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Assay Detail

CHEMBL866173

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Functional
Agonist activity at human recombinant P2Y6 receptor expressed in 1321N1 cells assessed as PLC-mediated [3H]IP production
25
Total Activities
25
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 Expert

Target

P2Y purinoceptor 6 (CHEMBL4714)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships of uridine 5'-diphosphate analogues at the human P2Y6 receptor.
Besada P, Shin DH, Costanzi S, Ko H, Mathé C, Gagneron J, Gosselin G, Maddileti S, Harden TK, Jacobson KA.
J Med Chem (2006) 49 : 5532 -5543
PubMed 16942026 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 25 5.80 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL130266 URIDINE_DIPHOSPHATE 1 7.89
CHEMBL1161882 1 7.82
CHEMBL1161875 1 7.22
CHEMBL384992 1 7.10
CHEMBL212090 1 6.64
CHEMBL1161880 1 6.55
CHEMBL1161881 1 6.25
CHEMBL1161884 1 6.10
CHEMBL1161876 1 5.96
CHEMBL609433 1 5.82
CHEMBL1161885 1 5.77
CHEMBL9519 1 5.76
CHEMBL378445 1 5.64
CHEMBL1161878 1 5.64
CHEMBL612021 1 5.60
CHEMBL215447 1 5.48
CHEMBL1161887 1 5.46
CHEMBL215911 1 5.41
CHEMBL1161879 1 5.31
CHEMBL1161886 1 5.26
CHEMBL1161877 1 5.06
CHEMBL1161874 1 4.75
CHEMBL384759 1 4.35
CHEMBL14830 ADENOSINE DIPHOSPHATE 0.5 1 4.19
CHEMBL425252 1 4.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL130266 URIDINE_DIPHOSPHATE EC50 = 13.0 nM 7.89
CHEMBL1161882 EC50 = 15.0 nM 7.82
CHEMBL1161875 EC50 = 60.0 nM 7.22
CHEMBL384992 EC50 = 80.0 nM 7.10
CHEMBL212090 EC50 = 230.0 nM 6.64
CHEMBL1161880 EC50 = 280.0 nM 6.55
CHEMBL1161881 EC50 = 560.0 nM 6.25
CHEMBL1161884 EC50 = 800.0 nM 6.10
CHEMBL1161876 EC50 = 1100.0 nM 5.96
CHEMBL609433 EC50 = 1500.0 nM 5.82
CHEMBL1161885 EC50 = 1700.0 nM 5.77
CHEMBL9519 EC50 = 1720.0 nM 5.76
CHEMBL378445 EC50 = 2300.0 nM 5.64
CHEMBL1161878 EC50 = 2300.0 nM 5.64
CHEMBL612021 EC50 = 2500.0 nM 5.60
CHEMBL215447 EC50 = 3300.0 nM 5.48
CHEMBL1161887 EC50 = 3500.0 nM 5.46
CHEMBL215911 EC50 = 3900.0 nM 5.41
CHEMBL1161879 EC50 = 4900.0 nM 5.31
CHEMBL1161886 EC50 = 5500.0 nM 5.26
CHEMBL1161877 EC50 = 8800.0 nM 5.06
CHEMBL1161874 EC50 = 18000.0 nM 4.75
CHEMBL384759 EC50 = 45000.0 nM 4.35
CHEMBL14830 ADENOSINE DIPHOSPHATE EC50 = 65000.0 nM 4.19
CHEMBL425252 EC50 = 88000.0 nM 4.06