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Assay Detail

CHEMBL963848

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

Binding
Inhibition of bovine PDE5
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL3478)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Quinazolines as potent and highly selective PDE5 inhibitors as potential therapeutics for male erectile dysfunction.
Kim YH, Choi H, Lee J, Hwang IC, Moon SK, Kim SJ, Lee HW, Im DS, Lee SS, Ahn SK, Kim SW, Han CK, Yoon JH, Lee KJ, Choi NS.
Bioorg Med Chem Lett (2008) 18 : 6279 -6282
PubMed 18976905 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.63 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL521075 1 9.00
CHEMBL512174 1 8.40
CHEMBL471702 1 8.30
CHEMBL473301 1 8.10
CHEMBL192 SILDENAFIL 4.0 1 8.00
CHEMBL488265 1 8.00
CHEMBL470310 1 7.92
CHEMBL779 TADALAFIL 4.0 1 7.92
CHEMBL472559 1 7.92
CHEMBL470492 1 7.85
CHEMBL471703 1 7.85
CHEMBL471529 1 7.75
CHEMBL520074 1 7.75
CHEMBL471701 1 7.72
CHEMBL513593 1 7.72
CHEMBL488080 1 7.68
CHEMBL471528 1 7.54
CHEMBL488091 1 7.50
CHEMBL472558 1 7.50
CHEMBL524871 1 7.15
CHEMBL473507 1 6.24
CHEMBL470311 1 5.96
CHEMBL487247 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL521075 IC50 = 1.0 nM 9.00
CHEMBL512174 IC50 = 4.0 nM 8.40
CHEMBL471702 IC50 = 5.0 nM 8.30
CHEMBL473301 IC50 = 8.0 nM 8.10
CHEMBL192 SILDENAFIL IC50 = 10.0 nM 8.00
CHEMBL488265 IC50 = 10.0 nM 8.00
CHEMBL470310 IC50 = 12.0 nM 7.92
CHEMBL779 TADALAFIL IC50 = 12.0 nM 7.92
CHEMBL472559 IC50 = 12.0 nM 7.92
CHEMBL470492 IC50 = 14.0 nM 7.85
CHEMBL471703 IC50 = 14.0 nM 7.85
CHEMBL471529 IC50 = 18.0 nM 7.75
CHEMBL520074 IC50 = 18.0 nM 7.75
CHEMBL471701 IC50 = 19.0 nM 7.72
CHEMBL513593 IC50 = 19.0 nM 7.72
CHEMBL488080 IC50 = 21.0 nM 7.68
CHEMBL471528 IC50 = 29.0 nM 7.54
CHEMBL488091 IC50 = 32.0 nM 7.50
CHEMBL472558 IC50 = 32.0 nM 7.50
CHEMBL524871 IC50 = 71.0 nM 7.15
CHEMBL473507 IC50 = 570.0 nM 6.24
CHEMBL470311 IC50 = 1100.0 nM 5.96
CHEMBL487247 IC50 = 1600.0 nM 5.80