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Assay Detail

CHEMBL774072

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

Functional
Relaxant effect on isolated rabbit corpus cavernosum
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Corpus cavernosum
Confidence 8 — Homologous single protein target
Curated By Expert

Target

cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel, potent, and selective phosphodiesterase 5 inhibitors: synthesis and biological activities of a series of 4-aryl-1-isoquinolinone derivatives.
Ukita T, Nakamura Y, Kubo A, Yamamoto Y, Moritani Y, Saruta K, Higashijima T, Kotera J, Takagi M, Kikkawa K, Omori K.
J Med Chem (2001) 44 : 2204 -2218
PubMed 11405657 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 7.68 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL553371 1 8.10
CHEMBL192 SILDENAFIL 4.0 1 8.06
CHEMBL544289 1 8.02
CHEMBL553786 1 7.92
CHEMBL541818 1 7.43
CHEMBL538498 1 7.36
CHEMBL540539 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL553371 EC50 = 7.9 nM 8.10
CHEMBL192 SILDENAFIL EC50 = 8.7 nM 8.06
CHEMBL544289 EC50 = 9.5 nM 8.02
CHEMBL553786 EC50 = 12.0 nM 7.92
CHEMBL541818 EC50 = 37.0 nM 7.43
CHEMBL538498 EC50 = 44.0 nM 7.36
CHEMBL540539 EC50 = 130.0 nM 6.89