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Assay Detail

CHEMBL5653931

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

Binding
Inhibition of PKA (unknown origin)
15
Total Activities
15
Compounds Tested
1
Activity Types
4
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

cAMP-dependent protein kinase (PKA) (CHEMBL2094138)
Type PROTEIN FAMILY
Organism Homo sapiens

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 15 5.65 6.30

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
CHEMBL124072 1 6.30
CHEMBL270875 1 6.30
CHEMBL403771 1 5.92
CHEMBL5661941 1 5.82
CHEMBL266487 RO-316233 1 5.70
CHEMBL7463 GF-109203 1 5.70
CHEMBL5661886 1 5.70
CHEMBL5661906 1 5.60
CHEMBL5661881 1 5.52
CHEMBL268769 1 5.46
CHEMBL446199 1 5.36
CHEMBL5661916 1 5.35
CHEMBL5661889 1 5.22
CHEMBL5661912 1 5.18
CHEMBL5661835 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL124072 IC50 = 500.0 nM 6.30
CHEMBL270875 IC50 = 500.0 nM 6.30
CHEMBL403771 IC50 = 1200.0 nM 5.92
CHEMBL5661941 IC50 = 1500.0 nM 5.82
CHEMBL266487 RO-316233 IC50 = 2000.0 nM 5.70
CHEMBL7463 GF-109203 IC50 = 2000.0 nM 5.70
CHEMBL5661886 IC50 = 2000.0 nM 5.70
CHEMBL5661906 IC50 = 2500.0 nM 5.60
CHEMBL5661881 IC50 = 3000.0 nM 5.52
CHEMBL268769 IC50 = 3500.0 nM 5.46
CHEMBL446199 IC50 = 4400.0 nM 5.36
CHEMBL5661916 IC50 = 4500.0 nM 5.35
CHEMBL5661889 IC50 = 6000.0 nM 5.22
CHEMBL5661912 IC50 = 6600.0 nM 5.18
CHEMBL5661835 IC50 > 10000.0 nM -