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Assay Detail

CHEMBL1786811

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Functional
Agonist activity at human P2Y2
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

P2Y purinoceptor 2 (CHEMBL4398)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrimidine nucleotides with 4-alkyloxyimino and terminal tetraphosphate δ-ester modifications as selective agonists of the P2Y(4) receptor.
Maruoka H, Jayasekara MP, Barrett MO, Franklin DA, de Castro S, Kim N, Costanzi S, Harden TK, Jacobson KA.
J Med Chem (2011) 54 : 4018 -4033
PubMed 21528910 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 6.25 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL373780 1 8.10
CHEMBL336296 URIDINE TRIPHOSPHATE 3.0 1 7.22
CHEMBL499138 1 6.52
CHEMBL1767408 DIQUAFOSOL TETRASODIUM 4.0 1 5.88
CHEMBL474886 1 5.72
CHEMBL502712 1 5.64
CHEMBL519835 1 5.60
CHEMBL1784888 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL373780 EC50 = 8.0 nM 8.10
CHEMBL336296 URIDINE TRIPHOSPHATE EC50 = 60.0 nM 7.22
CHEMBL499138 EC50 = 300.0 nM 6.52
CHEMBL1767408 DIQUAFOSOL TETRASODIUM EC50 = 1310.0 nM 5.88
CHEMBL474886 EC50 = 1890.0 nM 5.72
CHEMBL502712 EC50 = 2270.0 nM 5.64
CHEMBL519835 EC50 = 2510.0 nM 5.60
CHEMBL1784888 EC50 = 5000.0 nM 5.30