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

CHEMBL761833

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

Binding
In vitro inhibitory activity against bovine phosphodiesterase 5
33
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL3478)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.
Daugan A, Grondin P, Ruault C, Le Monnier de Gouville AC, Coste H, Linget JM, Kirilovsky J, Hyafil F, Labaudinière R.
J Med Chem (2003) 46 : 4533 -4542
PubMed 14521415 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 7.72 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL138466 2 8.52
CHEMBL342459 1 8.52
CHEMBL343553 1 8.30
CHEMBL343941 1 8.30
CHEMBL779 TADALAFIL 4.0 2 8.30
CHEMBL138504 1 8.30
CHEMBL141307 1 8.22
CHEMBL140599 1 8.22
CHEMBL434797 2 8.22
CHEMBL139771 1 8.10
CHEMBL336716 1 8.05
CHEMBL142143 1 8.00
CHEMBL342008 NORTADALAFIL 2 7.96
CHEMBL142138 1 7.82
CHEMBL141703 1 7.77
CHEMBL445576 1 7.75
CHEMBL436019 1 7.64
CHEMBL139597 1 7.58
CHEMBL334684 1 7.39
CHEMBL342876 1 7.22
CHEMBL141518 1 7.22
CHEMBL343325 1 7.16
CHEMBL139028 1 7.05
CHEMBL344700 1 7.04
CHEMBL2111963 1 6.86
CHEMBL336050 1 6.12
CHEMBL139521 1 5.22
CHEMBL344855 1 -
CHEMBL341939 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL138466 IC50 = 3.0 nM 8.52
CHEMBL342459 IC50 = 3.0 nM 8.52
CHEMBL779 TADALAFIL IC50 = 5.0 nM 8.30
CHEMBL138466 IC50 = 5.0 nM 8.30
CHEMBL779 TADALAFIL IC50 = 5.0 nM 8.30
CHEMBL343553 IC50 = 5.0 nM 8.30
CHEMBL138504 IC50 = 5.0 nM 8.30
CHEMBL343941 IC50 = 5.0 nM 8.30
CHEMBL141307 IC50 = 6.0 nM 8.22
CHEMBL140599 IC50 = 6.0 nM 8.22
CHEMBL434797 IC50 = 6.0 nM 8.22
CHEMBL139771 IC50 = 8.0 nM 8.10
CHEMBL434797 IC50 = 8.0 nM 8.10
CHEMBL336716 IC50 = 9.0 nM 8.05
CHEMBL142143 IC50 = 10.0 nM 8.00
CHEMBL342008 NORTADALAFIL IC50 = 11.0 nM 7.96
CHEMBL342008 NORTADALAFIL IC50 = 12.0 nM 7.92
CHEMBL142138 IC50 = 15.0 nM 7.82
CHEMBL141703 IC50 = 17.0 nM 7.77
CHEMBL445576 IC50 = 18.0 nM 7.75
CHEMBL436019 IC50 = 23.0 nM 7.64
CHEMBL139597 IC50 = 26.0 nM 7.58
CHEMBL334684 IC50 = 41.0 nM 7.39
CHEMBL342876 IC50 = 60.0 nM 7.22
CHEMBL141518 IC50 = 60.0 nM 7.22
CHEMBL343325 IC50 = 70.0 nM 7.16
CHEMBL139028 IC50 = 90.0 nM 7.05
CHEMBL344700 IC50 = 91.0 nM 7.04
CHEMBL2111963 IC50 = 138.0 nM 6.86
CHEMBL336050 IC50 = 758.0 nM 6.12
CHEMBL139521 IC50 = 6000.0 nM 5.22
CHEMBL344855 IC50 > 10000.0 nM -
CHEMBL341939 IC50 > 10000.0 nM -