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Assay Detail

CHEMBL4015229

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

Functional
Positive allosteric modulation of Gi coupled human GPR84 expressed in CHO cells assessed as potentiation of decanoic acid-induced inhibition of forskolin-induced cAMP accumulation by measuring decanoic acid EC50 at 0.3 uM after 15 mins in presence of [3H]-cAMP by radiometric assay (Rvb = 9.22 to 13.1 uM)
2
Total Activities
2
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

G-protein coupled receptor 84 (CHEMBL3714079)
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 2 5.33 5.45

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4088884 1 5.45
CHEMBL446452 ARUNDINE 3.0 1 5.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4088884 EC50 = 3580.0 nM 5.45
CHEMBL446452 ARUNDINE EC50 = 6280.0 nM 5.20