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Assay Detail

CHEMBL5385171

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Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 6-OAU induced calcium response by measuring 6-OAU EC50 at 100 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 0.070 microM)
1
Total Activities
1
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

Unsymmetrical Phosphodiesters as GPR84 Antagonists with High Blood Exposure for the Treatment of Lung Inflammation.
Li SX, Wang SW, Chen LH, Zhang Q, Lu D, Chen J, Fang YC, Gu M, Xie X, Nan FJ.
J Med Chem (2023) 66 : 5820 -5838
PubMed 37053384 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 6.45 6.45

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3716365 GLPG-1205 2.0 1 6.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3716365 GLPG-1205 EC50 = 358.0 nM 6.45