Page last updated: 2024-11-11

nnc 05-2090

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

NNC 05-2090: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9888030
CHEMBL ID1446457
CHEBI ID93487
SCHEMBL ID4293184
MeSH IDM0279486

Synonyms (20)

Synonym
BRD-K85015012-003-01-1
nnc052090
NCGC00167843-01
CHEMBL1446457 ,
bdbm50419338
1-[3-(9h-carbazol-9-yl)propyl]-4-(2-methoxyphenyl)piperidin-4-ol
nnc 05-2090
gtpl4610
SCHEMBL4293184
nnc-05-2090
CHEBI:93487
1-(3-(9h-carbazol-9-yl)-1-propyl)-4-(2-methoxyphenyl)-4-piperidinol
nnc05-2090
1-(3-(9h-carbazol-9-yl)propyl)-4-(2-methoxyphenyl)piperidin-4-ol
Q27087962
nnc-052090
nnc 052090
AKOS040749033
HY-120146
CS-0077017

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" In addition, BGT-1 deficiency or dosing with NNC 05-2090 stimulated the expression of the anti-apoptotic gene, c-Met in the liver, suggesting the involvement of c-Met in the function on hepatocytes of BGT-1 apoptosis."( Betaine/GABA transporter-1 (BGT-1) deficiency in mouse prevents acute liver failure in vivo and hepatocytes apoptosis in vitro.
Ci, L; Fei, J; Huang, F; Huang, Q; Li, Q; Liu, Z; Lu, T; Shen, R; Shi, J; Sun, R; Wan, Z; Wang, Z; Yang, H; Yang, X; Zhang, M, 2020
)
0.82
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
carbazoles
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
phosphopantetheinyl transferaseBacillus subtilisPotency17.78280.141337.9142100.0000AID1490
[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)IC50 (µMol)11.40000.01013.090310.0000AID1188930
Sodium- and chloride-dependent GABA transporter 1Mus musculus (house mouse)IC50 (µMol)16.09580.03712.19228.5114AID1195448; AID631146; AID631154
Sodium- and chloride-dependent GABA transporter 1Mus musculus (house mouse)Ki19.00000.02750.05310.1862AID1476509
Sodium- and chloride-dependent GABA transporter 2Mus musculus (house mouse)IC50 (µMol)16.84701.41255.26838.1283AID1195450; AID631147; AID631155
Sodium- and chloride-dependent GABA transporter 3Mus musculus (house mouse)IC50 (µMol)20.65561.54883.67618.1283AID1195451; AID631148; AID631156; AID631157
Sodium- and chloride-dependent betaine transporterMus musculus (house mouse)IC50 (µMol)1.40000.18003.188010.0000AID1195449
Sodium- and chloride-dependent betaine transporterMus musculus (house mouse)Ki1.40001.40001.40001.4000AID1476512
Sodium- and chloride-dependent betaine transporterHomo sapiens (human)IC50 (µMol)5.10000.85116.052136.0000AID1188933; AID764975
Sodium- and chloride-dependent GABA transporter 3Homo sapiens (human)IC50 (µMol)8.92001.00004.13318.9200AID1188932
Sodium- and chloride-dependent GABA transporter 2Homo sapiens (human)IC50 (µMol)6.20006.20006.20006.2000AID1188931
[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 (25)

Assay IDTitleYearJournalArticle
AID1476510Inhibition of mouse GAT2 expressed in hamster BHK 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).
AID631157Inhibition of mouse GAT4-mediated [3H]GABA uptake expressed in BHK cells2011Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
Aminomethyltetrazoles as potential inhibitors of the γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation.
AID1195451Inhibition of mouse mGAT4 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
Structure activity relationship of selective GABA uptake inhibitors.
AID764975Inhibition of human BGT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Cyclopropane-based conformational restriction of GABA by a stereochemical diversity-oriented strategy: identification of an efficient lead for potent inhibitors of GABA transports.
AID1188930Inhibition of human GAT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Conformationally Restricted GABA with Bicyclo[3.1.0]hexane Backbone as the First Highly Selective BGT-1 Inhibitor.
AID1195448Inhibition of mouse mGAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
Structure activity relationship of selective GABA uptake inhibitors.
AID631155Inhibition of mouse GAT2-mediated [3H]GABA uptake expressed in BHK cells2011Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
Aminomethyltetrazoles as potential inhibitors of the γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation.
AID1188931Inhibition of human GAT2 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Conformationally Restricted GABA with Bicyclo[3.1.0]hexane Backbone as the First Highly Selective BGT-1 Inhibitor.
AID1195449Inhibition of mouse mGAT2 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
Structure activity relationship of selective GABA uptake inhibitors.
AID631147Inhibition of mouse GAT2-mediated [3H]GABA uptake expressed in human HEK cells2011Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
Aminomethyltetrazoles as potential inhibitors of the γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation.
AID1476509Inhibition of mouse GAT1 expressed in hamster BHK 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).
AID631146Inhibition of mouse GAT1-mediated [3H]GABA uptake expressed in human HEK cells2011Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
Aminomethyltetrazoles as potential inhibitors of the γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation.
AID1188933Inhibition of human BGT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Conformationally Restricted GABA with Bicyclo[3.1.0]hexane Backbone as the First Highly Selective BGT-1 Inhibitor.
AID631154Inhibition of mouse GAT1-mediated [3H]GABA uptake expressed in BHK cells2011Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
Aminomethyltetrazoles as potential inhibitors of the γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation.
AID631149Inhibition of mouse GAT4-mediated [3H]GABA uptake expressed in human HEK cells2011Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
Aminomethyltetrazoles as potential inhibitors of the γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation.
AID1195450Inhibition of mouse mGAT3 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
Structure activity relationship of selective GABA uptake inhibitors.
AID1188934Selectivity index, ratio of IC50 for human GAT3 to IC50 for human BGT12014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Conformationally Restricted GABA with Bicyclo[3.1.0]hexane Backbone as the First Highly Selective BGT-1 Inhibitor.
AID1476512Inhibition of mouse BGT1 expressed in hamster BHK 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).
AID631156Inhibition of mouse GAT3-mediated [3H]GABA uptake expressed in BHK cells2011Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
Aminomethyltetrazoles as potential inhibitors of the γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation.
AID631148Inhibition of mouse GAT3-mediated [3H]GABA uptake expressed in human HEK cells2011Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
Aminomethyltetrazoles as potential inhibitors of the γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation.
AID1188932Inhibition of human GAT3 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Conformationally Restricted GABA with Bicyclo[3.1.0]hexane Backbone as the First Highly Selective BGT-1 Inhibitor.
AID1476511Inhibition of mouse GAT3 expressed in hamster BHK 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).
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1346975Mouse BGT1 (GABA transporter subfamily)1997British journal of pharmacology, Mar, Volume: 120, Issue:6
1-(3-(9H-carbazol-9-yl)-1-propyl)-4-(2-methoxyphenyl)-4-piperidinol, a novel subtype selective inhibitor of the mouse type II GABA-transporter.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (18.18)18.2507
2000's0 (0.00)29.6817
2010's6 (54.55)24.3611
2020's3 (27.27)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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%
Other11 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]