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Assay Detail

CHEMBL3270103

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Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
20
Total Activities
20
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 4 (CHEMBL2123)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-Alkyloxyimino derivatives of uridine-5'-triphosphate: distal modification of potent agonists as a strategy for molecular probes of P2Y2, P2Y4, and P2Y6 receptors.
Jayasekara PS, Barrett MO, Ball CB, Brown KA, Hammes E, Balasubramanian R, Harden TK, Jacobson KA.
J Med Chem (2014) 57 : 3874 -3883
PubMed 24712832 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 6.96 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3261372 1 7.70
CHEMBL3261369 1 7.64
CHEMBL3261376 1 7.40
CHEMBL3261375 1 7.33
CHEMBL3261360 1 7.27
CHEMBL3261378 1 7.16
CHEMBL3261368 1 7.08
CHEMBL3261366 1 7.04
CHEMBL3261367 1 7.02
CHEMBL3261362 1 7.00
CHEMBL3261363 1 6.98
CHEMBL3261365 1 6.94
CHEMBL3261374 1 6.89
CHEMBL3261364 1 6.85
CHEMBL3261377 1 6.70
CHEMBL3261371 1 6.60
CHEMBL3261370 1 6.52
CHEMBL3261373 1 6.39
CHEMBL3261361 1 6.37
CHEMBL3261359 1 6.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3261372 EC50 = 20.0 nM 7.70
CHEMBL3261369 EC50 = 23.0 nM 7.64
CHEMBL3261376 EC50 = 40.0 nM 7.40
CHEMBL3261375 EC50 = 47.0 nM 7.33
CHEMBL3261360 EC50 = 54.0 nM 7.27
CHEMBL3261378 EC50 = 70.0 nM 7.16
CHEMBL3261368 EC50 = 84.0 nM 7.08
CHEMBL3261366 EC50 = 91.0 nM 7.04
CHEMBL3261367 EC50 = 95.0 nM 7.02
CHEMBL3261362 EC50 = 100.0 nM 7.00
CHEMBL3261363 EC50 = 105.0 nM 6.98
CHEMBL3261365 EC50 = 114.0 nM 6.94
CHEMBL3261374 EC50 = 128.0 nM 6.89
CHEMBL3261364 EC50 = 141.0 nM 6.85
CHEMBL3261377 EC50 = 200.0 nM 6.70
CHEMBL3261371 EC50 = 250.0 nM 6.60
CHEMBL3261370 EC50 = 300.0 nM 6.52
CHEMBL3261373 EC50 = 410.0 nM 6.39
CHEMBL3261361 EC50 = 430.0 nM 6.37
CHEMBL3261359 EC50 = 470.0 nM 6.33