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Assay Detail

CHEMBL762498

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Binding
Inhibitory activity against human Phosphodiesterase 5
16
Total Activities
16
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

Structure-activity relationships of N-acyl pyrroloquinolone PDE-5 inhibitors.
Lanter JC, Sui Z, Macielag MJ, Fiordeliso JJ, Jiang W, Qiu Y, Bhattacharjee S, Kraft P, John TM, Haynes-Johnson D, Craig E, Clancy J.
J Med Chem (2004) 47 : 656 -662
PubMed 14736245 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 8.39 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL158374 1 9.66
CHEMBL351813 1 9.64
CHEMBL158817 1 9.54
CHEMBL263000 1 9.46
CHEMBL157819 1 9.24
CHEMBL161408 1 8.97
CHEMBL192 SILDENAFIL 4.0 1 8.72
CHEMBL344366 1 8.60
CHEMBL158829 1 8.46
CHEMBL345179 1 8.34
CHEMBL160847 1 7.96
CHEMBL157701 1 7.90
CHEMBL422006 1 7.63
CHEMBL158633 1 6.95
CHEMBL160556 1 6.93
CHEMBL349299 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL158374 Ki = 0.22 nM 9.66
CHEMBL351813 Ki = 0.23 nM 9.64
CHEMBL158817 Ki = 0.29 nM 9.54
CHEMBL263000 Ki = 0.35 nM 9.46
CHEMBL157819 Ki = 0.58 nM 9.24
CHEMBL161408 Ki = 1.06 nM 8.97
CHEMBL192 SILDENAFIL Ki = 1.91 nM 8.72
CHEMBL344366 Ki = 2.49 nM 8.60
CHEMBL158829 Ki = 3.48 nM 8.46
CHEMBL345179 Ki = 4.53 nM 8.34
CHEMBL160847 Ki = 11.0 nM 7.96
CHEMBL157701 Ki = 12.5 nM 7.90
CHEMBL422006 Ki = 23.3 nM 7.63
CHEMBL158633 Ki = 113.0 nM 6.95
CHEMBL160556 Ki = 118.0 nM 6.93
CHEMBL349299 Ki = 601.0 nM 6.22