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Assay Detail

CHEMBL1045263

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Functional
Agonist activity at human P2Y6 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating Gq protein assessed as [3H]inositol phosphate production
19
Total Activities
19
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 Intermediate

Target

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

Publication

Human P2Y(14) receptor agonists: truncation of the hexose moiety of uridine-5'-diphosphoglucose and its replacement with alkyl and aryl groups.
Das A, Ko H, Burianek LE, Barrett MO, Harden TK, Jacobson KA.
J Med Chem (2010) 53 : 471 -480
PubMed 19902968 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 5.89 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL567321 1 7.38
CHEMBL1204010 1 7.16
CHEMBL566925 1 6.90
CHEMBL507060 1 6.47
CHEMBL216011 1 6.35
CHEMBL130266 URIDINE_DIPHOSPHATE 1 6.28
CHEMBL612064 1 5.82
CHEMBL375951 URIDINE DIPHOSPHATE GLUCOSE 1 5.80
CHEMBL611791 1 5.70
CHEMBL1162556 1 5.69
CHEMBL384992 1 5.63
CHEMBL612119 1 5.56
CHEMBL1162561 1 5.13
CHEMBL1162559 1 5.13
CHEMBL612063 1 5.10
CHEMBL1162553 1 5.04
CHEMBL608851 1 4.98
CHEMBL1162552 1 -
CHEMBL488133 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL567321 EC50 = 42.0 nM 7.38
CHEMBL1204010 EC50 = 70.0 nM 7.16
CHEMBL566925 EC50 = 127.0 nM 6.90
CHEMBL507060 EC50 = 339.0 nM 6.47
CHEMBL216011 EC50 = 447.0 nM 6.35
CHEMBL130266 URIDINE_DIPHOSPHATE EC50 = 530.0 nM 6.28
CHEMBL612064 EC50 = 1520.0 nM 5.82
CHEMBL375951 URIDINE DIPHOSPHATE GLUCOSE EC50 = 1600.0 nM 5.80
CHEMBL611791 EC50 = 1990.0 nM 5.70
CHEMBL1162556 EC50 = 2040.0 nM 5.69
CHEMBL384992 EC50 = 2360.0 nM 5.63
CHEMBL612119 EC50 = 2760.0 nM 5.56
CHEMBL1162561 EC50 = 7370.0 nM 5.13
CHEMBL1162559 EC50 = 7400.0 nM 5.13
CHEMBL612063 EC50 = 8000.0 nM 5.10
CHEMBL1162553 EC50 = 9100.0 nM 5.04
CHEMBL608851 EC50 = 10400.0 nM 4.98
CHEMBL1162552 EC50 = 108000.0 nM -
CHEMBL488133 EC50 - -