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Assay Detail

CHEMBL763667

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

Binding
Inhibitory activity against phosphodiesterase 5 (PDE5) isolated from canine lung
16
Total Activities
16
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 Intermediate

Target

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

Publication

1,7- and 2,7-naphthyridine derivatives as potent and highly specific PDE5 inhibitors.
Ukita T, Nakamura Y, Kubo A, Yamamoto Y, Moritani Y, Saruta K, Higashijima T, Kotera J, Fujishige K, Takagi M, Kikkawa K, Omori K.
Bioorg Med Chem Lett (2003) 13 : 2341 -2345
PubMed 12824030 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 8.93 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL540031 1 9.66
CHEMBL540294 1 9.64
CHEMBL541822 1 9.54
CHEMBL77795 1 9.51
CHEMBL542409 1 9.42
CHEMBL553729 1 9.29
CHEMBL539783 1 9.28
CHEMBL192 SILDENAFIL 4.0 1 9.00
CHEMBL77971 1 9.00
CHEMBL539357 1 8.92
CHEMBL1202833 1 8.74
CHEMBL542410 1 8.72
CHEMBL539266 1 8.64
CHEMBL541823 1 8.59
CHEMBL539778 1 7.96
CHEMBL77893 1 7.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL540031 IC50 = 0.22 nM 9.66
CHEMBL540294 IC50 = 0.23 nM 9.64
CHEMBL541822 IC50 = 0.29 nM 9.54
CHEMBL77795 IC50 = 0.31 nM 9.51
CHEMBL542409 IC50 = 0.38 nM 9.42
CHEMBL553729 IC50 = 0.51 nM 9.29
CHEMBL539783 IC50 = 0.52 nM 9.28
CHEMBL192 SILDENAFIL IC50 = 1.0 nM 9.00
CHEMBL77971 IC50 = 1.0 nM 9.00
CHEMBL539357 IC50 = 1.2 nM 8.92
CHEMBL1202833 IC50 = 1.8 nM 8.74
CHEMBL542410 IC50 = 1.9 nM 8.72
CHEMBL539266 IC50 = 2.3 nM 8.64
CHEMBL541823 IC50 = 2.6 nM 8.59
CHEMBL539778 IC50 = 11.0 nM 7.96
CHEMBL77893 IC50 = 94.0 nM 7.03