Details of the Target

General Information of Target

Target ID LDTP02213
Target Name Beta-2 adrenergic receptor (ADRB2)
Gene Name ADRB2
Gene ID 154
Synonyms
ADRB2R; B2AR; Beta-2 adrenergic receptor; Beta-2 adrenoreceptor; Beta-2 adrenoceptor
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGQPGNGSAFLLAPNGSHAPDHDVTQERDEVWVVGMGIVMSLIVLAIVFGNVLVITAIAK
FERLQTVTNYFITSLACADLVMGLAVVPFGAAHILMKMWTFGNFWCEFWTSIDVLCVTAS
IETLCVIAVDRYFAITSPFKYQSLLTKNKARVIILMVWIVSGLTSFLPIQMHWYRATHQE
AINCYANETCCDFFTNQAYAIASSIVSFYVPLVIMVFVYSRVFQEAKRQLQKIDKSEGRF
HVQNLSQVEQDGRTGHGLRRSSKFCLKEHKALKTLGIIMGTFTLCWLPFFIVNIVHVIQD
NLIRKEVYILLNWIGYVNSGFNPLIYCRSPDFRIAFQELLCLRRSSLKAYGNGYSSNGNT
GEQSGYHVEQEKENKLLCEDLPGTEDFVGHQGTVPSDNIDSQGRNCSTNDSLL
Target Type
Successful
Target Bioclass
GPCR
Family
G-protein coupled receptor 1 family, Adrenergic receptor subfamily, ADRB2 sub-subfamily
Subcellular location
Cell membrane
Function
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine.
TTD ID
T52522
Uniprot ID
P07550
DrugMap ID
TT2CJVK
Ensemble ID
ENST00000305988.6
HGNC ID
HGNC:286
ChEMBL ID
CHEMBL210

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
m-APA
 Probe Info  		9.92  LDD0402  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0156  Aniline NCI-H1299 14.83  LDD0403  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Monoglyceride lipase (MGLL) Monoacylglycerol lipase family Q99685
Putative inactive beta-glucuronidase-like protein SMA3 (GUSBP1) Glycosyl hydrolase 2 family Q15486
Proto-oncogene tyrosine-protein kinase Src (SRC) Tyr protein kinase family P12931
E3 ubiquitin-protein ligase RNF138 (RNF138) . Q8WVD3
RING finger protein 208 (RNF208) . Q9H0X6
Transporter and channel
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Arrestin domain-containing protein 3 (ARRDC3) Arrestin family Q96B67
Beta-arrestin-2 (ARRB2) Arrestin family P32121
ATPase inhibitor, mitochondrial (ATP5IF1) ATPase inhibitor family Q9UII2
Na(+)/H(+) exchange regulatory cofactor NHE-RF1 (NHERF1) . O14745
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Transcription factor E2F8 (E2F8) E2F/DP family A0AVK6
GPCR
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Adenosine receptor A1 (ADORA1) G-protein coupled receptor 1 family P30542
Beta-2 adrenergic receptor (ADRB2) G-protein coupled receptor 1 family P07550
Other
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Putative elongation factor 1-delta-like protein (EEF1DP3) EF-1-beta/EF-1-delta family Q658K8
RNA polymerase II elongation factor ELL2 (ELL2) ELL/occludin family O00472
Membrane-associated guanylate kinase, WW and PDZ domain-containing protein 3 (MAGI3) MAGUK family Q5TCQ9
SNW domain-containing protein 1 (SNW1) SNW family Q13573
Heterogeneous nuclear ribonucleoprotein K (HNRNPK) . P61978
Transmembrane protein 61 (TMEM61) . Q8N0U2

The Drug(s) Related To This Target

Approved
Click To Hide/Show 65 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Acebutolol Small molecular drug DB01193
Amiodarone Small molecular drug DB01118
Amphetamine Small molecular drug DB00182
Arbutamine Small molecular drug DB01102
Arformoterol Small molecular drug DB01274
Aripiprazole Small molecular drug DB01238
Asenapine Small molecular drug DB06216
Atenolol Small molecular drug DB00335
Betaxolol Small molecular drug DB00195
Bethanidine Small molecular drug DB00217
Bisoprolol Small molecular drug DB00612
Cabergoline Small molecular drug DB00248
Carteolol Small molecular drug DB00521
Carvedilol Small molecular drug DB01136
Celiprolol Small molecular drug DB04846
Clenbuterol Small molecular drug DB01407
Cryptenamine Small molecular drug DB00785
Desipramine Small molecular drug DB01151
Dipivefrin Small molecular drug DB00449
Dobutamine Small molecular drug DB00841
Droxidopa Small molecular drug DB06262
Ephedrine Small molecular drug DB01364
Epinephrine Small molecular drug DB00668
Fenoterol Small molecular drug DB01288
Formoterol Small molecular drug DB00983
Indacaterol Small molecular drug DB05039
Isoetharine Small molecular drug DB00221
Isoprenaline Small molecular drug DB01064
Labetalol Small molecular drug DB00598
Levobunolol Small molecular drug DB01210
Levosalbutamol Small molecular drug DB13139
Metipranolol Small molecular drug DB01214
Metoprolol Small molecular drug DB00264
Nadolol Small molecular drug DB01203
Nebivolol Small molecular drug DB04861
Norepinephrine Small molecular drug DB00368
Nortriptyline Small molecular drug DB00540
Olanzapine Small molecular drug DB00334
Olodaterol Small molecular drug DB09080
Orciprenaline Small molecular drug DB00816
Oxprenolol Small molecular drug DB01580
Paroxetine Small molecular drug DB00715
Penbutolol Small molecular drug DB01359
Phenoxybenzamine Small molecular drug DB00925
Phenylpropanolamine Small molecular drug DB00397
Pindolol Small molecular drug DB00960
Pirbuterol Small molecular drug DB01291
Procaterol Small molecular drug DB01366
Propafenone Small molecular drug DB01182
Propranolol Small molecular drug DB00571
Pseudoephedrine Small molecular drug DB00852
Ritodrine Small molecular drug DB00867
Salbutamol Small molecular drug DB01001
Salmeterol Small molecular drug DB00938
Sotalol Small molecular drug DB00489
Terbutaline Small molecular drug DB00871
Timolol Small molecular drug DB00373
Trimipramine Small molecular drug DB00726
Vilanterol Small molecular drug DB09082
Dl-methylephedrine . DB11278
Etafedrine . DB11587
Methoxyphenamine . DB13624
Protokylol . DB06814
Racepinephrine . DB11124
Viloxazine . DB09185
Phase 2
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bamosiran Small interfering RNA D4RD0C
Syl-040012 siRNA drug D0Q8LL
Investigative
Click To Hide/Show 16 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Alprenolol Small molecular drug DB00866
Bambuterol Small molecular drug DB01408
Bevantolol Small molecular drug DB01295
Bopindolol Small molecular drug DB08807
Bupranolol Small molecular drug DB08808
Doxofylline Small molecular drug DB09273
Ephedra Sinica Root Small molecular drug DB01363
Putrescine Small molecular drug DB01917
Spermidine Small molecular drug DB03566
Spermine Small molecular drug DB00127
(S)-carazolol . DB07543
Arotinolol . DB09204
Bedoradrine . DB05590
Befunolol . DB09013
Ncx 950 . DB05849
Tulobuterol . DB12248
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bitolterol Small molecular drug DB00901

References

1 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.