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Assay Detail

CHEMBL5385176

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

Functional
Non-competitive antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of 3-OH-C12 induced calcium response by measuring 3-OH-C12 EC50 at 30 nM incubated for 10 mins by calcium mobilization based schild analysis (Rvb = 18.82 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 4.69 4.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3716365 GLPG-1205 2.0 1 4.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3716365 GLPG-1205 EC50 = 20330.0 nM 4.69