Assay Detail

CHEMBL4675996

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

Binding

Displacement of [3H]-9-(2-phenylethyl)-2-(2-pyrazin-2-yloxyethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one from recombinant FLAG-tagged GPR84 (unknown origin) expressed in T-REx-293 cells co-expressing Galphai2 incubated for 1 hr by liquid scintillation counting analysis

ChEMBL ↗

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Target

G-protein coupled receptor 84 (CHEMBL3714079) ↗

Open DB target context

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G-protein coupled receptor 84 (CHEMBL3714079) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target G-protein coupled receptor 84

CHEMBL3714079

Anchored from Assay target.

Protein identity G-protein coupled receptor 84

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Cell Type	T-REx-293
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

G-protein coupled receptor 84 (CHEMBL3714079) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of 9-Cyclopropylethynyl-2-((S)-1-[1,4]dioxan-2-ylmethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one (GLPG1205), a Unique GPR84 Negative Allosteric Modulator Undergoing Evaluation in a Phase II Clinical Trial.

Labéguère F,Dupont S,Alvey L,Soulas F,Newsome G,Tirera A,Quenehen V,Mai TTT,Deprez P,Blanqué R,Oste L,Le Tallec S,De Vos S,Hagers A,Vandevelde A,Nelles L,Vandervoort N,Conrath K,Christophe T,van der Aar E,Wakselman E,Merciris D,Cottereaux C,da Costa C,Saniere L,Clement-Lacroix P,Jenkins L,Milligan G,Fletcher S,Brys R,Gosmini R
J Med Chem (2020) 63 : 13526 -13545
PubMed 32902984 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Activity	2	-	-
Ki	1	7.52	7.52

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3716365	GLPG-1205	2.0	1	7.52
CHEMBL4088884	—	—	1	-
CHEMBL107498	DECANOIC ACID	—	1	-

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3716365	GLPG-1205	Ki	=	30.2	nM	7.52
CHEMBL4088884	—	Activity		-	—	-
CHEMBL107498	DECANOIC ACID	Activity		-	—	-