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Assay Detail

CHEMBL1068968

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Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
12
Total Activities
12
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 Autocuration

Target

P2Y purinoceptor 2 (CHEMBL4398)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-OMe-UDP is a potent and selective P2Y(6)-receptor agonist.
Ginsburg-Shmuel T, Haas M, Schumann M, Reiser G, Kalid O, Stern N, Fischer B.
J Med Chem (2010) 53 : 1673 -1685
PubMed 20095577 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 6.52 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL373780 1 8.10
CHEMBL606210 N-METHANOCARBA-UTP 1 7.80
CHEMBL336296 URIDINE TRIPHOSPHATE 3.0 1 7.00
CHEMBL221326 DIQUAFOSOL 4.0 1 7.00
CHEMBL507282 DENUFOSOL 3.0 1 6.66
CHEMBL601439 1 5.70
CHEMBL384527 1 5.69
CHEMBL602071 1 5.52
CHEMBL1774 1 5.22
CHEMBL130266 URIDINE_DIPHOSPHATE 1 -
CHEMBL601438 1 -
CHEMBL590738 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL373780 EC50 = 8.0 nM 8.10
CHEMBL606210 N-METHANOCARBA-UTP EC50 = 15.9 nM 7.80
CHEMBL336296 URIDINE TRIPHOSPHATE EC50 = 100.0 nM 7.00
CHEMBL221326 DIQUAFOSOL EC50 = 100.0 nM 7.00
CHEMBL507282 DENUFOSOL EC50 = 220.0 nM 6.66
CHEMBL601439 EC50 = 2000.0 nM 5.70
CHEMBL384527 EC50 = 2060.0 nM 5.69
CHEMBL602071 EC50 = 3000.0 nM 5.52
CHEMBL1774 EC50 = 6000.0 nM 5.22
CHEMBL130266 URIDINE_DIPHOSPHATE EC50 - -
CHEMBL601438 EC50 - -
CHEMBL590738 EC50 - -