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Assay Detail

CHEMBL930968

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

Functional
Antagonist activity at LPA2 expressed in RH7777 cells with Gi4-protein and aequorin by calcium mobilization assay
17
Total Activities
17
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 2 (CHEMBL3724)
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 17 6.33 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL256470 1 7.77
CHEMBL270865 1 7.46
CHEMBL401756 1 6.77
CHEMBL404452 1 6.58
CHEMBL427893 1 6.51
CHEMBL401747 1 6.14
CHEMBL429681 1 6.14
CHEMBL270877 1 5.89
CHEMBL401543 1 5.73
CHEMBL270878 1 5.50
CHEMBL270237 1 5.18
CHEMBL256478 1 -
CHEMBL272352 1 -
CHEMBL406676 1 -
CHEMBL257899 1 -
CHEMBL272087 1 -
CHEMBL404575 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL256470 IC50 = 17.0 nM 7.77
CHEMBL270865 IC50 = 35.0 nM 7.46
CHEMBL401756 IC50 = 170.0 nM 6.77
CHEMBL404452 IC50 = 260.0 nM 6.58
CHEMBL427893 IC50 = 310.0 nM 6.51
CHEMBL401747 IC50 = 730.0 nM 6.14
CHEMBL429681 IC50 = 730.0 nM 6.14
CHEMBL270877 IC50 = 1300.0 nM 5.89
CHEMBL401543 IC50 = 1860.0 nM 5.73
CHEMBL270878 IC50 = 3200.0 nM 5.50
CHEMBL270237 IC50 = 6610.0 nM 5.18
CHEMBL256478 IC50 > 30000.0 nM -
CHEMBL272352 IC50 > 30000.0 nM -
CHEMBL406676 IC50 > 30000.0 nM -
CHEMBL257899 IC50 > 30000.0 nM -
CHEMBL272087 IC50 > 50000.0 nM -
CHEMBL404575 IC50 > 50000.0 nM -