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Assay Detail

CHEMBL895696

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Functional
Antagonist activity at human P2X3 receptor expressed in Xenopus oocytes assessed as inhibition of ATP-induced ion current by two electrode voltage clamping technique
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Oocyte
Confidence 9 — Direct single protein target
Curated By Expert

Target

P2X purinoceptor 3 (CHEMBL2998)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationship studies of spinorphin as a potent and selective human P2X(3) receptor antagonist.
Jung KY, Moon HD, Lee GE, Lim HH, Park CS, Kim YC.
J Med Chem (2007) 50 : 4543 -4547
PubMed 17676725 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.35 7.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL238310 1 7.84
CHEMBL395723 1 7.49
CHEMBL397926 1 7.08
CHEMBL69727 ISOPPADS 1 6.97
CHEMBL395493 SPINORPHIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL238310 IC50 = 14.3 nM 7.84
CHEMBL395723 IC50 = 32.4 nM 7.49
CHEMBL397926 IC50 = 82.4 nM 7.08
CHEMBL69727 ISOPPADS IC50 = 108.0 nM 6.97
CHEMBL395493 SPINORPHIN IC50 = 0.0083 nM -