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Assay Detail

CHEMBL4011255

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

Binding
Antagonist activity at human P2Y12 receptor expressed in CHO cells assessed as inhibition of 2-MeSADP-induced beta-arrestin translocation preincubated for 30 mins followed by 2-MeSADP addition measured after 90 mins by luminescence-based topcount method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
IC50 6 5.83 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4069492 1 7.22
CHEMBL4099292 1 5.63
CHEMBL4087247 1 5.62
CHEMBL4081274 1 5.53
CHEMBL256057 ACID BLUE 25 1 5.51
CHEMBL4090874 1 5.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4069492 IC50 = 60.4 nM 7.22
CHEMBL4099292 IC50 = 2340.0 nM 5.63
CHEMBL4087247 IC50 = 2410.0 nM 5.62
CHEMBL4081274 IC50 = 2960.0 nM 5.53
CHEMBL256057 ACID BLUE 25 IC50 = 3120.0 nM 5.51
CHEMBL4090874 IC50 = 3590.0 nM 5.45