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Assay Detail

CHEMBL1680820

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

Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
14
Total Activities
14
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 4 (CHEMBL2123)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent competitive antagonists and positive modulators of the P2X2 receptor.
Baqi Y, Hausmann R, Rosefort C, Rettinger J, Schmalzing G, Müller CE.
J Med Chem (2011) 54 : 817 -830
PubMed 21207957 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.08 5.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL499580 1 5.84
CHEMBL496030 1 5.65
CHEMBL223344 RB 2 1 5.01
CHEMBL1671995 1 5.00
CHEMBL496401 1 5.00
CHEMBL1672105 1 5.00
CHEMBL1672106 1 5.00
CHEMBL271672 1 4.66
CHEMBL256057 ACID BLUE 25 1 4.59
CHEMBL445413 1 -
CHEMBL1672100 1 -
CHEMBL1672101 1 -
CHEMBL1672104 1 -
CHEMBL509572 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL499580 IC50 = 1450.0 nM 5.84
CHEMBL496030 IC50 = 2220.0 nM 5.65
CHEMBL223344 RB 2 IC50 = 9790.0 nM 5.01
CHEMBL1671995 IC50 = 10000.0 nM 5.00
CHEMBL496401 IC50 = 10000.0 nM 5.00
CHEMBL1672105 IC50 = 10000.0 nM 5.00
CHEMBL1672106 IC50 = 10000.0 nM 5.00
CHEMBL271672 IC50 = 21800.0 nM 4.66
CHEMBL256057 ACID BLUE 25 IC50 = 25800.0 nM 4.59
CHEMBL445413 IC50 > 10000.0 nM -
CHEMBL1672100 IC50 > 10000.0 nM -
CHEMBL1672101 IC50 - -
CHEMBL1672104 IC50 > 10000.0 nM -
CHEMBL509572 IC50 > 10000.0 nM -