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Assay Detail

CHEMBL917101

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Functional
Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
18
Total Activities
18
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 2 (CHEMBL4398)
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 18 6.37 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL373780 1 8.10
CHEMBL217803 1 7.46
CHEMBL336296 URIDINE TRIPHOSPHATE 3.0 1 7.31
CHEMBL385098 1 7.21
CHEMBL14249 ADENOSINE TRIPHOSPHATE 2.0 1 7.07
CHEMBL221326 DIQUAFOSOL 4.0 1 6.68
CHEMBL220200 1 6.62
CHEMBL507282 DENUFOSOL 3.0 1 6.57
CHEMBL221162 1 6.33
CHEMBL220940 THYMIDINE_TRIPHOSPHATE 1 6.32
CHEMBL384527 1 6.12
CHEMBL220398 1 6.08
CHEMBL374361 1 5.97
CHEMBL219779 1 5.75
CHEMBL410594 1 5.73
CHEMBL220011 1 5.25
CHEMBL376430 1 5.19
CHEMBL220337 1 4.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL373780 EC50 = 8.0 nM 8.10
CHEMBL217803 EC50 = 35.0 nM 7.46
CHEMBL336296 URIDINE TRIPHOSPHATE EC50 = 49.0 nM 7.31
CHEMBL385098 EC50 = 62.0 nM 7.21
CHEMBL14249 ADENOSINE TRIPHOSPHATE EC50 = 85.0 nM 7.07
CHEMBL221326 DIQUAFOSOL EC50 = 210.0 nM 6.68
CHEMBL220200 EC50 = 240.0 nM 6.62
CHEMBL507282 DENUFOSOL EC50 = 270.0 nM 6.57
CHEMBL221162 EC50 = 470.0 nM 6.33
CHEMBL220940 THYMIDINE_TRIPHOSPHATE EC50 = 480.0 nM 6.32
CHEMBL384527 EC50 = 750.0 nM 6.12
CHEMBL220398 EC50 = 830.0 nM 6.08
CHEMBL374361 EC50 = 1080.0 nM 5.97
CHEMBL219779 EC50 = 1800.0 nM 5.75
CHEMBL410594 EC50 = 1880.0 nM 5.73
CHEMBL220011 EC50 = 5600.0 nM 5.25
CHEMBL376430 EC50 = 6500.0 nM 5.19
CHEMBL220337 EC50 = 14300.0 nM 4.84