Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL828235

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

Binding
Inhibition of human Phosphodiesterase 5 purified from MCF-7 cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MCF7
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: design, synthesis and structure-activity relationship studies.
Vergne F, Bernardelli P, Lorthiois E, Pham N, Proust E, Oliveira C, Mafroud AK, Royer F, Wrigglesworth R, Schellhaas J, Barvian M, Moreau F, Idrissi M, Tertre A, Bertin B, Coupe M, Berna P, Soulard P.
Bioorg Med Chem Lett (2004) 14 : 4607 -4613
PubMed 15324874 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 4.93 5.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL184017 1 5.40
CHEMBL182227 1 5.29
CHEMBL185203 1 5.16
CHEMBL185604 1 5.14
CHEMBL263311 1 5.12
CHEMBL185532 1 4.96
CHEMBL182574 1 4.75
CHEMBL184837 1 4.73
CHEMBL360874 1 4.70
CHEMBL363673 1 4.63
CHEMBL183156 1 4.39
CHEMBL365206 1 -
CHEMBL361512 1 -
CHEMBL184960 1 -
CHEMBL363709 1 -
CHEMBL185531 1 -
CHEMBL362719 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL184017 IC50 = 3970.0 nM 5.40
CHEMBL182227 IC50 = 5180.0 nM 5.29
CHEMBL185203 IC50 = 7000.0 nM 5.16
CHEMBL185604 IC50 = 7270.0 nM 5.14
CHEMBL263311 IC50 = 7560.0 nM 5.12
CHEMBL185532 IC50 = 10940.0 nM 4.96
CHEMBL182574 IC50 = 17880.0 nM 4.75
CHEMBL184837 IC50 = 18770.0 nM 4.73
CHEMBL360874 IC50 = 20160.0 nM 4.70
CHEMBL363673 IC50 = 23600.0 nM 4.63
CHEMBL183156 IC50 = 40350.0 nM 4.39
CHEMBL365206 IC50 > 101000.0 nM -
CHEMBL361512 IC50 > 101000.0 nM -
CHEMBL184960 IC50 > 101000.0 nM -
CHEMBL363709 IC50 > 101000.0 nM -
CHEMBL185531 IC50 > 101000.0 nM -
CHEMBL362719 IC50 = 101000.0 nM -