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Assay Detail

CHEMBL905037

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Functional
Inhibition of 5.0 ug/mL collagen-induced platelet aggregation in human platelet rich plasma
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Plasma
Confidence 1 — Organism
Curated By Autocuration

Target

Plasma (CHEMBL613652)
Type TISSUE
Organism Rattus norvegicus

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 31 5.38 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL228776 1 6.55
CHEMBL228617 1 6.36
CHEMBL229417 1 6.29
CHEMBL228618 1 6.10
CHEMBL388774 1 5.96
CHEMBL228614 1 5.89
CHEMBL229362 1 5.75
CHEMBL228726 1 5.72
CHEMBL229243 1 5.72
CHEMBL388203 1 5.68
CHEMBL387776 1 5.59
CHEMBL388548 1 5.44
CHEMBL228668 1 5.42
CHEMBL228778 1 5.38
CHEMBL228619 1 5.19
CHEMBL228613 1 5.18
CHEMBL228669 1 5.15
CHEMBL228777 1 5.11
CHEMBL229956 1 5.06
CHEMBL375726 1 4.98
CHEMBL189 MILRINONE 4.0 1 4.92
CHEMBL387991 1 4.74
CHEMBL229568 1 4.62
CHEMBL442062 1 4.47
CHEMBL799 CILOSTAZOL 4.0 1 4.40
CHEMBL228779 1 4.14
CHEMBL612001 1 -
CHEMBL228729 1 -
CHEMBL25 ASPIRIN 4.0 1 -
CHEMBL229566 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL228776 IC50 = 284.0 nM 6.55
CHEMBL228617 IC50 = 440.0 nM 6.36
CHEMBL229417 IC50 = 510.0 nM 6.29
CHEMBL228618 IC50 = 800.0 nM 6.10
CHEMBL388774 IC50 = 1100.0 nM 5.96
CHEMBL228614 IC50 = 1300.0 nM 5.89
CHEMBL229362 IC50 = 1800.0 nM 5.75
CHEMBL228726 IC50 = 1900.0 nM 5.72
CHEMBL229243 IC50 = 1920.0 nM 5.72
CHEMBL388203 IC50 = 2100.0 nM 5.68
CHEMBL387776 IC50 = 2580.0 nM 5.59
CHEMBL388548 IC50 = 3600.0 nM 5.44
CHEMBL228668 IC50 = 3800.0 nM 5.42
CHEMBL228778 IC50 = 4200.0 nM 5.38
CHEMBL228619 IC50 = 6400.0 nM 5.19
CHEMBL228613 IC50 = 6600.0 nM 5.18
CHEMBL228669 IC50 = 7100.0 nM 5.15
CHEMBL228777 IC50 = 7700.0 nM 5.11
CHEMBL229956 IC50 = 8800.0 nM 5.06
CHEMBL375726 IC50 = 10400.0 nM 4.98
CHEMBL189 MILRINONE IC50 = 12000.0 nM 4.92
CHEMBL387991 IC50 = 18300.0 nM 4.74
CHEMBL229568 IC50 = 24200.0 nM 4.62
CHEMBL442062 IC50 = 34200.0 nM 4.47
CHEMBL799 CILOSTAZOL IC50 = 40000.0 nM 4.40
CHEMBL228779 IC50 = 72000.0 nM 4.14
CHEMBL612001 IC50 > 1000000.0 nM -
CHEMBL228729 IC50 = 169000.0 nM -
CHEMBL25 ASPIRIN IC50 = 183000.0 nM -
CHEMBL229566 IC50 = 144000.0 nM -
CHEMBL375923 IC50 = 169000.0 nM -