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Assay Detail

CHEMBL822064

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

Binding
Tested for inhibition of cGMP-dependent protein kinase from bovine lung
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Expert

Target

cGMP-dependent protein kinase 1 (CHEMBL3183)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Novel indolocarbazole protein kinase c inhibitors with improved biochemical and physicochemical properties
Kleinschroth J, Hartenstein J, Rudolph C, Schachtele C
Bioorg Med Chem Lett (1995) 5 : 55 -60
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.80 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 7.75
CHEMBL155929 1 6.66
CHEMBL154245 1 6.38
CHEMBL157892 1 6.06
CHEMBL156433 1 6.00
CHEMBL346467 1 5.70
CHEMBL156172 1 5.68
CHEMBL157822 1 5.32
CHEMBL302449 GO-6976 1 5.21
CHEMBL348177 1 5.14
CHEMBL346038 1 5.03
CHEMBL345639 1 4.64
CHEMBL345593 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 18.0 nM 7.75
CHEMBL155929 IC50 = 220.0 nM 6.66
CHEMBL154245 IC50 = 420.0 nM 6.38
CHEMBL157892 IC50 = 870.0 nM 6.06
CHEMBL156433 IC50 = 1000.0 nM 6.00
CHEMBL346467 IC50 = 2000.0 nM 5.70
CHEMBL156172 IC50 = 2100.0 nM 5.68
CHEMBL157822 IC50 = 4800.0 nM 5.32
CHEMBL302449 GO-6976 IC50 = 6200.0 nM 5.21
CHEMBL348177 IC50 = 7200.0 nM 5.14
CHEMBL346038 IC50 = 9400.0 nM 5.03
CHEMBL345639 IC50 = 23000.0 nM 4.64
CHEMBL345593 IC50 > 3000.0 nM -