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Assay Detail

CHEMBL971533

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antagonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type 1321-N1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.
Hillmann P, Ko GY, Spinrath A, Raulf A, von Kügelgen I, Wolff SC, Nicholas RA, Kostenis E, Höltje HD, Müller CE.
J Med Chem (2009) 52 : 2762 -2775
PubMed 19419204 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 4.61 4.61

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL401735 1 4.61
CHEMBL223344 RB 2 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL401735 IC50 = 24600.0 nM 4.61
CHEMBL223344 RB 2 IC50 > 100000.0 nM -