Details of the Drug Therapeutic Target (DTT)

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

• DTT Name: Adrenergic receptor alpha-1A (ADRA1A)
• Synonyms: Alpha-adrenergic receptor 1c; Alpha-1C adrenergic receptor; Alpha-1A adrenoreceptor; Alpha-1A adrenoceptor; Alpha-1A adrenergic receptor; Alpha adrenergic receptor 1c; Alpha 1A-adrenoreceptor; Alpha 1A-adrenoceptor; ADRA1C
• Gene Name: ADRA1A
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: ADA1A_HUMAN
• TTD ID: T92609
• Sequence:
  MVFLSGNASDSSNCTQPPAPVNISKAILLGVILGGLILFGVLGNILVILSVACHRHLHSV
  THYYIVNLAVADLLLTSTVLPFSAIFEVLGYWAFGRVFCNIWAAVDVLCCTASIMGLCII
  SIDRYIGVSYPLRYPTIVTQRRGLMALLCVWALSLVISIGPLFGWRQPAPEDETICQINE
  EPGYVLFSALGSFYLPLAIILVMYCRVYVVAKRESRGLKSGLKTDKSDSEQVTLRIHRKN
  APAGGSGMASAKTKTHFSVRLLKFSREKKAAKTLGIVVGCFVLCWLPFFLVMPIGSFFPD
  FKPSETVFKIVFWLGYLNSCINPIIYPCSSQEFKKAFQNVLRIQCLCRKQSSKHALGYTL
  HPPSQAVEGQHKDMVRIPVGSRETFYRISKTDGVCEWKFFSSMPRGSARITVSKDQSSCT
  TARVRSKSFLQVCCCVGPSTPSLDKNHQVPTIKVHTISLSENGEEV
• Function: Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes. This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.
• KEGG Pathway:
  Calcium signaling pathway (hsa04020)
  cGMP-PKG signaling pathway (hsa04022)
  Neuroactive ligand-receptor interaction (hsa04080)
  AMPK signaling pathway (hsa04152)
  Adrenergic signaling in cardiomyocytes (hsa04261)
  Vascular smooth muscle contraction (hsa04270)
  Salivary secretion (hsa04970)
• Reactome Pathway:
  G alpha (q) signalling events (R-HSA-416476)
  G alpha (12/13) signalling events (R-HSA-416482)
  Adrenoceptors (R-HSA-390696)

Molecular Interaction Atlas (MIA) of This DTT

4 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
NAFTOPIDIL	DMQ8R4E	Hypertension	BA00-BA04	Approved	[2]
SILODOSIN	DMJSBT6	Benign prostatic hyperplasia	GA90	Approved	[2]
Tamsulosin	DM5QF9V	Benign prostatic hyperplasia	GA90	Approved	[3]
Xatral	DMLHOA0	Benign prostatic hyperplasia	GA90	Approved	[1]

3 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Besipirdine	DMLVNTA	Cognitive impairment	6D71	Phase 3	[4]
Dutasteride + tamsulosin	DM6P8HU	Benign prostatic hyperplasia	GA90	Phase 3	[5]
MEDETOMIDINE	DMX9Y7V	Pain	MG30-MG3Z	Phase 2	[6]

2 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID30124346-Compound-LDT66	DMJMTNL	Benign prostatic hyperplasia	GA90	Patented	[7]
PMID30124346-Compound-LDT8	DM5MUNG	Benign prostatic hyperplasia	GA90	Patented	[7]

24 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sunepitron	DM6M8ZX	N. A.	N. A.	Discontinued in Phase 3	[8]
TIOSPIRONE	DME5QDP	N. A.	N. A.	Discontinued in Phase 3	[9]
L-771688	DMW8NOH	Prostate disease	GA91	Discontinued in Phase 2	[2]
MAZAPERTINE	DMRHYAU	N. A.	N. A.	Discontinued in Phase 2	[10]
RBx-2258	DM7OD3J	Prostate hyperplasia	GA90	Discontinued in Phase 2	[11]
REC-15-2739	DMX4ZWK	Prostate disease	GA91	Discontinued in Phase 2	[2]
SOU-001	DMPAEK5	Urinary incontinence	MF50.2	Discontinued in Phase 2	[12]
Taprizosin	DMF1VY4	Prostate hyperplasia	GA90	Discontinued in Phase 2	[13]
RS-100975	DM94R8B	Prostate disease	GA91	Discontinued in Phase 1	[14]
SDZ-NVI-085	DMTOH03	Major depressive disorder	6A70.3	Discontinued in Phase 1	[15]
A-131701	DM6CSRU	N. A.	N. A.	Terminated	[2]
A-204176	DMPEJ4O	Stress urinary incontinence	MF50.20	Terminated	[17]
ABANOQUIL	DMDOQCV	N. A.	N. A.	Terminated	[18]
AGN-193080	DMVS6BN	N. A.	N. A.	Terminated	[19]
BMY-7378	DMRHCEG	N. A.	N. A.	Terminated	[20]
KRG-3332	DMXT2SL	Glaucoma/ocular hypertension	9C61	Terminated	[21]
L-757464	DM17S85	Prostate hyperplasia	GA90	Terminated	[22]
NIGULDIPINE	DMSPWMF	N. A.	N. A.	Terminated	[23]
Siramesine	DMB6T7K	N. A.	N. A.	Terminated	[24]
SK&F-104078	DMRADBU	N. A.	N. A.	Terminated	[23]
SK&F-104856	DMN91EK	N. A.	N. A.	Terminated	[23]
SNAP-5089	DMROJEN	Heart arrhythmia	BC65	Terminated	[23]
SNAP-6201	DMNE4TS	N. A.	N. A.	Terminated	[2]
WB-4101	DMQU8B1	N. A.	N. A.	Terminated	[18]

1 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CM-2236	DMP9EJ7	Post-traumatic stress disorder	6B40	Preclinical	[16]

64 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(+/-)-nantenine	DM0L3GE	Discovery agent	N.A.	Investigative	[25]
(-)-SNAP-5399	DMFE3YK	Discovery agent	N.A.	Investigative	[2]
(2,6-Dichloro-phenyl)-(1H-imidazol-2-yl)-amine	DM27TH9	Discovery agent	N.A.	Investigative	[26]
(2-Bromo-phenyl)-(1H-imidazol-2-yl)-amine	DM8N79M	Discovery agent	N.A.	Investigative	[26]
1',2',3',6'-Tetrahydro-[2,4']bipyridinyl	DMFDK4N	Discovery agent	N.A.	Investigative	[27]
1-(2-Chloro-phenyl)-piperazine	DM5RE71	Discovery agent	N.A.	Investigative	[28]
1-(2-Methoxy-phenyl)-piperazine	DM3M4RA	Discovery agent	N.A.	Investigative	[28]
1-(3-Fluoro-pyridin-2-yl)-4-methyl-piperazine	DMWFU3T	Discovery agent	N.A.	Investigative	[27]
1-(pyridin-2-yl)piperazine	DMKE7FG	Discovery agent	N.A.	Investigative	[27]
2-(4-tert-Butyl-phenyl)-4,5-dihydro-1H-imidazole	DM1A4BS	Discovery agent	N.A.	Investigative	[29]
2-Pyridin-4-yl-1,2,3,4-tetrahydro-isoquinoline	DM5D09Q	Discovery agent	N.A.	Investigative	[30]
4-((E)-1-Naphthalen-1-yl-propenyl)-1H-imidazole	DMDOJ4E	Discovery agent	N.A.	Investigative	[31]
4-((Z)-1-Naphthalen-1-yl-propenyl)-1H-imidazole	DM1UK3G	Discovery agent	N.A.	Investigative	[31]
4-(1-Naphthalen-1-yl-ethyl)-1H-imidazole	DMFYBLH	Discovery agent	N.A.	Investigative	[6]
4-(1-Naphthalen-1-yl-propyl)-1H-imidazole	DM64THP	Discovery agent	N.A.	Investigative	[31]
4-(1-Naphthalen-1-yl-vinyl)-1H-imidazole	DM49PR1	Discovery agent	N.A.	Investigative	[31]
4-(2,3-Dihydro-1H-phenalen-1-yl)-1H-imidazole	DMVIQ7F	Discovery agent	N.A.	Investigative	[31]
4-(3,4-Dihydro-1H-isoquinolin-2-yl)-quinoline	DMCOJIL	Discovery agent	N.A.	Investigative	[30]
4-(3-Hydroxy-piperidin-3-yl)-benzene-1,2-diol	DMUQWJZ	Discovery agent	N.A.	Investigative	[32]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	DMM9X0G	Discovery agent	N.A.	Investigative	[33]
4-(4-chlorobenzyl)-2-allylphthalazin-1(2H)-one	DMRBEZD	Discovery agent	N.A.	Investigative	[34]
4-(4-chlorobenzyl)-2-methylphthalazin-1(2H)-one	DMNYQGV	Discovery agent	N.A.	Investigative	[34]
4-(4-chlorobenzyl)phthalazin-1(2H)-one	DM9AEF0	Discovery agent	N.A.	Investigative	[34]
4-(4-Isopropyl-morpholin-2-yl)-benzene-1,2-diol	DMC9Z45	Discovery agent	N.A.	Investigative	[32]
4-(4-Methyl-indan-1-yl)-1H-imidazole	DMYZHXR	Discovery agent	N.A.	Investigative	[35]
4-Benzo[b]thiophen-4-yl-1H-imidazole	DM02Q8N	Discovery agent	N.A.	Investigative	[36]
4-benzyl-2-methylphthalazin-1(2H)-one	DM8MVU4	Discovery agent	N.A.	Investigative	[34]
4-Morpholin-2-yl-benzene-1,2-diol	DM049QO	Discovery agent	N.A.	Investigative	[32]
5-Bromo-8-piperazin-1-yl-imidazo[1,2-a]pyrazine	DMSVCJM	Discovery agent	N.A.	Investigative	[37]
8-Piperazin-1-yl-imidazo[1,2-a]pyrazine	DM958EN	Discovery agent	N.A.	Investigative	[37]
A-119637	DM1DWRN	Discovery agent	N.A.	Investigative	[2]
A-123189	DMZ51UJ	Discovery agent	N.A.	Investigative	[2]
A-315456	DMV8MKP	Discovery agent	N.A.	Investigative	[2]
AGN-192172	DM946RA	Discovery agent	N.A.	Investigative	[19]
Beta-methoxyamphetamine	DMA9CSG	Discovery agent	N.A.	Investigative	[38]
CORYNANTHEINE	DM18CUZ	Discovery agent	N.A.	Investigative	[2]
FLUANISONE	DMQSDM7	Discovery agent	N.A.	Investigative	[39]
GG-818	DMU82JV	Prostate disease	GA91	Investigative	[40]
Imidazolidin-2-ylidene-o-tolyl-amine	DMTGRAF	Discovery agent	N.A.	Investigative	[19]
Imidazolidin-2-ylidene-quinoxalin-6-yl-amine	DMZ5ISH	Discovery agent	N.A.	Investigative	[19]
ISOCLOZAPINE	DM52CPU	Discovery agent	N.A.	Investigative	[41]
L-765314	DMH0TUZ	Discovery agent	N.A.	Investigative	[2]
LEVONORDEFRIN	DMWDJ0H	Discovery agent	N.A.	Investigative	[31]
N-(5-Bromo-quinoxalin-6-yl)-guanidine	DMD5E8G	Discovery agent	N.A.	Investigative	[19]
OCTOCLOTHEPIN	DM0UADK	Discovery agent	N.A.	Investigative	[42]
R-226161	DM4BP7S	Discovery agent	N.A.	Investigative	[43]
REC2615	DMJ0FCG	Female sexual arousal dysfunction	HA01.1	Investigative	[44]
Ro-11-04253	DMOQ0CE	Discovery agent	N.A.	Investigative	[2]
RS-100329	DMDKC0J	Discovery agent	N.A.	Investigative	[2]
RS-513815	DMLI5U2	Discovery agent	N.A.	Investigative	[2]
RWJ-38063	DMPJTLM	Discovery agent	N.A.	Investigative	[2]
RWJ-68141	DMUZW80	Discovery agent	N.A.	Investigative	[2]
RWJ-68157	DMUK7LX	Discovery agent	N.A.	Investigative	[2]
RWJ-69736	DM2EOBM	Discovery agent	N.A.	Investigative	[2]
SK&F-105854	DMYRKEJ	Discovery agent	N.A.	Investigative	[2]
SK&F-106686	DMHETY7	Discovery agent	N.A.	Investigative	[23]
SK&F-86466	DM4RHEZ	Discovery agent	N.A.	Investigative	[23]
SNAP-5036	DMEJ5CP	Discovery agent	N.A.	Investigative	[2]
SNAP-7915	DM3KN2F	Discovery agent	N.A.	Investigative	[2]
SNAP-8719	DMCHPMA	Discovery agent	N.A.	Investigative	[20]
SNAP-94847	DMMHQDX	Discovery agent	N.A.	Investigative	[45]
UH-301	DM5NYWV	N. A.	N. A.	Investigative	[46]
[3H]RX821002	DM6IRN4	Discovery agent	N.A.	Investigative	[47]
[3H]spiperone	DMWHEV8	Discovery agent	N.A.	Investigative	[2]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Prostate cancer	2C82	Prostate	2.24E-04	0.45	0.83
Major depressive disorder	6A20	Pre-frontal cortex	9.43E-01	-0.03	-0.25

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