Page last updated: 2024-08-07 16:01:54
Translocator protein
A protein that is a translation product of the Tspo gene in rat. [PRO:DNx, UniProtKB:P16257]
Synonyms
Mitochondrial benzodiazepine receptor;
PKBS;
Peripheral-type benzodiazepine receptor;
PBR
Research
Bioassay Publications (50)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 1 (2.00) | 18.7374 |
| 1990's | 14 (28.00) | 18.2507 |
| 2000's | 15 (30.00) | 29.6817 |
| 2010's | 18 (36.00) | 24.3611 |
| 2020's | 2 (4.00) | 2.80 |
Compounds (65)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 8-hydroxy-2-(di-n-propylamino)tetralin | Rattus norvegicus (Norway rat) | Ki | 0.0043 | 1 | 1 |
| pk 11195 | Rattus norvegicus (Norway rat) | IC50 | 0.0030 | 11 | 12 |
| pk 11195 | Rattus norvegicus (Norway rat) | Ki | 0.0050 | 13 | 13 |
| ro 5-4864 | Rattus norvegicus (Norway rat) | IC50 | 0.0340 | 2 | 2 |
| ro 5-4864 | Rattus norvegicus (Norway rat) | Ki | 0.0190 | 8 | 8 |
| acetazolamide | Rattus norvegicus (Norway rat) | Ki | 0.5780 | 1 | 1 |
| chlordiazepoxide | Rattus norvegicus (Norway rat) | Ki | 0.4380 | 1 | 1 |
| diazepam | Rattus norvegicus (Norway rat) | Ki | 0.0049 | 1 | 1 |
| ethoxzolamide | Rattus norvegicus (Norway rat) | Ki | 0.8400 | 1 | 1 |
| ketoconazole | Rattus norvegicus (Norway rat) | IC50 | 3.7600 | 1 | 1 |
| midazolam | Rattus norvegicus (Norway rat) | Ki | 0.0020 | 1 | 1 |
| zolpidem | Rattus norvegicus (Norway rat) | IC50 | 4.7000 | 1 | 1 |
| zonisamide | Rattus norvegicus (Norway rat) | Ki | 38.4500 | 1 | 1 |
| veratrole | Rattus norvegicus (Norway rat) | Ki | 14.3200 | 1 | 1 |
| benzenesulfonamide | Rattus norvegicus (Norway rat) | Ki | 1.1200 | 1 | 1 |
| indopan | Rattus norvegicus (Norway rat) | Ki | 1.1245 | 1 | 2 |
| 2-methylcyclohexanone | Rattus norvegicus (Norway rat) | Ki | 8.9300 | 1 | 1 |
| alpidem | Rattus norvegicus (Norway rat) | IC50 | 0.0074 | 2 | 2 |
| alpidem | Rattus norvegicus (Norway rat) | Ki | 0.0040 | 4 | 4 |
| norharman | Rattus norvegicus (Norway rat) | IC50 | 1.6218 | 1 | 1 |
| 1-benzylimidazole | Rattus norvegicus (Norway rat) | IC50 | 154.2000 | 1 | 1 |
| nicotine | Rattus norvegicus (Norway rat) | Ki | 0.5063 | 2 | 4 |
| n,n-dipropyl-2-aminotetralin | Rattus norvegicus (Norway rat) | Ki | 0.0370 | 1 | 1 |
| 2,5-dihydro-2-(4-methoxyphenyl)-3h-pyrazolo(4,3-c)quinolin-3-one | Rattus norvegicus (Norway rat) | IC50 | 0.0001 | 1 | 1 |
| lobeline | Rattus norvegicus (Norway rat) | Ki | 3.9741 | 2 | 4 |
| beta-carboline-3-carboxylic acid ethyl ester | Rattus norvegicus (Norway rat) | IC50 | 0.0050 | 1 | 1 |
| beta-carboline-3-carboxylic acid methyl ester | Rattus norvegicus (Norway rat) | IC50 | 0.0050 | 1 | 1 |
| 3-ethoxy-beta-carboline | Rattus norvegicus (Norway rat) | IC50 | 0.0240 | 1 | 1 |
| tert-butyl beta-carboline-3-carboxylate | Rattus norvegicus (Norway rat) | IC50 | 0.0100 | 1 | 1 |
| n,n-di-n-hexyl-2-(4-fluorophenyl)indole-3-acetamide | Rattus norvegicus (Norway rat) | IC50 | 0.0100 | 1 | 1 |
| n,n-di-n-hexyl-2-(4-fluorophenyl)indole-3-acetamide | Rattus norvegicus (Norway rat) | Ki | 0.0047 | 2 | 2 |
| isofagomine | Rattus norvegicus (Norway rat) | Ki | 5.2000 | 1 | 1 |
| tropacocaine | Rattus norvegicus (Norway rat) | Ki | 23.7359 | 2 | 4 |
| 2-(4-chlorophenyl)-4-(ethylthio)-6-(1-pyrrolidinyl)pyrimidine | Rattus norvegicus (Norway rat) | IC50 | 10.0000 | 1 | 0 |
| 4-methoxy-6-phenyl-1H-pyrimidine-2-thione | Rattus norvegicus (Norway rat) | IC50 | 10.0000 | 1 | 0 |
| orlistat | Rattus norvegicus (Norway rat) | IC50 | 1.0000 | 1 | 1 |
| 2-(dichloromethyl)-4-(4-methylphenyl)-6-(methylthio)-1,3,5-triazine | Rattus norvegicus (Norway rat) | IC50 | 4.0400 | 1 | 0 |
| 3-propoxy-beta-carboline | Rattus norvegicus (Norway rat) | IC50 | 0.0110 | 1 | 1 |
| sq 109 | Rattus norvegicus (Norway rat) | Ki | 0.3600 | 1 | 1 |
| harman | Rattus norvegicus (Norway rat) | IC50 | 12.3880 | 1 | 1 |
| 1-Ethyl-9H-pyrido[3,4-b]indole | Rattus norvegicus (Norway rat) | IC50 | 250.0350 | 1 | 1 |
| su 11248 | Rattus norvegicus (Norway rat) | IC50 | 0.0390 | 1 | 2 |
| cb 34 | Rattus norvegicus (Norway rat) | IC50 | 0.0200 | 1 | 1 |
| 8-hydroxy-2-(di-n-propylamino)tetralin, (r)-isomer | Rattus norvegicus (Norway rat) | Ki | 0.0013 | 1 | 1 |
| n-(2-methoxybenzyl)-n-(4-phenoxypyridin-3-yl)acetamide | Rattus norvegicus (Norway rat) | Ki | 0.0007 | 1 | 1 |
| 3-(5-pyridin-2-yl-2h-tetrazol-2-yl)benzonitrile | Rattus norvegicus (Norway rat) | Ki | 0.1860 | 1 | 1 |
| 4-phenoxyphenoxyethyl thiocyanate | Rattus norvegicus (Norway rat) | Ki | 1.5000 | 1 | 1 |
| 3-fluoro-5-(5-pyridin-2-yl-2h-tetrazol-2-yl)benzonitrile | Rattus norvegicus (Norway rat) | Ki | 0.0140 | 1 | 1 |
| daa 1106 | Rattus norvegicus (Norway rat) | IC50 | 0.0016 | 1 | 1 |
| daa 1106 | Rattus norvegicus (Norway rat) | Ki | 0.0003 | 2 | 2 |
| dpa-713 | Rattus norvegicus (Norway rat) | Ki | 0.0122 | 1 | 1 |
| omdm 169 | Rattus norvegicus (Norway rat) | IC50 | 2.8000 | 1 | 1 |
| raltegravir potassium | Rattus norvegicus (Norway rat) | IC50 | 0.1300 | 1 | 1 |
| pf 04457845 | Rattus norvegicus (Norway rat) | Ki | 1.1441 | 1 | 0 |
| dpa 714 | Rattus norvegicus (Norway rat) | Ki | 0.0084 | 2 | 2 |
| 2-(methylthio)-4-phenyl-6-propan-2-yl-1,3,5-triazine | Rattus norvegicus (Norway rat) | IC50 | 10.0000 | 1 | 0 |
| n-fluoroacetyl-n-(2,5-dimethoxybenzyl)-2-phenoxyaniline | Rattus norvegicus (Norway rat) | Ki | 0.0002 | 2 | 2 |
| mk-7246 | Rattus norvegicus (Norway rat) | Ki | 1.1185 | 1 | 0 |
| n,n-diallyl-5-methoxytryptamine | Rattus norvegicus (Norway rat) | Ki | 0.6775 | 1 | 2 |
| cfi-400945 | Rattus norvegicus (Norway rat) | Ki | 0.0003 | 1 | 1 |
| a-1155463 | Rattus norvegicus (Norway rat) | Ki | 0.7941 | 1 | 0 |
| 2-(ethylthio)-6-phenyl-1H-pyrimidin-4-one | Rattus norvegicus (Norway rat) | IC50 | 10.0000 | 1 | 0 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| diazepam | Rattus norvegicus (Norway rat) | Activity | 0.0030 | 1 | 1 |
The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities.Journal of medicinal chemistry, , 04-08, Volume: 64, Issue:7, 2021
An update into the medicinal chemistry of translocator protein (TSPO) ligands.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO).European journal of medicinal chemistry, , Mar-26, Volume: 93, 2015
Deepening the Topology of the Translocator Protein Binding Site by Novel N,N-Dialkyl-2-arylindol-3-ylglyoxylamides.Journal of medicinal chemistry, , Aug-13, Volume: 58, Issue:15, 2015
Synthesis, Characterization, and in Vitro Evaluation of a New TSPO-Selective Bifunctional Chelate Ligand.ACS medicinal chemistry letters, , Jun-12, Volume: 5, Issue:6, 2014
Exploration of the structure-activity relationship of the diaryl anilide class of ligands for translocator protein--potential novel positron emitting tomography imaging agents.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 22, Issue:18, 2012
Design, synthesis and structure-activity relationships of novel benzoxazolone derivatives as 18 kDa translocator protein (TSPO) ligands.Bioorganic & medicinal chemistry, , Sep-15, Volume: 20, Issue:18, 2012
N-(4-cyanotetrahydro-2H-pyran-4-yl) and N-(1-cyanocyclohexyl) derivatives of 1,5-diarylpyrazole-3-carboxamides showing high affinity for 18 kDa translocator protein and/or cannabinoid receptors.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Tertiary amides with a five-membered heteroaromatic ring as new probes for the translocator protein.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
The translocator protein (18 kDa): central nervous system disease and drug design.Journal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
Synthesis and structure-activity relationship studies in peripheral benzodiazepine receptor ligands related to alpidem.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation.Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
N,N-dialkyl-2-phenylindol-3-ylglyoxylamides. A new class of potent and selective ligands at the peripheral benzodiazepine receptor.Journal of medicinal chemistry, , Mar-25, Volume: 47, Issue:7, 2004
Structure-activity relationships in carboxamide derivatives based on the targeted delivery of radionuclides and boron atoms by means of peripheral benzodiazepine receptor ligands.Journal of medicinal chemistry, , Aug-14, Volume: 46, Issue:17, 2003
[18F]FMDAA1106 and [18F]FEDAA1106: two positron-emitter labeled ligands for peripheral benzodiazepine receptor (PBR).Bioorganic & medicinal chemistry letters, , Jan-20, Volume: 13, Issue:2, 2003
Mapping the peripheral benzodiazepine receptor binding site by conformationally restrained derivatives of 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3- isoquinolinecarboxamide (PK11195).Journal of medicinal chemistry, , Aug-29, Volume: 40, Issue:18, 1997
Molecular basis of peripheral vs central benzodiazepine receptor selectivity in a new class of peripheral benzodiazepine receptor ligands related to alpidem.Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
Synthesis, biological activity, and SARs of pyrrolobenzoxazepine derivatives, a new class of specific "peripheral-type" benzodiazepine receptor ligands.Journal of medicinal chemistry, , Aug-30, Volume: 39, Issue:18, 1996
A concerted study using binding measurements, X-ray structural data, and molecular modeling on the stereochemical features responsible for the affinity of 6-arylpyrrolo[2,1-d][1,5]benzothiazepines toward mitochondrial benzodiazepine receptors.Journal of medicinal chemistry, , Nov-10, Volume: 38, Issue:23, 1995
A comparative molecular field analysis model for 6-arylpyrrolo[2,1-d] [1,5]benzothiazepines binding selectively to the mitochondrial benzodiazepine receptor.Journal of medicinal chemistry, , Nov-25, Volume: 37, Issue:24, 1994
Novel ligands specific for mitochondrial benzodiazepine receptors: 6-arylpyrrolo[2,1-d][1,5]benzothiazepine derivatives. Synthesis, structure-activity relationships, and molecular modeling studies.Journal of medicinal chemistry, , May-13, Volume: 37, Issue:10, 1994
The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities.Journal of medicinal chemistry, , 04-08, Volume: 64, Issue:7, 2021
Deepening the Topology of the Translocator Protein Binding Site by Novel N,N-Dialkyl-2-arylindol-3-ylglyoxylamides.Journal of medicinal chemistry, , Aug-13, Volume: 58, Issue:15, 2015
Design, synthesis and structure-activity relationships of novel benzoxazolone derivatives as 18 kDa translocator protein (TSPO) ligands.Bioorganic & medicinal chemistry, , Sep-15, Volume: 20, Issue:18, 2012
Tertiary amides with a five-membered heteroaromatic ring as new probes for the translocator protein.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
The translocator protein (18 kDa): central nervous system disease and drug design.Journal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation.Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
N,N-dialkyl-2-phenylindol-3-ylglyoxylamides. A new class of potent and selective ligands at the peripheral benzodiazepine receptor.Journal of medicinal chemistry, , Mar-25, Volume: 47, Issue:7, 2004
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.Journal of medicinal chemistry, , May-23, Volume: 40, Issue:11, 1997
(S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist.Journal of medicinal chemistry, , Jun-21, Volume: 39, Issue:13, 1996
A concerted study using binding measurements, X-ray structural data, and molecular modeling on the stereochemical features responsible for the affinity of 6-arylpyrrolo[2,1-d][1,5]benzothiazepines toward mitochondrial benzodiazepine receptors.Journal of medicinal chemistry, , Nov-10, Volume: 38, Issue:23, 1995
Novel ligands specific for mitochondrial benzodiazepine receptors: 6-arylpyrrolo[2,1-d][1,5]benzothiazepine derivatives. Synthesis, structure-activity relationships, and molecular modeling studies.Journal of medicinal chemistry, , May-13, Volume: 37, Issue:10, 1994
Radioiodinated benzodiazepines: agents for mapping glial tumors.Journal of medicinal chemistry, , Volume: 31, Issue:11, 1988
The translocator protein (18 kDa): central nervous system disease and drug design.Journal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality.Journal of medicinal chemistry, , Apr-08, Volume: 42, Issue:7, 1999
A concerted study using binding measurements, X-ray structural data, and molecular modeling on the stereochemical features responsible for the affinity of 6-arylpyrrolo[2,1-d][1,5]benzothiazepines toward mitochondrial benzodiazepine receptors.Journal of medicinal chemistry, , Nov-10, Volume: 38, Issue:23, 1995
An update into the medicinal chemistry of translocator protein (TSPO) ligands.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation.Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
N,N-dialkyl-2-phenylindol-3-ylglyoxylamides. A new class of potent and selective ligands at the peripheral benzodiazepine receptor.Journal of medicinal chemistry, , Mar-25, Volume: 47, Issue:7, 2004
Synthesis and binding affinity of 2-phenylimidazo[1,2-alpha]pyridine derivatives for both central and peripheral benzodiazepine receptors. A new series of high-affinity and selective ligands for the peripheral type.Journal of medicinal chemistry, , Sep-12, Volume: 40, Issue:19, 1997
Molecular basis of peripheral vs central benzodiazepine receptor selectivity in a new class of peripheral benzodiazepine receptor ligands related to alpidem.Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
The translocator protein (18 kDa): central nervous system disease and drug design.Journal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
(S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist.Journal of medicinal chemistry, , Jun-21, Volume: 39, Issue:13, 1996
Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands.Journal of medicinal chemistry, , Oct-01, Volume: 36, Issue:20, 1993
Exploration of the structure-activity relationship of the diaryl anilide class of ligands for translocator protein--potential novel positron emitting tomography imaging agents.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 22, Issue:18, 2012
Single-step high-yield radiosynthesis and evaluation of a sensitive 18F-labeled ligand for imaging brain peripheral benzodiazepine receptors with PET.Journal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
[18F]FMDAA1106 and [18F]FEDAA1106: two positron-emitter labeled ligands for peripheral benzodiazepine receptor (PBR).Bioorganic & medicinal chemistry letters, , Jan-20, Volume: 13, Issue:2, 2003
Synthesis and structure-activity relationships of 5,6,7-substituted pyrazolopyrimidines: discovery of a novel TSPO PET ligand for cancer imaging.Journal of medicinal chemistry, , Apr-25, Volume: 56, Issue:8, 2013
The translocator protein (18 kDa): central nervous system disease and drug design.Journal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
Exploration of the structure-activity relationship of the diaryl anilide class of ligands for translocator protein--potential novel positron emitting tomography imaging agents.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 22, Issue:18, 2012
Single-step high-yield radiosynthesis and evaluation of a sensitive 18F-labeled ligand for imaging brain peripheral benzodiazepine receptors with PET.Journal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009