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Assay Detail

CHEMBL759849

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

Binding
Inhibition of cyclic GMP sensitive phosphodiesterase PDE 2 of human lung
5
Total Activities
5
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

cGMP-dependent 3',5'-cyclic phosphodiesterase (CHEMBL2652)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity.
Weishaar RE, Cain MH, Bristol JA.
J Med Chem (1985) 28 : 537 -545
PubMed 2985781 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.60 4.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL275084 ISOBUTYLMETHYLXANTHINE 1 4.92
CHEMBL19224 PAPAVERINE 3.0 1 4.77
CHEMBL150764 BUFROLIN 2.0 1 4.10
CHEMBL28079 ZAPRINAST 2.0 1 -
CHEMBL18701 RO-201724 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL275084 ISOBUTYLMETHYLXANTHINE IC50 = 12000.0 nM 4.92
CHEMBL19224 PAPAVERINE IC50 = 17000.0 nM 4.77
CHEMBL150764 BUFROLIN IC50 = 80000.0 nM 4.10
CHEMBL28079 ZAPRINAST IC50 = 170000.0 nM -
CHEMBL18701 RO-201724 IC50 = 390000.0 nM -