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Assay Detail

CHEMBL905040

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Binding
Inhibition of human platelet PDE3
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Phosphodiesterase 3 (CHEMBL2094125)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Synthesis and in vitro antiplatelet activity of new 4-(1-piperazinyl)coumarin derivatives. Human platelet phosphodiesterase 3 inhibitory properties of the two most effective compounds described and molecular modeling study on their interactions with phosphodiesterase 3A catalytic site.
Roma G, Di Braccio M, Grossi G, Piras D, Leoncini G, Bruzzese D, Signorello MG, Fossa P, Mosti L.
J Med Chem (2007) 50 : 2886 -2895
PubMed 17500510 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.94 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL229417 1 7.43
CHEMBL228776 1 7.11
CHEMBL189 MILRINONE 4.0 1 6.68
CHEMBL799 CILOSTAZOL 4.0 1 6.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL229417 IC50 = 37.0 nM 7.43
CHEMBL228776 IC50 = 78.0 nM 7.11
CHEMBL189 MILRINONE IC50 = 210.0 nM 6.68
CHEMBL799 CILOSTAZOL IC50 = 280.0 nM 6.55