Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3386398

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

Binding
Inhibition of dog lungs PDE5 using [3H]cGMP as substrate after 30 mins by scintillation counting analysis
26
Total Activities
26
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

The discovery of avanafil for the treatment of erectile dysfunction: a novel pyrimidine-5-carboxamide derivative as a potent and highly selective phosphodiesterase 5 inhibitor.
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 : 5460 -5465
PubMed 25455484 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 8.02 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3354285 1 9.05
CHEMBL3354279 1 8.92
CHEMBL3354284 1 8.74
CHEMBL3354264 1 8.68
CHEMBL3354266 1 8.57
CHEMBL3354273 1 8.46
CHEMBL3354265 1 8.38
CHEMBL1963681 AVANAFIL 4.0 1 8.28
CHEMBL3354287 1 8.26
CHEMBL3354270 1 8.25
CHEMBL3354286 1 8.21
CHEMBL3354278 1 8.19
CHEMBL3352836 1 8.18
CHEMBL3354272 1 7.92
CHEMBL3354267 1 7.92
CHEMBL3354271 1 7.89
CHEMBL3354269 1 7.82
CHEMBL3354282 1 7.60
CHEMBL3354274 1 7.50
CHEMBL3354275 1 7.50
CHEMBL3354283 1 7.44
CHEMBL3354277 1 7.27
CHEMBL3354276 1 7.23
CHEMBL3354281 1 7.20
CHEMBL3354268 1 7.07
CHEMBL3354280 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3354285 IC50 = 0.9 nM 9.05
CHEMBL3354279 IC50 = 1.2 nM 8.92
CHEMBL3354284 IC50 = 1.8 nM 8.74
CHEMBL3354264 IC50 = 2.1 nM 8.68
CHEMBL3354266 IC50 = 2.7 nM 8.57
CHEMBL3354273 IC50 = 3.5 nM 8.46
CHEMBL3354265 IC50 = 4.2 nM 8.38
CHEMBL1963681 AVANAFIL IC50 = 5.2 nM 8.28
CHEMBL3354287 IC50 = 5.5 nM 8.26
CHEMBL3354270 IC50 = 5.6 nM 8.25
CHEMBL3354286 IC50 = 6.1 nM 8.21
CHEMBL3354278 IC50 = 6.5 nM 8.19
CHEMBL3352836 IC50 = 6.6 nM 8.18
CHEMBL3354272 IC50 = 12.0 nM 7.92
CHEMBL3354267 IC50 = 12.0 nM 7.92
CHEMBL3354271 IC50 = 13.0 nM 7.89
CHEMBL3354269 IC50 = 15.0 nM 7.82
CHEMBL3354282 IC50 = 25.0 nM 7.60
CHEMBL3354274 IC50 = 32.0 nM 7.50
CHEMBL3354275 IC50 = 32.0 nM 7.50
CHEMBL3354283 IC50 = 36.0 nM 7.44
CHEMBL3354277 IC50 = 54.0 nM 7.27
CHEMBL3354276 IC50 = 59.0 nM 7.23
CHEMBL3354281 IC50 = 63.0 nM 7.20
CHEMBL3354268 IC50 = 85.0 nM 7.07
CHEMBL3354280 IC50 > 100.0 nM -