General Information of Target

Target ID LDTP04469
Target Name G-protein coupled receptor 143 (GPR143)
Gene Name GPR143
Gene ID 4935
Synonyms
OA1; G-protein coupled receptor 143; Ocular albinism type 1 protein
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MASPRLGTFCCPTRDAATQLVLSFQPRAFHALCLGSGGLRLALGLLQLLPGRRPAGPGSP
ATSPPASVRILRAAAACDLLGCLGMVIRSTVWLGFPNFVDSVSDMNHTEIWPAAFCVGSA
MWIQLLYSACFWWLFCYAVDAYLVIRRSAGLSTILLYHIMAWGLATLLCVEGAAMLYYPS
VSRCERGLDHAIPHYVTMYLPLLLVLVANPILFQKTVTAVASLLKGRQGIYTENERRMGA
VIKIRFFKIMLVLIICWLSNIINESLLFYLEMQTDINGGSLKPVRTAAKTTWFIMGILNP
AQGFLLSLAFYGWTGCSLGFQSPRKEIQWESLTTSAAEGAHPSPLMPHENPASGKVSQVG
GQTSDEALSMLSEGSDASTIEIHTASESCNKNEGDPALPTHGDL
Target Bioclass
GPCR
Family
G-protein coupled receptor OA family
Subcellular location
Melanosome membrane
Function
Receptor for tyrosine, L-DOPA and dopamine. After binding to L-DOPA, stimulates Ca(2+) influx into the cytoplasm, increases secretion of the neurotrophic factor SERPINF1 and relocalizes beta arrestin at the plasma membrane; this ligand-dependent signaling occurs through a G(q)-mediated pathway in melanocytic cells. Its activity is mediated by G proteins which activate the phosphoinositide signaling pathway. Also plays a role as an intracellular G protein-coupled receptor involved in melanosome biogenesis, organization and transport.
Uniprot ID
P51810
Ensemble ID
ENST00000467482.6
HGNC ID
HGNC:20145
ChEMBL ID
CHEMBL4523867

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
DBIA
 Probe Info 
C33(2.72)  LDD3369  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 A2058 C33(1.51)  LDD2253  [1]
 LDCM0023  KB03 A2058 C33(2.12)  LDD2670  [1]
 LDCM0024  KB05 OAW-42 C33(2.72)  LDD3369  [1]

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840