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Assay Detail

CHEMBL931968

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

Functional
Antagonist activity at LPA3 expressed in RH7777 cells with Gi4-protein and aequorin by calcium mobilization assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type RH7777
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Lysophosphatidic acid receptor 3 (CHEMBL3250)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent LPA2 (EDG4) antagonists as potential anticancer agents.
Beck HP, Kohn T, Rubenstein S, Hedberg C, Schwandner R, Hasslinger K, Dai K, Li C, Liang L, Wesche H, Frank B, An S, Wickramasinghe D, Jaen J, Medina J, Hungate R, Shen W.
Bioorg Med Chem Lett (2008) 18 : 1037 -1041
PubMed 18178086 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.16 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL272087 1 7.40
CHEMBL404575 1 4.92
CHEMBL404452 1 -
CHEMBL256470 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL272087 IC50 = 40.0 nM 7.40
CHEMBL404575 IC50 = 12000.0 nM 4.92
CHEMBL404452 IC50 > 50000.0 nM -
CHEMBL256470 IC50 > 50000.0 nM -