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Assay Detail

CHEMBL760836

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

Binding
Inhibitory activity against Phosphodiesterase 6 isolated from bovine retina
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Phosphodiesterase 6 (CHEMBL2096979)
Type PROTEIN FAMILY
Organism Bos taurus

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 15 7.41 8.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL77795 1 8.36
CHEMBL541822 1 8.11
CHEMBL540031 1 8.07
CHEMBL542409 1 7.96
CHEMBL553729 1 7.66
CHEMBL1202833 1 7.66
CHEMBL192 SILDENAFIL 4.0 1 7.55
CHEMBL77971 1 7.55
CHEMBL539266 1 7.42
CHEMBL542410 1 7.38
CHEMBL540294 1 7.25
CHEMBL539783 1 7.14
CHEMBL539778 1 6.64
CHEMBL541823 1 6.55
CHEMBL77893 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL77795 IC50 = 4.4 nM 8.36
CHEMBL541822 IC50 = 7.7 nM 8.11
CHEMBL540031 IC50 = 8.6 nM 8.07
CHEMBL542409 IC50 = 11.0 nM 7.96
CHEMBL553729 IC50 = 22.0 nM 7.66
CHEMBL1202833 IC50 = 22.0 nM 7.66
CHEMBL192 SILDENAFIL IC50 = 28.0 nM 7.55
CHEMBL77971 IC50 = 28.0 nM 7.55
CHEMBL539266 IC50 = 38.0 nM 7.42
CHEMBL542410 IC50 = 42.0 nM 7.38
CHEMBL540294 IC50 = 56.0 nM 7.25
CHEMBL539783 IC50 = 72.0 nM 7.14
CHEMBL539778 IC50 = 230.0 nM 6.64
CHEMBL541823 IC50 = 280.0 nM 6.55
CHEMBL77893 IC50 = 1400.0 nM 5.85