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Assay Detail

CHEMBL831691

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Binding
Inhibition of human phosphodiesterase 4
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2093863)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.
Boyle CD, Xu R, Asberom T, Chackalamannil S, Clader JW, Greenlee WJ, Guzik H, Hu Y, Hu Z, Lankin CM, Pissarnitski DA, Stamford AW, Wang Y, Skell J, Kurowski S, Vemulapalli S, Palamanda J, Chintala M, Wu P, Myers J, Wang P.
Bioorg Med Chem Lett (2005) 15 : 2365 -2369
PubMed 15837326 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.41 5.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL373102 1 5.85
CHEMBL1520 VARDENAFIL 4.0 1 5.35
CHEMBL192 SILDENAFIL 4.0 1 5.02
CHEMBL779 TADALAFIL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL373102 IC50 = 1400.0 nM 5.85
CHEMBL1520 VARDENAFIL IC50 = 4500.0 nM 5.35
CHEMBL192 SILDENAFIL IC50 = 9600.0 nM 5.02
CHEMBL779 TADALAFIL IC50 > 10000.0 nM -