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Assay Detail

CHEMBL5345747

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

Functional
Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

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 4 8.21 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4444010 1 8.60
CHEMBL124977 1 8.30
CHEMBL4538049 1 8.15
CHEMBL3827832 1 7.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4444010 EC50 = 2.5 nM 8.60
CHEMBL124977 EC50 = 5.0 nM 8.30
CHEMBL4538049 EC50 = 7.1 nM 8.15
CHEMBL3827832 EC50 = 17.0 nM 7.77