General Information of the Protein
Protein ID
PT05702
Protein Name
Mas-related G-protein coupled receptor member X2
Gene Name
MRGPRX2
Secondarily
Gene Name
MRGX2
Sequence
MDPTTPAWGTESTTVNGNDQALLLLCGKETLIPVFLILFIALVGLVGNGFVLWLLGFRMRRNAFSVYVLSLAGADFLFLCFQIINCLVYLSNFFCSISINFPSFFTTVMTCAYLAGLSMLSTVSTERCLSVLWPIWYRCRRPRHLSAVVCVLLWALSLLLSILEGKFCGFLFSDGDSGWCQTFDFITAAWLIFLFMVLCGSSLALLVRILCGSRGLPLTRLYLTILLTVLVFLLCGLPFGIQWFLILWIWKDSDVLFCHIHPVSVVLSSLNSSANPIIYFFVGSFRKQWRLQQPILKLALQRALQDIAEVDHSEGCFRQGTPEMSRSSLV
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
Function
Mast cell-specific receptor for basic secretagogues, i.e. cationic amphiphilic drugs, as well as endo- or exogenous peptides, consisting of a basic head group and a hydrophobic core (PubMed:25517090). Recognizes and binds small molecules containing a cyclized tetrahydroisoquinoline (THIQ), such as non-steroidal neuromuscular blocking drugs (NMBDs), including tubocurarine and atracurium. In response to these compounds, mediates pseudo-allergic reactions characterized by histamine release, inflammation and airway contraction (By similarity). Acts as a receptor for a number of other ligands, including peptides and alkaloids, such as cortistatin-14, proadrenomedullin N-terminal peptides PAMP-12 and, at lower extent, PAMP-20, antibacterial protein LL-37, PMX-53 peptide, beta-defensins, and complanadine A.
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Uniprot ID
Primary ID:
Q96LB1

Secondarily ID:
B5B0C7
Q4QXW4
Q4QXW7
Q4QXX0
Q4QXX2
Q4QXX3
Q4QXX4
Q4QXX6
Q4QXX7
W8W3L5
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Ensembl ID
ENSG00000183695
HGNC ID
HGNC:17983
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0574496
(2S)-2-[(3S)-4,4-difluoro-3-(1-oxidopyridin-1-ium-4-yl)piperidin-1-yl]-N-[5-(2,4-difluorophenoxy)pyrazin-2-yl]propanamide
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C23H21F4N5O3
 1
1
IC50 = 2.512 nM
   TI
   LI
   LO
   TS
CP0952804
2-((S)-3-(5-(aminomethyl)-6-oxo-1,6-dihydropyridin-3-yl)-4,4-difluoropiperidin-1-yl)-N-(5-phenoxypyridin-2-yl)propanamide
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C25H27F2N5O3
 1
1
IC50 <= 10 nM
   TI
   LI
   LO
   TS
CP0952805
2-(4,4-difluoro-3-(6-oxo-1,6-dihydropyridin-3-yl)cyclohexyl)-N-(5-(4-fluorophenoxy)pyridin-2-yl)propanamide
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C25H24F3N3O3
 1
1
IC50 <= 10 nM
   TI
   LI
   LO
   TS
CP0968144
N-(5-(4-chloro-6-fluoropyridin-3-yloxy)pyridin-2-yl)-2-((S)-4,4-difluoro-3-(6-oxo-1,6-dihydropyridin-3-yl)piperidin-1-yl)propanamide
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C23H21ClF3N5O3
 1
1
IC50 <= 10 nM
   TI
   LI
   LO
   TS
CP0968898
(S)-2-((S)-4,4-difluoro-3-(5-(methylsulfonylmethyl)-6-oxo-1,6-dihydropyridin-3-yl)piperidin-1-yl)-N-(5-(2,4-difluorophenoxy)pyridin-2-yl)propanamide
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C26H26F4N4O5S
 1
1
IC50 <= 10 nM
   TI
   LI
   LO
   TS
CP0970614
2-(4,4-difluoro-3-(5-((2-hydroxyethylamino)methyl)-6-oxo-1,6-dihydropyridin-3-yl)piperidin-1-yl)-N-(5-(4-fluorophenoxy)pyridin-2-yl)propanamide
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C27H30F3N5O4
 1
1
IC50 <= 10 nM
   TI
   LI
   LO
   TS
Clinical Information about the Protein
Target 1 ( Mas-related gene 2 (MRGX2) )
Target Type Literature-reported Target