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Assay Detail

CHEMBL932639

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

Binding
Inhibition of GSK3-beta in human U87MG cells by ELISA
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type U-87MG ATCC
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Identification of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidines as selective inhibitors of protein kinase B through fragment elaboration.
Caldwell JJ, Davies TG, Donald A, McHardy T, Rowlands MG, Aherne GW, Hunter LK, Taylor K, Ruddle R, Raynaud FI, Verdonk M, Workman P, Garrett MD, Collins I.
J Med Chem (2008) 51 : 2147 -2157
PubMed 18345609 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.05 6.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL260000 1 6.35
CHEMBL406863 1 6.23
CHEMBL260577 1 6.23
CHEMBL405384 1 6.23
CHEMBL263664 1 6.18
CHEMBL98350 LY-294002 -1.0 1 5.09
CHEMBL259998 1 -
CHEMBL260463 1 -
CHEMBL259999 1 -
CHEMBL407504 1 -
CHEMBL409503 1 -
CHEMBL260358 1 -
CHEMBL261034 1 -
CHEMBL261247 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL260000 IC50 = 450.0 nM 6.35
CHEMBL406863 IC50 = 590.0 nM 6.23
CHEMBL260577 IC50 = 590.0 nM 6.23
CHEMBL405384 IC50 = 590.0 nM 6.23
CHEMBL263664 IC50 = 660.0 nM 6.18
CHEMBL98350 LY-294002 IC50 = 8100.0 nM 5.09
CHEMBL259998 IC50 < 1000.0 nM -
CHEMBL260463 IC50 - -
CHEMBL259999 IC50 - -
CHEMBL407504 IC50 - -
CHEMBL409503 IC50 - -
CHEMBL260358 IC50 - -
CHEMBL261034 IC50 - -
CHEMBL261247 IC50 - -