Assay Detail

CHEMBL4675931

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Functional

Inhibition of embelin-induced migration of rat neutrophils preincubated for 30 mins followed by embelin addition and measured after 1 hr by celltiter-glo assay

ChEMBL ↗

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Target

Unchecked (CHEMBL612545) ↗

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Primary target Unchecked

CHEMBL612545

Anchored from Assay target.

Protein identity Unchecked

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	Functional
Organism	Rattus norvegicus
Cell Type	Neutrophil
Confidence	0 — Uncurated / Unknown
Curated By	Autocuration

Target

Unchecked (CHEMBL612545) ↗

Type

UNCHECKED

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
IC50	2	6.89	6.96

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3716365	GLPG-1205	2.0	1	6.96
CHEMBL3717363	—	—	1	6.82

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3716365	GLPG-1205	IC50	=	111.0	nM	6.96
CHEMBL3717363	—	IC50	=	153.0	nM	6.82