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Assay Detail

CHEMBL1664617

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

Binding
Inhibition of human recombinant PDE5A-mediated hydrolysis of cGMP after 30 mins by fluorescence polarization assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and molecular modeling of novel tetrahydro-β-carboline derivatives with phosphodiesterase 5 inhibitory and anticancer properties.
Mohamed HA, Girgis NM, Wilcken R, Bauer MR, Tinsley HN, Gary BD, Piazza GA, Boeckler FM, Abadi AH.
J Med Chem (2011) 54 : 495 -509
PubMed 21189023 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.34 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1650866 1 8.70
CHEMBL779 TADALAFIL 4.0 1 8.52
CHEMBL1650676 1 8.15
CHEMBL1650673 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1650866 IC50 = 2.0 nM 8.70
CHEMBL779 TADALAFIL IC50 = 3.0 nM 8.52
CHEMBL1650676 IC50 = 7.0 nM 8.15
CHEMBL1650673 IC50 = 10.0 nM 8.00