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Assay Detail

CHEMBL2211468

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

Binding
Inhibition of GSK3beta
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Structure-Based Design of Potent and Selective CK1γ Inhibitors.
Huang H, Acquaviva L, Berry V, Bregman H, Chakka N, O'Connor A, DiMauro EF, Dovey J, Epstein O, Grubinska B, Goldstein J, Gunaydin H, Hua Z, Huang X, Huang L, Human J, Long A, Newcomb J, Patel VF, Saffran D, Serafino R, Schneider S, Strathdee C, Tang J, Turci S, White R, Yu V, Zhao H, Wilson C, Martin MW.
ACS Med Chem Lett (2012) 3 : 1059 -1064
PubMed 24900428 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.84 8.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2203552 1 8.83
CHEMBL2203556 1 7.80
CHEMBL2203555 1 7.01
CHEMBL2203559 1 5.95
CHEMBL2203553 1 5.91
CHEMBL2203562 1 5.40
CHEMBL2203561 1 5.11
CHEMBL2203563 1 4.97
CHEMBL2203554 1 4.59
CHEMBL2203565 1 4.42
CHEMBL2203564 1 4.27
CHEMBL2203560 1 -
CHEMBL2203558 1 -
CHEMBL2203557 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2203552 IC50 = 1.491 nM 8.83
CHEMBL2203556 IC50 = 16.0 nM 7.80
CHEMBL2203555 IC50 = 98.0 nM 7.01
CHEMBL2203559 IC50 = 1120.0 nM 5.95
CHEMBL2203553 IC50 = 1220.0 nM 5.91
CHEMBL2203562 IC50 = 4000.0 nM 5.40
CHEMBL2203561 IC50 = 7830.0 nM 5.11
CHEMBL2203563 IC50 = 10800.0 nM 4.97
CHEMBL2203554 IC50 = 25600.0 nM 4.59
CHEMBL2203565 IC50 = 38100.0 nM 4.42
CHEMBL2203564 IC50 = 53300.0 nM 4.27
CHEMBL2203560 IC50 > 62500.0 nM -
CHEMBL2203558 IC50 > 62500.0 nM -
CHEMBL2203557 IC50 > 30000.0 nM -