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Target
Mu-type opioid receptor
Ligand
BDBM50272081
Substrate
n/a
Meas. Tech.
ChEMBL_148858 (CHEMBL756654)
Ki
0.16±n/a nM
Citation
 Balboni, G; Guerrini, R; Salvadori, S; Bianchi, C; Rizzi, D; Bryant, SD; Lazarus, LH Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties. J Med Chem 45:713-20 (2002) [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:
BDBM50272081
Synonyms:
2-[2-Amino-3-(4-hydroxy-2,6-dimethyl-phenyl)-propionyl]-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid phenylcarbamoylmethyl-amide | CHEMBL501451 | H-Dmt-Tic-Gly-NH-Ph
Type:
Small organic molecule
Emp. Form.:
C29H32N4O4
Mol. Mass.:
500.5888
SMILES:
Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C(=O)NCC(=O)Nc1ccccc1 |r|
Structure:
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