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Assay Detail

CHEMBL3387066

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

Binding
Inhibition of canine lung PDE5 using [3H]cGMP substrate by radiolabeled nucleotide method
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Canis lupus familiaris
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL2304402)
Type SINGLE PROTEIN
Organism Canis lupus familiaris

Publication

Design and synthesis of novel 5-(3,4,5-trimethoxybenzoyl)-4-aminopyrimidine derivatives as potent and selective phosphodiesterase 5 inhibitors: scaffold hopping using a pseudo-ring by intramolecular hydrogen bond formation.
Sakamoto T, Koga Y, Hikota M, Matsuki K, Murakami M, Kikkawa K, Fujishige K, Kotera J, Omori K, Morimoto H, Yamada K.
Bioorg Med Chem Lett (2014) 24 : 5175 -5180
PubMed 25442307 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.87 10.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3338455 1 10.28
CHEMBL3338445 1 9.89
CHEMBL3338448 1 9.42
CHEMBL3338444 1 9.18
CHEMBL3338452 1 9.13
CHEMBL3338453 1 8.82
CHEMBL3338447 1 8.82
CHEMBL3338450 1 8.77
CHEMBL3338454 1 8.74
CHEMBL3338443 1 8.70
CHEMBL3338451 1 8.57
CHEMBL3338449 1 8.47
CHEMBL3338442 1 8.46
CHEMBL3338446 1 8.30
CHEMBL3338441 1 7.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3338455 IC50 = 0.053 nM 10.28
CHEMBL3338445 IC50 = 0.13 nM 9.89
CHEMBL3338448 IC50 = 0.38 nM 9.42
CHEMBL3338444 IC50 = 0.66 nM 9.18
CHEMBL3338452 IC50 = 0.74 nM 9.13
CHEMBL3338453 IC50 = 1.5 nM 8.82
CHEMBL3338447 IC50 = 1.5 nM 8.82
CHEMBL3338450 IC50 = 1.7 nM 8.77
CHEMBL3338454 IC50 = 1.8 nM 8.74
CHEMBL3338443 IC50 = 2.0 nM 8.70
CHEMBL3338451 IC50 = 2.7 nM 8.57
CHEMBL3338449 IC50 = 3.4 nM 8.47
CHEMBL3338442 IC50 = 3.5 nM 8.46
CHEMBL3338446 IC50 = 5.0 nM 8.30
CHEMBL3338441 IC50 = 34.0 nM 7.47