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Assay Detail

CHEMBL832578

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

Functional
Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA1 receptor
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type RH7777
Confidence 9 — Direct single protein target
Curated By Expert

Target

Lysophosphatidic acid receptor 1 (CHEMBL3819)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, structure-activity relationships, and biological evaluation of fatty alcohol phosphates as lysophosphatidic acid receptor ligands, activators of PPARgamma, and inhibitors of autotaxin.
Durgam GG, Virag T, Walker MD, Tsukahara R, Yasuda S, Liliom K, van Meeteren LA, Moolenaar WH, Wilke N, Siess W, Tigyi G, Miller DD.
J Med Chem (2005) 48 : 4919 -4930
PubMed 16033271 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.62 6.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361501 1 6.12
CHEMBL188591 1 5.66
CHEMBL187633 PHOSPHORIC ACID MONOTETRADECYL ESTER 1 5.64
CHEMBL188859 1 5.60
CHEMBL187711 PHOSPHORIC ACID MONODODECYL ESTER 1 5.55
CHEMBL190430 1 5.52
CHEMBL191055 1 5.26
CHEMBL363776 1 -
CHEMBL188081 1 -
CHEMBL190349 1 -
CHEMBL190999 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361501 IC50 = 762.0 nM 6.12
CHEMBL188591 IC50 = 2200.0 nM 5.66
CHEMBL187633 PHOSPHORIC ACID MONOTETRADECYL ESTER IC50 = 2300.0 nM 5.64
CHEMBL188859 IC50 = 2500.0 nM 5.60
CHEMBL187711 PHOSPHORIC ACID MONODODECYL ESTER IC50 = 2800.0 nM 5.55
CHEMBL190430 IC50 = 3000.0 nM 5.52
CHEMBL191055 IC50 = 5500.0 nM 5.26
CHEMBL363776 IC50 > 10000.0 nM -
CHEMBL188081 IC50 > 10000.0 nM -
CHEMBL190349 IC50 > 10000.0 nM -
CHEMBL190999 IC50 ~ 10000.0 nM -