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Assay Detail

CHEMBL1960464

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as stimulation of PLC-induced [3H]inositol phosphate production after 30 mins by scintillation counting
14
Total Activities
14
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

Synthesis and P2Y₂ receptor agonist activities of uridine 5'-phosphonate analogues.
Van Poecke S, Barrett MO, Santhosh Kumar T, Sinnaeve D, Martins JC, Jacobson KA, Kendall Harden T, Van Calenbergh S.
Bioorg Med Chem (2012) 20 : 2304 -2315
PubMed 22386981 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 6.03 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL336296 URIDINE TRIPHOSPHATE 3.0 1 7.70
CHEMBL1957440 1 6.40
CHEMBL1957444 1 6.30
CHEMBL1957443 1 6.16
CHEMBL1957442 1 6.00
CHEMBL1957438 1 5.82
CHEMBL1957439 1 5.68
CHEMBL1957441 1 5.51
CHEMBL1957448 1 5.40
CHEMBL522015 1 5.29
CHEMBL1957447 1 -
CHEMBL1957446 1 -
CHEMBL1957445 1 -
CHEMBL1957449 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL336296 URIDINE TRIPHOSPHATE EC50 = 20.0 nM 7.70
CHEMBL1957440 EC50 = 400.0 nM 6.40
CHEMBL1957444 EC50 = 500.0 nM 6.30
CHEMBL1957443 EC50 = 700.0 nM 6.16
CHEMBL1957442 EC50 = 1000.0 nM 6.00
CHEMBL1957438 EC50 = 1500.0 nM 5.82
CHEMBL1957439 EC50 = 2100.0 nM 5.68
CHEMBL1957441 EC50 = 3100.0 nM 5.51
CHEMBL1957448 EC50 = 4000.0 nM 5.40
CHEMBL522015 EC50 = 5100.0 nM 5.29
CHEMBL1957447 EC50 > 20000.0 nM -
CHEMBL1957446 EC50 > 20000.0 nM -
CHEMBL1957445 EC50 > 20000.0 nM -
CHEMBL1957449 EC50 > 20000.0 nM -