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Assay Detail

CHEMBL958064

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Functional
Agonist activity at human P2Y6 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
33
Total Activities
33
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 6 (CHEMBL4714)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists.
Ko H, Carter RL, Cosyn L, Petrelli R, de Castro S, Besada P, Zhou Y, Cappellacci L, Franchetti P, Grifantini M, Van Calenbergh S, Harden TK, Jacobson KA.
Bioorg Med Chem (2008) 16 : 6319 -6332
PubMed 18514530 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 33 5.61 6.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL239151 1 6.57
CHEMBL130266 URIDINE_DIPHOSPHATE 1 6.52
CHEMBL488132 1 6.21
CHEMBL507060 1 6.18
CHEMBL507282 DENUFOSOL 3.0 1 6.02
CHEMBL505403 1 5.99
CHEMBL509434 1 5.98
CHEMBL221326 DIQUAFOSOL 4.0 1 5.94
CHEMBL217803 1 5.82
CHEMBL503798 1 5.69
CHEMBL527872 1 5.33
CHEMBL484290 1 5.29
CHEMBL503256 1 5.26
CHEMBL521451 1 5.19
CHEMBL482485 1 5.17
CHEMBL482683 1 5.13
CHEMBL483502 1 5.12
CHEMBL499138 1 5.11
CHEMBL444212 1 5.09
CHEMBL482895 1 5.09
CHEMBL483913 1 5.09
CHEMBL484105 1 -
CHEMBL519835 1 -
CHEMBL482472 1 -
CHEMBL484295 1 -
CHEMBL519991 1 -
CHEMBL474887 1 -
CHEMBL448985 1 -
CHEMBL500840 1 -
CHEMBL508122 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL239151 EC50 = 270.0 nM 6.57
CHEMBL130266 URIDINE_DIPHOSPHATE EC50 = 300.0 nM 6.52
CHEMBL488132 EC50 = 610.0 nM 6.21
CHEMBL507060 EC50 = 660.0 nM 6.18
CHEMBL507282 DENUFOSOL EC50 = 950.0 nM 6.02
CHEMBL505403 EC50 = 1030.0 nM 5.99
CHEMBL509434 EC50 = 1050.0 nM 5.98
CHEMBL221326 DIQUAFOSOL EC50 = 1160.0 nM 5.94
CHEMBL217803 EC50 = 1500.0 nM 5.82
CHEMBL503798 EC50 = 2030.0 nM 5.69
CHEMBL527872 EC50 = 4700.0 nM 5.33
CHEMBL484290 EC50 = 5150.0 nM 5.29
CHEMBL503256 EC50 = 5490.0 nM 5.26
CHEMBL521451 EC50 = 6460.0 nM 5.19
CHEMBL482485 EC50 = 6830.0 nM 5.17
CHEMBL482683 EC50 = 7330.0 nM 5.13
CHEMBL483502 EC50 = 7560.0 nM 5.12
CHEMBL499138 EC50 = 7830.0 nM 5.11
CHEMBL444212 EC50 = 8190.0 nM 5.09
CHEMBL482895 EC50 = 8190.0 nM 5.09
CHEMBL483913 EC50 = 8160.0 nM 5.09
CHEMBL484105 EC50 > 10000.0 nM -
CHEMBL519835 EC50 > 10000.0 nM -
CHEMBL482472 EC50 > 10000.0 nM -
CHEMBL484295 EC50 > 10000.0 nM -
CHEMBL519991 EC50 > 10000.0 nM -
CHEMBL474887 EC50 > 10000.0 nM -
CHEMBL448985 EC50 > 10000.0 nM -
CHEMBL500840 EC50 > 10000.0 nM -
CHEMBL508122 EC50 > 10000.0 nM -
CHEMBL454230 EC50 > 10000.0 nM -
CHEMBL336296 URIDINE TRIPHOSPHATE EC50 > 10000.0 nM -
CHEMBL502712 EC50 > 10000.0 nM -