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

CHEMBL1106508

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

Binding
Inhibition of PDE5
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

1-(2-(2,2,2-trifluoroethoxy)ethyl-1H-pyrazolo[4,3-d]pyrimidines as potent phosphodiesterase 5 (PDE5) inhibitors.
Tollefson MB, Acker BA, Jacobsen EJ, Hughes RO, Walker JK, Fox DN, Palmer MJ, Freeman SK, Yu Y, Bond BR.
Bioorg Med Chem Lett (2010) 20 : 3125 -3128
PubMed 20400309 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 8.99 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1095121 1 10.15
CHEMBL1095406 1 10.05
CHEMBL1098752 1 9.85
CHEMBL1099069 1 9.82
CHEMBL1098055 1 9.52
CHEMBL1098751 1 9.46
CHEMBL1094399 1 9.40
CHEMBL1097717 1 9.19
CHEMBL1097718 1 9.11
CHEMBL1098056 1 9.07
CHEMBL1095122 1 9.03
CHEMBL1097719 1 9.00
CHEMBL1095176 1 8.73
CHEMBL1098654 1 8.73
CHEMBL1095455 1 8.53
CHEMBL1095440 1 8.50
CHEMBL1095405 1 8.48
CHEMBL192 SILDENAFIL 4.0 1 8.46
CHEMBL1095123 1 8.41
CHEMBL1095760 1 8.19
CHEMBL1097983 1 8.02
CHEMBL1094098 1 8.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1095121 IC50 = 0.07 nM 10.15
CHEMBL1095406 IC50 = 0.09 nM 10.05
CHEMBL1098752 IC50 = 0.14 nM 9.85
CHEMBL1099069 IC50 = 0.15 nM 9.82
CHEMBL1098055 IC50 = 0.3 nM 9.52
CHEMBL1098751 IC50 = 0.35 nM 9.46
CHEMBL1094399 IC50 = 0.4 nM 9.40
CHEMBL1097717 IC50 = 0.65 nM 9.19
CHEMBL1097718 IC50 = 0.78 nM 9.11
CHEMBL1098056 IC50 = 0.86 nM 9.07
CHEMBL1095122 IC50 = 0.94 nM 9.03
CHEMBL1097719 IC50 = 1.01 nM 9.00
CHEMBL1095176 IC50 = 1.84 nM 8.73
CHEMBL1098654 IC50 = 1.84 nM 8.73
CHEMBL1095455 IC50 = 2.96 nM 8.53
CHEMBL1095440 IC50 = 3.15 nM 8.50
CHEMBL1095405 IC50 = 3.28 nM 8.48
CHEMBL192 SILDENAFIL IC50 = 3.5 nM 8.46
CHEMBL1095123 IC50 = 3.92 nM 8.41
CHEMBL1095760 IC50 = 6.48 nM 8.19
CHEMBL1097983 IC50 = 9.52 nM 8.02
CHEMBL1094098 IC50 = 9.79 nM 8.01