Page last updated: 2024-11-09

n-(1-benzyl-4-piperidinyl)-2,4-dichlorobenzamide

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Description

N-(1-benzyl-4-piperidinyl)-2,4-dichlorobenzamide: inhibits the betaine-GABA transporter 1; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID1069892
CHEMBL ID1882801
MeSH IDM0588111

Synonyms (23)

Synonym
CBMICRO_018714 ,
smr000502170
MLS001185535
OPREA1_510498
BIM-0018815.P001
n-(1-benzylpiperidin-4-yl)-2,4-dichlorobenzamide
STK053506
AKOS001766690
CCG-6976
HMS2820D15
REGID_FOR_CID_1069892
AB00082098-01
cambridge id 5349520
CHEMBL1882801 ,
sr-01000519597
SR-01000519597-1
n-(1-benzyl-4-piperidinyl)-2,4-dichlorobenzamide
bdbm50250267
bpdba
312281-74-6
CS-0070026
HY-119591
n-(1-benzyl-4-piperidyl)-2,4-dichlorobenzamide
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency20.59620.000811.382244.6684AID686978
[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)
Sodium- and chloride-dependent GABA transporter 1Homo sapiens (human)Ki100.00000.01700.03240.0479AID1476513
Sodium- and chloride-dependent GABA transporter 1Mus musculus (house mouse)IC50 (µMol)200.00000.03712.19228.5114AID1476517
Sodium- and chloride-dependent GABA transporter 2Mus musculus (house mouse)IC50 (µMol)200.00001.41255.26838.1283AID1476519
Sodium- and chloride-dependent GABA transporter 3Mus musculus (house mouse)IC50 (µMol)200.00001.54883.67618.1283AID1476520
Sodium- and chloride-dependent betaine transporterMus musculus (house mouse)IC50 (µMol)31.81140.18003.188010.0000AID1476518
Sodium- and chloride-dependent betaine transporterHomo sapiens (human)IC50 (µMol)29.71290.85116.052136.0000AID1476514; AID1476529; AID1476530; AID1476531; AID1476532; AID1476533; AID1476534; AID1476535; AID1476536; AID1476537; AID1476538; AID1476539; AID1476540; AID1476541; AID1476542; AID1476543; AID1476544; AID1476545; AID1476546; AID1476547; AID1476548; AID1476549; AID1476550; AID1476551; AID1476553; AID1476554; AID1476555
Sodium- and chloride-dependent GABA transporter 3Homo sapiens (human)IC50 (µMol)405.69601.00004.13318.9200AID1476507; AID1476552
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (31)

Processvia Protein(s)Taxonomy
memorySodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
associative learningSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
synapse organizationSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
chemical synaptic transmissionSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to toxic substanceSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to sucroseSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to inorganic substanceSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to lead ionSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
positive regulation of gamma-aminobutyric acid secretionSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to purine-containing compoundSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
negative regulation of synaptic transmission, GABAergicSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to estradiolSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to cocaineSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
response to calcium ionSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
gamma-aminobutyric acid reuptakeSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
gamma-aminobutyric acid importSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
inorganic anion import across plasma membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
sodium ion import across plasma membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
transport across blood-brain barrierSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
chloride transmembrane transportSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
sodium ion transmembrane transportSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
amino acid transportSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
amino acid transmembrane transportSodium- and chloride-dependent betaine transporterHomo sapiens (human)
amino acid transportSodium- and chloride-dependent betaine transporterHomo sapiens (human)
monocarboxylic acid transportSodium- and chloride-dependent betaine transporterHomo sapiens (human)
gamma-aminobutyric acid transportSodium- and chloride-dependent betaine transporterHomo sapiens (human)
glycine betaine transportSodium- and chloride-dependent betaine transporterHomo sapiens (human)
gamma-aminobutyric acid reuptakeSodium- and chloride-dependent betaine transporterHomo sapiens (human)
sodium ion transmembrane transportSodium- and chloride-dependent betaine transporterHomo sapiens (human)
amino acid transmembrane transportSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
response to xenobiotic stimulusSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
monocarboxylic acid transportSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
taurine transmembrane transportSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
gamma-aminobutyric acid reuptakeSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
sodium ion transmembrane transportSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
amino acid transportSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
nitrogen compound transportSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
monocarboxylic acid transportSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
taurine transmembrane transportSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
creatine transmembrane transportSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
gamma-aminobutyric acid reuptakeSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
gamma-aminobutyric acid importSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
nitrogen compound transportSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
amino acid import across plasma membraneSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
transport across blood-brain barrierSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
amino acid transportSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
sodium ion transmembrane transportSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
gamma-aminobutyric acid:sodium:chloride symporter activitySodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
protein bindingSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
gamma-aminobutyric acid transmembrane transporter activitySodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
sodium:chloride symporter activitySodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
identical protein bindingSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
metal ion bindingSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
gamma-aminobutyric acid:sodium:chloride symporter activitySodium- and chloride-dependent betaine transporterHomo sapiens (human)
protein bindingSodium- and chloride-dependent betaine transporterHomo sapiens (human)
monocarboxylic acid transmembrane transporter activitySodium- and chloride-dependent betaine transporterHomo sapiens (human)
amino acid transmembrane transporter activitySodium- and chloride-dependent betaine transporterHomo sapiens (human)
gamma-aminobutyric acid:sodium:chloride symporter activitySodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
taurine:sodium symporter activitySodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
monocarboxylic acid transmembrane transporter activitySodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
amino acid bindingSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
amino acid:sodium symporter activitySodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
creatine transmembrane transporter activitySodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
gamma-aminobutyric acid:sodium:chloride symporter activitySodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
taurine transmembrane transporter activitySodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
taurine:sodium symporter activitySodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
monocarboxylic acid transmembrane transporter activitySodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
amino acid transmembrane transporter activitySodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
gamma-aminobutyric acid transmembrane transporter activitySodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
plasma membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
plasma membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
axonSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
presynaptic membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
neuronal cell bodySodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
postsynaptic membraneSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
GABA-ergic synapseSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
axonSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
cell surfaceSodium- and chloride-dependent GABA transporter 1Homo sapiens (human)
plasma membraneSodium- and chloride-dependent betaine transporterHomo sapiens (human)
membraneSodium- and chloride-dependent betaine transporterHomo sapiens (human)
basolateral plasma membraneSodium- and chloride-dependent betaine transporterHomo sapiens (human)
presynapseSodium- and chloride-dependent betaine transporterHomo sapiens (human)
cell projectionSodium- and chloride-dependent betaine transporterHomo sapiens (human)
plasma membraneSodium- and chloride-dependent betaine transporterHomo sapiens (human)
plasma membraneSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
membraneSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
presynaptic membraneSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
postsynaptic membraneSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
GABA-ergic synapseSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
plasma membraneSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
cell projectionSodium- and chloride-dependent GABA transporter 3Homo sapiens (human)
plasma membraneSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
basolateral plasma membraneSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
extracellular exosomeSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
presynapseSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
plasma membraneSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
cell projectionSodium- and chloride-dependent GABA transporter 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (60)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
AID1476548Inhibition of human BGT1 I386F mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476545Inhibition of human BGT1 S381A mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476516Inhibition of human GAT3 expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476554Inhibition of human BGT1/human GAT3 chimera C expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476521Displacement of [3H]GR125743 from human 5-HT1D receptor expressed in HEKT cell membranes at 10 uM after 90 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476543Inhibition of human BGT1 F367Y mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476553Inhibition of human BGT1/human GAT3 chimera B expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476555Inhibition of human BGT1/human GAT3 chimera D expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476536Inhibition of human BGT1 A328G mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476531Inhibition of human BGT1 K310N mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476530Inhibition of human BGT1 Q299L mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476518Inhibition of mouse BGT1 expressed in HEK293 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476547Inhibition of human BGT1 I386M mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476546Inhibition of human BGT1 C382T mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476533Inhibition of human BGT1 K317R mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476507Inhibition of human GAT3 L314Q mutant expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476540Inhibition of human BGT1 S345A mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476535Inhibition of human BGT1 F324C mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476526Displacement of [3H]rauwolscine from human alpha-2C adrenergic receptor expressed in MDCK cell membranes at 10 uM after 90 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476532Inhibition of human BGT1 H312N mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476537Inhibition of human BGT1 V336A mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476539Inhibition of human BGT1 I340V mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476524Displacement of [3H]N-methylspiperone from human Dopamine receptor D2 receptor expressed in fibroblast cell membranes at 10 uM after 90 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476538Inhibition of human BGT1 V337I mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476550Inhibition of human BGT1 Y453A mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476542Inhibition of human BGT1 S353A mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476527Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in HEK cell membranes at 10 uM after 90 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476541Inhibition of human BGT1 Q346Y mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476529Inhibition of human BGT1 F295Y mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476515Inhibition of human GAT2 expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476523Displacement of [3H]SCH23390 from human Dopamine receptor D1 receptor expressed in HEKT cell membranes at 10 uM after 90 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476520Inhibition of mouse GAT3 expressed in HEK293 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476552Inhibition of human GAT3 S468Y mutant expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476534Inhibition of human BGT1 A321M mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476544Inhibition of human BGT1 Q378P mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476513Inhibition of human GAT1 expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476551Inhibition of human BGT1 Y453S/Y454A double mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476517Inhibition of mouse GAT1 expressed in HEK293 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476514Inhibition of human BGT1 expresses in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476522Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes at 10 uM after 90 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476549Inhibition of human BGT1 Y453S mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476508Solubility of compound in pH 7.4 phosphate buffer after 24 hrs by HPLC-UV method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476519Inhibition of mouse GAT2 expressed in HEK293 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1476525Displacement of [3H]N-methylspiperone from human Dopamine receptor D4 receptor at 10 uM after 90 mins by scintillation counting method2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159536qHTS Confirmatory assay for TAG accumulators in algae2017Plant physiology, Aug, Volume: 174, Issue:4
Identification and Metabolite Profiling of Chemical Activators of Lipid Accumulation in Green Algae.
AID1159537qHTS screening for TAG (triacylglycerol) accumulators in algae2017Plant physiology, Aug, Volume: 174, Issue:4
Identification and Metabolite Profiling of Chemical Activators of Lipid Accumulation in Green Algae.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (10.00)29.6817
2010's7 (70.00)24.3611
2020's2 (20.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.11

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 Index12.11 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.11)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other10 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]