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Assay Detail

CHEMBL1955237

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Functional
Agonist activity at rat P2Y purinoceptor 6 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry
15
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type 1321-N1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

P2Y purinoceptor 6 (CHEMBL3543)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Boranophosphate isoster controls P2Y-receptor subtype selectivity and metabolic stability of dinucleoside polyphosphate analogues.
Yelovitch S, Camden J, Weisman GA, Fischer B.
J Med Chem (2012) 55 : 437 -448
PubMed 22107038 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 5.65 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL130266 URIDINE_DIPHOSPHATE 1 6.70
CHEMBL2029008 2 6.52
CHEMBL2029004 2 6.01
CHEMBL2029005 2 5.89
CHEMBL2029010 2 5.41
CHEMBL2029006 2 4.93
CHEMBL2029007 2 -
CHEMBL2029009 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL130266 URIDINE_DIPHOSPHATE EC50 = 200.0 nM 6.70
CHEMBL2029008 EC50 = 300.0 nM 6.52
CHEMBL2029008 EC50 = 720.0 nM 6.14
CHEMBL2029004 EC50 = 980.0 nM 6.01
CHEMBL2029005 EC50 = 1290.0 nM 5.89
CHEMBL2029005 EC50 = 1920.0 nM 5.72
CHEMBL2029004 EC50 = 1930.0 nM 5.71
CHEMBL2029010 EC50 = 3900.0 nM 5.41
CHEMBL2029006 EC50 = 11700.0 nM 4.93
CHEMBL2029006 EC50 = 20900.0 nM 4.68
CHEMBL2029010 EC50 = 36100.0 nM 4.44
CHEMBL2029007 EC50 - -
CHEMBL2029007 EC50 - -
CHEMBL2029009 EC50 - -
CHEMBL2029009 EC50 - -