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Assay Detail

CHEMBL768661

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

Binding
Inhibitory activity against cGMP-phosphodiesterase from porcine aorta
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Cyclic GMP phosphodiesterase inhibitors. 2. Requirement of 6-substitution of quinazoline derivatives for potent and selective inhibitory activity.
Takase Y, Saeki T, Watanabe N, Adachi H, Souda S, Saito I.
J Med Chem (1994) 37 : 2106 -2111
PubMed 8027992 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 6.11 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL66620 1 7.72
CHEMBL304927 1 7.51
CHEMBL67243 1 7.05
CHEMBL67276 1 7.00
CHEMBL66323 1 6.64
CHEMBL66855 1 6.46
CHEMBL67061 1 6.42
CHEMBL63259 1 6.42
CHEMBL67239 1 6.28
CHEMBL419806 1 6.21
CHEMBL308657 1 6.14
CHEMBL63 ROLIPRAM 2.0 1 6.14
CHEMBL189 MILRINONE 4.0 1 6.13
CHEMBL63428 1 6.11
CHEMBL294731 1 6.09
CHEMBL68072 1 6.09
CHEMBL66913 1 6.08
CHEMBL68337 1 6.03
CHEMBL63637 1 6.00
CHEMBL305771 1 5.96
CHEMBL68448 1 5.85
CHEMBL63416 1 5.80
CHEMBL67736 1 5.64
CHEMBL67892 1 5.64
CHEMBL304277 1 5.57
CHEMBL302588 1 5.44
CHEMBL66732 1 5.38
CHEMBL63379 1 5.23
CHEMBL304275 1 5.12
CHEMBL67418 1 5.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL66620 IC50 = 19.0 nM 7.72
CHEMBL304927 IC50 = 31.0 nM 7.51
CHEMBL67243 IC50 = 90.0 nM 7.05
CHEMBL67276 IC50 = 100.0 nM 7.00
CHEMBL66323 IC50 = 230.0 nM 6.64
CHEMBL66855 IC50 = 350.0 nM 6.46
CHEMBL67061 IC50 = 380.0 nM 6.42
CHEMBL63259 IC50 = 380.0 nM 6.42
CHEMBL67239 IC50 = 530.0 nM 6.28
CHEMBL419806 IC50 = 620.0 nM 6.21
CHEMBL308657 IC50 = 730.0 nM 6.14
CHEMBL63 ROLIPRAM IC50 = 720.0 nM 6.14
CHEMBL189 MILRINONE IC50 = 740.0 nM 6.13
CHEMBL63428 IC50 = 770.0 nM 6.11
CHEMBL294731 IC50 = 810.0 nM 6.09
CHEMBL68072 IC50 = 810.0 nM 6.09
CHEMBL66913 IC50 = 840.0 nM 6.08
CHEMBL68337 IC50 = 930.0 nM 6.03
CHEMBL63637 IC50 = 1000.0 nM 6.00
CHEMBL305771 IC50 = 1100.0 nM 5.96
CHEMBL68448 IC50 = 1400.0 nM 5.85
CHEMBL63416 IC50 = 1600.0 nM 5.80
CHEMBL67736 IC50 = 2300.0 nM 5.64
CHEMBL67892 IC50 = 2300.0 nM 5.64
CHEMBL304277 IC50 = 2700.0 nM 5.57
CHEMBL302588 IC50 = 3600.0 nM 5.44
CHEMBL66732 IC50 = 4200.0 nM 5.38
CHEMBL63379 IC50 = 5900.0 nM 5.23
CHEMBL304275 IC50 = 7500.0 nM 5.12
CHEMBL67418 IC50 = 8700.0 nM 5.06