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Assay Detail

CHEMBL761830

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

Binding
Inhibitory activity against bovine PDE5 (phosphodiesterase-5).
32
Total Activities
32
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. 1: 5,6,11,11a-tetrahydro-1H-imidazo[1',5':1,6]pyrido[3,4-b]indole-1,3(2H)-dione analogues.
Daugan A, Grondin P, Ruault C, Le Monnier de Gouville AC, Coste H, Kirilovsky J, Hyafil F, Labaudinière R.
J Med Chem (2003) 46 : 4525 -4532
PubMed 14521414 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 7.40 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL141631 1 8.52
CHEMBL141918 1 8.40
CHEMBL337587 1 8.30
CHEMBL140874 1 8.22
CHEMBL192 SILDENAFIL 4.0 1 8.22
CHEMBL138658 1 8.15
CHEMBL334910 1 8.15
CHEMBL422104 1 8.10
CHEMBL344173 1 8.00
CHEMBL140828 1 8.00
CHEMBL343832 1 7.75
CHEMBL344630 1 7.70
CHEMBL336457 1 7.70
CHEMBL138256 1 7.70
CHEMBL337770 1 7.70
CHEMBL141577 1 7.52
CHEMBL335148 1 7.52
CHEMBL141633 1 7.30
CHEMBL139048 1 7.30
CHEMBL502020 1 7.30
CHEMBL423550 1 7.22
CHEMBL140493 1 7.05
CHEMBL141980 1 7.00
CHEMBL344676 1 7.00
CHEMBL28079 ZAPRINAST 2.0 1 6.70
CHEMBL2110369 1 6.52
CHEMBL141506 1 6.52
CHEMBL11709 1 6.10
CHEMBL141975 1 6.05
CHEMBL504118 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL141631 IC50 = 3.0 nM 8.52
CHEMBL141918 IC50 = 4.0 nM 8.40
CHEMBL337587 IC50 = 5.0 nM 8.30
CHEMBL140874 IC50 = 6.0 nM 8.22
CHEMBL192 SILDENAFIL IC50 = 6.0 nM 8.22
CHEMBL138658 IC50 = 7.0 nM 8.15
CHEMBL334910 IC50 = 7.0 nM 8.15
CHEMBL422104 IC50 = 8.0 nM 8.10
CHEMBL344173 IC50 = 10.0 nM 8.00
CHEMBL140828 IC50 = 10.0 nM 8.00
CHEMBL343832 IC50 = 18.0 nM 7.75
CHEMBL344630 IC50 = 20.0 nM 7.70
CHEMBL336457 IC50 = 20.0 nM 7.70
CHEMBL138256 IC50 = 20.0 nM 7.70
CHEMBL337770 IC50 = 20.0 nM 7.70
CHEMBL335148 IC50 = 30.0 nM 7.52
CHEMBL141577 IC50 = 30.0 nM 7.52
CHEMBL141633 IC50 = 50.0 nM 7.30
CHEMBL139048 IC50 = 50.0 nM 7.30
CHEMBL502020 IC50 = 50.0 nM 7.30
CHEMBL423550 IC50 = 60.0 nM 7.22
CHEMBL140493 IC50 = 90.0 nM 7.05
CHEMBL141980 IC50 = 100.0 nM 7.00
CHEMBL344676 IC50 = 100.0 nM 7.00
CHEMBL28079 ZAPRINAST IC50 = 200.0 nM 6.70
CHEMBL2110369 IC50 = 300.0 nM 6.52
CHEMBL141506 IC50 = 300.0 nM 6.52
CHEMBL11709 IC50 = 800.0 nM 6.10
CHEMBL141975 IC50 = 900.0 nM 6.05
CHEMBL504118 IC50 = 1000.0 nM 6.00
CHEMBL138359 IC50 = 2000.0 nM 5.70
CHEMBL140605 IC50 > 10000.0 nM -