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Assay Detail

CHEMBL876977

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

Binding
Inhibition of human phosphodiesterase 11
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 Expert

Target

Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A (CHEMBL2717)
Type SINGLE PROTEIN
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 6.57 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL779 TADALAFIL 4.0 1 7.48
CHEMBL1520 VARDENAFIL 4.0 1 6.89
CHEMBL373102 1 6.27
CHEMBL192 SILDENAFIL 4.0 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL779 TADALAFIL IC50 = 33.0 nM 7.48
CHEMBL1520 VARDENAFIL IC50 = 130.0 nM 6.89
CHEMBL373102 IC50 = 540.0 nM 6.27
CHEMBL192 SILDENAFIL IC50 = 2300.0 nM 5.64