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Assay Detail

CHEMBL5653932

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

Binding
Inhibition of Phosphorylase kinase in rabbit muscle tissue in presence of [p32-gamma]-ATP measured after 10 mins by scintillation counter analysis
14
Total Activities
14
Compounds Tested
1
Activity Types
4
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Tissue Muscle tissue
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.
Toullec D, Pianetti P, Coste H, Bellevergue P, Grand-Perret T, Ajakane M, Baudet V, Boissin P, Boursier E, Loriolle F.
J Biol Chem (1991) 266 : 15771 -15781
PubMed 1874734 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.04 7.32

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - EFO:0000365
EFO_ID EFO_ID - MONDO:0018177
EFO_TERM EFO_TERM - colorectal adenocarcinoma
EFO_TERM EFO_TERM - glioblastoma

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 7.32
CHEMBL270875 1 6.75
CHEMBL124072 1 6.70
CHEMBL403771 1 6.40
CHEMBL7463 GF-109203 1 6.16
CHEMBL5661886 1 6.12
CHEMBL5661906 1 5.92
CHEMBL268769 1 5.77
CHEMBL5661889 1 5.75
CHEMBL5661912 1 5.70
CHEMBL5661881 1 5.70
CHEMBL5661835 1 5.56
CHEMBL266487 RO-316233 1 5.50
CHEMBL446199 1 5.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 48.0 nM 7.32
CHEMBL270875 IC50 = 180.0 nM 6.75
CHEMBL124072 IC50 = 200.0 nM 6.70
CHEMBL403771 IC50 = 400.0 nM 6.40
CHEMBL7463 GF-109203 IC50 = 700.0 nM 6.16
CHEMBL5661886 IC50 = 750.0 nM 6.12
CHEMBL5661906 IC50 = 1200.0 nM 5.92
CHEMBL268769 IC50 = 1700.0 nM 5.77
CHEMBL5661889 IC50 = 1800.0 nM 5.75
CHEMBL5661912 IC50 = 2000.0 nM 5.70
CHEMBL5661881 IC50 = 2000.0 nM 5.70
CHEMBL5661835 IC50 = 2750.0 nM 5.56
CHEMBL266487 RO-316233 IC50 = 3200.0 nM 5.50
CHEMBL446199 IC50 = 5700.0 nM 5.24