General Information of the Protein
Protein ID
PT01817
Protein Name
Translocator protein
Secondarily
Protein Name
Mitochondrial benzodiazepine receptor
PKBS
Peripheral-type benzodiazepine receptor
Gene Name
TSPO
Secondarily
Gene Name
BZRP
MBR
Sequence
MAPPWVPAMGFTLAPSLGCFVGSRFVHGEGLRWYAGLQKPSWHPPHWVLGPVWGTLYSAMGYGSYLVWKELGGFTEKAVVPLGLYTGQLALNWAWPPIFFGARQMGWALVDLLLVSGAAAATTVAWYQVSPLAARLLYPYLAWLAFTTTLNYCVWRDNHGWRGGRRLPE
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
Function
Can bind protoporphyrin IX and may play a role in the transport of porphyrins and heme (By similarity). Promotes the transport of cholesterol across mitochondrial membranes and may play a role in lipid metabolism (PubMed:24814875), 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 (PubMed:1847678).
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Uniprot ID
Primary ID:
P30536

Secondarily ID:
Q53Y59
Q6ICF9
Q96TF6
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Ensembl ID
ENSG00000100300
HGNC ID
HGNC:1158
Subcellular Location
Mitochondrion membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000025 , HEK-293T
Compound ID Compound Name Compound Formula
CP0570930
N-benzyl-N-ethyl-2-[2-(4-methoxyphenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl]acetamide
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C26H28N4O2
 2
1
Ki = 6.2 nM
   TI
   LI
   LO
   TS
2
Ki = 80.6 nM
   TI
   LI
   LO
   TS
CP0515546
N-benzyl-N-ethyl-2-(7-methyl-8-oxo-2-phenylpurin-9-yl)acetamide
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C23H23N5O2
 2
1
Ki = 6.4 nM
   TI
   LI
   LO
   TS
2
Ki = 31.3 nM
   TI
   LI
   LO
   TS
CP0443260
2-[2-(4'-Methoxyphenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl]-N,N-diethylacetamide
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C21H26N4O2
 3
1
Ki = 8.2 nM
   TI
   LI
   LO
   TS
2
Ki = 19.5 nM
   TI
   LI
   LO
   TS
3
Ki = 98.8 nM
   TI
   LI
   LO
   TS
CP0450928
N-benzyl-2-[2-(4-methoxyphenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl]-N-methylacetamide
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C25H26N4O2
 2
1
Ki = 9.3 nM
   TI
   LI
   LO
   TS
2
Ki = 27.3 nM
   TI
   LI
   LO
   TS
CP0520737
N-benzyl-N-ethyl-2-(6-oxo-5H-benzo[b][1,4]benzodiazepin-11-yl)acetamide
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C24H23N3O2
 2
1
Ki = 15.8 nM
   TI
   LI
   LO
   TS
2
Ki = 99.4 nM
   TI
   LI
   LO
   TS
CP0905654
N,N-Diethyl-2-(3-(2-methoxyphenyl)-9H-carbazol-9-yl)acetamide
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C25H26N2O2
 2
1
Ki = 25.4 nM
   TI
   LI
   LO
   TS
2
Ki = 137.3 nM
   TI
   LI
   LO
   TS
CP0443261
N,N-diethyl-2-[2-(4-methoxyphenyl)-4,6-dimethylindol-1-yl]acetamide
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C23H28N2O2
 1
1
Ki = 28.13 nM
   TI
   LI
   LO
   TS
CP0930152
N,N-Diethyl-2-(3-(4-methoxyphenyl)-9H-carbazole-9-yl)acetamide
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C25H26N2O2
 2
1
Ki = 28.9 nM
   TI
   LI
   LO
   TS
2
Ki = 93.4 nM
   TI
   LI
   LO
   TS
CP0443262
N,N-diethyl-2-[2-(4-methoxyphenyl)-5,7-dimethylimidazo[4,5-b]pyridin-3-yl]acetamide
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C21H26N4O2
 1
1
Ki = 29.11 nM
   TI
   LI
   LO
   TS
CP0003888
1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)isoquinoline-3-carboxamide
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C21H21ClN2O
 2
1
Ki = 29.2 nM
   TI
   LI
   LO
   TS
2
Ki = 36 nM
   TI
   LI
   LO
   TS
CP0444586
2-carbazol-9-yl-N,N-diethylacetamide
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C18H20N2O
 2
1
Ki = 30.1 nM
   TI
   LI
   LO
   TS
2
Ki = 176.6 nM
   TI
   LI
   LO
   TS
CP0926699
2-(3-Bromo-9H-carbazole-9-yl)-N,N-diethylacetamide
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C18H19BrN2O
 2
1
Ki = 31.5 nM
   TI
   LI
   LO
   TS
2
Ki = 160.9 nM
   TI
   LI
   LO
   TS
CP0962322
N,N-Diethyl-2-(3-phenyl-9H-carbazole-9-yl)acetamide
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C24H24N2O
 2
1
Ki = 31.6 nM
   TI
   LI
   LO
   TS
2
Ki = 159.8 nM
   TI
   LI
   LO
   TS
CP0546103
N-benzyl-N-methyl-2-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)acetamide
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C21H23N5O
 2
1
Ki = 41.3 nM
   TI
   LI
   LO
   TS
2
Ki = 199.5 nM
   TI
   LI
   LO
   TS
CP0546104
N-benzyl-N-ethyl-2-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)acetamide
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C22H25N5O
 2
1
Ki = 41.3 nM
   TI
   LI
   LO
   TS
2
Ki = 226.9 nM
   TI
   LI
   LO
   TS
CP0444015
N-benzyl-2-carbazol-9-yl-N-methylacetamide
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C22H20N2O
 2
1
Ki = 53 nM
   TI
   LI
   LO
   TS
2
Ki = 132 nM
   TI
   LI
   LO
   TS
CP0926697
N-Benzyl-2-(3-bromo-9H-carbazol-9-yl)-N-ethylacetamide
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C23H21BrN2O
 2
1
Ki = 54.3 nM
   TI
   LI
   LO
   TS
2
Ki = 123.4 nM
   TI
   LI
   LO
   TS
CP0562032
N-benzyl-N-methyl-2-(6-oxo-5H-benzo[b][1,4]benzodiazepin-11-yl)acetamide
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C23H21N3O2
 2
1
Ki = 76.8 nM
   TI
   LI
   LO
   TS
2
Ki = 159.4 nM
   TI
   LI
   LO
   TS
CP0422965
N-benzyl-2-carbazol-9-yl-N-ethylacetamide
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C23H22N2O
 2
1
Ki = 91.6 nM
   TI
   LI
   LO
   TS
2
Ki = 459.6 nM
   TI
   LI
   LO
   TS
CP0560543
N,N-diethyl-2-(6-oxo-5H-benzo[b][1,4]benzodiazepin-11-yl)acetamide
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C19H21N3O2
 2
1
Ki = 200.5 nM
   TI
   LI
   LO
   TS
2
Ki = 2357.8 nM
   TI
   LI
   LO
   TS
CP0508581
N,N-diethyl-2-[2-(4-methoxyphenyl)-4,6-dimethylbenzimidazol-1-yl]acetamide
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C22H27N3O2
 1
1
Ki = 224.46 nM
   TI
   LI
   LO
   TS
CP0570929
2-[2-(4-methoxyphenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl]-N,N-dimethylacetamide
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C19H22N4O2
 2
1
Ki = 337.9 nM
   TI
   LI
   LO
   TS
2
Ki = 559.8 nM
   TI
   LI
   LO
   TS
CP0520736
N,N-diethyl-2-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)acetamide
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C17H23N5O
 2
1
Ki = 493 nM
   TI
   LI
   LO
   TS
2
Ki = 2256.6 nM
   TI
   LI
   LO
   TS
CP0458452
N,N-diethyl-2-[8-(4-methoxyphenyl)-2,6-dimethylpurin-9-yl]acetamide
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C20H25N5O2
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0444029
N,N-dimethyl-2-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)acetamide
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C15H19N5O
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0444585
2-carbazol-9-yl-N,N-dimethylacetamide
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C16H16N2O
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0570931
N,N-dimethyl-2-(6-oxo-5H-benzo[b][1,4]benzodiazepin-11-yl)acetamide
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C17H17N3O2
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0003888
1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)isoquinoline-3-carboxamide
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C21H21ClN2O
 9
1 Activity = 0.63 nM
2 IC50 = 1.1 nM
3 IC50 = 2.5 nM
4 IC50 = 490 nM
5 Kd = 2 nM
6 Kd = 11.1 nM
7 Ki = 2.3 nM
8 Ki = 4.5 nM
9 Ki = 7.11 nM
CP0142350
2-[6,8-Dichloro-2-(4-chloro-phenyl)-imidazo[1,2-a]pyridin-3-yl]-N,N-dipropyl-acetamide
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C21H22Cl3N3O
 1
1 Ki = 0.41 nM
CP0003889
2-(6,8-Dichloro-2-(4-methoxyphenyl)imidazo[1,2-a]pyridin-3-yl)-N,N-dipropylacetamide
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C22H25Cl2N3O2
 1
1 Ki = 0.537 nM
Clinical Information about the Protein
Target 1 ( Translocator protein (TSPO) )
Target Type Successful Target
Disease 9 Target-related Diseases  9
1 Anxiety disorder [ICD-11: 6B00-6B0Z]
2 Epilepsy [ICD-11: 8A60-8A68]
3 Insomnia [ICD-11: 7A00-7A0Z]
4 Benzodiazepine overdose [ICD-11: PC91]
5 Irritability [ICD-11: MB24]
6 Brain disease [ICD-11: 8C70-8E61]
7 Rheumatoid arthritis [ICD-11: FA20]
8 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
9 Gram-positive bacterial infection [ICD-11: 1B74-1G40]
Approved Drug(s) 17 Approved Drugs  17
1 Adinazolam Approved
Anxiety disorder
2 Alpidem Approved
Anxiety disorder
3 Alprazolam Approved
Anxiety disorder
4 Chlormezanone Approved
Anxiety disorder
5 Diazepam Approved
Epilepsy
6 Estazolam Approved
Insomnia
7 Eszopiclone Approved
Insomnia
8 Flumazenil Approved
Benzodiazepine overdose
9 Flunitrazepam Approved
Insomnia
10 Flurazepam Approved
Insomnia
11 Halazepam Approved
Anxiety disorder
12 Lorazepam Approved
Anxiety disorder
13 Midazolam Approved
Irritability
14 Oxazepam Approved
Anxiety disorder
15 Prazepam Approved
Anxiety disorder
16 Temazepam Approved
Insomnia
17 Triazolam Approved
Insomnia
Clinical Trial Drug(s) 3 Clinical Trial Drugs  3
1 11C-PBR-28 Phase 2
Brain disease
2 SSR-180575 Phase 2
Rheumatoid arthritis
3 TLN-4601 Phase 2
Solid tumour/cancer
Discontinued Drug(s) 4 Discontinued Drugs  4
1 Ro-16-6028 Discontinued in Phase 3
Anxiety disorder
2 Emapunil Discontinued in Phase 2
Anxiety disorder
3 DAA-1097 Terminated
Anxiety disorder
4 Miltirone Terminated
Anxiety disorder
Investigative Drug(s) 1 Investigative Drug  1
1 Ro 5-4864 Investigative
Gram-positive bacterial infection