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Assay Detail

CHEMBL759160

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

Binding
Inhibition of cAMP PDE III enzyme
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Phosphodiesterase 3 (CHEMBL2094125)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Cardiotonic agents. 8. Selective inhibitors of adenosine 3',5'-cyclic phosphate phosphodiesterase III. Elaboration of a five-point model for positive inotropic activity.
Moos WH, Humblet CC, Sircar I, Rithner C, Weishaar RE, Bristol JA, McPhail AT.
J Med Chem (1987) 30 : 1963 -1972
PubMed 2822927 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.34 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL299631 1 6.92
CHEMBL440593 CI-930 1 6.22
CHEMBL58005 1 5.92
CHEMBL58460 1 5.80
CHEMBL300175 1 5.75
CHEMBL61692 1 5.72
CHEMBL189 MILRINONE 4.0 1 5.60
CHEMBL287398 1 5.14
CHEMBL12831 IMAZODAN 2.0 1 5.10
CHEMBL58355 PIROXIMONE 2.0 1 5.07
CHEMBL58728 1 4.92
CHEMBL249856 ENOXIMONE 3.0 1 4.85
CHEMBL30367 1 4.40
CHEMBL12856 INAMRINONE 4.0 1 4.34
CHEMBL31105 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL299631 IC50 = 120.0 nM 6.92
CHEMBL440593 CI-930 IC50 = 600.0 nM 6.22
CHEMBL58005 IC50 = 1200.0 nM 5.92
CHEMBL58460 IC50 = 1600.0 nM 5.80
CHEMBL300175 IC50 = 1800.0 nM 5.75
CHEMBL61692 IC50 = 1900.0 nM 5.72
CHEMBL189 MILRINONE IC50 = 2500.0 nM 5.60
CHEMBL287398 IC50 = 7200.0 nM 5.14
CHEMBL12831 IMAZODAN IC50 = 8000.0 nM 5.10
CHEMBL58355 PIROXIMONE IC50 = 8600.0 nM 5.07
CHEMBL58728 IC50 = 12000.0 nM 4.92
CHEMBL249856 ENOXIMONE IC50 = 14000.0 nM 4.85
CHEMBL30367 IC50 = 40000.0 nM 4.40
CHEMBL12856 INAMRINONE IC50 = 46000.0 nM 4.34
CHEMBL31105 IC50 = 50000.0 nM 4.30