Details of the Target

General Information of Target

Target ID LDTP02317
Target Name Alpha-2A adrenergic receptor (ADRA2A)
Gene Name ADRA2A
Gene ID 150
Synonyms
ADRA2R; ADRAR; Alpha-2A adrenergic receptor; Alpha-2 adrenergic receptor subtype C10; Alpha-2A adrenoreceptor; Alpha-2A adrenoceptor; Alpha-2AAR
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MFRQEQPLAEGSFAPMGSLQPDAGNASWNGTEAPGGGARATPYSLQVTLTLVCLAGLLML
LTVFGNVLVIIAVFTSRALKAPQNLFLVSLASADILVATLVIPFSLANEVMGYWYFGKAW
CEIYLALDVLFCTSSIVHLCAISLDRYWSITQAIEYNLKRTPRRIKAIIITVWVISAVIS
FPPLISIEKKGGGGGPQPAEPRCEINDQKWYVISSCIGSFFAPCLIMILVYVRIYQIAKR
RTRVPPSRRGPDAVAAPPGGTERRPNGLGPERSAGPGGAEAEPLPTQLNGAPGEPAPAGP
RDTDALDLEESSSSDHAERPPGPRRPERGPRGKGKARASQVKPGDSLPRRGPGATGIGTP
AAGPGEERVGAAKASRWRGRQNREKRFTFVLAVVIGVFVVCWFPFFFTYTLTAVGCSVPR
TLFKFFFWFGYCNSSLNPVIYTIFNHDFRRAFKKILCRGDRKRIV
Target Type
Successful
Target Bioclass
GPCR
Family
G-protein coupled receptor 1 family, Adrenergic receptor subfamily, ADRA2A sub-subfamily
Subcellular location
Cell membrane
Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianserine > chlorpromazine = spiperone = prazosin > propanolol > alprenolol = pindolol.
TTD ID
T11448
Uniprot ID
P08913
DrugMap ID
TTWG9A4
Ensemble ID
ENST00000280155.4
HGNC ID
HGNC:281
ChEMBL ID
CHEMBL1867

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FBPP2
 Probe Info  		4.40  LDD0324  [1]
OPA-S-S-alkyne
 Probe Info  		K190(2.31)  LDD3494  [2]
NAIA_4
 Probe Info  		N.A.  LDD2226  [3]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 81 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Amitriptyline Small molecular drug DB00321
Amoxapine Small molecular drug DB00543
Amphetamine Small molecular drug DB00182
Apomorphine Small molecular drug DB00714
Apraclonidine Small molecular drug DB00964
Aripiprazole Small molecular drug DB01238
Asenapine Small molecular drug DB06216
Benzphetamine Small molecular drug DB00865
Bethanidine Small molecular drug DB00217
Brimonidine Small molecular drug DB00484
Bromocriptine Small molecular drug DB01200
Cabergoline Small molecular drug DB00248
Carvedilol Small molecular drug DB01136
Celiprolol Small molecular drug DB04846
Chlorpromazine Small molecular drug DB00477
Clonidine Small molecular drug DB00575
Clozapine Small molecular drug DB00363
Connexyn Small molecular drug D0WD8M
Desipramine Small molecular drug DB01151
Dexmedetomidine Small molecular drug DB00633
Dextroamphetamine Small molecular drug DB01576
Dihydroergotamine Small molecular drug DB00320
Dipivefrin Small molecular drug DB00449
Dronedarone Small molecular drug DB04855
Droxidopa Small molecular drug DB06262
Epinastine Small molecular drug DB00751
Epinephrine Small molecular drug DB00668
Ergotamine Small molecular drug DB00696
Escitalopram Small molecular drug DB01175
Fenoldopam Small molecular drug DB00800
Guanabenz Small molecular drug DB00629
Guanfacine Small molecular drug DB01018
Haloperidol Small molecular drug DB00502
Lamotrigine Small molecular drug DB00555
Lisuride Small molecular drug DB00589
Lofexidine Small molecular drug D0K0MW
Loxapine Small molecular drug DB00408
Lurasidone Small molecular drug DB08815
Maprotiline Small molecular drug DB00934
Metamfetamine Small molecular drug DB01577
Methotrimeprazine Small molecular drug DB01403
Methyldopa Small molecular drug DB00968
Mianserin Small molecular drug DB06148
Mirtazapine Small molecular drug DB00370
Moxonidine Small molecular drug D0E9PK
Moxonidine Small molecular drug DB09242
Naphazoline Small molecular drug DB06711
Nefazodone Small molecular drug DB01149
Norepinephrine Small molecular drug DB00368
Nortriptyline Small molecular drug DB00540
Oxymetazoline Small molecular drug DB00935
Paliperidone Small molecular drug DB01267
Paroxetine Small molecular drug DB00715
Pergolide Small molecular drug DB01186
Periciazine Small molecular drug DB01608
Phenoxybenzamine Small molecular drug DB00925
Phentolamine Small molecular drug DB00692
Phenylpropanolamine Small molecular drug DB00397
Pizotifen Small molecular drug DB06153
Pramipexole Small molecular drug DB00413
Prazosin Small molecular drug DB00457
Prochlorperazine Small molecular drug DB00433
Promethazine Small molecular drug DB01069
Pseudoephedrine Small molecular drug DB00852
Quetiapine Small molecular drug DB01224
Rilmenidine Small molecular drug DB11738
Ropinirole Small molecular drug DB00268
Tizanidine Small molecular drug DB00697
Tolazoline Small molecular drug DB00797
Tramadol Small molecular drug DB00193
Trazodone Small molecular drug DB00656
Trimipramine Small molecular drug DB00726
Xylometazoline Small molecular drug DB06694
Yohimbine Small molecular drug DB01392
Ziprasidone Small molecular drug DB00246
Zuclopenthixol Small molecular drug DB01624
Aripiprazole Lauroxil . DB14185
Dl-methylephedrine . DB11278
Dosulepin . DB09167
Lorpiprazole . DB09195
Racepinephrine . DB11124
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Medetomidine Small molecular drug D0F2ML
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Dsp-1200 . D0AI8V
Investigative
Click To Hide/Show 77 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(1,2,3,4-tetrahydro-isoquinolin-3-yl)-methanol Small molecular drug D0Y8DJ
(1h-benzoimidazol-5-yl)-(1h-imidazol-2-yl)-amine Small molecular drug D0S4VR
(1h-imidazol-2-yl)-quinoxalin-6-yl-amine Small molecular drug D0ZC4S
(2,6-dichloro-phenyl)-(1h-imidazol-2-yl)-amine Small molecular drug D0A6GK
(2-bromo-phenyl)-(1h-imidazol-2-yl)-amine Small molecular drug D06HHJ
(2-methyl-indol-1-yl)-propyl-pyridin-4-yl-amine Small molecular drug D0W5IN
(3-ethyl-indol-1-yl)-propyl-pyridin-4-yl-amine Small molecular drug D03HBZ
(3-methyl-indol-1-yl)-propyl-pyridin-4-yl-amine Small molecular drug D0P8BE
(R)-3-methyl-1,2,3,4-tetrahydro-isoquinoline Small molecular drug D0E0KG
(S)-3-methyl-1,2,3,4-tetrahydro-isoquinoline Small molecular drug D02KIS
1',2',3',6'-tetrahydro-[2,4bipyridinyl Small molecular drug D08UDY
1,2,3,4,4a,5,10,10a-octahydro-benzo[G]Quinoline Small molecular drug D0P3HP
1,2,3,4,5,6-hexahydro-benzo[C]Azocine Small molecular drug D09JZG
1,2,3,4-tetrahydro-benzo[H]Isoquinolin-8-ol Small molecular drug D04RBQ
1,2,3,4-tetrahydro-isoquinolin-7-ol Small molecular drug D0QO8X
1,2,3,4-tetrahydro-pyrazino[1,2-a]Indole Small molecular drug D0C1SE
1,2,3,4-tetrahydroisoquinoline Small molecular drug D03EPY
1-((S)-2-aminopropyl)-1h-indazol-6-ol Small molecular drug D01KAX
1-(3-fluoro-pyridin-2-yl)-4-methyl-piperazine Small molecular drug D0MH0S
1-(Pyridin-2-yl)Piperazine Small molecular drug D07JMN
2,3,4,5-tetrahydro-1h-benzo[C]Azepine Small molecular drug D0QH0X
2,3,4,5-tetrahydro-1h-benzo[E][1,4]Diazepine Small molecular drug D0V0NJ
2,3,4,5-tetrahydro-benzo[F][1,4]Oxazepine Small molecular drug D0M8FL
2,3-dihydro-1h-isoindole Small molecular drug D07SYG
2-bfi Small molecular drug D0LI3J
3-fluoromethyl-1,2,3,4-tetrahydro-isoquinoline Small molecular drug D0E8HU
3-methoxymethyl-1,2,3,4-tetrahydro-isoquinoline Small molecular drug D0TN2R
3-methyl-1,2,3,4-tetrahydro-isoquinoline Small molecular drug D0Z7XI
3-methyl-7-nitro-1,2,3,4-tetrahydro-isoquinoline Small molecular drug D01SRS
4-(1-naphthalen-1-yl-ethyl)-1h-imidazole Small molecular drug D0P5PW
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Small molecular drug D0T2RY
4-(4-methyl-indan-1-yl)-1h-imidazole Small molecular drug D0L9WN
4-benzo[B]Thiophen-4-yl-1h-imidazole Small molecular drug D0H3NA
5-aminomethyl-naphthalen-2-ol Small molecular drug D07RLW
6,7,8,9-tetrahydro-5-thia-8-aza-benzocycloheptene Small molecular drug D0B2BO
7-methoxy-2,3,4,9-tetrahydro-1h-beta-carboline Small molecular drug D05GDP
7-nitro-1,2,3,4-tetrahydro-isoquinoline Small molecular drug D01SRL
8-methoxy-1,2,3,4-tetrahydro-benzo[H]Isoquinoline Small molecular drug D02QXT
Akuammigine Small molecular drug D03DMN
Ar-129330 Small molecular drug D0K0KR
Beta-methoxyamphetamine Small molecular drug D0R7ZC
Brl 44408 Small molecular drug D08OLL
Butyl-indol-1-yl-pyridin-4-yl-amine Small molecular drug D0AE9M
C-(6-methoxy-naphthalen-1-yl)-methylamine Small molecular drug D03LRY
C-naphthalen-1-yl-methylamine Small molecular drug D08ZRA
Chloroethylclonidine Small molecular drug D05QTJ
Ciproxifan Small molecular drug D0I3XA
Cirazoline Small molecular drug DB09202
Ephedra Sinica Root Small molecular drug DB01363
Ethyl-indol-1-yl-pyridin-4-yl-amine Small molecular drug D0F5TA
Flupirtine Small molecular drug DB06623
Gnf-pf-2857 Small molecular drug D0E3OL
Gnf-pf-3878 Small molecular drug D07ICV
Indol-1-yl-methyl-pyridin-4-yl-amine Small molecular drug D0R1XT
Indol-1-yl-prop-2-ynyl-pyridin-4-yl-amine Small molecular drug D0ZS3M
Indol-1-yl-pyridin-4-yl-amine Small molecular drug D0D1RU
Jp1302 Small molecular drug D0L7IZ
Methylnoradrenaline Small molecular drug D06SYS
Mezilamine Small molecular drug D06BWZ
Ocaperidone Small molecular drug DB06229
Piperoxan Small molecular drug D04PYQ
R-226161 Small molecular drug D0PN9R
S-34324 Small molecular drug D0FU5E
Sk&f-29661 Small molecular drug D0H1WR
Sk&f-64139 Small molecular drug D0C9DC
Snap-5150 Small molecular drug D0V3IT
Tiapride Small molecular drug DB13025
Tracizoline Small molecular drug D09BIV
Tramazoline Small molecular drug D0ZT8D
Tryptoline Small molecular drug D03LPH
[3h]Rx821002 Small molecular drug D08KLH
(+/-)-nantenine . D0L5MW
Aranidipine . DB09229
Epicept Np-1 . DB05492
Esmirtazapine . DB06678
Pipamperone . DB09286
Pirlindole . DB09244
Discontinued
Click To Hide/Show 9 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
4-methoxyamphetamine Small molecular drug DB01472
A-80426 Small molecular drug D0K9JP
Mazapertine Small molecular drug D01WJZ
Sk&f-104078 Small molecular drug D08OWQ
Snap-5089 Small molecular drug D06HRY
Wb-4101 Small molecular drug D03QMR
Etoperidone . DB09194
Nmi-870 . D0ZI0K
S-18616 . D0KC5X

References

1 Tranylcypromine specificity for monoamine oxidase is limited by promiscuous protein labelling and lysosomal trapping. RSC Chem Biol. 2020 Aug 12;1(4):209-213. doi: 10.1039/d0cb00048e. eCollection 2020 Oct 1.
Mass spectrometry data entry: PXD018580
2 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
3 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264