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Assay Detail

CHEMBL762496

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

Binding
Phosphodiesterase 5 activity of human corpus cavernosum
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrimidinylpyrroloquinolones as highly potent and selective PDE5 inhibitors for treatment of erectile dysfunction.
Sui Z, Guan J, Macielag MJ, Jiang W, Zhang S, Qiu Y, Kraft P, Bhattacharjee S, John TM, Haynes-Johnson D, Clancy J.
J Med Chem (2002) 45 : 4094 -4096
PubMed 12213052 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 9.07 9.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1744059 1 9.68
CHEMBL336815 1 9.68
CHEMBL130721 1 9.64
CHEMBL133687 1 9.54
CHEMBL131718 1 9.51
CHEMBL130811 1 9.40
CHEMBL131892 1 9.28
CHEMBL280439 1 9.28
CHEMBL132689 1 8.97
CHEMBL336291 1 8.94
CHEMBL341092 1 8.92
CHEMBL131541 1 8.76
CHEMBL192 SILDENAFIL 4.0 1 8.73
CHEMBL133285 1 8.05
CHEMBL130612 1 7.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1744059 Ki = 0.21 nM 9.68
CHEMBL336815 Ki = 0.21 nM 9.68
CHEMBL130721 Ki = 0.23 nM 9.64
CHEMBL133687 Ki = 0.29 nM 9.54
CHEMBL131718 Ki = 0.31 nM 9.51
CHEMBL130811 Ki = 0.4 nM 9.40
CHEMBL131892 Ki = 0.52 nM 9.28
CHEMBL280439 Ki = 0.53 nM 9.28
CHEMBL132689 Ki = 1.08 nM 8.97
CHEMBL336291 Ki = 1.14 nM 8.94
CHEMBL341092 Ki = 1.2 nM 8.92
CHEMBL131541 Ki = 1.75 nM 8.76
CHEMBL192 SILDENAFIL Ki = 1.87 nM 8.73
CHEMBL133285 Ki = 8.86 nM 8.05
CHEMBL130612 Ki = 24.7 nM 7.61