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Assay Detail

CHEMBL765553

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Binding
Inhibitory concentration against cAMP PDE I enzyme in guinea pig
13
Total Activities
13
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 1 (CHEMBL2095150)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Cardiotonic agents. 7. Inhibition of separated forms of cyclic nucleotide phosphodiesterase from guinea pig cardiac muscle by 4,5-dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3(2H)-pyridazinones and related compounds. Structure-activity relationships and correlation with in vivo positive inotropic activity.
Sircar I, Weishaar RE, Kobylarz D, Moos WH, Bristol JA.
J Med Chem (1987) 30 : 1955 -1962
PubMed 2822926 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.10 4.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282765 TETRAHYDROBENXIMIDAZOLE 1 4.12
CHEMBL30908 1 4.07
CHEMBL31112 1 -
CHEMBL31105 1 -
CHEMBL30362 1 -
CHEMBL30368 1 -
CHEMBL30623 1 -
CHEMBL30358 1 -
CHEMBL58728 1 -
CHEMBL448467 1 -
CHEMBL30367 1 -
CHEMBL30402 1 -
CHEMBL286502 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282765 TETRAHYDROBENXIMIDAZOLE IC50 = 75000.0 nM 4.12
CHEMBL30908 IC50 = 86000.0 nM 4.07
CHEMBL31112 IC50 > 1000000.0 nM -
CHEMBL31105 IC50 = 660000.0 nM -
CHEMBL30362 IC50 > 1000000.0 nM -
CHEMBL30368 IC50 = 790000.0 nM -
CHEMBL30623 IC50 = 180000.0 nM -
CHEMBL30358 IC50 = 380000.0 nM -
CHEMBL58728 IC50 = 460000.0 nM -
CHEMBL448467 IC50 > 500000.0 nM -
CHEMBL30367 IC50 = 930000.0 nM -
CHEMBL30402 IC50 = 280000.0 nM -
CHEMBL286502 IC50 > 1000000.0 nM -