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Assay Detail

CHEMBL2188786

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Functional
Agonist activity at rat P2Y1R expressed in HEK293 cells assessed as release of intracellular calcium by fluorescence based assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

P2Y purinoceptor 1 (CHEMBL2497)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Identification of a promising drug candidate for the treatment of type 2 diabetes based on a P2Y(1) receptor agonist.
Yelovitch S, Barr HM, Camden J, Weisman GA, Shai E, Varon D, Fischer B.
J Med Chem (2012) 55 : 7623 -7635
PubMed 22873688 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.65 8.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2181943 1 8.59
CHEMBL14249 ADENOSINE TRIPHOSPHATE 2.0 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2181943 EC50 = 2.6 nM 8.59
CHEMBL14249 ADENOSINE TRIPHOSPHATE EC50 = 200.0 nM 6.70