S1PR1

Summary

S1PR1 (sphingosine-1-phosphate receptor 1, HGNC:3165) is a protein-coding gene on chromosome 1p21.2, encoding Sphingosine 1-phosphate receptor 1 (P21453). G-protein coupled receptor for the bioactive lysosphingolipid sphingosine 1-phosphate (S1P) that seems to be coupled to the G(i) subclass of heteromeric G proteins.

The protein encoded by this gene is structurally similar to G protein-coupled receptors and is highly expressed in endothelial cells. It binds the ligand sphingosine-1-phosphate with high affinity and high specificity, and suggested to be involved in the processes that regulate the differentiation of endothelial cells. Activation of this receptor induces cell-cell adhesion. Alternative splicing results in multiple transcript variants.

Source: NCBI Gene 1901 — RefSeq curated summary.

At a glance

• GWAS associations: 15
• Clinical variants (ClinVar): 28 total
• Druggable target: yes — 13 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001400

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:3165
Approved symbol	S1PR1
Name	sphingosine-1-phosphate receptor 1
Location	1p21.2
Locus type	gene with protein product
Status	Approved
Aliases	edg-1, D1S3362, CD363
Ensembl gene	ENSG00000170989
Ensembl biotype	protein_coding
OMIM	601974
Entrez	1901

Gene structure

Transcript identifiers

Ensembl transcripts: 10 — 9 protein_coding, 1 protein_coding_CDS_not_defined

ENST00000305352, ENST00000475289, ENST00000475821, ENST00000561748, ENST00000648480, ENST00000649383, ENST00000876129, ENST00000876130, ENST00000945456, ENST00000945457

RefSeq mRNA: 2 — MANE Select: NM_001400 NM_001320730, NM_001400

CCDS: CCDS777

Canonical transcript exons

ENST00000305352 — 2 exons

Exon	Start	End
ENSE00001167649	101238822	101241518
ENSE00001356737	101237019	101237099

Expression profiles

Bgee: expression breadth ubiquitous, 234 present calls, max score 97.46.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 37.1880 / max 678.4133, expressed in 1264 samples.

FANTOM5 promoters (11 alternative TSS)

Promoter ID	TPM avg	Samples expressed
4274	19.2770	1020
4277	9.3688	1034
4273	3.3973	518
4272	2.0522	492
4276	0.7981	395
4275	0.7692	339
4279	0.6389	237
4278	0.2929	157
4281	0.2416	143
4282	0.2138	94

Top tissues by expression

279 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
right lung	UBERON:0002167	97.46	gold quality
upper lobe of left lung	UBERON:0008952	97.01	gold quality
ventricular zone	UBERON:0003053	96.70	gold quality
omental fat pad	UBERON:0010414	96.60	gold quality
peritoneum	UBERON:0002358	96.50	gold quality
upper lobe of lung	UBERON:0008948	96.42	gold quality
adipose tissue of abdominal region	UBERON:0007808	96.12	gold quality
granulocyte	CL:0000094	95.89	gold quality
subcutaneous adipose tissue	UBERON:0002190	95.18	gold quality
apex of heart	UBERON:0002098	94.00	gold quality
adipose tissue	UBERON:0001013	93.77	gold quality
heart left ventricle	UBERON:0002084	93.43	gold quality
cardiac ventricle	UBERON:0002082	93.16	gold quality
right atrium auricular region	UBERON:0006631	93.06	gold quality
lung	UBERON:0002048	92.98	gold quality
caudate nucleus	UBERON:0001873	92.69	gold quality
connective tissue	UBERON:0002384	92.59	gold quality
right lobe of thyroid gland	UBERON:0001119	92.19	gold quality
ganglionic eminence	UBERON:0004023	92.16	gold quality
nucleus accumbens	UBERON:0001882	92.06	gold quality
amygdala	UBERON:0001876	92.05	gold quality
spleen	UBERON:0002106	92.05	gold quality
gall bladder	UBERON:0002110	91.95	gold quality
heart	UBERON:0000948	91.82	gold quality
putamen	UBERON:0001874	91.56	gold quality
left lobe of thyroid gland	UBERON:0001120	91.49	gold quality
adrenal tissue	UBERON:0018303	91.10	gold quality
cardiac atrium	UBERON:0002081	91.05	gold quality
tibial nerve	UBERON:0001323	90.56	gold quality
left uterine tube	UBERON:0001303	90.51	gold quality

Single-cell (SCXA)

Detected in 17 experiment(s), a significant marker in 12.

Experiment	Marker?	Max mean expression
E-GEOD-135922	yes	44.96
E-MTAB-8410	yes	29.08
E-CURD-46	yes	29.06
E-GEOD-93593	yes	18.27
E-MTAB-9067	yes	16.20
E-GEOD-84465	yes	13.55
E-MTAB-8498	yes	11.38
E-MTAB-9543	yes	11.04
E-MTAB-5061	yes	6.43
E-GEOD-130148	yes	4.92
E-MTAB-9801	yes	4.69
E-MTAB-8205	no	369.90
E-CURD-95	no	272.67
E-MTAB-8911	no	201.47
E-CURD-112	no	3.85

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): ATF6, CEBPB, ESR1, FLI1, FOS, FOXO1, KLF2, MYC, NFKB1, PITX2, PPARA, PPARG, STAT3, TEAD4

miRNA regulators (miRDB)

110 targeting S1PR1, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-4262	100.00	73.26	3931
HSA-MIR-3162-3P	100.00	65.37	363
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-181A-5P	99.99	72.96	2995
HSA-MIR-181B-5P	99.99	72.97	2996
HSA-MIR-181C-5P	99.99	72.95	2996
HSA-MIR-181D-5P	99.99	73.04	2997
HSA-MIR-548AW	99.99	72.57	3559
HSA-MIR-4789-3P	99.99	70.75	2484
HSA-MIR-19A-3P	99.98	75.33	2762
HSA-MIR-19B-3P	99.98	75.44	2754
HSA-MIR-3065-5P	99.97	71.56	3281
HSA-MIR-1468-3P	99.96	72.74	3797
HSA-MIR-551B-5P	99.96	71.28	3493
HSA-MIR-9-3P	99.96	70.88	2068
HSA-MIR-559	99.95	72.28	3609
HSA-MIR-548AB	99.95	71.31	3488
HSA-MIR-548A-5P	99.94	71.27	3482
HSA-MIR-548AD-5P	99.94	71.23	3502
HSA-MIR-548AE-5P	99.94	71.23	3502
HSA-MIR-548AK	99.94	71.24	3488
HSA-MIR-548AM-5P	99.94	71.24	3488
HSA-MIR-548AP-5P	99.94	71.14	3489
HSA-MIR-548AQ-5P	99.94	71.34	3426
HSA-MIR-548AR-5P	99.94	71.28	3515
HSA-MIR-548AS-5P	99.94	71.22	3482
HSA-MIR-548AU-5P	99.94	71.24	3488
HSA-MIR-548AY-5P	99.94	71.23	3502
HSA-MIR-548B-5P	99.94	71.23	3502
HSA-MIR-548BB-5P	99.94	71.27	3509

Literature-anchored findings (GeneRIF, showing 40)

• in mouse, this protein is essential for vascular maturation (PMID:11032855)
• phosphorylation of the sphingosine 1-phosphate (SSP) receptor “endothelial differentiation gene 1” (EDG1 or S1P(1)) receptor is increased in response to either SSP or phorbol 12-myristate 13-acetate (PMA) exposure but not lysophosphatidic acid (PMID:11741892)
• functions as an intracellular signaling molecule and angiogenesis factor (PMID:11915345)
• activates Rho family G proteins and cell motility (PMID:11915348)
• S1P(1) inhibits Ca(2+) signalling most likely via G(i) proteins and classical PKC isoforms. Co-expression of S1P(1) with S1P(3), but not S1P(2), reversed the inhibitory effect of S1P(1), furthermore suggesting a specific interplay of S1P receptor subtypes (PMID:12742228)
• S1P1 receptors expressed in mouse Th1 cells mediate suppression of T cell proliferation and cytokine production. (PMID:14500646)
• Immunosuppressant FTY720 activates sphingosine 1-phosphate receptors that affect responsiveness of lymphocytes to chemokines such as stromal cell-derived factor 1. (PMID:14988150)
• cross-communication between the prototypical barrier-protective S1P and barrier-disruptive PAR1 pathway (PMID:15626732)
• Persistent expression of S1P1 receptor by lymphocytes of S1P1 receptor-transgenic mice suppresses delayed-type hypersensitivity and results in production of significantly more IgE antibody (Ab) and less IgG2 Ab than in wild-type mice. (PMID:15699128)
• endothelial protein C receptor ligation and sphingosine 1-phosphate receptor transactivation results in endothelial cell cytoskeletal rearrangement and barrier protection through activated protein C (PMID:15710622)
• Signaling by S1P1 receptor-transgenic mice affects systemic trafficking of peripheral T cells and primary immune responses; levels of S1P1 receptor expression represent an important mechanism of immune regulation. (PMID:15728452)
• Tyrosine sulfation of S1P1 may be a major controller of S1P effects on T cell traffic (PMID:16148028)
• S1P-induced recruitment of S1P1 to CEM fractions promotes PI3 kinase-mediated Tiam1/Rac1 activation required for alpha-actinin-1/4-regulated cortical actin rearrangement and EC barrier enhancement (PMID:16195373)
• The constitutively active endogenous S1P1 receptor enhances PDGF-induced cell migration. (PMID:16319133)
• heterotrimeric G protein-dependent ERK1/2 activation is mediated by IGF-1 and IGF-2 by transactivating sphingosine 1-phosphate receptors (PMID:16926156)
• Transactivation of sphingosine 1-phosphate receptors is essential for vascular barrier regulation (PMID:16963454)
• FTY720-P targets the S1P1 receptor to the ubiquitinylation and proteasomal degradation pathway (PMID:17237497)
• Sphingosine 1-phosphate-induced inflammatory response genes expression is mediated through S1P(1) and S1P(3) (PMID:17331465)
• FTY720 induces time-dependent modulation of S1P receptors on human OPCs with consequent functional responses that are directly relevant for the remyelination process. (PMID:17918267)
• S1P(1) receptor, without stimulating Ca(2+) increases, mediates chemotaxis of keratinocytes (PMID:18172456)
• S1P-mediated signaling via the S1P1/Gi/Rho GTPases pathway activates integrin alpha v beta 3, which is indispensable for S1P-stimulated chemotactic response of ECs. (PMID:18247041)
• S1P promotes lymphangiogenesis by stimulating S1P1/G(i)/phospholipase C/Ca(2+) signaling pathways. (PMID:18541717)
• HDL has endothelial barrier promoting activities, which are attributable to its S1P component and signaling through the S1P1/Akt pathway. (PMID:18606817)
• Datas suggest that filamin A links sphingosine kinase 1 and sphingosine-1-phosphate receptor 1 to locally influence the dynamics of actin cytoskeletal structures at lamellipodia to promote cell movement. (PMID:18644866)
• Plays essential roles in the pathogenesis of rheumatoid arthritis by modulating fibroblast-like synoviocyte migration, cytokine/chemokine production, and cell survival. (PMID:18658144)
• FOXO1 controls the expression of L-selectin and EDG1 and EDG6, receptors that regulate lymphocyte trafficking (PMID:18713968)
• S1P(1) acts as an inhibitor of CXCR4-dependent migration of hematopoietic cells to sites of SDF-1 production. (PMID:18760838)
• subconfluent pulmonary artery smooth muscle cells express predominantly S1P2 and S1P3 receptors; S1P1 receptor mRNA levels are significantly up-regulated following bFGF treatment (PMID:18773427)
• the crucial role of activation of the SPHK1S1PS1P1 signaling pathway in response to inflammatory mediators in endothelial cells in regulating endothelial barrier homeostasis. (PMID:18849324)
• plasma membrane S1P(1) receptors are rapidly internalized and subsequently translocated to nuclear compartment upon S1P stimulation; nuclear S1P(1) is able to regulate the transcription of Cyr61 and CTGF (PMID:18936953)
• S1PR1 has an important role in disease-related angiogenesis, especially in the processes of migration/invasion and tube formation. (PMID:19150609)
• Data suggest that human antibodies to the amino terminus of the type 1 sphingosine 1-phosphate receptor suppress T-cell trafficking sufficiently to impair host defense and provide therapeutic immunosuppression. (PMID:19158154)
• Akt-mediated transactivation of the S1P1 receptor in caveolin-enriched microdomains regulates endothelial barrier enhancement by oxidized phospholipids. (PMID:19286607)
• IGFBP-3 in MCF-10A cells requires SphK1 activity and S1P1/S1P3, suggesting that S1P, the product of SphK activity and ligand for S1P1 and S1P3 (PMID:19633297)
• The activation of S1PR results in increased chemotactic response of CD34(+) hematopoietic stem cells to SDF-1. (PMID:19778812)
• downregulation of S1P(1) expression enhances the malignancy of glioblastoma by increasing cell proliferation and correlates with the shorter survival of patients with glioblastoma. (PMID:19810093)
• S1P(1) signaling linked to cell migration is facilitated by a functional interaction with P-Rex1 via a mechanism that involves the maintenance of S1P(1) receptors at the cell membrane. (PMID:20036214)
• Sphingosine-1-phosphate receptor 1 immunohistochemistry may be useful in the histological diagnosis of mantle cell lymphoma with formalin-fixed and paraffin-embedded sections. (PMID:20081804)
• Protein S controls hypoxic/ischemic blood-brain barrier disruption through the TAM receptor Tyro3 and sphingosine 1-phosphate receptor1. (PMID:20348395)
• Mobilization with rhG-CSF obviously down-regulates the expression of S1P1 in CD4+ T cells. (PMID:20416181)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	s1pr1	ENSDARG00000042690
mus_musculus	S1pr1	ENSMUSG00000045092
rattus_norvegicus	S1pr1	ENSRNOG00000013683

Paralogs (18): LPAR2 (ENSG00000064547), CNR1 (ENSG00000118432), MC3R (ENSG00000124089), S1PR4 (ENSG00000125910), GPR12 (ENSG00000132975), GPR6 (ENSG00000146360), GPR119 (ENSG00000147262), MC4R (ENSG00000166603), LPAR3 (ENSG00000171517), MC5R (ENSG00000176136), S1PR5 (ENSG00000180739), GPR3 (ENSG00000181773), MC2R (ENSG00000185231), CNR2 (ENSG00000188822), LPAR1 (ENSG00000198121), S1PR3 (ENSG00000213694), MC1R (ENSG00000258839), S1PR2 (ENSG00000267534)

Protein

Protein identifiers

Sphingosine 1-phosphate receptor 1 — P21453 (reviewed: P21453)

Alternative names: Endothelial differentiation G-protein coupled receptor 1, Sphingosine 1-phosphate receptor Edg-1

All UniProt accessions (2): P21453, A0A3B3IUD4

UniProt curated annotations — full annotation on UniProt →

Function. G-protein coupled receptor for the bioactive lysosphingolipid sphingosine 1-phosphate (S1P) that seems to be coupled to the G(i) subclass of heteromeric G proteins. Signaling leads to the activation of RAC1, SRC, PTK2/FAK1 and MAP kinases. Plays an important role in cell migration, probably via its role in the reorganization of the actin cytoskeleton and the formation of lamellipodia in response to stimuli that increase the activity of the sphingosine kinase SPHK1. Required for normal chemotaxis toward sphingosine 1-phosphate. Required for normal embryonic heart development and normal cardiac morphogenesis. Plays an important role in the regulation of sprouting angiogenesis and vascular maturation. Inhibits sprouting angiogenesis to prevent excessive sprouting during blood vessel development. Required for normal egress of mature T-cells from the thymus into the blood stream and into peripheral lymphoid organs. Plays a role in the migration of osteoclast precursor cells, the regulation of bone mineralization and bone homeostasis. Plays a role in responses to oxidized 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine by pulmonary endothelial cells and in the protection against ventilator-induced lung injury.

Subunit / interactions. Interacts with GNAI1 and GNAI3. Interacts with CD69; this interaction promotes S1PR1 degradation.

Subcellular location. Cell membrane. Endosome. Membrane raft.

Tissue specificity. Endothelial cells, and to a lesser extent, in vascular smooth muscle cells, fibroblasts, melanocytes, and cells of epithelioid origin.

Post-translational modifications. S1P-induced endothelial cell migration requires the PKB/AKT1-mediated phosphorylation of the third intracellular loop at the Thr-236 residue. Palmitoylated by ZDHHC5. Palmitoylation is required for targeting to plasma membrane, enabling G(i) coupling.

Induction. By the tumor promoter phorbol 12-myristate 13-acetate (PMA) in the presence of cycloheximide.

Similarity. Belongs to the G-protein coupled receptor 1 family.

RefSeq proteins (2): NP_001307659, NP_001391* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000987	EDG1	Family
IPR004061	S1P_rcpt	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (67 total): helix 13, mutagenesis site 10, topological domain 8, transmembrane region 7, turn 5, strand 5, modified residue 4, sequence variant 3, compositionally biased region 2, binding site 2, glycosylation site 2, disulfide bond 2, chain 1, region of interest 1, lipid moiety-binding region 1, sequence conflict 1

Structure

Experimental structures (PDB)

21 structures.

PDB	Method	Resolution (Å)
7TD4	ELECTRON MICROSCOPY	2.6
9VNZ	ELECTRON MICROSCOPY	2.79
9VO0	ELECTRON MICROSCOPY	2.79
3V2Y	X-RAY DIFFRACTION	2.8
7VIF	ELECTRON MICROSCOPY	2.83
7EO4	ELECTRON MICROSCOPY	2.86
7VIE	ELECTRON MICROSCOPY	2.86
7EO2	ELECTRON MICROSCOPY	2.89
7VIG	ELECTRON MICROSCOPY	2.89
9VO1	ELECTRON MICROSCOPY	2.97
7EVY	ELECTRON MICROSCOPY	2.98
7VIH	ELECTRON MICROSCOPY	2.98
7TD3	ELECTRON MICROSCOPY	3
7EVZ	ELECTRON MICROSCOPY	3.07
8G94	ELECTRON MICROSCOPY	3.15
7EW7	ELECTRON MICROSCOPY	3.27
3V2W	X-RAY DIFFRACTION	3.35
7WF7	ELECTRON MICROSCOPY	3.4
7EW0	ELECTRON MICROSCOPY	3.42
8YIC	ELECTRON MICROSCOPY	3.47
9VNY	ELECTRON MICROSCOPY	3.69

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P21453-F1	81.51	0.54

Antibody-complex structures (SAbDab): 12 — 7EO2, 7EO4, 7EVY, 7EVZ, 7EW0, 7EW7, 7VIE, 7VIF, 7VIG, 7VIH, 7WF7, 8G94

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Ligand- & substrate-binding residues (2): 120–121; 265–269

Post-translational modifications (5): 10, 236, 351, 353, 328

Disulfide bonds (2): 184–191, 282–287

Glycosylation sites (2): 30, 36

Mutagenesis-validated functional residues (10):

Position	Phenotype
120	drastically reduced affinity for sphingosine 1-phosphate.
121	drastically reduced affinity for sphingosine 1-phosphate.
121	slight activation of the receptor at maximal ligand concentration.
169	strongly reduced interaction with cd69.
180	strongly reduced interaction with cd69.
210	impairs sphingosine 1-phosphate binding and signaling.
236	acts as a dominant negative gpcr and inhibits s1p-induced rac activation, chemotaxis, and angiogenesis.
265	impairs sphingosine 1-phosphate binding and signaling.
269	impairs sphingosine 1-phosphate binding and signaling.
292	drastically reduced affinity for sphingosine 1-phosphate.

Function

Pathways and Gene Ontology

Reactome pathways

14 pathways

ID	Pathway
R-HSA-419408	Lysosphingolipid and LPA receptors
R-HSA-6785807	Interleukin-4 and Interleukin-13 signaling
R-HSA-9679191	Potential therapeutics for SARS
R-HSA-1280215	Cytokine Signaling in Immune system
R-HSA-162582	Signal Transduction
R-HSA-1643685	Disease
R-HSA-168256	Immune System
R-HSA-372790	Signaling by GPCR
R-HSA-373076	Class A/1 (Rhodopsin-like receptors)
R-HSA-449147	Signaling by Interleukins
R-HSA-500792	GPCR ligand binding
R-HSA-5663205	Infectious disease
R-HSA-9679506	SARS-CoV Infections
R-HSA-9824446	Viral Infection Pathways

MSigDB gene sets: 514 (showing top): RNGTGGGC_UNKNOWN, GOBP_EPITHELIUM_DEVELOPMENT, PID_S1P_S1P1_PATHWAY, BROWNE_HCMV_INFECTION_6HR_DN, GOBP_ACTIN_FILAMENT_BUNDLE_ORGANIZATION, GOBP_MUSCLE_TISSUE_DEVELOPMENT, GOBP_CELL_CHEMOTAXIS, GOBP_HEART_TRABECULA_MORPHOGENESIS, BIOCARTA_EDG1_PATHWAY, REACTOME_CYTOKINE_SIGNALING_IN_IMMUNE_SYSTEM, LFA1_Q6, GOBP_SPHINGOLIPID_MEDIATED_SIGNALING_PATHWAY, AREB6_03, GOBP_GROWTH, GOCC_CELL_SURFACE

GO Biological Process (31): angiogenesis (GO:0001525), blood vessel maturation (GO:0001955), cardiac muscle tissue growth involved in heart morphogenesis (GO:0003245), sphingosine-1-phosphate receptor signaling pathway (GO:0003376), chemotaxis (GO:0006935), cell adhesion (GO:0007155), G protein-coupled receptor signaling pathway (GO:0007186), adenylate cyclase-activating G protein-coupled receptor signaling pathway (GO:0007189), adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway (GO:0007193), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), brain development (GO:0007420), cell population proliferation (GO:0008283), cell migration (GO:0016477), transmission of nerve impulse (GO:0019226), lamellipodium assembly (GO:0030032), actin cytoskeleton organization (GO:0030036), regulation of cell adhesion (GO:0030155), neuron differentiation (GO:0030182), positive regulation of cell migration (GO:0030335), regulation of bone mineralization (GO:0030500), leukocyte chemotaxis (GO:0030595), regulation of bone resorption (GO:0045124), endothelial cell differentiation (GO:0045446), positive regulation of transcription by RNA polymerase II (GO:0045944), positive regulation of smooth muscle cell proliferation (GO:0048661), positive regulation of positive chemotaxis (GO:0050927), negative regulation of stress fiber assembly (GO:0051497), heart trabecula morphogenesis (GO:0061384), T cell migration (GO:0072678), signal transduction (GO:0007165), positive regulation of cell population proliferation (GO:0008284)

GO Molecular Function (5): G protein-coupled receptor binding (GO:0001664), G protein-coupled receptor activity (GO:0004930), sphingosine-1-phosphate receptor activity (GO:0038036), sphingolipid binding (GO:0046625), protein binding (GO:0005515)

GO Cellular Component (8): nucleoplasm (GO:0005654), cytoplasm (GO:0005737), endosome (GO:0005768), plasma membrane (GO:0005886), external side of plasma membrane (GO:0009897), membrane raft (GO:0045121), presynapse (GO:0098793), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-11 pathways:

Category	Pathways
Class A/1 (Rhodopsin-like receptors)	1
Signaling by Interleukins	1
SARS-CoV Infections	1
Immune System	1
Signal Transduction	1
GPCR ligand binding	1
Cytokine Signaling in Immune system	1
Signaling by GPCR	1
Disease	1
Viral Infection Pathways	1
Infectious disease	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	4
G protein-coupled receptor signaling pathway	3
cellular process	2
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	2
blood vessel morphogenesis	1
anatomical structure formation involved in morphogenesis	1
blood vessel development	1
anatomical structure maturation	1
heart morphogenesis	1
growth involved in heart morphogenesis	1
cardiac muscle tissue morphogenesis	1
cardiac muscle tissue growth	1
sphingolipid mediated signaling pathway	1
response to chemical	1
taxis	1
G protein-coupled receptor activity	1
signal transduction	1
adenylate cyclase activator activity	1
adenylate cyclase inhibitor activity	1
phospholipase C activator activity	1
central nervous system development	1
animal organ development	1
head development	1
cell motility	1
action potential	1
cell communication	1
chemical synaptic transmission	1
nervous system process	1
lamellipodium organization	1
plasma membrane bounded cell projection assembly	1
cytoskeleton organization	1
actin filament-based process	1
cell adhesion	1
regulation of cellular process	1
cell differentiation	1
generation of neurons	1
cell migration	1
regulation of cell migration	1
positive regulation of cell motility	1
regulation of ossification	1

Protein interactions and networks

STRING

1903 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
S1PR1	CD69	Q07108	993
S1PR1	SPHK1	Q9NYA1	918
S1PR1	SPHK2	Q9NRA0	870
S1PR1	KLF2	Q9Y5W3	822
S1PR1	SELL	P14151	801
S1PR1	F2RL1	P55085	786
S1PR1	ACER2	Q5QJU3	717
S1PR1	PROCR	Q9UNN8	714
S1PR1	CXCR5	P32302	698
S1PR1	CCR7	P32248	692
S1PR1	CXCR4	P30991	688
S1PR1	ARRB2	P32121	682
S1PR1	CXCR3	P49682	651
S1PR1	STAT3	P40763	640
S1PR1	IL6	P05231	631

IntAct

20 interactions, top by confidence:

A	B	Type	Score
TRDN	TMEM223	psi-mi:“MI:0914”(association)	0.640
CD69	S1PR1	psi-mi:“MI:0915”(physical association)	0.520
S1PR1	RAMP1	psi-mi:“MI:0915”(physical association)	0.400
RAMP2	S1PR1	psi-mi:“MI:0915”(physical association)	0.400
RAMP3	S1PR1	psi-mi:“MI:0915”(physical association)	0.400
S1PR1	RAMP3	psi-mi:“MI:0915”(physical association)	0.400
CMSS1	S1PR1	psi-mi:“MI:0915”(physical association)	0.370
CLEC2D	TMEM120B	psi-mi:“MI:0914”(association)	0.350
S1PR1	POTEF	psi-mi:“MI:0914”(association)	0.350
S1PR1	STXBP3	psi-mi:“MI:0914”(association)	0.350
S1PR1	TNPO2	psi-mi:“MI:0914”(association)	0.350
S1PR1	ISLR	psi-mi:“MI:0914”(association)	0.350
SCN3B	NBAS	psi-mi:“MI:0914”(association)	0.350
S1PR1	S1PR2	psi-mi:“MI:2364”(proximity)	0.270
SP1	S1PR1	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (123): S1PR1 (Reconstituted Complex), ACP2 (Affinity Capture-MS), ATP2B3 (Affinity Capture-MS), HK3 (Affinity Capture-MS), SRC (Affinity Capture-MS), GOLPH3L (Affinity Capture-MS), GNAQ (Affinity Capture-MS), ATP12A (Affinity Capture-MS), CD47 (Affinity Capture-MS), ARL10 (Affinity Capture-MS), GNG5 (Affinity Capture-MS), HRAS (Affinity Capture-MS), S1PR1 (Affinity Capture-MS), RAP2A (Affinity Capture-MS), LMBR1 (Affinity Capture-MS)

ESM2 similar proteins: A0A2R9YJI3, B2ZHY2, B4XF06, D4A3U0, O02777, O08530, O43194, O46635, P06199, P14842, P17200, P18599, P20272, P21453, P21554, P28223, P30372, P30544, P32240, P34979, P35363, P43114, P47746, P47936, P48303, P50128, P50129, P56971, Q333S9, Q5E9P3, Q5IS73, Q5U431, Q60F97, Q71SP5, Q75Z89, Q801M1, Q8BZL4, Q91178, Q91559, Q98894

Diamond homologs: O02777, O08530, O77408, O77621, O95136, P20272, P21453, P21554, P30546, P30966, P31389, P31390, P34972, P35367, P47746, P47752, P47936, P48303, P52592, P56971, P70174, Q17232, Q28928, Q333S9, Q5E9P3, Q5IS73, Q71SP5, Q7JQF1, Q801M1, Q90WY5, Q98894, Q98895, Q9DDK4, Q9H228, Q9I8K8, Q9N2B0, Q9N2B1, Q9N2B2, Q9PUI7, Q9PUQ8

SIGNOR signaling

11 interactions.

A	Effect	B	Mechanism
AKT	“up-regulates activity”	S1PR1	phosphorylation
“sphingosine 1-phosphate”	up-regulates	S1PR1	“chemical activation”
fingolimod	down-regulates	S1PR1	“chemical inhibition”
AKT1	“up-regulates activity”	S1PR1	phosphorylation
S1PR1	“up-regulates activity”	GNAI1	binding
S1PR1	“up-regulates activity”	GNAI3	binding
S1PR1	“up-regulates activity”	GNAO1	binding
S1PR1	“up-regulates activity”	GNAZ	binding
“sphingosine 1-phosphate(1-)”	“up-regulates activity”	S1PR1	“chemical activation”
ZDHHC5	“up-regulates activity”	S1PR1	palmitoylation
S1PR1	up-regulates	GNAI1

Disease & clinical

Cancer significance

Clinical variants and AI predictions

ClinVar

28 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	24
Likely benign	0
Benign	2

Top pathogenic / likely-pathogenic (0)

SpliceAI

277 predictions. Top by Δscore:

Variant	Effect	Δscore
1:101237095:GCGAG:G	donor_gain	1.0000
1:101237097:GAGG:G	donor_loss	1.0000
1:101237098:AGGTA:A	donor_loss	1.0000
1:101237101:T:G	donor_loss	1.0000
1:101238819:A:AG	acceptor_gain	0.9900
1:101238820:A:G	acceptor_gain	0.9900
1:101238821:G:GG	acceptor_gain	0.9900
1:101238817:TTAA:T	acceptor_loss	0.9800
1:101238819:AAG:A	acceptor_gain	0.9800
1:101238821:G:A	acceptor_gain	0.9800
1:101238821:GG:G	acceptor_loss	0.9800
1:101238821:GGCT:G	acceptor_gain	0.9800
1:101236992:G:GG	donor_gain	0.9700
1:101237097:GAG:G	donor_gain	0.9700
1:101237766:G:GG	donor_gain	0.9700
1:101238809:T:A	acceptor_gain	0.9600
1:101238820:AG:A	acceptor_gain	0.9600
1:101237100:G:GG	donor_gain	0.9300
1:101237753:G:GT	donor_gain	0.9300
1:101237097:G:GT	donor_gain	0.9200
1:101237676:TAG:T	acceptor_gain	0.9200
1:101238814:T:A	acceptor_gain	0.9100
1:101238820:AGGCT:A	acceptor_gain	0.9100
1:101238821:GGCTG:G	acceptor_gain	0.9100
1:101237678:G:T	acceptor_gain	0.9000
1:101238821:GGC:G	acceptor_gain	0.8900
1:101236990:GA:G	donor_gain	0.8800
1:101238809:T:TA	acceptor_loss	0.8800
1:101238824:T:A	acceptor_gain	0.8700
1:101237677:AG:A	acceptor_gain	0.8600

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000325160 (1:101238370 A>G), RS1000648737 (1:101237667 G>A), RS1000676695 (1:101237908 A>G), RS1001562306 (1:101238277 G>A,T), RS1001601173 (1:101237142 C>G,T), RS1001932612 (1:101238053 G>A,C,T), RS1001945715 (1:101237328 CT>C), RS1002036833 (1:101241987 T>C), RS1002333486 (1:101236052 C>A,T), RS1003729307 (1:101240585 C>T), RS1003907675 (1:101236536 G>C), RS1004546362 (1:101237239 C>A,T), RS1004563521 (1:101242503 C>CA), RS1004598569 (1:101237004 G>C), RS1005211950 (1:101240606 T>A)

Disease associations

OMIM: gene MIM:601974 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

15 associations (top):

Study	Trait	p-value
GCST004627_123	Lymphocyte count	3.000000e-10
GCST004627_124	Lymphocyte count	3.000000e-15
GCST004627_125	Lymphocyte count	2.000000e-19
GCST005997_7	Lymphocyte count	3.000000e-32
GCST006535_2	Irritable bowel syndrome	3.000000e-06
GCST007121_2	Multiple sclerosis and C-reactive protein levels (pleiotropy)	3.000000e-06
GCST007124_1	Multiple sclerosis and HDL levels (pleiotropy)	4.000000e-06
GCST009310_30	Sensorimotor dexterity	4.000000e-07
GCST010732_1	Sensory peripheral neuropathy in microtubule targeting agent-treated breast cancer	4.000000e-07
GCST90002388_615	Lymphocyte count	2.000000e-10
GCST90002388_616	Lymphocyte count	2.000000e-17
GCST90002388_617	Lymphocyte count	2.000000e-12
GCST90002388_618	Lymphocyte count	9.000000e-21
GCST90002389_63	Lymphocyte percentage of white cells	3.000000e-14
GCST90002389_64	Lymphocyte percentage of white cells	6.000000e-17

EFO canonical traits (6, from GWAS)

EFO ID	Trait name
EFO:0004587	lymphocyte count
EFO:0004458	C-reactive protein measurement
EFO:0004612	high density lipoprotein cholesterol measurement
EFO:0008354	cognitive function measurement
EFO:0005260	response to antimicrotubule agent
EFO:0007993	lymphocyte percentage of leukocytes

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL2363041 (PROTEIN FAMILY), CHEMBL4333 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

13 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 27,325 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1096146	PONESIMOD	4	672
CHEMBL2336071	SIPONIMOD	4	1,508
CHEMBL314854	FINGOLIMOD	4	16,015
CHEMBL3358920	ETRASIMOD	4	817
CHEMBL3707247	OZANIMOD	4	1,588
CHEMBL544665	FINGOLIMOD HYDROCHLORIDE	4	1,671
CHEMBL4297505	CENERIMOD	3	244
CHEMBL3707375	AMISELIMOD	2	399
CHEMBL405355	NIGULDIPINE	2	1,802
CHEMBL4097139	ICANBELIMOD	2	41
CHEMBL46874	PINAFIDE	2	2,444
CHEMBL4297350	ASP-4058	1	24
CHEMBL4297542	GSK-2018682	1	100

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: gpcr — Lysophospholipid (S1P) receptors

Most potent curated ligand interactions (35 total), top 25:

Ligand	Action	Affinity	Parameter
RP-001	Agonist	11.05	pEC50
amiselimod phosphate	Agonist	10.12	pEC50
siponimod	Agonist	10.11	pEC50
RP-101075	Agonist	9.57	pEC50
fingolimod-phosphate	Agonist	9.5	pEC50
ozanimod	Agonist	9.48	pEC50
NIBR-0213	Antagonist	9.43	pKd
sphingosine 1-phosphate	Agonist	9.41	pKd
etrasimod	Agonist	9.24	pEC50
BMS-986166	Partial agonist	9.22	pEC50
compound 26 [PMID: 16190743]	Agonist	9.22	pIC50
mocravimod-phosphate	Agonist	9.07	pEC50
cenerimod	Agonist	9.0	pEC50
AUY954	Agonist	8.92	pEC50
CYM5442	Agonist	8.91	pEC50
AFD(R)	Agonist	8.8	pEC50
compound 43 [PMID: 26751273]	Agonist	8.8	pEC50
BMS-986104 derivative 12	Biased agonist	8.68	pEC50
BMS-986104 derivative 24	Biased agonist	8.68	pEC50
CYM5181	Agonist	8.47	pEC50
ASP4058	Agonist	8.13	pIC50
ponesimod	Agonist	8.04	pEC50
icanbelimod	Agonist	8.01	pEC50
SAR247799	Biased agonist	7.9	pEC50
VPC23019	Antagonist	7.86	pKi

Binding affinities (BindingDB)

1428 measured of 1692 human assays (1705 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
(E)-3-amino-2-[2-[[5-[(4-chlorobenzyl)thio]-1,3,4-thiadiazol-2-yl]thio]acetyl]but-2-enenitrile	EC50	0.00314 nM
1-Phenylbenzimidazole deriv. 76	EC50	0.00399 nM
3-(4-ethoxy-3-methoxy-phenyl)-5-(3-pyridyl)-1,2,4-oxadiazole	EC50	0.0571 nM
3-(3-methyl-4-{5-[4-(propan-2-yloxy)-3-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-3-yl}phenyl)propanoic acid	EC50	0.08 nM
3-(4-{5-[3-cyano-4-(propan-2-yloxy)phenyl]-1,2,4-oxadiazol-3-yl}-3-methylphenyl)propanoic acid	EC50	0.08 nM
3-[[5-chloro-2-[[(1R)-1-(4-chloro-3-methylphenyl)propyl]amino]-4-pyridinyl]methylamino]propanoic acid	IC50	0.1 nM	US-8791100: Aryl benzylamine compounds
1-[[5-[[(1S)-1-(4-chloro-3-methylphenyl)-2,2,2-trifluoroethyl]amino]-2-methylphenyl]methyl]azetidine-3-carboxylic acid	IC50	0.1 nM	US-8791100: Aryl benzylamine compounds
1-[[5-[[(1S)-1-(4-chloro-3-methylphenyl)-2,2,2-trifluoroethyl]amino]-2-fluorophenyl]methyl]azetidine-3-carboxylic acid	IC50	0.1 nM	US-8791100: Aryl benzylamine compounds
1-[[4-[5-[1-cyclohexyl-5-(2-methoxyethyl)pyrazol-4-yl]-1,2,4-oxadiazol-3-yl]phenyl]methyl]azetidine-3-carboxylic acid	KI	0.1 nM	US-8802663: Pyrazole oxadiazole derivatives as S1P1 agonists
N-[(2S)-3-[2-ethyl-6-methyl-4-[5-[2-methyl-6-(2-methylpropyl)-4-pyridinyl]-1,2,4-oxadiazol-3-yl]phenoxy]-2-hydroxypropyl]-2-hydroxyacetamide	EC50	0.1 nM	US-9617250: Pyridin-4-yl derivatives
N-[(2S)-3-[4-[5-(2-cyclopentyl-4-pyridinyl)-1,2,4-oxadiazol-3-yl]-2-ethyl-6-methylphenoxy]-2-hydroxypropyl]-2-hydroxyacetamide	EC50	0.1 nM	US-9617250: Pyridin-4-yl derivatives
N-[(2S)-3-[2-ethyl-6-methyl-4-[5-(2-pentan-3-yl-4-pyridinyl)-1,2,4-oxadiazol-3-yl]phenoxy]-2-hydroxypropyl]-2-hydroxyacetamide	EC50	0.1 nM	US-9617250: Pyridin-4-yl derivatives
methyl 2-[7-[[4-cyclopentyl-3-(trifluoromethyl)phenyl]methoxy]-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]acetate	EC50	0.102 nM	US-9175320: Processes for the preparation of (R)-2-(7-4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[B]indol-3-yl)acetic acid and salts thereof
(2S)-3-[4-[5-[2-[1-(4-fluorophenyl)cyclohexyl]ethyl]-1,2,4-oxadiazol-3-yl]-2,6-dimethylphenoxy]propane-1,2-diol	IC50	0.12 nM	US-8822510: Substituted 3-phenyl-1,2,4-Oxadiazole compounds
3-(3-methyl-4-{5-[4-(propan-2-yloxy)-3-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-3-yl}phenyl)butanoic acid	EC50	0.12 nM
1-[[5-[1-(4-chloro-3-methylphenyl)propylamino]-2-methylphenyl]methyl]azetidine-3-carboxylic acid	IC50	0.2 nM	US-8791100: Aryl benzylamine compounds
1-[[2-chloro-5-[[(1S)-1-(4-chloro-3-methylphenyl)-2,2,2-trifluoroethyl]amino]phenyl]methyl]-3-methylazetidine-3-carboxylic acid	IC50	0.2 nM	US-8791100: Aryl benzylamine compounds
BDBM50165434	EC50	0.2 nM	US-9617250: Pyridin-4-yl derivatives
N-[(2S)-3-[4-[5-(2-cyclopentyl-6-methyl-4-pyridinyl)-1,2,4-oxadiazol-3-yl]-2-ethyl-6-methylphenoxy]-2-hydroxypropyl]-2-hydroxyacetamide	EC50	0.2 nM	US-9617250: Pyridin-4-yl derivatives
N-[(2S)-3-[2-ethyl-6-methyl-4-[5-[2-(2-methylpropyl)-4-pyridinyl]-1,2,4-oxadiazol-3-yl]phenoxy]-2-hydroxypropyl]-2-hydroxyacetamide	EC50	0.2 nM	US-9617250: Pyridin-4-yl derivatives
1-[[4-[5-[2-[1-(4-fluorophenyl)cyclohexyl]ethyl]-1,2,4-oxadiazol-3-yl]phenyl]methyl]azetidine-3-carboxylic acid	IC50	0.21 nM	US-8822510: Substituted 3-phenyl-1,2,4-Oxadiazole compounds
(1S,2S)-2-(3-methyl-4-{5-[4-(propan-2-yloxy)-3-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-3-yl}phenyl)cyclopropane-1-carboxylic acid	EC50	0.21 nM
3-[7-[5-[3-(methoxymethyl)-4-(2-methylphenyl)phenyl]-1,2,4-oxadiazol-3-yl]-3,4-dihydro-1H-isoquinolin-2-yl]propanoic acid	KI	0.23 nM	US-8741923: Oxadiazole fused heterocyclic derivatives useful for the treatment of multiple sclerosis
3-[[2-hydroxy-2-[4-[5-[3-phenyl-4-(trifluoromethyl)-1,2-oxazol-5-yl]-1,2,4-oxadiazol-3-yl]phenyl]acetyl]amino]-N,N-dimethylpropanamide	IC50	0.3 nM	US-8835470: Mandelamide heterocyclic compounds
2-methyl-3-(3-methyl-4-{5-[4-(propan-2-yloxy)-3-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-3-yl}phenyl)propanoic acid	EC50	0.3 nM
N-[(2S)-3-[2-ethyl-4-[5-(2-ethyl-6-methyl-4-pyridinyl)-1,2,4-oxadiazol-3-yl]-6-methylphenoxy]-2-hydroxypropyl]-2-hydroxyacetamide	EC50	0.3 nM	US-9617250: Pyridin-4-yl derivatives
N-[(2S)-3-[2-ethyl-6-methyl-4-[5-(2-propan-2-yl-4-pyridinyl)-1,2,4-oxadiazol-3-yl]phenoxy]-2-hydroxypropyl]-2-hydroxyacetamide	EC50	0.3 nM	US-9617250: Pyridin-4-yl derivatives
1-[[4-[5-[[1-(4-fluorophenyl)cyclohexyl]methoxymethyl]-1,2,4-oxadiazol-3-yl]phenyl]methyl]azetidine-3-carboxylic acid	IC50	0.31 nM	US-8822510: Substituted 3-phenyl-1,2,4-Oxadiazole compounds
1-[[3-[3-phenyl-4-(trifluoromethyl)-1,2-oxazol-5-yl]-4H-chromeno[4,3-c][1,2]oxazol-7-yl]methyl]azetidine-3-carboxylic acid	EC50	0.32 nM	US-9216972: Tricyclic heterocyclic compounds
1-[[3-[1-(4-chloro-3-methylphenyl)propylamino]-5-methylphenyl]methyl]azetidine-3-carboxylic acid	IC50	0.4 nM	US-8791100: Aryl benzylamine compounds
(3R)-1-[[2-chloro-5-[[(1S)-1-(4-chloro-3-methylphenyl)-2,2,2-trifluoroethyl]amino]phenyl]methyl]pyrrolidine-3-carboxylic acid	IC50	0.4 nM	US-8791100: Aryl benzylamine compounds
3-[[3-[[(1S)-1-(4-chloro-3-methylphenyl)-2,2,2-trifluoroethyl]amino]-2,6-dimethylphenyl]methylamino]propanoic acid	IC50	0.4 nM	US-8791100: Aryl benzylamine compounds
(3R)-1-[[5-chloro-2-[[(1S)-1-(4-chloro-3-methylphenyl)-2,2,2-trifluoroethyl]amino]-4-pyridinyl]methyl]pyrrolidine-3-carboxylic acid	IC50	0.4 nM	US-8791100: Aryl benzylamine compounds
[2-amino-7-[5-[4-propan-2-yloxy-3-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]-3,4-dihydro-1H-naphthalen-2-yl]methanol	IC50	0.4 nM	US-9315492: Heterocyclic group contained amino-methanol derivative, and salt, synthetic method and use thereof
[2-amino-7-[5-(3-methyl-4-propan-2-yloxyphenyl)-3H-1,2,4-triazol-3-yl]-3,4-dihydro-1H-naphthalen-2-yl]methanol	IC50	0.4 nM	US-9315492: Heterocyclic group contained amino-methanol derivative, and salt, synthetic method and use thereof
1-({4-[5-(4-cyclopentylphenyl)-1,2,4-oxadiazol-3-yl]phenyl}methyl)azetidine-3-carboxylic acid	IC50	0.4 nM
1-[(4-{5-[4-(3,3,3-trifluoropropyl)phenyl]-1,2,4-oxadiazol-3-yl}phenyl)methyl]azetidine-3-carboxylic acid	IC50	0.4 nM
N-[(2S)-3-[2-ethyl-6-methyl-4-[5-(2-methyl-6-propyl-4-pyridinyl)-1,2,4-oxadiazol-3-yl]phenoxy]-2-hydroxypropyl]-2-hydroxyacetamide	EC50	0.4 nM	US-9617250: Pyridin-4-yl derivatives
3-(5-{5-[3-cyano-4-(propan-2-yloxy)phenyl]-1,2,4-oxadiazol-3-yl}-6-methylpyridin-2-yl)propanoic acid	EC50	0.44 nM
(1S,2S)-2-(4-{5-[3-cyano-4-(propan-2-yloxy)phenyl]-1,2,4-oxadiazol-3-yl}-3-methylphenyl)cyclopropane-1-carboxylic acid	EC50	0.45 nM
N-(2-hydroxy-2-methylpropyl)-3-[[2-hydroxy-2-[4-[5-[3-phenyl-4-(trifluoromethyl)-1,2-oxazol-5-yl]-1,2,4-oxadiazol-3-yl]phenyl]acetyl]amino]propanamide	IC50	0.46 nM	US-8835470: Mandelamide heterocyclic compounds
1-[[4-[5-[3-[1-(4-fluorophenyl)cyclohexyl]propyl]-1,2,4-oxadiazol-3-yl]phenyl]methyl]azetidine-3-carboxylic acid	IC50	0.47 nM	US-8822510: Substituted 3-phenyl-1,2,4-Oxadiazole compounds
2-[7-[5-[4-(2-methylphenyl)-3-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-3-yl]-3,4-dihydro-1H-isoquinolin-2-yl]acetic acid	KI	0.49 nM	US-8741923: Oxadiazole fused heterocyclic derivatives useful for the treatment of multiple sclerosis
1-[1-[3-[[(1R)-1-(4-chloro-3-methylphenyl)propyl]amino]phenyl]ethyl]azetidine-3-carboxylic acid	IC50	0.5 nM	US-8791100: Aryl benzylamine compounds
(3R)-1-[[5-chloro-2-[[(1R)-1-(4-chloro-3-methylphenyl)propyl]amino]-4-pyridinyl]methyl]pyrrolidine-3-carboxylic acid	IC50	0.5 nM	US-8791100: Aryl benzylamine compounds
1-[[4-[5-[3-[1-(4-chlorophenyl)cyclohexyl]propyl]-1,2,4-oxadiazol-3-yl]phenyl]methyl]azetidine-3-carboxylic acid	IC50	0.54 nM	US-8822510: Substituted 3-phenyl-1,2,4-Oxadiazole compounds
1-[[3-[5-phenyl-4-(trifluoromethyl)-1,2-oxazol-3-yl]-4,5-dihydrobenzo[g][2,1]benzoxazol-7-yl]methyl]azetidine-3-carboxylic acid	EC50	0.59 nM	US-9216972: Tricyclic heterocyclic compounds
3-[7-[5-[4-(2-methylphenyl)-3-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-3-yl]-3,4-dihydro-1H-isoquinolin-2-yl]propanoic acid	KI	0.6 nM	US-8741923: Oxadiazole fused heterocyclic derivatives useful for the treatment of multiple sclerosis
1-[[3-[[(1R)-1-(4-chloro-3-methylphenyl)propyl]amino]-2,6-dimethylphenyl]methyl]azetidine-3-carboxylic acid	IC50	0.6 nM	US-8791100: Aryl benzylamine compounds
1-[[5-chloro-2-[[(1R)-1-(4-chloro-3-methylphenyl)propyl]amino]-4-pyridinyl]methyl]azetidine-3-carboxylic acid	IC50	0.6 nM	US-8791100: Aryl benzylamine compounds

ChEMBL bioactivities

4274 potent at pChembl≥5 of 4427 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
11.00	EC50	0.01	nM	CHEMBL2032300
11.00	IC50	0.01	nM	CHEMBL3403631
11.00	IC50	0.01	nM	CHEMBL3806205
10.92	EC50	0.012	nM	FTY720-P
10.90	EC50	0.01259	nM	CHEMBL2018176
10.85	IC50	0.014	nM	CHEMBL114606
10.85	IC50	0.014	nM	CHEMBL4637401
10.80	EC50	0.01585	nM	CHEMBL2059683
10.80	IC50	0.016	nM	CHEMBL4752394
10.74	EC50	0.018	nM	CHEMBL1093686
10.70	EC50	0.01995	nM	CHEMBL2059684
10.70	EC50	0.02	nM	CHEMBL114606
10.70	EC50	0.02	nM	FTY720-P
10.68	EC50	0.021	nM	CHEMBL3359523
10.60	EC50	0.02512	nM	CHEMBL2032301
10.60	EC50	0.025	nM	CHEMBL3359522
10.57	EC50	0.027	nM	CHEMBL4093489
10.57	EC50	0.027	nM	CHEMBL225155
10.56	EC50	0.02754	nM	CHEMBL4093489
10.52	EC50	0.03	nM	CHEMBL3403619
10.52	EC50	0.03	nM	CHEMBL378436
10.50	EC50	0.03162	nM	CHEMBL2018320
10.50	EC50	0.03162	nM	CHEMBL2032428
10.50	EC50	0.03162	nM	CHEMBL2032430
10.49	EC50	0.032	nM	CHEMBL3959509
10.40	EC50	0.03981	nM	CHEMBL2011746
10.40	EC50	0.03981	nM	CHEMBL2018321
10.40	EC50	0.04	nM	ETRASIMOD
10.40	EC50	0.04	nM	CHEMBL3400910
10.40	EC50	0.04	nM	CHEMBL3400909
10.40	EC50	0.04	nM	CHEMBL3403630
10.40	EC50	0.04	nM	CHEMBL3403631
10.40	EC50	0.04	nM	CHEMBL3403632
10.40	IC50	0.04	nM	CHEMBL4786296
10.39	EC50	0.041	nM	CHEMBL3358955
10.30	EC50	0.05012	nM	CHEMBL2018319
10.30	EC50	0.05	nM	CHEMBL3926787
10.30	EC50	0.05	nM	CHEMBL3924073
10.30	EC50	0.05	nM	CHEMBL3896496
10.30	EC50	0.05	nM	CHEMBL3984513
10.30	EC50	0.05	nM	CHEMBL3944842
10.30	EC50	0.05	nM	CHEMBL3926299
10.30	EC50	0.05	nM	CHEMBL3954097
10.30	EC50	0.05	nM	CHEMBL3916821
10.30	EC50	0.05	nM	CHEMBL3970830
10.30	EC50	0.05	nM	CHEMBL3979740
10.30	EC50	0.05	nM	CHEMBL3939008
10.30	EC50	0.05	nM	CHEMBL3940245
10.30	EC50	0.05	nM	CHEMBL3895822
10.30	EC50	0.05	nM	CHEMBL3918031

PubChem BioAssay actives

2344 with measured affinity, of 3485 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
[(2S)-2-amino-2-(hydroxymethyl)-4-(4-octylphenyl)butyl] dihydrogen phosphate	1176592: Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay	ec50	<0.0001	uM
1-[[6-[(2-methoxy-4-propylphenyl)methoxy]-1-methyl-3,4-dihydronaphthalen-2-yl]methyl]azetidine-3-carboxylic acid	1477093: Agonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISA	ec50	<0.0001	uM
[(1R,3S)-1-amino-3-[(6S)-6-[2-(2-methoxyphenyl)ethyl]-5,6,7,8-tetrahydronaphthalen-2-yl]cyclopentyl]methyl dihydrogen phosphate	1735816: Displacement of [33P]-SIP from human recombinant S1P1 expressed in CHO cell membranes measured after 45 mins by radioligand competitive binding analysis	ic50	<0.0001	uM
[(1R,3S)-1-amino-3-[(6R)-6-(3-ethoxypropyl)-5,6,7,8-tetrahydronaphthalen-2-yl]cyclopentyl]methyl dihydrogen phosphate	1730770: Displacement of [33P]-SIP from human recombinant S1P1 expressed in CHO cell membranes measured after 45 mins by TopCount scintillation counting method	ic50	<0.0001	uM
[(1R,3S)-1-amino-3-[(6R)-6-(5-methoxypentyl)-5,6,7,8-tetrahydronaphthalen-2-yl]cyclopentyl]methyl dihydrogen phosphate	1730770: Displacement of [33P]-SIP from human recombinant S1P1 expressed in CHO cell membranes measured after 45 mins by TopCount scintillation counting method	ic50	<0.0001	uM
3-[4-[5-(3-chloro-4-propan-2-yloxyphenyl)-1,2,4-oxadiazol-3-yl]indol-1-yl]propanoic acid	662678: Agonist activity at SIP1 receptor by tango assay	ec50	<0.0001	uM
3-[4-[5-[3-cyano-4-(1,1,1-trifluoropropan-2-yloxy)phenyl]-1,2,4-oxadiazol-3-yl]-3-methylphenyl]propanoic acid	268302: Agonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake	ec50	<0.0001	uM
3-[7-[5-(3-chloro-4-propan-2-yloxyphenyl)-1,2,4-oxadiazol-3-yl]-1H-indol-3-yl]propanoic acid	656694: Agonist activity at S1P1 receptor by Tango assay	ec50	<0.0001	uM
3-[7-[5-(3-chloro-4-propan-2-yloxyphenyl)-1,2,4-oxadiazol-3-yl]-1-methylindol-3-yl]propanoic acid	656694: Agonist activity at S1P1 receptor by Tango assay	ec50	<0.0001	uM
3-[7-[5-(3-chloro-4-propan-2-yloxyphenyl)-1,2,4-oxadiazol-3-yl]-4-fluoro-1-methylindol-3-yl]propanoic acid	656694: Agonist activity at S1P1 receptor by Tango assay	ec50	<0.0001	uM
Etrasimod	1176592: Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay	ec50	<0.0001	uM
2-[6-[[4-cyclopentyl-3-(trifluoromethyl)phenyl]methoxy]-2,3-dihydro-1H-pyrrolo[1,2-a]indol-3-yl]acetic acid	1176728: Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay	ec50	<0.0001	uM
[(2R)-2-amino-2-[(2S)-6-octyl-1,2,3,4-tetrahydronaphthalen-2-yl]propyl] dihydrogen phosphate	473717: Agonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assay	ec50	<0.0001	uM
2-[6-[[4-cyclopentyl-3-(trifluoromethyl)phenyl]methoxy]-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl]acetic acid	1192396: Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay	ec50	<0.0001	uM
2-[6-[(3-cyano-4-propan-2-yloxyphenyl)methoxy]-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl]acetic acid	1192396: Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay	ec50	<0.0001	uM
2-[6-[[4-(2-methylpropyl)-3-(trifluoromethyl)phenyl]methoxy]-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl]acetic acid	1192396: Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay	ec50	<0.0001	uM
2-[10-chloro-8-[[4-cyclopentyl-3-(trifluoromethyl)phenyl]methoxy]-3,4-dihydro-1H-[1,4]oxazino[4,3-a]indol-1-yl]acetic acid	1192396: Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay	ec50	<0.0001	uM
2-[10-chloro-8-[[4-propan-2-yloxy-3-(trifluoromethyl)phenyl]methoxy]-3,4-dihydro-1H-[1,4]oxazino[4,3-a]indol-1-yl]acetic acid	1192396: Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay	ec50	<0.0001	uM
2-[10-chloro-8-[(3-cyano-4-propan-2-yloxyphenyl)methoxy]-3,4-dihydro-1H-[1,4]oxazino[4,3-a]indol-1-yl]acetic acid	1192396: Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay	ec50	<0.0001	uM
3-[[4-[5-(3-cyano-4-propan-2-yloxyphenyl)-1,2,4-oxadiazol-3-yl]-2,3-dihydro-1H-inden-1-yl]amino]propanoic acid	2033333: Modulation of S1PR1 (unknown origin)	ec50	<0.0001	uM
[(E,2S,3R)-2-amino-3-hydroxyoctadec-4-enyl] dihydrogen phosphate	473717: Agonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assay	ec50	<0.0001	uM
1-[[3-[3-phenyl-4-(trifluoromethyl)-1,2-oxazol-5-yl]-4,5-dihydrobenzo[g][2,1]benzoxazol-7-yl]methyl]azetidine-3-carboxylic acid	1686123: Agonist activity at human S1P1 assessed as stimulation of cAMP accumulation	ec50	<0.0001	uM
2-[(3R)-4-chloro-6-[[4-propan-2-yloxy-3-(trifluoromethyl)phenyl]methoxy]-2,3-dihydro-1H-pyrrolo[1,2-a]indol-3-yl]acetic acid	1176728: Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay	ec50	<0.0001	uM
2-[2-[2-ethyl-3-[5-[4-propan-2-yloxy-3-(trifluoromethyl)phenyl]-1,2,4-thiadiazol-3-yl]phenyl]ethylamino]acetic acid	672824: Agonist activity against S1P1 receptor by cell based FRET assay	ec50	<0.0001	uM
2-[2-[2-ethyl-3-[5-[4-propan-2-yloxy-3-(trifluoromethyl)phenyl]-1,2,4-thiadiazol-3-yl]phenyl]ethyl-methylamino]acetic acid	672824: Agonist activity against S1P1 receptor by cell based FRET assay	ec50	<0.0001	uM
3-[7-[5-(3-chloro-4-propan-2-yloxyphenyl)-1,2,4-oxadiazol-3-yl]-5-fluoro-1-methylindol-3-yl]propanoic acid	656694: Agonist activity at S1P1 receptor by Tango assay	ec50	<0.0001	uM
2-[(3R)-4-chloro-6-[(3-cyano-4-propan-2-yloxyphenyl)methoxy]-2,3-dihydro-1H-pyrrolo[1,2-a]indol-3-yl]acetic acid	1176728: Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay	ec50	<0.0001	uM
3-[7-[5-(3-chloro-4-propan-2-yloxyphenyl)-1,2,4-oxadiazol-3-yl]-1H-indol-3-yl]propanamide	656694: Agonist activity at S1P1 receptor by Tango assay	ec50	<0.0001	uM
3-[2-[2-[4-phenyl-3-(trifluoromethyl)phenyl]-1,3-benzoxazol-5-yl]ethylamino]propanoic acid	662678: Agonist activity at SIP1 receptor by tango assay	ec50	<0.0001	uM
3-[7-[5-(3-chloro-4-propan-2-yloxyphenyl)-1,2,4-oxadiazol-3-yl]-1H-indol-3-yl]-N-methylpropanamide	656694: Agonist activity at S1P1 receptor by Tango assay	ec50	<0.0001	uM
2-[3-[2-[4-phenyl-3-(trifluoromethyl)phenyl]-1,3-benzoxazol-5-yl]propylamino]acetic acid	662678: Agonist activity at SIP1 receptor by tango assay	ec50	<0.0001	uM
3-[4-[5-[butyl-[4-(trifluoromethyl)benzoyl]amino]-1,3,4-thiadiazol-2-yl]indol-1-yl]propanoic acid	652657: Agonist activity at human S1P1 receptor expressed in human U2OS cells assessed as beta-arrestin-mediated receptor internalization by beta-lactamase reporter assay	ec50	<0.0001	uM
3-[3-chloro-4-[5-(3-chloro-4-propan-2-yloxyphenyl)-1,2,4-oxadiazol-3-yl]indol-1-yl]propanoic acid	662678: Agonist activity at SIP1 receptor by tango assay	ec50	<0.0001	uM
[(1R,3S)-1-amino-3-[(6R)-6-hexyl-5,6,7,8-tetrahydronaphthalen-2-yl]cyclopentyl]methyl dihydrogen phosphate	1300062: Displacement of 33-P-S1P from from human S1P receptor expressed in CHO cell membranes after 50 mins by scintillation counting	ic50	<0.0001	uM
[2-amino-2-(hydroxymethyl)-4-(4-octylphenyl)butyl] dihydrogen phosphate	1300062: Displacement of 33-P-S1P from from human S1P receptor expressed in CHO cell membranes after 50 mins by scintillation counting	ic50	<0.0001	uM
[(1R,3R)-3-amino-1-hydroxy-5-(4-octylphenyl)pentyl]phosphonic acid	1474269: Displacement of [33P]-S1P from human S1P1 receptor expressed in CHO cell membranes	ic50	0.0001	uM
[(2R)-2-amino-2-(hydroxymethyl)-4-(4-octylphenyl)butyl] dihydrogen phosphate	466802: Agonist activity at human S1P1 receptor expressed in CHO cells assessed as induction of [S35]GTPgammaS binding	ec50	0.0001	uM
3-[3-methyl-4-[5-[4-propan-2-yloxy-3-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-3-yl]phenyl]butanoic acid	1798174: Ligand-Induced Uptake of [35S]-GTP-gamma-S from Article 10.1016/j.bmcl.2006.10.057: “SAR studies of 3-arylpropionic acids as potent and selective agonists of sphingosine-1-phosphate receptor-1 (S1P1) with enhanced pharmacokinetic properties.”	ec50	0.0001	uM
3-[4-[5-(3-bromo-4-propan-2-yloxyphenyl)-1,2,4-oxadiazol-3-yl]-3-methylphenyl]propanoic acid	268302: Agonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake	ec50	0.0001	uM
3-[4-[5-(3-chloro-4-propan-2-yloxyphenyl)-1,2,4-oxadiazol-3-yl]-3-methylphenyl]propanoic acid	268555: Agonist activity at S1P1 receptor assessed as induction of [35S]GTP-gamma-S binding	ec50	0.0001	uM
1-[[6-[(2-methoxy-4-propylphenyl)methoxy]-1,5-dimethyl-3,4-dihydronaphthalen-2-yl]methyl]azetidine-3-carboxylic acid	1477093: Agonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISA	ec50	0.0001	uM
3-[4-[5-[5-chloro-6-(1,1,1-trifluoropropan-2-yloxy)-3-pyridinyl]-1,2,4-oxadiazol-3-yl]-3-methylphenyl]propanoic acid	268302: Agonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake	ec50	0.0001	uM
3-[4-[5-(3-cyano-4-propan-2-yloxyphenyl)-1,2,4-oxadiazol-3-yl]-3-methylphenyl]propanoic acid	1798174: Ligand-Induced Uptake of [35S]-GTP-gamma-S from Article 10.1016/j.bmcl.2006.10.057: “SAR studies of 3-arylpropionic acids as potent and selective agonists of sphingosine-1-phosphate receptor-1 (S1P1) with enhanced pharmacokinetic properties.”	ec50	0.0001	uM
5-[3-[4-[(2R)-2-amino-3-hydroxypropoxy]-2-chloro-5-fluorophenyl]-1,2,4-oxadiazol-5-yl]-2-propan-2-yloxybenzonitrile	1271835: Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay	ec50	0.0001	uM
3-[[2-hydroxy-2-[4-[5-(5-phenyl-4-propyl-1,2-oxazol-3-yl)-1,2,4-oxadiazol-3-yl]phenyl]ethyl]amino]propanoic acid	1626256: Displacement of [33P]S1P from human S1P1 expressed in CHO cell membranes measured after 45 mins by TopCount method	ic50	0.0001	uM
3-[4-[5-[3-cyano-4-(2,2,2-trifluoroethoxy)phenyl]-1,2,4-oxadiazol-3-yl]-3-methylphenyl]propanoic acid	268302: Agonist activity at S1P1 receptor expressed in CHO cells measured as S1P-induced [35S]GTP-gamma-S uptake	ec50	0.0001	uM
2-amino-2-[2-[4-heptoxy-3-(trifluoromethyl)phenyl]ethyl]propane-1,3-diol	2033333: Modulation of S1PR1 (unknown origin)	ec50	0.0001	uM
3-[3-methyl-4-[5-[4-propan-2-yloxy-3-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-3-yl]phenyl]propanoic acid	1798174: Ligand-Induced Uptake of [35S]-GTP-gamma-S from Article 10.1016/j.bmcl.2006.10.057: “SAR studies of 3-arylpropionic acids as potent and selective agonists of sphingosine-1-phosphate receptor-1 (S1P1) with enhanced pharmacokinetic properties.”	ec50	0.0001	uM
[2-amino-3-hydroxy-2-[(2R)-6-octyl-1,2,3,4-tetrahydronaphthalen-2-yl]propyl] dihydrogen phosphate	473717: Agonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assay	ec50	0.0001	uM
[(2R)-2-amino-2-[(2R)-6-octyl-1,2,3,4-tetrahydronaphthalen-2-yl]propyl] dihydrogen phosphate	473717: Agonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assay	ec50	0.0001	uM

CTD chemical–gene interactions

54 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	increases abundance, affects reaction, increases activity, increases expression, decreases expression (+1 more)	4
Valproic Acid	decreases expression, increases expression	4
sphingosine 1-phosphate	affects binding, affects reaction, increases expression	3
Arsenic	affects expression, increases methylation, affects cotreatment, increases abundance, increases expression	3
trichostatin A	affects expression, decreases expression, affects cotreatment	2
nickel sulfate	affects cotreatment, decreases expression	2
Fingolimod Hydrochloride	decreases reaction, increases expression, affects binding, decreases expression, decreases activity	2
Benzo(a)pyrene	decreases methylation, increases expression	2
Aflatoxin B1	affects expression, decreases expression	2
triphenyl phosphate	affects expression	1
kaempferol	decreases expression, decreases reaction	1
tryptoquivaline	decreases reaction, increases secretion	1
2-methyl-4-isothiazolin-3-one	increases expression	1
terbufos	increases methylation	1
mono-(2-ethylhexyl)phthalate	increases expression	1
cobaltous chloride	decreases expression	1
manganese chloride	increases abundance, increases expression, affects cotreatment	1
ochratoxin A	decreases expression	1
butylbenzyl phthalate	increases expression, increases secretion, affects reaction, decreases reaction	1
S-(1,2-dichlorovinyl)cysteine	affects cotreatment, decreases expression, affects response to substance, increases expression	1
diallyl trisulfide	increases expression	1
di-n-butylphosphoric acid	affects expression	1
perfluoro-n-nonanoic acid	decreases expression	1
macrophage stimulatory lipopeptide 2	affects cotreatment, decreases expression	1
2-palmitoylglycerol	increases expression	1
entinostat	increases expression	1
lipopolysaccharide, Escherichia coli O111 B4	decreases expression, decreases reaction	1
abrine	decreases expression	1
FTY 720P	affects binding	1
(+)-JQ1 compound	decreases expression	1

ChEMBL screening assays

385 unique, capped per target: 194 functional, 191 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1029035	Binding	Displacement of [33P]sphingosine-1-phosphate from human S1P1 receptor	Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists. — Bioorg Med Chem Lett
CHEMBL1029040	Functional	Agonist activity at human S1P1 receptor assessed as stimulation of [35S]GTPgammaS binding	Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists. — Bioorg Med Chem Lett

Cellosaurus cell lines

16 cell lines: 8 cancer cell line, 3 embryonic stem cell, 3 transformed cell line, 2 spontaneously immortalized cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_A6D6	SEES3-1V human S1PR1, clone1	Embryonic stem cell	Male
CVCL_A6D7	SEES3-1V human S1PR1, clone2	Embryonic stem cell	Male
CVCL_A6D8	SEES3-1V human S1PR1, clone3	Embryonic stem cell	Male
CVCL_B2EK	Abcam HeLa S1PR1 KO	Cancer cell line	Female
CVCL_C0SL	ACTOne EDG1	Transformed cell line	Female
CVCL_D9R6	Ubigene HEK293 S1PR1 KO	Transformed cell line	Female
CVCL_E0N5	Ubigene HeLa S1PR1 KO	Cancer cell line	Female
CVCL_E7C3	Abcam SK-HEP-1 S1PR1 KO	Cancer cell line	Male
CVCL_KV12	cAMP Hunter CHO-K1 EDG1 Gi	Spontaneously immortalized cell line	Female
CVCL_KW92	PathHunter CHO-K1 EDG1 beta-arrestin	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.