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Assay Detail

CHEMBL5159664

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Functional
Antagonist activity at human GPR84 expressed in HEK293 cells assessed as reversal of 6-OAU induced inhibition of forskolin induced intracellular cAMP production
3
Total Activities
3
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
IC50 3 6.86 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3716365 GLPG-1205 2.0 1 7.24
CHEMBL5179395 1 6.97
CHEMBL5194984 1 6.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3716365 GLPG-1205 IC50 = 58.0 nM 7.24
CHEMBL5179395 IC50 = 107.0 nM 6.97
CHEMBL5194984 IC50 = 413.0 nM 6.38