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Assay Detail

CHEMBL751122

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Functional
Inhibition of inward ion current elicited by ATP was determined at recombinant P2X3 receptor expressed in Xenopus oocytes
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

P2X purinoceptor 3 (CHEMBL4824)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity relationships of pyridoxal phosphate derivatives as potent and selective antagonists of P2X1 receptors.
Kim YC, Brown SG, Harden TK, Boyer JL, Dubyak G, King BF, Burnstock G, Jacobson KA.
J Med Chem (2001) 44 : 340 -349
PubMed 11462975 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.61 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL119416 1 7.60
CHEMBL331250 1 7.44
CHEMBL69727 ISOPPADS 1 7.13
CHEMBL119180 1 6.89
CHEMBL119235 1 6.85
CHEMBL117766 1 6.84
CHEMBL69234 1 6.62
CHEMBL331358 1 6.48
CHEMBL118007 1 6.32
CHEMBL116926 1 6.32
CHEMBL304765 1 4.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL119416 IC50 = 25.0 nM 7.60
CHEMBL331250 IC50 = 36.0 nM 7.44
CHEMBL69727 ISOPPADS IC50 = 74.0 nM 7.13
CHEMBL119180 IC50 = 128.0 nM 6.89
CHEMBL119235 IC50 = 140.0 nM 6.85
CHEMBL117766 IC50 = 145.0 nM 6.84
CHEMBL69234 IC50 = 240.0 nM 6.62
CHEMBL331358 IC50 = 330.0 nM 6.48
CHEMBL118007 IC50 = 480.0 nM 6.32
CHEMBL116926 IC50 = 480.0 nM 6.32
CHEMBL304765 IC50 = 58300.0 nM 4.23