General Information of Target

Target ID LDTP11790
Target Name Sphingosine 1-phosphate receptor 5 (S1PR5)
Gene Name S1PR5
Gene ID 53637
Synonyms
EDG8; Sphingosine 1-phosphate receptor 5; S1P receptor 5; S1P5; Endothelial differentiation G-protein-coupled receptor 8; Sphingosine 1-phosphate receptor Edg-8; S1P receptor Edg-8
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAFPAGFGWAAATAAYQVEGGWDADGKGPCVWDTFTHQGGERVFKNQTGDVACGSYTLWE
EDLKCIKQLGLTHYRFSLSWSRLLPDGTTGFINQKGIDYYNKIIDDLLKNGVTPIVTLYH
FDLPQTLEDQGGWLSEAIIESFDKYAQFCFSTFGDRVKQWITINEANVLSVMSYDLGMFP
PGIPHFGTGGYQAAHNLIKAHARSWHSYDSLFRKKQKGMVSLSLFAVWLEPADPNSVSDQ
EAAKRAITFHLDLFAKPIFIDGDYPEVVKSQIASMSQKQGYPSSRLPEFTEEEKKMIKGT
ADFFAVQYYTTRLIKYQENKKGELGILQDAEIEFFPDPSWKNVDWIYVVPWGVCKLLKYI
KDTYNNPVIYITENGFPQSDPAPLDDTQRWEYFRQTFQELFKAIQLDKVNLQVYCAWSLL
DNFEWNQGYSSRFGLFHVDFEDPARPRVPYTSAKEYAKIIRNNGLEAHL
Target Type
Clinical trial
Target Bioclass
GPCR
Family
G-protein coupled receptor 1 family
Subcellular location
Cell membrane
Function
Receptor for the lysosphingolipid sphingosine 1-phosphate (S1P). S1P is a bioactive lysophospholipid that elicits diverse physiological effect on most types of cells and tissues. Is coupled to both the G(i/0)alpha and G(12) subclass of heteromeric G-proteins. May play a regulatory role in the transformation of radial glial cells into astrocytes and may affect proliferative activity of these cells.
TTD ID
T50089
Uniprot ID
Q9H228
DrugMap ID
TTDZCKV
Ensemble ID
ENST00000333430.6
HGNC ID
HGNC:14299
ChEMBL ID
CHEMBL2274

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A498 SNV: p.G160C .
FTC133 SNV: p.A91T .
HCT116 SNV: p.A170V .
HCT15 SNV: p.P70S .
HT1197 SNV: p.S345F .
JURKAT SNV: p.R349H .
LNCaP clone FGC SNV: p.S237L; p.R239Q .
MOLT4 SNV: p.L301P .
NALM6 SNV: p.V41G .
OVK18 SNV: p.R214C .
TOV21G SNV: p.G35S .
WM115 SNV: p.P187L .
WM2664 SNV: p.P187L .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
BTD
 Probe Info 
C323(0.82)  LDD2100  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0548  1-(4-(Benzo[d][1,3]dioxol-5-ylmethyl)piperazin-1-yl)-2-nitroethan-1-one MDA-MB-231 C322(0.81)  LDD2142  [1]
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C322(0.91)  LDD2112  [1]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C323(0.82)  LDD2100  [1]

References

1 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761