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Assay Detail

CHEMBL4615151

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Binding
Antagonist activity at rat P2X1 receptor
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

P2X purinoceptor 1 (CHEMBL2530)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 5 7.06 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1253351 1 9.55
CHEMBL337395 1 8.22
CHEMBL265502 SURAMIN 3.0 1 6.00
CHEMBL69234 1 6.00
CHEMBL190141 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1253351 IC50 = 0.28 nM 9.55
CHEMBL337395 IC50 = 6.0 nM 8.22
CHEMBL265502 SURAMIN IC50 = 1000.0 nM 6.00
CHEMBL69234 IC50 = 1000.0 nM 6.00
CHEMBL190141 IC50 = 3000.0 nM 5.52