Details of the Drug Therapeutic Target (DTT)

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

• DTT Name: Translocator protein (TSPO)
• Synonyms: Peripheral-type benzodiazepine receptor; Peripheral benzodiazepine receptor; PKBS; PBR; Mitochondrial benzodiazepine receptor; MBR; BZRP
• Gene Name: TSPO
• DTT Type: Successful target; [1]
• BioChemical Class: Cholesterol/porphyrin uptake translocator
• UniProt ID: TSPO_HUMAN
• TTD ID: T75440
• Sequence:
  MAPPWVPAMGFTLAPSLGCFVGSRFVHGEGLRWYAGLQKPSWHPPHWVLGPVWGTLYSAM
  GYGSYLVWKELGGFTEKAVVPLGLYTGQLALNWAWPPIFFGARQMGWALVDLLLVSGAAA
  ATTVAWYQVSPLAARLLYPYLAWLAFTTTLNYCVWRDNHGWRGGRRLPE
• Function: Promotes the transport of cholesterol across mitochondrial membranes and may play a role in lipid metabolism, but its precise physiological role is controversial. It is apparently not required for steroid hormone biosynthesis. Was initially identified as peripheral-type benzodiazepine receptor; can also bind isoquinoline carboxamides. Can bind protoporphyrin IX and may play a role in the transport of porphyrins and heme.
• KEGG Pathway:
  Neuroactive ligand-receptor interaction (hsa04080)
  HTLV-I infection (hsa05166)
• Reactome Pathway: Pregnenolone biosynthesis (R-HSA-196108)

Molecular Interaction Atlas (MIA) of This DTT

23 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Adinazolam	DMBHO9Y	Anxiety disorder	6B00-6B0Z	Approved	[2]
Alpidem	DMN7Y9K	Anxiety disorder	6B00-6B0Z	Approved	[3]
Alprazolam	DMC7XDN	Anxiety		Approved	[1]
Chlordiazepoxide	DMTN5XI	Alcohol withdrawal		Approved	[4]
Chlormezanone	DMTWUXR	Anxiety disorder	6B00-6B0Z	Approved	[5]
Cinolazepam	DMDX1ZC	Muscle spasm	MB47.3	Approved	[6]
Clorazepate	DMC3JST	Alcohol withdrawal		Approved	[4]
Clotiazepam	DM59AZT	Anxiety disorder	6B00-6B0Z	Approved	[7]
Diazepam	DM08E9O	Alcohol withdrawal		Approved	[8]
Estazolam	DMZGXUM	Insomnia	7A00-7A0Z	Approved	[9]
Eszopiclone	DM8RZ9H	Insomnia	7A00-7A0Z	Approved	[10]
Fludiazepam	DMD2K4I	Anxiety disorder	6B00-6B0Z	Approved	[11]
Flumazenil	DMPCG2L	Benzodiazepine overdose	PC91	Approved	[12]
Flunitrazepam	DMGR5Z3	Insomnia	7A00-7A0Z	Approved	[1]
Flurazepam	DMAL4G0	Insomnia	7A00-7A0Z	Approved	[4]
Halazepam	DMPFWO6	Anxiety disorder	6B00-6B0Z	Approved	[4]
Lorazepam	DM84ZXF	Absence epilepsy		Approved	[4]
Midazolam	DMXOELT	Agitation	6A70.3	Approved	[4]
Oxazepam	DMXNZM4	Alcohol withdrawal delirium		Approved	[13]
Prazepam	DMEWC7N	Anxiety		Approved	[4]
Quazepam	DMY4D87	Insomnia	7A00-7A0Z	Approved	[4]
Temazepam	DM02A65	Insomnia	7A00-7A0Z	Approved	[4]
Triazolam	DMETYK5	Insomnia	7A00-7A0Z	Approved	[4]

7 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
11C-PBR-28	DMSLMY7	Brain disease	8C70-8E61	Phase 2	[14]
Dextofisopam	DM9L15R	Irritable bowel syndrome	DD91.0	Phase 2	[15]
ONO-2952	DMOGYQ0	Irritable bowel syndrome	DD91.0	Phase 2	[16]
SSR-180575	DMA0QZH	Rheumatoid arthritis	FA20	Phase 2	[17]
TLN-4601	DMVXLQ7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[18]
18F-FEDAA-1106	DMZ5YMX	Alzheimer disease	8A20	Phase 1	[19]
BAY-85-8102	DMOUVE7	Brain disease	8C70-8E61	Phase 1	[12]

93 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Aryl oxyanilide derivative 1	DML1IXV	N. A.	N. A.	Patented	[20]
Aryl oxyanilide derivative 2	DM47V3I	N. A.	N. A.	Patented	[20]
Aryl oxyanilide derivative 3	DMSGO7D	N. A.	N. A.	Patented	[20]
Benzimidazolone acetamide derivative 1	DMRZELF	N. A.	N. A.	Patented	[20]
Benzimidazolone acetamide derivative 2	DMD9VC1	N. A.	N. A.	Patented	[20]
Benzodiazepine derivative 1	DMFXC5L	N. A.	N. A.	Patented	[20]
Benzothiazepine analog 1	DM9FPK1	N. A.	N. A.	Patented	[20]
Benzothiazepine analog 2	DMZ3NSJ	N. A.	N. A.	Patented	[20]
Benzothiazepine analog 3	DM24NZG	N. A.	N. A.	Patented	[20]
Benzothiazepine analog 4	DMV4OTD	N. A.	N. A.	Patented	[20]
Benzothiazepine analog 5	DMCH1WX	N. A.	N. A.	Patented	[20]
Benzothiazepine analog 6	DMB5KLD	N. A.	N. A.	Patented	[20]
Benzothiazepine analog 7	DM25ZY4	N. A.	N. A.	Patented	[20]
Benzothiazepine analog 8	DMAXDV5	N. A.	N. A.	Patented	[20]
Benzothiazepine analog 9	DMONDMG	N. A.	N. A.	Patented	[20]
Benzoxazepine analog 1	DMIYXS8	N. A.	N. A.	Patented	[20]
Bidentate pyrazolopyrimidine acetamide analog 1	DMPWKAH	N. A.	N. A.	Patented	[20]
Bidentate pyrazolopyrimidine acetamide analog 2	DM6SPTJ	N. A.	N. A.	Patented	[20]
Bidentate pyrazolopyrimidine acetamide analog 3	DMC7UHT	N. A.	N. A.	Patented	[20]
Bidentate pyrazolopyrimidine acetamide analog 4	DMKZLCQ	N. A.	N. A.	Patented	[20]
Imidazopyridine acetamide analog 1	DMO41ZB	N. A.	N. A.	Patented	[20]
Imidazopyridine acetamide analog 2	DMIKMBO	N. A.	N. A.	Patented	[20]
Imidazopyridine acetamide analog 3	DMZ08LD	N. A.	N. A.	Patented	[20]
Imidazopyridine acetamide analog 4	DMPHK87	N. A.	N. A.	Patented	[20]
Imidazopyridine acetamide analog 5	DMMFCRU	N. A.	N. A.	Patented	[20]
Imidazopyridine acetamide analog 6	DME7M5R	N. A.	N. A.	Patented	[20]
Imidazopyridine acetamide analog 7	DMQDA3I	N. A.	N. A.	Patented	[20]
Imidazopyridine derivative 1	DM8EB57	N. A.	N. A.	Patented	[20]
Imidazopyridine derivative 2	DM9FRV7	N. A.	N. A.	Patented	[20]
Imidazo[1,2-b]pyridazine acetamide derivative 1	DM654Z0	N. A.	N. A.	Patented	[20]
Imidazo[1,2-b]pyridazine acetamide derivative 2	DMVX7YB	N. A.	N. A.	Patented	[20]
Imidazo[1,2-b]pyridazine acetamide derivative 3	DMARLZ6	N. A.	N. A.	Patented	[20]
Imidazo[1,2-b]pyridazine acetamide derivative 4	DM5J09E	N. A.	N. A.	Patented	[20]
Imidazo[1,2-b]pyridazine acetamide derivative 5	DMGWYJR	N. A.	N. A.	Patented	[20]
Imidazo[1,2-b]pyridazine acetamide derivative 6	DM73ESA	N. A.	N. A.	Patented	[20]
Imidazo[1,2-b]pyridazine acetamide derivative 7	DMQLJU2	N. A.	N. A.	Patented	[20]
Indole-based analog 10	DMAM6YC	N. A.	N. A.	Patented	[21]
Indole-based analog 5	DM5JUR2	N. A.	N. A.	Patented	[21]
Indole-based analog 9	DMFI2H6	N. A.	N. A.	Patented	[21]
Iodophenyl-N-methyl-N-fluoroalkyl-3-isoquinoline carboxamide derivative 1	DMI3YO7	N. A.	N. A.	Patented	[20]
Iodophenyl-N-methyl-N-fluoroalkyl-3-isoquinoline carboxamide derivative 2	DM8LNXQ	N. A.	N. A.	Patented	[20]
Iodophenyl-N-methyl-N-fluoroalkyl-3-isoquinoline carboxamide derivative 3	DM39H1F	N. A.	N. A.	Patented	[20]
Isoquinoline carboxamide derivative 1	DMOAY3Q	N. A.	N. A.	Patented	[20]
Phenylpurine acetamide analog 1	DMLSWKR	N. A.	N. A.	Patented	[20]
Phenylpurine acetamide analog 2	DMMGBLC	N. A.	N. A.	Patented	[20]
PMID27599163-Compound-52	DM5KARO	N. A.	N. A.	Patented	[21]
PMID27599163-Compound-75	DMYCQR4	N. A.	N. A.	Patented	[21]
PMID27599163-Compound-76	DMODPFU	N. A.	N. A.	Patented	[21]
PMID27599163-Compound-77	DM2TNH4	N. A.	N. A.	Patented	[21]
PMID27599163-Compound-78	DMZC58R	N. A.	N. A.	Patented	[21]
PMID27599163-Compound-79	DMVUWYB	N. A.	N. A.	Patented	[21]
PMID27599163-Compound-81	DMZ5QC4	N. A.	N. A.	Patented	[21]
PMID27599163-Compound-82	DMO74I9	N. A.	N. A.	Patented	[21]
PMID27607364-Compound-10	DM5RBFC	N. A.	N. A.	Patented	[20]
PMID27607364-Compound-141	DMMF4XO	N. A.	N. A.	Patented	[20]
PMID27607364-Compound-162	DM0F6VU	N. A.	N. A.	Patented	[20]
PMID27607364-Compound-4	DMKBZDP	N. A.	N. A.	Patented	[20]
PMID27607364-Compound-58	DMXJVW4	N. A.	N. A.	Patented	[20]
PMID27607364-Compound-59	DMLY7I3	N. A.	N. A.	Patented	[20]
PMID27607364-Compound-60	DM584EP	N. A.	N. A.	Patented	[20]
PMID27607364-Compound-61	DMWE6NZ	N. A.	N. A.	Patented	[20]
PMID27607364-Compound-62	DMXGT2A	N. A.	N. A.	Patented	[20]
PMID27607364-Compound-63	DMVTPHY	N. A.	N. A.	Patented	[20]
PMID27607364-Compound-64	DMZSI15	N. A.	N. A.	Patented	[20]
PMID27607364-Compound-65	DM9NEFG	N. A.	N. A.	Patented	[20]
Pyrazolopyrimidine acetamide analog 1	DMRAS8L	N. A.	N. A.	Patented	[20]
Pyrazolopyrimidine acetamide analog 2	DMK7F3A	N. A.	N. A.	Patented	[20]
Quinazoline derivative 2	DMGECO2	N. A.	N. A.	Patented	[20]
Quinazoline derivative 3	DMF05GL	N. A.	N. A.	Patented	[20]
Quinazoline derivative 4	DMJIDLU	N. A.	N. A.	Patented	[20]
Quinazoline derivative 5	DMEIH73	N. A.	N. A.	Patented	[20]
Quinazoline derivative 6	DMKZ6MD	N. A.	N. A.	Patented	[20]
Quinazoline derivative 7	DMIBRE5	N. A.	N. A.	Patented	[20]
Quinoline carboxamide derivative 10	DMZTQVF	N. A.	N. A.	Patented	[20]
Quinoline carboxamide derivative 4	DMVUNYD	N. A.	N. A.	Patented	[20]
Quinoline carboxamide derivative 5	DM14029	N. A.	N. A.	Patented	[20]
Quinoline carboxamide derivative 6	DMQ9ATN	N. A.	N. A.	Patented	[20]
Quinoline carboxamide derivative 7	DM8AG0Z	N. A.	N. A.	Patented	[20]
Quinoline carboxamide derivative 8	DM3IXYL	N. A.	N. A.	Patented	[20]
Quinoline carboxamide derivative 9	DM7YFBT	N. A.	N. A.	Patented	[20]
Tricyclic indole compound 1	DM4HBWU	N. A.	N. A.	Patented	[21]
Tricyclic indole compound 10	DMK1QTH	N. A.	N. A.	Patented	[21]
Tricyclic indole compound 11	DML724H	N. A.	N. A.	Patented	[21]
Tricyclic indole compound 12	DMEZQ29	N. A.	N. A.	Patented	[21]
Tricyclic indole compound 14	DMXVNSR	N. A.	N. A.	Patented	[21]
Tricyclic indole compound 2	DMHRY63	N. A.	N. A.	Patented	[21]
Tricyclic indole compound 3	DM5B92W	N. A.	N. A.	Patented	[21]
Tricyclic indole compound 4	DMUZ4L3	N. A.	N. A.	Patented	[21]
Tricyclic indole compound 5	DMX5YG9	N. A.	N. A.	Patented	[21]
Tricyclic indole compound 6	DMXAS8P	N. A.	N. A.	Patented	[21]
Tricyclic indole compound 7	DMFQSU8	N. A.	N. A.	Patented	[21]
Tricyclic indole compound 8	DMYAUVM	N. A.	N. A.	Patented	[21]
Tricyclic indole compound 9	DMVA7BC	N. A.	N. A.	Patented	[21]

11 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ro-16-6028	DM8M1X0	Anxiety disorder	6B00-6B0Z	Discontinued in Phase 3	[22]
Emapunil	DM0RXCK	Anxiety disorder	6B00-6B0Z	Discontinued in Phase 2	[23]
Lirequinil	DM5ENKG	Anxiety disorder	6B00-6B0Z	Discontinued in Phase 2	[24]
S-8510	DM9BEDL	Cognitive impairment	6D71	Discontinued in Phase 2	[25]
TRO-40303	DMZ98Y4	Lateral sclerosis	8B61	Discontinued in Phase 2	[26]
Imepitoin	DM8OYZB	Convulsion	8A68.Z	Discontinued in Phase 1	[27]
DAA-1097	DM3LJK5	Anxiety disorder	6B00-6B0Z	Terminated	[28]
Ginkgolide B (GKB)	DMX0N9P	N. A.	N. A.	Terminated	[29]
Miltirone	DMZNWAV	Anxiety disorder	6B00-6B0Z	Terminated	[30]
NNC-13-8119	DMMOAN0	Anxiety disorder	6B00-6B0Z	Terminated	[31]
NS-2979	DM19OGY	Pain	MG30-MG3Z	Terminated	[32]

17 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(R)PK-11195	DM03N5V	Discovery agent	N.A.	Investigative	[33]
11C-PBR-170	DMYGE3K	Discovery agent	N.A.	Investigative	[12]
2-(2-Phenyl-1H-indol-3-yl)-N,N-dipropyl-acetamide	DM1K0U5	Discovery agent	N.A.	Investigative	[34]
4-Methoxy-5-phenyl-6-thia-10b-aza-benzo[e]azulene	DMID40H	Discovery agent	N.A.	Investigative	[35]
5-Phenyl-6-thia-10b-aza-benzo[e]azulen-4-one	DMLK2VT	Discovery agent	N.A.	Investigative	[36]
5-Phenyl-6-thia-10b-aza-benzo[e]azulene	DMUBCVL	Discovery agent	N.A.	Investigative	[35]
6-Thia-10b-aza-benzo[e]azulen-4-one	DMVGC7H	Discovery agent	N.A.	Investigative	[36]
Benzodiazepine	DM9H34M	Anxiety disorder	6B00-6B0Z	Investigative	[12]
FGIN-1-27	DM4T5DY	Discovery agent	N.A.	Investigative	[37]
N,N-Diethyl-2-(2-phenyl-1H-indol-3-yl)-acetamide	DMBFASY	Discovery agent	N.A.	Investigative	[34]
N,N-Dihexyl-2-(2-phenyl-1H-indol-3-yl)-acetamide	DMV8QTR	Discovery agent	N.A.	Investigative	[34]
N,N-Dimethyl-2-(2-phenyl-1H-indol-3-yl)-acetamide	DM73PXI	Discovery agent	N.A.	Investigative	[34]
N-Hexyl-2-(2-phenyl-1H-indol-3-yl)-acetamide	DMM0F2G	Discovery agent	N.A.	Investigative	[34]
PK 11195	DMDOZPU	Discovery agent	N.A.	Investigative	[37]
Ro 5-4864	DMTQP0K	Gram-positive bacterial infection	1B74-1G40	Investigative	[37]
TGSC01AA(4)	DM1BVW3	Anxiety disorder	6B00-6B0Z	Investigative	[12]
U-89854	DMI6VAX	Anxiety disorder	6B00-6B0Z	Investigative	[12]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Rheumatoid arthritis	FA20	Synovial tissue	2.65E-05	1.98	4.26
Irritable bowel syndrome	DD91.0	Rectal colon tissue	1.60E-01	-0.64	-0.84
Alzheimer's disease	8A00.0	Entorhinal cortex	3.93E-10	0.43	1.02
Lateral sclerosis	8A00.0	Cervical spinal cord	7.49E-01	-0.14	-0.32

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