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Assay Detail

CHEMBL761831

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Binding
Inhibition of phosphodiesterase 5 from bovine lung
13
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Expert

Target

cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL3478)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Synthesis and evaluation of polycyclic pyrazolo[3,4-d]pyrimidines as PDE1 and PDE5 cGMP phosphodiesterase inhibitors.
Xia Y, Chackalamannil S, Czarniecki M, Tsai H, Vaccaro H, Cleven R, Cook J, Fawzi A, Watkins R, Zhang H.
J Med Chem (1997) 40 : 4372 -4377
PubMed 9435906 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.49 7.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL137400 1 7.12
CHEMBL68152 1 7.10
CHEMBL140173 2 7.00
CHEMBL140185 1 7.00
CHEMBL137712 1 6.85
CHEMBL344852 1 6.72
CHEMBL71768 1 6.65
CHEMBL343781 1 6.40
CHEMBL343973 1 6.00
CHEMBL139501 1 5.68
CHEMBL136367 1 5.54
CHEMBL343971 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL137400 IC50 = 75.0 nM 7.12
CHEMBL68152 IC50 = 80.0 nM 7.10
CHEMBL140173 IC50 = 100.0 nM 7.00
CHEMBL140185 IC50 = 100.0 nM 7.00
CHEMBL137712 IC50 = 140.0 nM 6.85
CHEMBL140173 IC50 = 140.0 nM 6.85
CHEMBL344852 IC50 = 190.0 nM 6.72
CHEMBL71768 IC50 = 225.0 nM 6.65
CHEMBL343781 IC50 = 400.0 nM 6.40
CHEMBL343973 IC50 = 1000.0 nM 6.00
CHEMBL139501 IC50 = 2100.0 nM 5.68
CHEMBL136367 IC50 = 2900.0 nM 5.54
CHEMBL343971 IC50 = 3100.0 nM 5.51