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Assay Detail

CHEMBL760828

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

Binding
Inhibitory activity against Phosphodiesterase 5 (PDE5) was evaluated
29
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

Furoyl and benzofuroyl pyrroloquinolones as potent and selective PDE5 inhibitors for treatment of erectile dysfunction.
Jiang W, Sui Z, Macielag MJ, Walsh SP, Fiordeliso JJ, Lanter JC, Guan J, Qiu Y, Kraft P, Bhattacharjee S, Craig E, Haynes-Johnson D, John TM, Clancy J.
J Med Chem (2003) 46 : 441 -444
PubMed 12540243 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 8.98 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL139785 1 9.82
CHEMBL334903 2 9.70
CHEMBL342159 1 9.62
CHEMBL138949 1 9.51
CHEMBL336003 1 9.46
CHEMBL343596 1 9.33
CHEMBL423180 1 9.28
CHEMBL424280 1 9.21
CHEMBL344431 1 9.21
CHEMBL342922 1 9.15
CHEMBL335784 1 9.14
CHEMBL342404 1 9.12
CHEMBL344152 1 9.01
CHEMBL142030 1 9.00
CHEMBL136521 1 9.00
CHEMBL422100 1 8.89
CHEMBL138511 1 8.77
CHEMBL136498 1 8.76
CHEMBL342197 1 8.75
CHEMBL192 SILDENAFIL 4.0 1 8.72
CHEMBL423177 1 8.68
CHEMBL336921 1 8.68
CHEMBL344366 1 8.60
CHEMBL337782 1 8.58
CHEMBL337560 1 8.57
CHEMBL138799 1 8.48
CHEMBL335090 1 8.43
CHEMBL337804 1 8.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL139785 Ki = 0.15 nM 9.82
CHEMBL334903 Ki = 0.2 nM 9.70
CHEMBL342159 Ki = 0.24 nM 9.62
CHEMBL138949 Ki = 0.31 nM 9.51
CHEMBL336003 Ki = 0.35 nM 9.46
CHEMBL343596 Ki = 0.47 nM 9.33
CHEMBL423180 Ki = 0.53 nM 9.28
CHEMBL424280 Ki = 0.61 nM 9.21
CHEMBL344431 Ki = 0.61 nM 9.21
CHEMBL342922 Ki = 0.71 nM 9.15
CHEMBL335784 Ki = 0.73 nM 9.14
CHEMBL342404 Ki = 0.76 nM 9.12
CHEMBL344152 Ki = 0.98 nM 9.01
CHEMBL142030 Ki = 0.99 nM 9.00
CHEMBL136521 Ki = 1.01 nM 9.00
CHEMBL422100 Ki = 1.3 nM 8.89
CHEMBL138511 Ki = 1.71 nM 8.77
CHEMBL136498 Ki = 1.74 nM 8.76
CHEMBL342197 Ki = 1.78 nM 8.75
CHEMBL334903 Ki = 1.82 nM 8.74
CHEMBL192 SILDENAFIL Ki = 1.91 nM 8.72
CHEMBL423177 Ki = 2.07 nM 8.68
CHEMBL336921 Ki = 2.09 nM 8.68
CHEMBL344366 Ki = 2.49 nM 8.60
CHEMBL337782 Ki = 2.64 nM 8.58
CHEMBL337560 Ki = 2.71 nM 8.57
CHEMBL138799 Ki = 3.32 nM 8.48
CHEMBL335090 Ki = 3.74 nM 8.43
CHEMBL337804 Ki = 4.66 nM 8.33