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Assay Detail

CHEMBL917103

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Functional
Agonist activity at human recombinant P2Y6 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type 1321-N1
Confidence 9 — Direct single protein target
Curated By Expert

Target

P2Y purinoceptor 6 (CHEMBL4714)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Molecular modeling of the human P2Y2 receptor and design of a selective agonist, 2'-amino-2'-deoxy-2-thiouridine 5'-triphosphate.
Ivanov AA, Ko H, Cosyn L, Maddileti S, Besada P, Fricks I, Costanzi S, Harden TK, Calenbergh SV, Jacobson KA.
J Med Chem (2007) 50 : 1166 -1176
PubMed 17302398 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.37 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL220940 THYMIDINE_TRIPHOSPHATE 1 6.85
CHEMBL220011 1 6.48
CHEMBL219779 1 6.33
CHEMBL217803 1 5.82
CHEMBL410594 1 -
CHEMBL385098 1 -
CHEMBL373780 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL220940 THYMIDINE_TRIPHOSPHATE EC50 = 140.0 nM 6.85
CHEMBL220011 EC50 = 333.0 nM 6.48
CHEMBL219779 EC50 = 467.0 nM 6.33
CHEMBL217803 EC50 = 1500.0 nM 5.82
CHEMBL410594 EC50 - -
CHEMBL385098 EC50 > 100000.0 nM -
CHEMBL373780 EC50 > 10000.0 nM -