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Assay Detail

CHEMBL1767475

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Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
27
Total Activities
27
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

Structural modifications of UMP, UDP, and UTP leading to subtype-selective agonists for P2Y2, P2Y4, and P2Y6 receptors.
El-Tayeb A, Qi A, Nicholas RA, Müller CE.
J Med Chem (2011) 54 : 2878 -2890
PubMed 21417463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 27 5.57 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1767409 1 7.64
CHEMBL336296 URIDINE TRIPHOSPHATE 3.0 1 7.05
CHEMBL1767410 1 5.82
CHEMBL519835 1 5.42
CHEMBL1765118 1 5.41
CHEMBL1767418 1 5.36
CHEMBL1767414 1 5.35
CHEMBL1767411 1 5.31
CHEMBL1233534 1 5.30
CHEMBL1767412 1 5.22
CHEMBL1765115 1 5.14
CHEMBL1765116 1 5.10
CHEMBL1765119 1 5.03
CHEMBL130266 URIDINE_DIPHOSPHATE 1 4.85
CHEMBL1767422 1 -
CHEMBL1767421 1 -
CHEMBL1767423 1 -
CHEMBL1230331 1 -
CHEMBL1765114 1 -
CHEMBL1767420 1 -
CHEMBL1767419 1 -
CHEMBL1767417 1 -
CHEMBL1765117 1 -
CHEMBL1767416 1 -
CHEMBL1767415 1 -
CHEMBL1765120 1 -
CHEMBL1767413 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1767409 EC50 = 23.0 nM 7.64
CHEMBL336296 URIDINE TRIPHOSPHATE EC50 = 88.4 nM 7.05
CHEMBL1767410 EC50 = 1520.0 nM 5.82
CHEMBL519835 EC50 = 3850.0 nM 5.42
CHEMBL1765118 EC50 = 3930.0 nM 5.41
CHEMBL1767418 EC50 = 4330.0 nM 5.36
CHEMBL1767414 EC50 = 4490.0 nM 5.35
CHEMBL1767411 EC50 = 4900.0 nM 5.31
CHEMBL1233534 EC50 = 4980.0 nM 5.30
CHEMBL1767412 EC50 = 5980.0 nM 5.22
CHEMBL1765115 EC50 = 7300.0 nM 5.14
CHEMBL1765116 EC50 = 7870.0 nM 5.10
CHEMBL1765119 EC50 = 9300.0 nM 5.03
CHEMBL130266 URIDINE_DIPHOSPHATE EC50 = 14000.0 nM 4.85
CHEMBL1767422 EC50 > 100000.0 nM -
CHEMBL1767421 EC50 > 100000.0 nM -
CHEMBL1767423 EC50 > 100000.0 nM -
CHEMBL1230331 EC50 > 100000.0 nM -
CHEMBL1765114 EC50 >= 100000.0 nM -
CHEMBL1767420 EC50 > 100000.0 nM -
CHEMBL1767419 EC50 > 100000.0 nM -
CHEMBL1767417 EC50 > 100000.0 nM -
CHEMBL1765117 EC50 > 100000.0 nM -
CHEMBL1767416 EC50 >= 100000.0 nM -
CHEMBL1767415 EC50 >= 100000.0 nM -
CHEMBL1765120 EC50 > 100000.0 nM -
CHEMBL1767413 EC50 >= 100000.0 nM -