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Target
Mu-type opioid receptor
Ligand
BDBM50199863
Substrate
n/a
Meas. Tech.
ChEMBL_441142 (CHEMBL891361)
Ki
0.26±n/a nM
Citation
 Li, T; Jinsmaa, Y; Nedachi, M; Miyazaki, A; Tsuda, Y; Ambo, A; Sasaki, Y; Bryant, SD; Marczak, E; Li, Q; Swartzwelder, HS; Lazarus, LH; Okada, Y Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists. Bioorg Med Chem 15:1237-51 (2007) [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:
BDBM50199863
Synonyms:
(S)-1-((S)-2-(allylamino)-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl)-N-((S)-1-((S)-1-amino-1-oxo-3-phenylpropan-2-ylamino)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)pyrrolidine-2-carboxamide | CHEMBL412924
Type:
Small organic molecule
Emp. Form.:
C39H46N6O5
Mol. Mass.:
678.8197
SMILES:
Cc1cc(O)cc(C)c1C[C@H](NCC=C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O
Structure:
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