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Assay Detail

CHEMBL846805

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

Binding
Inhibition of crude cGMP phosphodiesterase from canine thoracic aorta
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Canis lupus familiaris
Tissue Thoracic aorta
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Novel compounds possessing potent cAMP and cGMP phosphodiesterase inhibitory activity. Synthesis and cardiovascular effects of a series of imidazo[1,2-a]quinoxalinones and imidazo[1,5-a]quinoxalinones and their aza analogues.
Davey DD, Erhardt PW, Cantor EH, Greenberg SS, Ingebretsen WR, Wiggins J.
J Med Chem (1991) 34 : 2671 -2677
PubMed 1654425 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.05 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL330540 1 6.52
CHEMBL91789 1 6.40
CHEMBL420615 1 6.05
CHEMBL90068 1 5.52
CHEMBL90932 1 5.52
CHEMBL92555 1 5.40
CHEMBL90929 1 5.30
CHEMBL92216 1 5.16
CHEMBL88794 1 4.89
CHEMBL93452 1 4.85
CHEMBL327854 1 4.77
CHEMBL90931 1 4.72
CHEMBL92009 1 4.62
CHEMBL443233 1 4.57
CHEMBL312971 1 4.57
CHEMBL275084 ISOBUTYLMETHYLXANTHINE 1 4.55
CHEMBL88818 1 4.44
CHEMBL316356 1 4.42
CHEMBL88763 1 4.41
CHEMBL554030 1 4.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL330540 IC50 = 300.0 nM 6.52
CHEMBL91789 IC50 = 400.0 nM 6.40
CHEMBL420615 IC50 = 900.0 nM 6.05
CHEMBL90068 IC50 = 3000.0 nM 5.52
CHEMBL90932 IC50 = 3000.0 nM 5.52
CHEMBL92555 IC50 = 4000.0 nM 5.40
CHEMBL90929 IC50 = 5000.0 nM 5.30
CHEMBL92216 IC50 = 7000.0 nM 5.16
CHEMBL88794 IC50 = 13000.0 nM 4.89
CHEMBL93452 IC50 = 14000.0 nM 4.85
CHEMBL327854 IC50 = 17000.0 nM 4.77
CHEMBL90931 IC50 = 19000.0 nM 4.72
CHEMBL92009 IC50 = 24000.0 nM 4.62
CHEMBL443233 IC50 = 27000.0 nM 4.57
CHEMBL312971 IC50 = 27000.0 nM 4.57
CHEMBL275084 ISOBUTYLMETHYLXANTHINE IC50 = 28000.0 nM 4.55
CHEMBL88818 IC50 = 36000.0 nM 4.44
CHEMBL316356 IC50 = 38000.0 nM 4.42
CHEMBL88763 IC50 = 39000.0 nM 4.41
CHEMBL554030 IC50 = 44000.0 nM 4.36