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Assay Detail

CHEMBL1776795

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

P2Y purinoceptor 14 (CHEMBL1770046)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

The identification of 4,7-disubstituted naphthoic acid derivatives as UDP-competitive antagonists of P2Y14.
Gauthier JY, Belley M, Deschênes D, Fournier JF, Gagné S, Gareau Y, Hamel M, Hénault M, Hyjazie H, Kargman S, Lavallée G, Levesque JF, Li L, Mamane Y, Mancini J, Morin N, Mulrooney E, Robichaud J, Thérien M, Tranmer G, Wang Z, Wu J, Black WC.
Bioorg Med Chem Lett (2011) 21 : 2836 -2839
PubMed 21507640 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.80 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1774901 1 8.40
CHEMBL1774903 1 8.10
CHEMBL1774900 1 7.89
CHEMBL1774892 1 7.85
CHEMBL1774899 1 7.70
CHEMBL1774891 1 7.58
CHEMBL1774902 1 7.29
CHEMBL1774893 1 7.27
CHEMBL1774890 1 6.96
CHEMBL1774887 1 6.96
CHEMBL1774898 1 6.72
CHEMBL1774886 1 6.72
CHEMBL1774897 1 6.48
CHEMBL1774896 1 6.46
CHEMBL1774894 1 6.42
CHEMBL1774895 1 5.89
CHEMBL1774888 1 5.68
CHEMBL1774882 1 5.46
CHEMBL1774884 1 5.31
CHEMBL1774889 1 4.89
CHEMBL1774885 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1774901 IC50 = 4.0 nM 8.40
CHEMBL1774903 IC50 = 8.0 nM 8.10
CHEMBL1774900 IC50 = 13.0 nM 7.89
CHEMBL1774892 IC50 = 14.0 nM 7.85
CHEMBL1774899 IC50 = 20.0 nM 7.70
CHEMBL1774891 IC50 = 26.0 nM 7.58
CHEMBL1774902 IC50 = 51.0 nM 7.29
CHEMBL1774893 IC50 = 54.0 nM 7.27
CHEMBL1774890 IC50 = 110.0 nM 6.96
CHEMBL1774887 IC50 = 110.0 nM 6.96
CHEMBL1774898 IC50 = 190.0 nM 6.72
CHEMBL1774886 IC50 = 190.0 nM 6.72
CHEMBL1774897 IC50 = 330.0 nM 6.48
CHEMBL1774896 IC50 = 350.0 nM 6.46
CHEMBL1774894 IC50 = 380.0 nM 6.42
CHEMBL1774895 IC50 = 1300.0 nM 5.89
CHEMBL1774888 IC50 = 2100.0 nM 5.68
CHEMBL1774882 IC50 = 3500.0 nM 5.46
CHEMBL1774884 IC50 = 4900.0 nM 5.31
CHEMBL1774889 IC50 = 13000.0 nM 4.89
CHEMBL1774885 IC50 > 13000.0 nM -