Assay Detail

CHEMBL3381004

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Binding

Agonist activity at human S1P5 receptor by beta-arrestin recruitment assay

ChEMBL ↗

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Target

Sphingosine 1-phosphate receptor 5 (CHEMBL2274) ↗

Open DB target context

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Sphingosine 1-phosphate receptor 5 (CHEMBL2274) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Sphingosine 1-phosphate receptor 5

CHEMBL2274

Anchored from Assay target.

Protein identity Sphingosine 1-phosphate receptor 5

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
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Sphingosine 1-phosphate receptor 5 (CHEMBL2274) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor.

Buzard DJ, Kim SH, Lopez L, Kawasaki A, Zhu X, Moody J, Thoresen L, Calderon I, Ullman B, Han S, Lehmann J, Gharbaoui T, Sengupta D, Calvano L, Montalban AG, Ma YA, Sage C, Gao Y, Semple G, Edwards J, Barden J, Morgan M, Chen W, Usmani K, Chen C, Sadeque A, Christopher RJ, Thatte J, Fu L, Solomon M, Mills D, Whelan K, Al-Shamma H, Gatlin J, Le M, Gaidarov I, Anthony T, Unett DJ, Blackburn A, Rueter J, Stirn S, Behan DP, Jones RM.
ACS Med Chem Lett (2014) 5 : 1313 -1317
PubMed 25516790 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
EC50	1	7.61	7.61

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3358920	ETRASIMOD	4.0	1	7.61

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3358920	ETRASIMOD	EC50	=	24.4	nM	7.61