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Assay Detail

CHEMBL762497

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

Binding
Inhibitory activity against PDE5 from human corpus cavernosum
31
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

Synthesis and biological activities of novel beta-carbolines as PDE5 inhibitors.
Sui Z, Guan J, Macielag MJ, Jiang W, Qiu Y, Kraft P, Bhattacharjee S, John TM, Craig E, Haynes-Johnson D, Clancy J.
Bioorg Med Chem Lett (2003) 13 : 761 -765
PubMed 12639576 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 7.14 8.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL192 SILDENAFIL 4.0 1 8.73
CHEMBL163905 1 8.40
CHEMBL433708 1 8.09
CHEMBL133285 1 8.05
CHEMBL350187 1 7.75
CHEMBL351744 1 7.62
CHEMBL349359 1 7.49
CHEMBL166018 1 7.30
CHEMBL349947 2 7.20
CHEMBL349204 1 7.19
CHEMBL166025 1 7.11
CHEMBL165117 1 6.91
CHEMBL164755 1 6.90
CHEMBL446433 1 6.90
CHEMBL164181 1 6.89
CHEMBL165168 1 6.88
CHEMBL350515 1 6.84
CHEMBL163890 1 6.81
CHEMBL350962 1 6.75
CHEMBL423088 2 6.73
CHEMBL163712 1 6.66
CHEMBL164906 2 6.61
CHEMBL349495 1 6.26
CHEMBL350400 1 6.07
CHEMBL433528 1 -
CHEMBL165110 1 -
CHEMBL166157 1 -
CHEMBL164907 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL192 SILDENAFIL Ki = 1.87 nM 8.73
CHEMBL163905 Ki = 4.0 nM 8.40
CHEMBL433708 Ki = 8.11 nM 8.09
CHEMBL133285 Ki = 8.86 nM 8.05
CHEMBL350187 Ki = 18.0 nM 7.75
CHEMBL351744 Ki = 24.0 nM 7.62
CHEMBL349359 Ki = 32.3 nM 7.49
CHEMBL166018 Ki = 50.6 nM 7.30
CHEMBL349947 Ki = 62.8 nM 7.20
CHEMBL349947 Ki = 62.8 nM 7.20
CHEMBL349204 Ki = 64.2 nM 7.19
CHEMBL166025 Ki = 77.5 nM 7.11
CHEMBL165117 Ki = 123.0 nM 6.91
CHEMBL164755 Ki = 126.0 nM 6.90
CHEMBL446433 Ki = 126.0 nM 6.90
CHEMBL164181 Ki = 130.0 nM 6.89
CHEMBL165168 Ki = 132.0 nM 6.88
CHEMBL350515 Ki = 145.0 nM 6.84
CHEMBL163890 Ki = 154.0 nM 6.81
CHEMBL350962 Ki = 179.0 nM 6.75
CHEMBL423088 Ki = 188.0 nM 6.73
CHEMBL423088 Ki = 189.0 nM 6.72
CHEMBL163712 Ki = 219.0 nM 6.66
CHEMBL164906 Ki = 246.0 nM 6.61
CHEMBL164906 Ki = 246.0 nM 6.61
CHEMBL349495 Ki = 543.0 nM 6.26
CHEMBL350400 Ki = 850.0 nM 6.07
CHEMBL433528 Ki > 10000.0 nM -
CHEMBL166157 Ki > 5000.0 nM -
CHEMBL165110 Ki > 1000.0 nM -
CHEMBL164907 Ki > 100.0 nM -