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Assay Detail

CHEMBL1102984

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

Binding
Inhibition of PKCalpha
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Protein kinase C alpha type (CHEMBL299)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent and bioavailable GSK-3beta inhibitors.
Gong L, Hirschfeld D, Tan YC, Heather Hogg J, Peltz G, Avnur Z, Dunten P.
Bioorg Med Chem Lett (2010) 20 : 1693 -1696
PubMed 20138512 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 5.89 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26501 RO-320432 1 7.66
CHEMBL1082153 1 6.58
CHEMBL1087243 1 6.42
CHEMBL1082152 1 6.40
CHEMBL1082151 1 6.13
CHEMBL431933 1 6.12
CHEMBL1081294 1 6.00
CHEMBL1088724 1 5.98
CHEMBL1081617 1 5.85
CHEMBL1081972 1 5.85
CHEMBL54547 1 5.72
CHEMBL1081973 1 5.66
CHEMBL1081128 1 5.54
CHEMBL1081616 1 5.38
CHEMBL1088149 1 5.26
CHEMBL293542 1 5.22
CHEMBL1087242 1 5.18
CHEMBL53745 1 5.05
CHEMBL1080933 1 -
CHEMBL1086732 1 -
CHEMBL1087380 1 -
CHEMBL1081293 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26501 RO-320432 IC50 = 22.0 nM 7.66
CHEMBL1082153 IC50 = 260.0 nM 6.58
CHEMBL1087243 IC50 = 380.0 nM 6.42
CHEMBL1082152 IC50 = 400.0 nM 6.40
CHEMBL1082151 IC50 = 740.0 nM 6.13
CHEMBL431933 IC50 = 760.0 nM 6.12
CHEMBL1081294 IC50 = 1000.0 nM 6.00
CHEMBL1088724 IC50 = 1050.0 nM 5.98
CHEMBL1081617 IC50 = 1400.0 nM 5.85
CHEMBL1081972 IC50 = 1400.0 nM 5.85
CHEMBL54547 IC50 = 1900.0 nM 5.72
CHEMBL1081973 IC50 = 2200.0 nM 5.66
CHEMBL1081128 IC50 = 2900.0 nM 5.54
CHEMBL1081616 IC50 = 4200.0 nM 5.38
CHEMBL1088149 IC50 = 5500.0 nM 5.26
CHEMBL293542 IC50 = 6000.0 nM 5.22
CHEMBL1087242 IC50 = 6600.0 nM 5.18
CHEMBL53745 IC50 = 8900.0 nM 5.05
CHEMBL1080933 IC50 - -
CHEMBL1086732 IC50 - -
CHEMBL1087380 IC50 > 30000.0 nM -
CHEMBL1081293 IC50 - -