Page last updated: 2024-12-04

ro 5-4864

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Description

4'-chlorodiazepam: selectively binds peripheral benzodiazepine receptor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID1688
CHEMBL ID286346
SCHEMBL ID60200
MeSH IDM0091700

Synonyms (53)

Synonym
MLS001074199
ro5-4864
14439-61-3
7-chloro-5-(4-chlorophenyl)-1-methyl-3h-1,4-benzodiazepin-2-one
2h-1,4-benzodiazepin-2-one, 7-chloro-5-(4-chlorophenyl)-1,3-dihydro-1-methyl-
ro 5-4864
smr000058205
4'-chlorodiazepam
4 -chlorodiazepam
ro-4864
4' cl-diazepam
7-chloro-5-(4-chlorophenyl)-1-methyl-2,3-dihydro-1h-1,4-benzodiazepin-2-one
chembl286346 ,
bdbm22040
7-chloro-5-(4-chlorophenyl)-1-methyl-1,3-dihydro-2h-1,4-benzodiazepin-2-one
AE-641/30111005
brn 0685202
4-chlorodiazepam
hsdb 6958
2h-1,4-benzodiazepin-2-one, 7-chloro-5-(p-chlorophenyl)-1,3-dihydro-1-methyl-
7-chloro-1,3-dihydro-1-methyl-5-(p-chlorophenyl)-2h-1,4-benzodiazepin-2-one
ro-05-4864
PDSP2_000631
OPREA1_280237
PDSP2_000580
PDSP1_000583
PDSP1_000636
4'-chlorodiazepam, >=98% (tlc)
PDSP1_001759
MLS000069627 ,
PDSP2_001742
NCGC00018222-01
ro-5-4864
AKOS005066448
NCGC00018222-02
NCGC00018222-03
unii-2qw0ik1742
5-24-04-00337 (beilstein handbook reference)
2qw0ik1742 ,
HMS2230H04
7-chloro-5-(4-chlorophenyl)-1,3-dihydro-1-methyl-2h-1,4-benzodiazepin-2-one
4-chlorodiazepam [hsdb]
4'-chlorodiazepam [nflis-drug]
HMS3371O04
SCHEMBL60200
PUMYFTJOWAJIKF-UHFFFAOYSA-N
7-chloro-5-(4-chlorophenyl)-1-methyl-1,3-dihydro-2h-1,4-benzodiazepin-2-one #
OPERA_ID_1710
DTXSID3041116
7-chloro-5-(4-chlorophenyl)-1-methyl-1h-benzo[e][1,4]diazepin-2(3h)-one
AS-73428
(z)-7-chloro-5-(4-chlorophenyl)-1-methyl-1h-benzo[e][1,4]diazepin-2(3h)-one
Q7339205

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" In the present study, we have shown that micromolar concentrations of FGIN-1-27 and Ro 5-4864, two chemically unrelated PBR ligands are toxic for both PBR-expressing SK-N-BE neuroblastoma cells and PBR-deficient Jurkat lymphoma cells."( Peripheral benzodiazepine receptor (PBR) ligand cytotoxicity unrelated to PBR expression.
Belachew, S; Hans, G; Lallemend, F; Malgrange, B; Moonen, G; Nguyen, L; Rigo, JM; Robe, P; Rogister, B; Wislet-Gendebien, S, 2005
)
0.55

Compound-Compound Interactions

ExcerptReferenceRelevance
"The effects of several compounds believed to act at the GABA-benzodiazepine receptor complex and which have anticonvulsant or proconvulsant properties when administered in combination with picrotoxin and pentetrazol (leptazol, pentylenetetrazole) were investigated in combination with the convulsant benzodiazepine Ro 5-4864."( Pro- and anti-convulsant drug effects in combination with the convulsant benzodiazepine Ro 5-4864.
File, SE; Pellow, S, 1985
)
0.67

Dosage Studied

ExcerptRelevanceReference
" In Experiment 1, using a cumulative dosing paradigm, the effect of DZ on noise potentiation was found to be dose related."( Modulation of noise-potentiated acoustic startle via the benzodiazepine--gamma-aminobutyric acid receptor complex.
Bitran, D; Ison, JR; Kellogg, CK; Sullivan, AT, 1991
)
0.28
" The present study examined whether pretreatment with a dose-response regimen of sodium pentobarbital would impact the stress-induced reduction in renal PBR."( Pentobarbital blocks the stress-induced decrease in [3H]Ro 5-4864 binding in rat kidney.
Drugan, RC; Holmes, PV; Stringer, AP, 1990
)
0.53
" Also, Ro5-4864 caused a rightward shift in GABA dose-response curves, increasing the IC50 value for GABA more than 6 fold."( Dependence on gamma-aminobutyric acid of pyrethroid and 4'-chlorodiazepam modulation of the binding of t-[35S]butylbicyclophosphorothionate in piscine brain.
Eshleman, AJ; Murray, TF, 1990
)
0.28
" When platelets were pretreated with either BDZR ligand, and then exposed to various concentrations of WEB 2086, there was no alteration of the dose-response relationship of the hetrazepine on PAF-induced aggregation, as reflected by threshold concentration, ED50, or maximum inhibition seen with WEB 2086."( The benzodiazepine receptor ligands RO 5-4864 and RO 15-1788 do not block the inhibition of PAF-induced platelet aggregation seen with the hetrazepine WEB2086.
Griffin, K; Hong, T; Levy, JV, 1989
)
0.55
" Enhancement of submaximal GABA responses by benzodiazepines was demonstrated using a multibarrel pipette to construct complete benzodiazepine dose-response curves for single cells in culture."( Benzodiazepine interactions with GABAA receptors on chick ciliary ganglion neurons.
Berg, DK; McEachern, AE, 1988
)
0.27
" No significant tolerance developed to the anticonvulsant action of PK 11195 (30 mg kg-1) even after 25 days of dosing daily."( Pro- and anti-convulsant properties of PK 11195, a ligand for benzodiazepine binding sites: development of tolerance.
File, SE, 1984
)
0.27
" The enhancement of [3H]flunitrazepam binding to the benzodiazepine receptor by loreclezole as well as the effect of loreclezole on CL218872/[3H]flunitrazepam dose-response curves suggest that loreclezole does not act through the benzodiazepine site on the GABAA receptor complex, nor does it selectively modulate benzodiazepine receptor subtypes."( Loreclezole modulates [35S]t-butylbicyclophosphorothionate and [3H]flunitrazepam binding via a distinct site on the GABAA receptor complex.
Friend, JM; Gee, KW; Xue, BG, 1996
)
0.29
" It appears that in female rats, at least at these doses and dosing schedules, there is no correlation between the impact of chronic in vivo exposure to these agents on PBR density and ovarian and adrenal hormone levels."( Peripheral-type benzodiazepine receptor ligands and serum steroid hormones.
Gavish, M; Leschiner, S; Schlegel, W; Weizman, R, 1997
)
0.3
" Specifically, the TSPO ligand RT significantly fitted both with steroidogenic efficacy (Emax) and with area under the dose-response curve, a parameter combining drug potency and efficacy."( TSPO ligand residence time: a new parameter to predict compound neurosteroidogenic efficacy.
Barresi, E; Costa, B; Da Pozzo, E; Da Settimo, F; Giacomelli, C; Martini, C; Taliani, S, 2016
)
0.43
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (40)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency28.18380.044717.8581100.0000AID485341
ATAD5 protein, partialHomo sapiens (human)Potency23.10930.004110.890331.5287AID504467
TDP1 proteinHomo sapiens (human)Potency29.09290.000811.382244.6684AID686978
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency10.00000.28189.721235.4813AID2326
IDH1Homo sapiens (human)Potency29.09290.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency39.81070.035520.977089.1251AID504332
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency31.62280.036619.637650.1187AID1466; AID2242
importin subunit beta-1 isoform 1Homo sapiens (human)Potency5.62345.804836.130665.1308AID540263
snurportin-1Homo sapiens (human)Potency5.62345.804836.130665.1308AID540263
gemininHomo sapiens (human)Potency23.10930.004611.374133.4983AID624296
lamin isoform A-delta10Homo sapiens (human)Potency7.94330.891312.067628.1838AID1487
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency31.62283.548118.039535.4813AID1466
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Potency31.62283.548118.039535.4813AID1466
Alpha-synucleinHomo sapiens (human)Potency11.22020.56239.398525.1189AID652106
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Mcl-1Homo sapiens (human)IC50 (µMol)54.00000.40007.134454.0000AID1418
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Ki1.00000.00020.656110.0000AID40679
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC50 (µMol)54.00000.00052.773925.1700AID1418
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC50 (µMol)54.00000.00052.891925.1700AID1418
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC50 (µMol)54.00000.00052.747825.1700AID1418
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC50 (µMol)54.00000.00052.780225.1700AID1418
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC50 (µMol)54.00000.00053.314249.5000AID1418
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Ki1.00000.00020.656110.0000AID40679
Translocator proteinRattus norvegicus (Norway rat)IC50 (µMol)0.03400.00010.63934.8100AID40100; AID42313
Translocator proteinRattus norvegicus (Norway rat)Ki0.01900.00010.65108.9300AID1236028; AID155960; AID1798152; AID1894699; AID275802; AID40374; AID619230; AID685342
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Ki1.00000.00020.656110.0000AID40679
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Ki1.00000.00020.561410.0000AID40679
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki1.00000.00020.635210.0000AID40679
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki1.00000.00020.621710.0000AID40679
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Ki1.00000.00020.675810.0000AID40679
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki1.00000.00020.646910.0000AID40679
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki1.00000.00020.656110.0000AID40679
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Ki1.00000.00020.656110.0000AID40679
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki1.00000.00020.671210.0000AID40679
Translocator proteinMus musculus (house mouse)IC50 (µMol)0.01000.01000.01000.0100AID42148
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki1.00000.00020.557710.0000AID40679
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Ki1.00000.00020.640310.0000AID40679
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Ki1.00000.00020.570810.0000AID40679
GABA theta subunitRattus norvegicus (Norway rat)Ki1.00000.00020.656110.0000AID40679
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Ki1.00000.00020.656110.0000AID40679
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Kd0.02170.00020.56294.4668AID39918; AID39920
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Kd0.02170.00020.56294.4668AID39918; AID39920
Translocator proteinRattus norvegicus (Norway rat)Kd1.61250.00060.82834.0000AID368145; AID39918; AID39919; AID39920
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Kd0.02170.00020.56294.4668AID39918; AID39920
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Kd0.02170.00020.56294.4668AID39918; AID39920
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Kd0.05800.00012.29338.5114AID39918
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Kd0.02170.00020.56294.4668AID39918; AID39920
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Kd0.02170.00020.56294.4668AID39918; AID39920
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Kd0.02170.00020.56294.4668AID39918; AID39920
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Kd0.02170.00020.56294.4668AID39918; AID39920
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Kd0.02170.00020.56294.4668AID39918; AID39920
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Kd0.02170.00020.56294.4668AID39918; AID39920
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Kd0.02170.00020.56294.4668AID39918; AID39920
Translocator proteinHomo sapiens (human)Kd0.00360.00110.00480.0111AID368145; AID408746
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Kd0.02170.00020.56294.4668AID39918; AID39920
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Kd0.02170.00020.56294.4668AID39918; AID39920
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Kd0.02170.00020.56294.4668AID39918; AID39920
GABA theta subunitRattus norvegicus (Norway rat)Kd0.02170.00020.56294.4668AID39918; AID39920
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Kd0.02170.00020.56294.4668AID39918; AID39920
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Translocator proteinHomo sapiens (human)Activity0.00730.00060.00510.0073AID368141
Translocator proteinMus musculus (house mouse)Activity0.00020.00020.00020.0002AID368143
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (114)

Processvia Protein(s)Taxonomy
protein targeting to mitochondrionTranslocator proteinHomo sapiens (human)
C21-steroid hormone biosynthetic processTranslocator proteinHomo sapiens (human)
heme biosynthetic processTranslocator proteinHomo sapiens (human)
monoatomic anion transportTranslocator proteinHomo sapiens (human)
chloride transportTranslocator proteinHomo sapiens (human)
steroid metabolic processTranslocator proteinHomo sapiens (human)
glial cell migrationTranslocator proteinHomo sapiens (human)
response to xenobiotic stimulusTranslocator proteinHomo sapiens (human)
response to manganese ionTranslocator proteinHomo sapiens (human)
response to vitamin B1Translocator proteinHomo sapiens (human)
peripheral nervous system axon regenerationTranslocator proteinHomo sapiens (human)
sterol transportTranslocator proteinHomo sapiens (human)
adrenal gland developmentTranslocator proteinHomo sapiens (human)
negative regulation of protein ubiquitinationTranslocator proteinHomo sapiens (human)
regulation of cholesterol transportTranslocator proteinHomo sapiens (human)
response to progesteroneTranslocator proteinHomo sapiens (human)
negative regulation of tumor necrosis factor productionTranslocator proteinHomo sapiens (human)
response to testosteroneTranslocator proteinHomo sapiens (human)
regulation of cell population proliferationTranslocator proteinHomo sapiens (human)
cholesterol homeostasisTranslocator proteinHomo sapiens (human)
positive regulation of apoptotic processTranslocator proteinHomo sapiens (human)
negative regulation of nitric oxide biosynthetic processTranslocator proteinHomo sapiens (human)
behavioral response to painTranslocator proteinHomo sapiens (human)
regulation of steroid biosynthetic processTranslocator proteinHomo sapiens (human)
positive regulation of mitochondrial depolarizationTranslocator proteinHomo sapiens (human)
positive regulation of calcium ion transportTranslocator proteinHomo sapiens (human)
contact inhibitionTranslocator proteinHomo sapiens (human)
positive regulation of glial cell proliferationTranslocator proteinHomo sapiens (human)
negative regulation of glial cell proliferationTranslocator proteinHomo sapiens (human)
positive regulation of programmed necrotic cell deathTranslocator proteinHomo sapiens (human)
cellular response to lipopolysaccharideTranslocator proteinHomo sapiens (human)
cellular response to zinc ionTranslocator proteinHomo sapiens (human)
cellular hypotonic responseTranslocator proteinHomo sapiens (human)
maintenance of protein location in mitochondrionTranslocator proteinHomo sapiens (human)
negative regulation of mitophagyTranslocator proteinHomo sapiens (human)
negative regulation of ATP metabolic processTranslocator proteinHomo sapiens (human)
response to acetylcholineTranslocator proteinHomo sapiens (human)
positive regulation of reactive oxygen species metabolic processTranslocator proteinHomo sapiens (human)
negative regulation of corticosterone secretionTranslocator proteinHomo sapiens (human)
calcium ion homeostasisAlpha-synucleinHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIAlpha-synucleinHomo sapiens (human)
microglial cell activationAlpha-synucleinHomo sapiens (human)
positive regulation of receptor recyclingAlpha-synucleinHomo sapiens (human)
positive regulation of neurotransmitter secretionAlpha-synucleinHomo sapiens (human)
negative regulation of protein kinase activityAlpha-synucleinHomo sapiens (human)
fatty acid metabolic processAlpha-synucleinHomo sapiens (human)
neutral lipid metabolic processAlpha-synucleinHomo sapiens (human)
phospholipid metabolic processAlpha-synucleinHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
mitochondrial membrane organizationAlpha-synucleinHomo sapiens (human)
adult locomotory behaviorAlpha-synucleinHomo sapiens (human)
response to xenobiotic stimulusAlpha-synucleinHomo sapiens (human)
response to iron(II) ionAlpha-synucleinHomo sapiens (human)
regulation of phospholipase activityAlpha-synucleinHomo sapiens (human)
negative regulation of platelet-derived growth factor receptor signaling pathwayAlpha-synucleinHomo sapiens (human)
regulation of glutamate secretionAlpha-synucleinHomo sapiens (human)
regulation of dopamine secretionAlpha-synucleinHomo sapiens (human)
synaptic vesicle exocytosisAlpha-synucleinHomo sapiens (human)
synaptic vesicle primingAlpha-synucleinHomo sapiens (human)
regulation of transmembrane transporter activityAlpha-synucleinHomo sapiens (human)
negative regulation of microtubule polymerizationAlpha-synucleinHomo sapiens (human)
receptor internalizationAlpha-synucleinHomo sapiens (human)
protein destabilizationAlpha-synucleinHomo sapiens (human)
response to magnesium ionAlpha-synucleinHomo sapiens (human)
negative regulation of transporter activityAlpha-synucleinHomo sapiens (human)
response to lipopolysaccharideAlpha-synucleinHomo sapiens (human)
negative regulation of monooxygenase activityAlpha-synucleinHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationAlpha-synucleinHomo sapiens (human)
response to type II interferonAlpha-synucleinHomo sapiens (human)
cellular response to oxidative stressAlpha-synucleinHomo sapiens (human)
SNARE complex assemblyAlpha-synucleinHomo sapiens (human)
positive regulation of SNARE complex assemblyAlpha-synucleinHomo sapiens (human)
regulation of locomotionAlpha-synucleinHomo sapiens (human)
dopamine biosynthetic processAlpha-synucleinHomo sapiens (human)
mitochondrial ATP synthesis coupled electron transportAlpha-synucleinHomo sapiens (human)
regulation of macrophage activationAlpha-synucleinHomo sapiens (human)
positive regulation of apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of neuron apoptotic processAlpha-synucleinHomo sapiens (human)
positive regulation of endocytosisAlpha-synucleinHomo sapiens (human)
negative regulation of exocytosisAlpha-synucleinHomo sapiens (human)
positive regulation of exocytosisAlpha-synucleinHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityAlpha-synucleinHomo sapiens (human)
synaptic vesicle endocytosisAlpha-synucleinHomo sapiens (human)
synaptic vesicle transportAlpha-synucleinHomo sapiens (human)
positive regulation of inflammatory responseAlpha-synucleinHomo sapiens (human)
regulation of acyl-CoA biosynthetic processAlpha-synucleinHomo sapiens (human)
protein tetramerizationAlpha-synucleinHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolAlpha-synucleinHomo sapiens (human)
neuron apoptotic processAlpha-synucleinHomo sapiens (human)
dopamine uptake involved in synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of dopamine uptake involved in synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of serotonin uptakeAlpha-synucleinHomo sapiens (human)
regulation of norepinephrine uptakeAlpha-synucleinHomo sapiens (human)
negative regulation of norepinephrine uptakeAlpha-synucleinHomo sapiens (human)
excitatory postsynaptic potentialAlpha-synucleinHomo sapiens (human)
long-term synaptic potentiationAlpha-synucleinHomo sapiens (human)
positive regulation of inositol phosphate biosynthetic processAlpha-synucleinHomo sapiens (human)
negative regulation of thrombin-activated receptor signaling pathwayAlpha-synucleinHomo sapiens (human)
response to interleukin-1Alpha-synucleinHomo sapiens (human)
cellular response to copper ionAlpha-synucleinHomo sapiens (human)
cellular response to epinephrine stimulusAlpha-synucleinHomo sapiens (human)
positive regulation of protein serine/threonine kinase activityAlpha-synucleinHomo sapiens (human)
supramolecular fiber organizationAlpha-synucleinHomo sapiens (human)
negative regulation of mitochondrial electron transport, NADH to ubiquinoneAlpha-synucleinHomo sapiens (human)
positive regulation of glutathione peroxidase activityAlpha-synucleinHomo sapiens (human)
positive regulation of hydrogen peroxide catabolic processAlpha-synucleinHomo sapiens (human)
regulation of synaptic vesicle recyclingAlpha-synucleinHomo sapiens (human)
regulation of reactive oxygen species biosynthetic processAlpha-synucleinHomo sapiens (human)
positive regulation of protein localization to cell peripheryAlpha-synucleinHomo sapiens (human)
negative regulation of chaperone-mediated autophagyAlpha-synucleinHomo sapiens (human)
regulation of presynapse assemblyAlpha-synucleinHomo sapiens (human)
amyloid fibril formationAlpha-synucleinHomo sapiens (human)
synapse organizationAlpha-synucleinHomo sapiens (human)
chemical synaptic transmissionAlpha-synucleinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (31)

Processvia Protein(s)Taxonomy
androgen bindingTranslocator proteinHomo sapiens (human)
protein bindingTranslocator proteinHomo sapiens (human)
benzodiazepine receptor activityTranslocator proteinHomo sapiens (human)
cholesterol bindingTranslocator proteinHomo sapiens (human)
transmembrane transporter bindingTranslocator proteinHomo sapiens (human)
cholesterol transfer activityTranslocator proteinHomo sapiens (human)
fatty acid bindingAlpha-synucleinHomo sapiens (human)
phospholipase D inhibitor activityAlpha-synucleinHomo sapiens (human)
SNARE bindingAlpha-synucleinHomo sapiens (human)
magnesium ion bindingAlpha-synucleinHomo sapiens (human)
transcription cis-regulatory region bindingAlpha-synucleinHomo sapiens (human)
actin bindingAlpha-synucleinHomo sapiens (human)
protein kinase inhibitor activityAlpha-synucleinHomo sapiens (human)
copper ion bindingAlpha-synucleinHomo sapiens (human)
calcium ion bindingAlpha-synucleinHomo sapiens (human)
protein bindingAlpha-synucleinHomo sapiens (human)
phospholipid bindingAlpha-synucleinHomo sapiens (human)
ferrous iron bindingAlpha-synucleinHomo sapiens (human)
zinc ion bindingAlpha-synucleinHomo sapiens (human)
lipid bindingAlpha-synucleinHomo sapiens (human)
oxidoreductase activityAlpha-synucleinHomo sapiens (human)
kinesin bindingAlpha-synucleinHomo sapiens (human)
Hsp70 protein bindingAlpha-synucleinHomo sapiens (human)
histone bindingAlpha-synucleinHomo sapiens (human)
identical protein bindingAlpha-synucleinHomo sapiens (human)
alpha-tubulin bindingAlpha-synucleinHomo sapiens (human)
cysteine-type endopeptidase inhibitor activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
tau protein bindingAlpha-synucleinHomo sapiens (human)
phosphoprotein bindingAlpha-synucleinHomo sapiens (human)
molecular adaptor activityAlpha-synucleinHomo sapiens (human)
dynein complex bindingAlpha-synucleinHomo sapiens (human)
cuprous ion bindingAlpha-synucleinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (26)

Processvia Protein(s)Taxonomy
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
mitochondrionTranslocator proteinHomo sapiens (human)
mitochondrial outer membraneTranslocator proteinHomo sapiens (human)
cytosolTranslocator proteinHomo sapiens (human)
intracellular membrane-bounded organelleTranslocator proteinHomo sapiens (human)
extracellular exosomeTranslocator proteinHomo sapiens (human)
endoplasmic reticulumTranslocator proteinHomo sapiens (human)
membraneTranslocator proteinHomo sapiens (human)
platelet alpha granule membraneAlpha-synucleinHomo sapiens (human)
extracellular regionAlpha-synucleinHomo sapiens (human)
extracellular spaceAlpha-synucleinHomo sapiens (human)
nucleusAlpha-synucleinHomo sapiens (human)
cytoplasmAlpha-synucleinHomo sapiens (human)
mitochondrionAlpha-synucleinHomo sapiens (human)
lysosomeAlpha-synucleinHomo sapiens (human)
cytosolAlpha-synucleinHomo sapiens (human)
plasma membraneAlpha-synucleinHomo sapiens (human)
cell cortexAlpha-synucleinHomo sapiens (human)
actin cytoskeletonAlpha-synucleinHomo sapiens (human)
membraneAlpha-synucleinHomo sapiens (human)
inclusion bodyAlpha-synucleinHomo sapiens (human)
axonAlpha-synucleinHomo sapiens (human)
growth coneAlpha-synucleinHomo sapiens (human)
synaptic vesicle membraneAlpha-synucleinHomo sapiens (human)
perinuclear region of cytoplasmAlpha-synucleinHomo sapiens (human)
postsynapseAlpha-synucleinHomo sapiens (human)
supramolecular fiberAlpha-synucleinHomo sapiens (human)
protein-containing complexAlpha-synucleinHomo sapiens (human)
cytoplasmAlpha-synucleinHomo sapiens (human)
axon terminusAlpha-synucleinHomo sapiens (human)
neuronal cell bodyAlpha-synucleinHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (85)

Assay IDTitleYearJournalArticle
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID165929Lymphotoxic activity against immortalized Ramos B cells in culture2003Bioorganic & medicinal chemistry letters, Oct-06, Volume: 13, Issue:19
Structure activity studies of a novel cytotoxic benzodiazepine.
AID40100Displacement of [3H]-PK 11195 from peripheral (mitochondrial) benzodiazepine receptor1994Journal of medicinal chemistry, May-13, Volume: 37, Issue:10
Novel ligands specific for mitochondrial benzodiazepine receptors: 6-arylpyrrolo[2,1-d][1,5]benzothiazepine derivatives. Synthesis, structure-activity relationships, and molecular modeling studies.
AID39921Binding affinity constant for Benzodiazepine receptor in normal rat brain homogenate1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
AID200785The compound was tested for cytotoxicity against SF-188 (human) Glioma cell lines1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
AID1138439Displacement of [3H]PK11195 from TSPO in rat kidney mitochondrial membranes2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Structure-activity relationship refinement and further assessment of 4-phenylquinazoline-2-carboxamide translocator protein ligands as antiproliferative agents in human glioblastoma tumors.
AID42148Displacement of [3H]PK11195 binding from peripheral benzodiazepine receptor in MA-10 mouse tumor Leydig cells1996Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13
(S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist.
AID672796Increase in pregnenolone production in rat C6 glioma cells at 40 uM after 2 hrs by ELISA2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Synthesis and biological evaluation of 4-phenylquinazoline-2-carboxamides designed as a novel class of potent ligands of the translocator protein.
AID1236028Inhibition of [3H]PK11195 binding to TSPO in rat kidney mitochondrial membranes2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Deepening the Topology of the Translocator Protein Binding Site by Novel N,N-Dialkyl-2-arylindol-3-ylglyoxylamides.
AID1236029Inhibition of [3H]flumazenil binding to benzodiazepine receptor in rat cerebral cortex membranes at 10 uM incubated for 90 mins2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Deepening the Topology of the Translocator Protein Binding Site by Novel N,N-Dialkyl-2-arylindol-3-ylglyoxylamides.
AID294528Antiproliferative activity against v-Src transformed mouse NIH 3T3 fibroblast after 72 hrs2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Novel 1,4-benzodiazepine derivatives with antiproliferative properties on tumor cell lines.
AID1894699Binding affinity rat kidney mitochondrial membrane TSPO receptor assessed as inhibition constant2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities.
AID200783The compound was tested for cytotoxicity against SF-126 (human) Glioma cell lines1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
AID155960Binding affinity for peripheral benzodiazepine receptor of rat kidney1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Radioiodinated benzodiazepines: agents for mapping glial tumors.
AID42179Benzodiazepine receptor density in rat RG-2 glioma cells1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
AID40374Binding affinity to peripheral benzodiazepine receptors using [3H]-PK11195 radioligand in rat kidney mitochondrial membrane2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
N,N-dialkyl-2-phenylindol-3-ylglyoxylamides. A new class of potent and selective ligands at the peripheral benzodiazepine receptor.
AID42178Benzodiazepine receptor density in rat C6 glioma cells1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
AID40679Binding affinity for GABA-A benzodiazepine receptor of rat brain1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Radioiodinated benzodiazepines: agents for mapping glial tumors.
AID685342Displacement of [3H]PK11195 from TSPO receptor in rat Sprague-Dawley kidney membranes after 1 hr by liquid scintillation counting2012Bioorganic & medicinal chemistry, Sep-15, Volume: 20, Issue:18
Design, synthesis and structure-activity relationships of novel benzoxazolone derivatives as 18 kDa translocator protein (TSPO) ligands.
AID1503633Inhibition of TSPO in mouse HT22 cells assessed as recovery of ATP production at 5 uM preincubated for 10 mins followed by amyloid beta (1 to 42) stimulation and measured after 7 hrs by luciferase based assay relative to control2017European journal of medicinal chemistry, Dec-01, Volume: 141Discovery of thienopyrrolotriazine derivatives to protect mitochondrial function against Aβ-induced neurotoxicity.
AID166691The compound was tested for cytotoxicity against RG-2 (Rat) Glioma cell lines1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
AID270650Cytotoxicity against rat C6 glioma cell line2006Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19
Discovery of antiglioma activity of biaryl 1,2,3,4-tetrahydroisoquinoline derivatives and conformationally flexible analogues.
AID306151Induction of reactive oxygen species response in Ramos cells after 1 hr2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Inhibition of the mitochondrial F1F0-ATPase by ligands of the peripheral benzodiazepine receptor.
AID368143Binding affinity to mitochondrial TSPO in mouse MA10 cells in presence of human chorionic gonadotropin2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
The translocator protein (18 kDa): central nervous system disease and drug design.
AID306154Induction of cell death in Jurkat cells after 24 hrs2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Inhibition of the mitochondrial F1F0-ATPase by ligands of the peripheral benzodiazepine receptor.
AID219916Stimulation of steroid (pregnenolone) biosynthesis in mouse Y-1 adrenocortical cells at 40 uM1996Journal of medicinal chemistry, Aug-30, Volume: 39, Issue:18
Synthesis, biological activity, and SARs of pyrrolobenzoxazepine derivatives, a new class of specific "peripheral-type" benzodiazepine receptor ligands.
AID672793Displacement of [3H]PK11195 from TSPO in rat kidney mitochondrial membranes by competitive binding assay2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Synthesis and biological evaluation of 4-phenylquinazoline-2-carboxamides designed as a novel class of potent ligands of the translocator protein.
AID1150161Sedative activity in mouse1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Electronic factors in the structure-activity relationship of some 1,4-benzodiazepin-2-ones.
AID408746Binding affinity to human PBR2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Synthesis, fluorine-18 radiolabeling, and in vitro characterization of 1-iodophenyl-N-methyl-N-fluoroalkyl-3-isoquinoline carboxamide derivatives as potential PET radioligands for imaging peripheral benzodiazepine receptor.
AID306149Inhibition of F1F0-ATPase hydrolysis activity in bovine submitochondrial particles2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Inhibition of the mitochondrial F1F0-ATPase by ligands of the peripheral benzodiazepine receptor.
AID480895Displacement of [3H]Ro5-4864 from TSPO in rat kidney mitochondrial membrane2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Novel irreversible fluorescent probes targeting the 18 kDa translocator protein: synthesis and biological characterization.
AID42313Displacement of [3H]PK11195 binding from peripheral benzodiazepine receptor in C6 rat glioma cell line1996Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13
(S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist.
AID294530Cytotoxicity against human A2058 cells after 72 hrs by WST-1 colorimetric test2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Novel 1,4-benzodiazepine derivatives with antiproliferative properties on tumor cell lines.
AID39919Binding affinity constant for Benzodiazepine receptor in rat C6 glioma cells1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
AID368141Displacement of [3H]Ro5-4864 from TSPO2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
The translocator protein (18 kDa): central nervous system disease and drug design.
AID672795Displacement of [3H]flumazenil from central benzodiazepine receptor in rat cerebral cortex membranes at 10 uM after 90 mins by competitive binding assay2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Synthesis and biological evaluation of 4-phenylquinazoline-2-carboxamides designed as a novel class of potent ligands of the translocator protein.
AID294531Cytotoxicity against human HeLa cells after 72 hrs by WST-1 colorimetric test2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Novel 1,4-benzodiazepine derivatives with antiproliferative properties on tumor cell lines.
AID1150162Muscle relaxant activity in mouse1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Electronic factors in the structure-activity relationship of some 1,4-benzodiazepin-2-ones.
AID1894700Activation of TSPO in rat C6 glioma cells assessed as increase in pregnenolone incubated for 2 hrs by radioimmuno assay2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities.
AID42180Benzodiazepine receptor density in normal rat brain homogenate1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
AID554238Displacement of [11C]PK11195 from TSPO in rat kidney mitochondrial membrane2011Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1
Evaluation of novel N1-methyl-2-phenylindol-3-ylglyoxylamides as a new chemotype of 18 kDa translocator protein-selective ligand suitable for the development of positron emission tomography radioligands.
AID1150163Taming activity in mouse assessed as suppression of electrical current-induced aggressive behavior by foot-shock test1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Electronic factors in the structure-activity relationship of some 1,4-benzodiazepin-2-ones.
AID1503634Cytotoxicity against mouse HT22 cells as cell viability at 5 uM after 24 hrs by MTT assay relative to control2017European journal of medicinal chemistry, Dec-01, Volume: 141Discovery of thienopyrrolotriazine derivatives to protect mitochondrial function against Aβ-induced neurotoxicity.
AID408747Displacement of [3H]PK11195 from PBR in rat kidney mitochondrial membrane2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Synthesis, fluorine-18 radiolabeling, and in vitro characterization of 1-iodophenyl-N-methyl-N-fluoroalkyl-3-isoquinoline carboxamide derivatives as potential PET radioligands for imaging peripheral benzodiazepine receptor.
AID169249Percent inhibition of [3H]flumazenil binding to rat GABA-A central benzodiazepine receptor 10 uM2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
N,N-dialkyl-2-phenylindol-3-ylglyoxylamides. A new class of potent and selective ligands at the peripheral benzodiazepine receptor.
AID368142Displacement of [3H]Ro5-4864 from GABAA receptor in rat brain membrane2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
The translocator protein (18 kDa): central nervous system disease and drug design.
AID306153Induction of cell death in Ramos cells after 24 hrs2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Inhibition of the mitochondrial F1F0-ATPase by ligands of the peripheral benzodiazepine receptor.
AID306150Inhibition of F1F0-ATPase synthesis activity in bovine submitochondrial particles2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Inhibition of the mitochondrial F1F0-ATPase by ligands of the peripheral benzodiazepine receptor.
AID1503636Displacement of [3H]PK11195 from TSPO in Sprague-Dawley rat cerebral cortex membranes after 60 mins by liquid scintillation counting analysis2017European journal of medicinal chemistry, Dec-01, Volume: 141Discovery of thienopyrrolotriazine derivatives to protect mitochondrial function against Aβ-induced neurotoxicity.
AID368148Antiapoptotic activity against TNF-alpha-induced apoptosis in human U937 cells2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
The translocator protein (18 kDa): central nervous system disease and drug design.
AID368145Displacement of [3H]Ro5-4864 from TSPO in rat kainate lesioned striatum2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
The translocator protein (18 kDa): central nervous system disease and drug design.
AID39920Binding affinity constant for Benzodiazepine receptor in rat RG-2 glioma cells1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
AID275802Displacement of [3H]PK 11195 from peripheral-type benzodiazepine receptor in rat kidney mitochondrial membranes2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation.
AID1150164Anticonvulsion activity in mouse assessed as protection against pentylenetetrazole-induced convulsion1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Electronic factors in the structure-activity relationship of some 1,4-benzodiazepin-2-ones.
AID363486Induction of pregnenolone biosynthesis in rat C6 cells assessed as increase in pregnenolone level at 40 uM after 2 hrs by ELISA relative to control2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Anxiolytic-like effects of N,N-dialkyl-2-phenylindol-3-ylglyoxylamides by modulation of translocator protein promoting neurosteroid biosynthesis.
AID363485Displacement of [3H]PK11195 from translocator protein in rat kidney mitochondrial membrane2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Anxiolytic-like effects of N,N-dialkyl-2-phenylindol-3-ylglyoxylamides by modulation of translocator protein promoting neurosteroid biosynthesis.
AID1503632Inhibition of TSPO in mouse HT22 cells assessed as reduction in amyloid beta (1 to 42) (unknown origin) induced mitochondrial permeability transition pore formation by measuring increase in green to red fluorescence ratio at 5 uM pretreated for 10 mins fo2017European journal of medicinal chemistry, Dec-01, Volume: 141Discovery of thienopyrrolotriazine derivatives to protect mitochondrial function against Aβ-induced neurotoxicity.
AID368149Induction of apoptosis in human U937 cells2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
The translocator protein (18 kDa): central nervous system disease and drug design.
AID306152Induction of reactive oxygen species response in Jurkat cells after 1 hr2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Inhibition of the mitochondrial F1F0-ATPase by ligands of the peripheral benzodiazepine receptor.
AID39918Binding affinity constant for peripheral (mitochondrial) Benzodiazepine receptor1995Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
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.
AID44482The compound was tested for cytotoxicity against C6 (Rat) Glioma cell lines1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
AID619230Displacement of [3H]PK11195 from TSPO receptor in rat kidney membranes2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Tertiary amides with a five-membered heteroaromatic ring as new probes for the translocator protein.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
AID1798152Radioligand Binding Assay from Article 10.1021/jm061137o: \\New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation.\\2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (577)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990243 (42.11)18.7374
1990's181 (31.37)18.2507
2000's86 (14.90)29.6817
2010's58 (10.05)24.3611
2020's9 (1.56)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 7.88

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index7.88 (24.57)
Research Supply Index6.39 (2.92)
Research Growth Index4.27 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (7.88)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews18 (3.04%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other575 (96.96%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]