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Assay Detail

CHEMBL1106526

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

Binding
Inhibition of PDE5 in human platelet by assessed as hydrolysis of [3H]cGMP scintillation proximity assay
33
Total Activities
33
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

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

Publication

1-(2-Ethoxyethyl)-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 : 3120 -3124
PubMed 20443228 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 9.38 10.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1098465 1 10.96
CHEMBL1094365 1 10.40
CHEMBL1094249 1 10.30
CHEMBL1094544 1 10.15
CHEMBL1097506 1 10.15
CHEMBL1098466 1 10.15
CHEMBL1098141 1 10.10
CHEMBL1097823 1 10.10
CHEMBL1094191 1 10.06
CHEMBL1097822 1 9.72
CHEMBL1094499 1 9.70
CHEMBL1094833 1 9.46
CHEMBL1095186 1 9.42
CHEMBL1094399 1 9.40
CHEMBL1094830 1 9.38
CHEMBL1094238 1 9.30
CHEMBL1095175 1 9.19
CHEMBL1095176 1 9.18
CHEMBL1098114 1 9.14
CHEMBL1097782 1 9.12
CHEMBL1094832 1 9.11
CHEMBL1094211 1 9.05
CHEMBL1094490 1 8.92
CHEMBL1097781 1 8.92
CHEMBL1095185 1 8.85
CHEMBL1094190 1 8.70
CHEMBL1094500 1 8.64
CHEMBL1097783 1 8.64
CHEMBL1097780 1 8.60
CHEMBL1094210 1 8.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1098465 IC50 = 0.011 nM 10.96
CHEMBL1094365 IC50 = 0.04 nM 10.40
CHEMBL1094249 IC50 = 0.05 nM 10.30
CHEMBL1094544 IC50 = 0.07 nM 10.15
CHEMBL1097506 IC50 = 0.07 nM 10.15
CHEMBL1098466 IC50 = 0.07 nM 10.15
CHEMBL1098141 IC50 = 0.08 nM 10.10
CHEMBL1097823 IC50 = 0.08 nM 10.10
CHEMBL1094191 IC50 = 0.087 nM 10.06
CHEMBL1097822 IC50 = 0.19 nM 9.72
CHEMBL1094499 IC50 = 0.2 nM 9.70
CHEMBL1094833 IC50 = 0.35 nM 9.46
CHEMBL1095186 IC50 = 0.38 nM 9.42
CHEMBL1094399 IC50 = 0.4 nM 9.40
CHEMBL1094830 IC50 = 0.42 nM 9.38
CHEMBL1094238 IC50 = 0.5 nM 9.30
CHEMBL1095175 IC50 = 0.65 nM 9.19
CHEMBL1095176 IC50 = 0.66 nM 9.18
CHEMBL1098114 IC50 = 0.72 nM 9.14
CHEMBL1097782 IC50 = 0.76 nM 9.12
CHEMBL1094832 IC50 = 0.78 nM 9.11
CHEMBL1094211 IC50 = 0.89 nM 9.05
CHEMBL1094490 IC50 = 1.2 nM 8.92
CHEMBL1097781 IC50 = 1.2 nM 8.92
CHEMBL1095185 IC50 = 1.4 nM 8.85
CHEMBL1094190 IC50 = 2.0 nM 8.70
CHEMBL1094500 IC50 = 2.3 nM 8.64
CHEMBL1097783 IC50 = 2.3 nM 8.64
CHEMBL1097780 IC50 = 2.5 nM 8.60
CHEMBL1094210 IC50 = 2.6 nM 8.59
CHEMBL1096785 IC50 = 3.3 nM 8.48
CHEMBL1094517 IC50 = 5.5 nM 8.26
CHEMBL1094489 IC50 = 0.007 nM -