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Assay Detail

CHEMBL4343754

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

Binding
Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

G-protein coupled receptor 84 (CHEMBL3714079)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

An Agonist Radioligand for the Proinflammatory Lipid-Activated G Protein-Coupled Receptor GPR84 Providing Structural Insights.
Köse M, Pillaiyar T, Namasivayam V, De Filippo E, Sylvester K, Ulven T, von Kügelgen I, Müller CE.
J Med Chem (2020) 63 : 2391 -2410
PubMed 31721581 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 5.70 6.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4456892 1 6.37
CHEMBL1232858 1 6.34
CHEMBL4538049 1 6.28
CHEMBL107874 TRIDECANOATE 2.0 1 5.77
CHEMBL4288936 1 5.49
CHEMBL108766 DODECANOATE 1 5.46
CHEMBL4448230 1 5.39
CHEMBL108030 UNDECANOATE 3.0 1 5.36
CHEMBL2004471 1 5.36
CHEMBL111077 MYRISTIC ACID -1.0 1 5.15
CHEMBL324846 OCTANOIC ACID 2.0 1 -
CHEMBL4447980 1 -
CHEMBL55068 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4456892 EC50 = 432.0 nM 6.37
CHEMBL1232858 EC50 = 452.0 nM 6.34
CHEMBL4538049 EC50 = 522.0 nM 6.28
CHEMBL107874 TRIDECANOATE EC50 = 1700.0 nM 5.77
CHEMBL4288936 EC50 = 3250.0 nM 5.49
CHEMBL108766 DODECANOATE EC50 = 3490.0 nM 5.46
CHEMBL4448230 EC50 = 4050.0 nM 5.39
CHEMBL108030 UNDECANOATE EC50 = 4360.0 nM 5.36
CHEMBL2004471 EC50 = 4360.0 nM 5.36
CHEMBL111077 MYRISTIC ACID EC50 = 7010.0 nM 5.15
CHEMBL324846 OCTANOIC ACID EC50 > 100000.0 nM -
CHEMBL4447980 EC50 > 100000.0 nM -
CHEMBL55068 EC50 > 100000.0 nM -