Assay Detail

CHEMBL3380989

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Binding

Induction of internalization of HA-tagged human S1P1 receptor expressed in CHO cells

ChEMBL ↗

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Target

Sphingosine 1-phosphate receptor 1 (CHEMBL4333) ↗

Open DB target context

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Sphingosine 1-phosphate receptor 1 (CHEMBL4333) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Sphingosine 1-phosphate receptor 1

CHEMBL4333

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	Binding
Organism	Homo sapiens
Cell Type	CHO
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Sphingosine 1-phosphate receptor 1 (CHEMBL4333) ↗

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
IC50	1	8.73	8.73

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3358920	ETRASIMOD	4.0	1	8.73

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3358920	ETRASIMOD	IC50	=	1.88	nM	8.73