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Assay Detail

CHEMBL829671

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

Binding
Inhibition of phosphodiesterase 5 in rat fetal lung fibroblast (RFL-6) cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type RFL-6
Confidence 9 — Direct single protein target
Curated By Expert

Target

cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL4567)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Pyrroloquinolone PDE5 inhibitors with improved pharmaceutical profiles for clinical studies on erectile dysfunction.
Jiang W, Guan J, Macielag MJ, Zhang S, Qiu Y, Kraft P, Bhattacharjee S, John TM, Haynes-Johnson D, Lundeen S, Sui Z.
J Med Chem (2005) 48 : 2126 -2133
PubMed 15771456 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 9.42 10.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL425690 1 10.72
CHEMBL369621 1 9.92
CHEMBL367206 1 9.82
CHEMBL178056 1 9.77
CHEMBL177881 1 9.72
CHEMBL177427 1 9.66
CHEMBL360793 1 9.62
CHEMBL178693 1 9.62
CHEMBL355574 1 9.54
CHEMBL367142 1 9.48
CHEMBL178541 1 9.44
CHEMBL173728 1 9.29
CHEMBL280439 1 9.28
CHEMBL130811 1 9.28
CHEMBL175987 1 9.19
CHEMBL192 SILDENAFIL 4.0 1 8.74
CHEMBL779 TADALAFIL 4.0 1 8.30
CHEMBL369259 1 8.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL425690 Ki = 0.019 nM 10.72
CHEMBL369621 Ki = 0.12 nM 9.92
CHEMBL367206 Ki = 0.15 nM 9.82
CHEMBL178056 Ki = 0.17 nM 9.77
CHEMBL177881 Ki = 0.19 nM 9.72
CHEMBL177427 Ki = 0.22 nM 9.66
CHEMBL360793 Ki = 0.24 nM 9.62
CHEMBL178693 Ki = 0.24 nM 9.62
CHEMBL355574 Ki = 0.29 nM 9.54
CHEMBL367142 Ki = 0.33 nM 9.48
CHEMBL178541 Ki = 0.36 nM 9.44
CHEMBL173728 Ki = 0.51 nM 9.29
CHEMBL280439 Ki = 0.53 nM 9.28
CHEMBL130811 Ki = 0.52 nM 9.28
CHEMBL175987 Ki = 0.65 nM 9.19
CHEMBL192 SILDENAFIL Ki = 1.8 nM 8.74
CHEMBL779 TADALAFIL Ki = 5.0 nM 8.30
CHEMBL369259 Ki = 6.43 nM 8.19