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Assay Detail

CHEMBL4011254

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

Functional
Antagonist activity at human P2Y6 receptor transfected in human 1321N1 cells assessed as inhibition of UDP-activated intracellular calcium mobilization preincubated for 30 mins followed by UDP addition by fluo-4-dye based fluorescence assay
6
Total Activities
6
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 6 (CHEMBL4714)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of Potent and Selective Antagonists for the UTP-Activated P2Y4 Receptor.
Rafehi M, Malik EM, Neumann A, Abdelrahman A, Hanck T, Namasivayam V, Müller CE, Baqi Y.
J Med Chem (2017) 60 : 3020 -3038
PubMed 28306255 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.34 5.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4081274 1 5.57
CHEMBL256057 ACID BLUE 25 1 5.55
CHEMBL4099292 1 5.36
CHEMBL4069492 1 5.32
CHEMBL4087247 1 4.90
CHEMBL4090874 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4081274 IC50 = 2670.0 nM 5.57
CHEMBL256057 ACID BLUE 25 IC50 = 2790.0 nM 5.55
CHEMBL4099292 IC50 = 4360.0 nM 5.36
CHEMBL4069492 IC50 = 4750.0 nM 5.32
CHEMBL4087247 IC50 = 12500.0 nM 4.90
CHEMBL4090874 IC50 > 100000.0 nM -