Assay Detail

CHEMBL3380994

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Functional

Agonist activity at dog S1P1 receptor assessed as cAMP accumulation by HTRF assay

ChEMBL ↗

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Target

Sphingosine-1-phosphate receptor 1 (CHEMBL3559680) ↗

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Sphingosine-1-phosphate receptor 1 (CHEMBL3559680) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Sphingosine-1-phosphate receptor 1

CHEMBL3559680

Anchored from Assay target.

Protein identity Sphingosine-1-phosphate receptor 1

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	Canis lupus familiaris
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Sphingosine-1-phosphate receptor 1 (CHEMBL3559680) ↗

Type	SINGLE PROTEIN
Organism	Canis lupus familiaris

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	9.47	9.47

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3358920	ETRASIMOD	4.0	1	9.47

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3358920	ETRASIMOD	EC50	=	0.34	nM	9.47