMBL4476606 IC50 > 10000.0 nM -
CHEMBL2347073 IC50 > 10000.0 nM -
CHEMBL3633203 IC50 > 10000.0 nM -
CHEMBL4448193 IC50 > 10000.0 nM -
CHEMBL4525020 IC50 > 10000.0 nM -
CHEMBL4580857 IC50 > 10000.0 nM -
CHEMBL4516094 IC50 > 10000.0 nM -
CHEMBL4585682 IC50 > 10000.0 nM -
CHEMBL4520227 IC50 > 10000.0 nM -
CHEMBL4545169 IC50 > 10000.0 nM -
CHEMBL4101711 IC50 > 10000.0 nM -
CHEMBL4085946 IC50 > 10000.0 nM -
CHEMBL4544396 IC50 > 10000.0 nM -
CHEMBL4464997 IC50 > 10000.0 nM -
CHEMBL4452454 IC50 > 10000.0 nM -
CHEMBL4442846 IC50 > 10000.0 nM -
CHEMBL3360387 IC50 > 10000.0 nM -
CHEMBL4586793 IC50 > 10000.0 nM -
CHEMBL4577668 IC50 > 10000.0 nM -
CHEMBL4549051 IC50 > 10000.0 nM -
CHEMBL4449604 IC50 > 10000.0 nM -