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Assay Detail

CHEMBL5159689

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

Functional
Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve by measuring agonist EC50 at 30 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
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

Phosphodiesters as GPR84 Antagonists for the Treatment of Ulcerative Colitis.
Chen LH, Zhang Q, Xiao YF, Fang YC, Xie X, Nan FJ.
J Med Chem (2022) 65 : 3991 -4006
PubMed 35195005 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.08 6.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3716365 GLPG-1205 2.0 1 6.21
CHEMBL5179395 1 5.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3716365 GLPG-1205 EC50 = 611.0 nM 6.21
CHEMBL5179395 EC50 = 1126.0 nM 5.95