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Assay Detail

CHEMBL4615164

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Binding
Antagonist activity P2X1 receptor in Apyrase pre-treated human platelets assessed as inhibition of collagen-induced platelet aggregation pre-incubated for 30 mins before collagen stimulation by aggregometry
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Platelet
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

P2X purinoceptor 1 (CHEMBL2094)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Structure Relationships of Salicylanilide Derivatives as Potent, Non-acidic P2X1 Receptor Antagonists.
Tian M, Abdelrahman A, Baqi Y, Fuentes E, Azazna D, Spanier C, Densborn S, Hinz S, Schmid R, Müller CE.
J Med Chem (2020) 63 : 6164 -6178
PubMed 32345019 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.78 6.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL536151 IMD-0354 1.0 1 6.24
CHEMBL2338696 1 5.94
CHEMBL2313113 1 5.68
CHEMBL2179173 1 5.52
CHEMBL2313133 1 5.50
CHEMBL2088014 1 -
CHEMBL2179174 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL536151 IMD-0354 IC50 = 570.0 nM 6.24
CHEMBL2338696 IC50 = 1140.0 nM 5.94
CHEMBL2313113 IC50 = 2100.0 nM 5.68
CHEMBL2179173 IC50 = 3030.0 nM 5.52
CHEMBL2313133 IC50 = 3130.0 nM 5.50
CHEMBL2088014 IC50 > 10000.0 nM -
CHEMBL2179174 IC50 >= 10000.0 nM -