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Assay Detail

CHEMBL5345749

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Functional
Agonist activity at hemagglutinin-tagged human GPR84 expressed in HEK293 cells assessed as inhibition of forskolin induced cAMP production incubated for 60 mins by HTRF assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Development of Highly Potent, G-Protein Pathway Biased, Selective, and Orally Bioavailable GPR84 Agonists.
Wang P, Raja A, Luscombe VB, Bataille CJR, Lucy D, Rogga VV, Greaves DR, Russell AJ.
J Med Chem (2024) 67 : 110 -137
PubMed 38146625 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.93 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL221598 1 8.80
CHEMBL221137 EMBELIN 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL221598 EC50 = 1.6 nM 8.80
CHEMBL221137 EMBELIN EC50 = 89.0 nM 7.05