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Assay Detail

CHEMBL963850

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

Binding
Inhibition of human recombinant PDE11
16
Total Activities
16
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

Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A (CHEMBL2717)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Quinazolines as potent and highly selective PDE5 inhibitors as potential therapeutics for male erectile dysfunction.
Kim YH, Choi H, Lee J, Hwang IC, Moon SK, Kim SJ, Lee HW, Im DS, Lee SS, Ahn SK, Kim SW, Han CK, Yoon JH, Lee KJ, Choi NS.
Bioorg Med Chem Lett (2008) 18 : 6279 -6282
PubMed 18976905 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.09 6.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL779 TADALAFIL 4.0 1 6.54
CHEMBL192 SILDENAFIL 4.0 1 5.52
CHEMBL512174 1 5.15
CHEMBL471702 1 5.11
CHEMBL520074 1 5.11
CHEMBL488080 1 5.11
CHEMBL471703 1 5.02
CHEMBL521075 1 4.98
CHEMBL471701 1 4.83
CHEMBL471529 1 4.64
CHEMBL488265 1 4.61
CHEMBL513593 1 4.41
CHEMBL471528 1 -
CHEMBL470492 1 -
CHEMBL488091 1 -
CHEMBL487247 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL779 TADALAFIL IC50 = 290.0 nM 6.54
CHEMBL192 SILDENAFIL IC50 = 3000.0 nM 5.52
CHEMBL512174 IC50 = 7100.0 nM 5.15
CHEMBL471702 IC50 = 7700.0 nM 5.11
CHEMBL520074 IC50 = 7800.0 nM 5.11
CHEMBL488080 IC50 = 7700.0 nM 5.11
CHEMBL471703 IC50 = 9500.0 nM 5.02
CHEMBL521075 IC50 = 10500.0 nM 4.98
CHEMBL471701 IC50 = 14700.0 nM 4.83
CHEMBL471529 IC50 = 22700.0 nM 4.64
CHEMBL488265 IC50 = 24300.0 nM 4.61
CHEMBL513593 IC50 = 39300.0 nM 4.41
CHEMBL471528 IC50 - -
CHEMBL470492 IC50 - -
CHEMBL488091 IC50 - -
CHEMBL487247 IC50 - -