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Target
Mu-type opioid receptor
Ligand
BDBM50266025
Substrate
n/a
Meas. Tech.
ChEMBL_540202 (CHEMBL1029831)
Ki
0.16±n/a nM
Citation
 Ballet, S; Feytens, D; Wachter, RD; Vlaeminck, MD; Marczak, ED; Salvadori, S; Graaf, C; Rognan, D; Negri, L; Lattanzi, R; Lazarus, LH; Tourwé, D; Balboni, G Conformationally constrained opioid ligands: the Dmt-Aba and Dmt-Aia versus Dmt-Tic scaffold. Bioorg Med Chem Lett 19:433-7 (2008) [PubMed]  Article 
Target
Name:
Mu-type opioid receptor
Synonyms:
MOR-1 | MUOR1 | Mu-type opioid receptor (MOR) | OPIATE Mu | OPRM_RAT | Opiate non-selective | Opioid receptor B | Oprm1 | Ror-b
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
44503.11
Organism:
Rattus norvegicus (rat)
Description:
Competition binding assays were carried out using membrane preparations from transfected HN9.10 cells that constitutively expressed the mu opioid receptor.
Residue:
398
Sequence:
MDSSTGPGNTSDCSDPLAQASCSPAPGSWLNLSHVDGNQSDPCGLNRTGLGGNDSLCPQTGSPSMVTAITIMALYSIVCVVGLFGNFLVMYVIVRYTKMKTATNIYIFNLALADALATSTLPFQSVNYLMGTWPFGTILCKIVISIDYYNMFTSIFTLCTMSVDRYIAVCHPVKALDFRTPRNAKIVNVCNWILSSAIGLPVMFMATTKYRQGSIDCTLTFSHPTWYWENLLKICVFIFAFIMPVLIITVCYGLMILRLKSVRMLSGSKEKDRNLRRITRMVLVVVAVFIVCWTPIHIYVIIKALITIPETTFQTVSWHFCIALGYTNSCLNPVLYAFLDENFKRCFREFCIPTSSTIEQQNSTRVRQNTREHPSTANTVDRTNHQLENLEAETAPLP
  
Inhibitor
Name:
BDBM50266025
Synonyms:
(S)-2-((S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl)-N-(2-(benzylamino)-2-oxoethyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide | 2-[2-Amino-3-(4-hydroxy-2,6-dimethyl-phenyl)-propionyl]-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid (benzylcarbamoyl-methyl)-amide | CHEMBL458631 | H-Dmt-Tic-Gly-NH-Bzl | H-Dmt-Tic-Gly-NH-CH2-Ph
Type:
Small organic molecule
Emp. Form.:
C30H34N4O4
Mol. Mass.:
514.6154
SMILES:
Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C(=O)NCC(=O)NCc1ccccc1 |r|
Structure:
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