Assay Detail

CHEMBL5046776

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Functional

Antagonist activity at S1P2 (unknown origin)

ChEMBL ↗

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Target

Sphingosine 1-phosphate receptor 2 (CHEMBL2955) ↗

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Sphingosine 1-phosphate receptor 2 (CHEMBL2955) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Sphingosine 1-phosphate receptor 2

CHEMBL2955

Anchored from Assay target.

Protein identity Sphingosine 1-phosphate receptor 2

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	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Sphingosine 1-phosphate receptor 2 (CHEMBL2955) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery and Optimization of Orally Bioavailable Phthalazone and Cinnolone Carboxylic Acid Derivatives as S1P2 Antagonists against Fibrotic Diseases.

Mammoliti O, Jansen K, El Bkassiny S, Palisse A, Triballeau N, Bucher D, Allart B, Jaunet A, Tricarico G, De Wachter M, Menet C, Blanc J, Letfus V, Rupčić R, Šmehil M, Poljak T, Coornaert B, Sonck K, Duys I, Waeckel L, Lecru L, Marsais F, Jagerschmidt C, Auberval M, Pujuguet P, Oste L, Borgonovi M, Wakselman E, Christophe T, Houvenaghel N, Jans M, Heckmann B, Sanière L, Brys R.
J Med Chem (2021) 64 : 14557 -14586
PubMed 34581584 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	7.77	7.77

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1368758	—	—	1	7.77

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1368758	—	IC50	=	17.0	nM	7.77