Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTR6W5O)

• DTT Name: Adrenergic receptor beta-1 (ADRB1)
• Synonyms: Beta-1 adrenoreceptor; Beta-1 adrenoceptor; Beta-1 adrenergic receptor; B1AR; ADRB1R
• Gene Name: ADRB1
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: ADRB1_HUMAN
• TTD ID: T44068
• Sequence:
  MGAGVLVLGASEPGNLSSAAPLPDGAATAARLLVPASPPASLLPPASESPEPLSQQWTAG
  MGLLMALIVLLIVAGNVLVIVAIAKTPRLQTLTNLFIMSLASADLVMGLLVVPFGATIVV
  WGRWEYGSFFCELWTSVDVLCVTASIETLCVIALDRYLAITSPFRYQSLLTRARARGLVC
  TVWAISALVSFLPILMHWWRAESDEARRCYNDPKCCDFVTNRAYAIASSVVSFYVPLCIM
  AFVYLRVFREAQKQVKKIDSCERRFLGGPARPPSPSPSPVPAPAPPPGPPRPAAAAATAP
  LANGRAGKRRPSRLVALREQKALKTLGIIMGVFTLCWLPFFLANVVKAFHRELVPDRLFV
  FFNWLGYANSAFNPIIYCRSPDFRKAFQRLLCCARRAARRRHATHGDRPRASGCLARPGP
  PPSPGAASDDDDDDVVGATPPARLLEPWAGCNGGAAADSDSSLDEPCRPGFASESKV
• Function: Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately equal affinity. Mediates Ras activation through G(s)-alpha- and cAMP-mediated signaling.
• KEGG Pathway:
  Calcium signaling pathway (hsa04020)
  cGMP-PKG signaling pathway (hsa04022)
  cAMP signaling pathway (hsa04024)
  Neuroactive ligand-receptor interaction (hsa04080)
  Endocytosis (hsa04144)
  Adrenergic signaling in cardiomyocytes (hsa04261)
  Gap junction (hsa04540)
  Salivary secretion (hsa04970)
  Dilated cardiomyopathy (hsa05414)
• Reactome Pathway:
  G alpha (s) signalling events (R-HSA-418555)
  Adrenoceptors (R-HSA-390696)

Molecular Interaction Atlas (MIA) of This DTT

30 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Acebutolol	DM0TI4U	Hypertension	BA00-BA04	Approved	[2]
Ajmalicine	DMPOD47	Circulatory disorder	BE2Z	Approved	[3]
Anisodamine	DMW51AX	Central and peripheral nervous disease	8A04-8E7Z	Approved	[3]
Anisodine	DMNOSWU	Central and peripheral nervous disease	8A04-8E7Z	Approved	[3]
Arbutamine	DMCY8AF	Coronary artery disease	BA80	Approved	[4]
Atenolol	DMNKG1Z	Angina pectoris	BA40	Approved	[2]
Betaxolol	DM6EUL5	Hypertension	BA00-BA04	Approved	[5]
Bisoprolol	DM3UZ95	Hypertension	BA00-BA04	Approved	[6]
Bretylium	DM1FX74	Long QT syndrome	BC65.0	Approved	[7]
Carteolol	DMFMDOB	Glaucoma/ocular hypertension	9C61	Approved	[8]
Dipivefrin	DMH5W0G	Chronic open-angle glaucoma	9C61.0	Approved	[9]
Dobutamine	DMD1B8Z	Heart failure	BD10-BD13	Approved	[10]
Epinephrine	DM3KJBC	Acute asthma	CA23	Approved	[11]
Esmolol	DM51TYR	Acute supraventricular tachycardia	BC81	Approved	[12]
Isoproterenol	DMK7MEY	Atrioventricular block		Approved	[13]
Levobetaxolol	DMSREPX	Chronic open-angle glaucoma	9C61.0	Approved	[14]
Levobunolol	DMTNFCQ	Ocular hypertension	9C61.01	Approved	[1]
Metipranolol	DMJMVKI	Ocular hypertension	9C61.01	Approved	[15]
Metoprolol	DMOJ0V6	Acute coronary syndrome	BA41	Approved	[2]
Nadolol	DMW6GVL	Angina pectoris	BA40	Approved	[16]
Nebivolol	DM7F1PA	Hypertension	BA00-BA04	Approved	[17]
Norepinephrine	DMOUC09	Alopecia	ED70	Approved	[18]
Oxprenolol	DM51OQW	Anxiety		Approved	[2]
Penbutolol	DM4ES8F	Hypertension	BA00-BA04	Approved	[19]
Pindolol	DMD2NV7	Hypertension	BA00-BA04	Approved	[20]
Practolol	DMGLZ26	Cardiac arrhythmias	BC9Z	Approved	[21]
Propranolol	DM79NTF	Angina pectoris	BA40	Approved	[22]
Protokylol Hydrochloride	DMAHZKR	Asthma	CA23	Approved	[23]
Sotalol	DML60TN	Sinus rhythm disorder	BC9Y	Approved	[24]
Timolol	DM3NXRU	High blood pressure	BA00	Approved	[25]

6 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BUCINDOLOL	DMV52CP	Atrial fibrillation	BC81.3	Phase 2/3	[26]
BRL 35135	DMLFGHX	Diabetic complication	5A2Y	Phase 2	[27]
COR-1	DMER82Z	Heart failure	BD10-BD13	Phase 2	[28]
Galnobax	DMQU4EI	Diabetic foot ulcer	BD54	Phase 1/2	[29]
L-796568	DMXKO1L	Obesity	5B81	Phase 1	[30]
YM-16151-4	DMNLY9R	Hypertension	BA00-BA04	Phase 1	[31]

4 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Alprenolol	DMYJ8Z3	Hypertension	BA00-BA04	Withdrawn from market	[32]
Bethanidine	DMJMHNL	Heart arrhythmia	BC65	Withdrawn from market	[33]
Cetamolol	DMIDFLV	Angina pectoris	BA40	Terminated	[34]
L-755507	DMPWBNU	N. A.	N. A.	Terminated	[35]

12 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(+/-)-nantenine	DM0L3GE	Discovery agent	N.A.	Investigative	[36]
(R,R)-(-)-fenoterol	DM3FQYS	Discovery agent	N.A.	Investigative	[37]
(R,S)-(-)-fenoterol	DMETQBI	Discovery agent	N.A.	Investigative	[37]
1-(1H-Indol-4-yloxy)-3-phenethylamino-propan-2-ol	DMSUPCD	Discovery agent	N.A.	Investigative	[38]
1-(2-allylphenoxy)-3-morpholinopropan-2-ol	DMLV0PQ	Discovery agent	N.A.	Investigative	[39]
1-(2-isopropylphenoxy)-3-morpholinopropan-2-ol	DMK209P	Discovery agent	N.A.	Investigative	[39]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	DMM9X0G	Discovery agent	N.A.	Investigative	[40]
Carazolol	DMEKI1J	Discovery agent	N.A.	Investigative	[13]
Cebutolol	DMUKGEA	Discovery agent	N.A.	Investigative	[13]
CGP 20712A	DML79NU	Discovery agent	N.A.	Investigative	[41]
Dichloroisoproterenol	DMSZ7UE	Discovery agent	N.A.	Investigative	[42]
[3H]CGP12177	DMZN1A3	Discovery agent	N.A.	Investigative	[35]

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