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Assay Detail

CHEMBL4015238

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

Functional
Antagonist activity at Gq protein coupled human FFAR1 expressed in human 1321N1 cells assessed as inhibition of TUG-424-induced intracellular calcium level preincubated for 30 mins followed by TUG-424 addition measured at 1.2 secs time interval by Fluo-4-AM dye based fluorescence assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Free fatty acid receptor 1 (CHEMBL4422)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Diindolylmethane Derivatives: Potent Agonists of the Immunostimulatory Orphan G Protein-Coupled Receptor GPR84.
Pillaiyar T, Köse M, Sylvester K, Weighardt H, Thimm D, Borges G, Förster I, von Kügelgen I, Müller CE.
J Med Chem (2017) 60 : 3636 -3655
PubMed 28406627 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 5.10 5.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4101219 1 5.19
CHEMBL4063898 1 5.05
CHEMBL4099626 1 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4101219 EC50 = 6490.0 nM 5.19
CHEMBL4063898 EC50 = 8810.0 nM 5.05
CHEMBL4099626 EC50 = 8890.0 nM 5.05