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Target
Sodium-dependent noradrenaline transporter
Ligand
BDBM436455
Substrate
n/a
Meas. Tech.
ChEMBL_2059157 (CHEMBL4714158)
Ki
356±n/a nM
Citation
 Díaz, JL; Cuevas, F; Pazos, G; Álvarez-Bercedo, P; Oliva, AI; Sarmentero, MÁ; Font, D; Jiménez-Aquino, A; Morón, M; Port, A; Pascual, R; Dordal, A; Portillo-Salido, E; Reinoso, RF; Vela, JM; Almansa, C Bicyclic Diazepinones as Dual Ligands of the ?2?-1 Subunit of Voltage-Gated Calcium Channels and the Norepinephrine Transporter. J Med Chem 64:2167-2185 (2021) [PubMed]  Article 
Target
Name:
Sodium-dependent noradrenaline transporter
Synonyms:
Monoamine transporter | NAT1 | NET | NET1 | Noradrenaline Transporter (NET) | Norepinephrine Transporter (NET) | Norepinephrine transporter protein (NET) | SC6A2_HUMAN | SLC6A2 | SLC6A5 | Sodium-dependent noradrenaline transporter (NET) | Solute carrier family 6 member 2
Type:
Multi-pass membrane protein
Mol. Mass.:
69337.72
Organism:
Homo sapiens (Human)
Description:
P23975
Residue:
617
Sequence:
MLLARMNPQVQPENNGADTGPEQPLRARKTAELLVVKERNGVQCLLAPRDGDAQPRETWGKKIDFLLSVVGFAVDLANVWRFPYLCYKNGGGAFLIPYTLFLIIAGMPLFYMELALGQYNREGAATVWKICPFFKGVGYAVILIALYVGFYYNVIIAWSLYYLFSSFTLNLPWTDCGHTWNSPNCTDPKLLNGSVLGNHTKYSKYKFTPAAEFYERGVLHLHESSGIHDIGLPQWQLLLCLMVVVIVLYFSLWKGVKTSGKVVWITATLPYFVLFVLLVHGVTLPGASNGINAYLHIDFYRLKEATVWIDAATQIFFSLGAGFGVLIAFASYNKFDNNCYRDALLTSSINCITSFVSGFAIFSILGYMAHEHKVNIEDVATEGAGLVFILYPEAISTLSGSTFWAVVFFVMLLALGLDSSMGGMEAVITGLADDFQVLKRHRKLFTFGVTFSTFLLALFCITKGGIYVLTLLDTFAAGTSILFAVLMEAIGVSWFYGVDRFSNDIQQMMGFRPGLYWRLCWKFVSPAFLLFVVVVSIINFKPLTYDDYIFPPWANWVGWGIALSSMVLVPIYVIYKFLSTQGSLWERLAYGITPENEHHLVAQRDIRQFQLQHWLAI
  
Inhibitor
Name:
BDBM436455
Synonyms:
2-(dimethylamino)-9- methyl-6-(3-(3- (methylamino)-1- (thiophen-2- yl)propoxy)phenyl)- 6,7,8,9-tetrahydro-5H- pyrimido[4,5- e][1,4]diazepin-5-one | US10590140, Example 230
Type:
Small organic molecule
Emp. Form.:
C24H30N6O2S
Mol. Mass.:
466.599
SMILES:
CNCCC(Oc1cccc(c1)N1CCN(C)c2nc(ncc2C1=O)N(C)C)c1cccs1
Structure:
Search PDB for entries with ligand similarity: