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Assay Detail

CHEMBL5653933

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

Binding
Inhibition of bovine brain PKC in presence of [p32-gamma]-ATP measured after 10 mins by scintillation counter analysis
24
Total Activities
24
Compounds Tested
1
Activity Types
4
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Tissue Brain
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 24 6.81 8.30

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
CHEMBL403771 1 8.30
CHEMBL7463 GF-109203 1 8.00
CHEMBL5661886 1 7.89
CHEMBL270875 1 7.58
CHEMBL268769 1 7.40
CHEMBL5661906 1 7.35
CHEMBL446199 1 7.28
CHEMBL5661881 1 7.16
CHEMBL5661912 1 7.10
CHEMBL266487 RO-316233 1 7.00
CHEMBL5661889 1 7.00
CHEMBL5661916 1 6.70
CHEMBL495845 ARCYRIARUBIN B 1 6.70
CHEMBL5661941 1 6.70
CHEMBL124072 1 6.58
CHEMBL298818 1 5.70
CHEMBL5661835 1 5.56
CHEMBL301741 1 5.00
CHEMBL268368 STAUROSPORINE AGLYCON 1 4.40
CHEMBL16958 STAUROSPORINONE 1 -
CHEMBL5661830 1 -
CHEMBL5661877 1 -
CHEMBL294450 1 -
CHEMBL291725 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL403771 IC50 = 5.0 nM 8.30
CHEMBL7463 GF-109203 IC50 = 10.0 nM 8.00
CHEMBL5661886 IC50 = 13.0 nM 7.89
CHEMBL270875 IC50 = 26.0 nM 7.58
CHEMBL268769 IC50 = 40.0 nM 7.40
CHEMBL5661906 IC50 = 45.0 nM 7.35
CHEMBL446199 IC50 = 52.0 nM 7.28
CHEMBL5661881 IC50 = 70.0 nM 7.16
CHEMBL5661912 IC50 = 80.0 nM 7.10
CHEMBL266487 RO-316233 IC50 = 100.0 nM 7.00
CHEMBL5661889 IC50 = 100.0 nM 7.00
CHEMBL5661916 IC50 = 200.0 nM 6.70
CHEMBL495845 ARCYRIARUBIN B IC50 = 200.0 nM 6.70
CHEMBL5661941 IC50 = 200.0 nM 6.70
CHEMBL124072 IC50 = 260.0 nM 6.58
CHEMBL298818 IC50 = 2000.0 nM 5.70
CHEMBL5661835 IC50 = 2750.0 nM 5.56
CHEMBL301741 IC50 = 10000.0 nM 5.00
CHEMBL268368 STAUROSPORINE AGLYCON IC50 = 40000.0 nM 4.40
CHEMBL16958 STAUROSPORINONE IC50 > 25000.0 nM -
CHEMBL5661830 IC50 > 20000.0 nM -
CHEMBL5661877 IC50 > 10000.0 nM -
CHEMBL294450 IC50 > 50000.0 nM -
CHEMBL291725 IC50 > 50000.0 nM -