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Assay Detail

CHEMBL4011257

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

Functional
Competitive antagonist activity at human P2Y12 receptor expressed in CHO cells assessed as forskolin/ 2-methylthio-ADP-induced cAMP production preincubated for 10 mins followed 2-methylthio-ADP addition measured after 3.5 hrs by luciferase reporter gene assay
1
Total Activities
1
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 12 (CHEMBL2001)
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
Kd 1 9.80 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL455536 1 9.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL455536 Kd = 0.1585 nM 9.80