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Assay Detail

CHEMBL762824

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

Binding
Inhibitory activity against phosphodiesterase 5 (PDE5) obtained from human corpus cavernosum tissue
30
Total Activities
28
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 (CHEMBL1827)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological activity of beta-carboline-based type-5 phosphodiesterase inhibitors.
Maw GN, Allerton CM, Gbekor E, Million WA.
Bioorg Med Chem Lett (2003) 13 : 1425 -1428
PubMed 12668004 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 8.03 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282515 2 9.15
CHEMBL418594 1 8.92
CHEMBL284070 1 8.82
CHEMBL33518 1 8.72
CHEMBL33121 1 8.70
CHEMBL32255 1 8.68
CHEMBL33627 1 8.60
CHEMBL34276 1 8.57
CHEMBL285737 1 8.44
CHEMBL286309 1 8.40
CHEMBL34628 1 8.40
CHEMBL779 TADALAFIL 4.0 1 8.17
CHEMBL34802 1 8.15
CHEMBL33147 1 8.08
CHEMBL34744 1 7.89
CHEMBL33381 1 7.88
CHEMBL284560 2 7.81
CHEMBL33944 1 7.80
CHEMBL284059 1 7.77
CHEMBL284627 1 7.70
CHEMBL286905 1 7.58
CHEMBL30936 1 7.25
CHEMBL284258 1 7.24
CHEMBL34169 1 6.90
CHEMBL284535 1 6.88
CHEMBL284594 1 6.87
CHEMBL284719 1 6.79
CHEMBL284745 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282515 IC50 = 0.7 nM 9.15
CHEMBL282515 IC50 = 0.8 nM 9.10
CHEMBL418594 IC50 = 1.2 nM 8.92
CHEMBL284070 IC50 = 1.5 nM 8.82
CHEMBL33518 IC50 = 1.9 nM 8.72
CHEMBL33121 IC50 = 2.0 nM 8.70
CHEMBL32255 IC50 = 2.1 nM 8.68
CHEMBL33627 IC50 = 2.5 nM 8.60
CHEMBL34276 IC50 = 2.7 nM 8.57
CHEMBL285737 IC50 = 3.6 nM 8.44
CHEMBL286309 IC50 = 4.0 nM 8.40
CHEMBL34628 IC50 = 4.0 nM 8.40
CHEMBL779 TADALAFIL IC50 = 6.7 nM 8.17
CHEMBL34802 IC50 = 7.1 nM 8.15
CHEMBL33147 IC50 = 8.4 nM 8.08
CHEMBL34744 IC50 = 12.8 nM 7.89
CHEMBL33381 IC50 = 13.2 nM 7.88
CHEMBL284560 IC50 = 15.6 nM 7.81
CHEMBL33944 IC50 = 15.7 nM 7.80
CHEMBL284059 IC50 = 17.0 nM 7.77
CHEMBL284627 IC50 = 19.8 nM 7.70
CHEMBL286905 IC50 = 26.0 nM 7.58
CHEMBL284560 IC50 = 28.6 nM 7.54
CHEMBL30936 IC50 = 56.0 nM 7.25
CHEMBL284258 IC50 = 57.0 nM 7.24
CHEMBL34169 IC50 = 127.0 nM 6.90
CHEMBL284535 IC50 = 132.0 nM 6.88
CHEMBL284594 IC50 = 134.0 nM 6.87
CHEMBL284719 IC50 = 164.0 nM 6.79
CHEMBL284745 IC50 > 1000.0 nM -