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Target
Mu-type opioid receptor
Ligand
BDBM50323868
Substrate
n/a
Meas. Tech.
ChEMBL_647574 (CHEMBL1217621)
EC50
130±n/a nM
Citation
 Yamamoto, T; Nair, P; Jacobsen, NE; Kulkarni, V; Davis, P; Ma, SW; Navratilova, E; Yamamura, HI; Vanderah, TW; Porreca, F; Lai, J; Hruby, VJ Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines. J Med Chem 53:5491-501 (2010) [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:
BDBM50323868
Synonyms:
(S)-1-((4R,7S,13R)-13-((S)-2-amino-3-(4-hydroxyphenyl)propanamido)-7-benzyl-3,3,14,14-tetramethyl-6,9,12-trioxo-1,2-dithia-5,8,11-triazacyclotetradecane-4-carbonyl)-N-((S)-1-((S)-1-(3,5-bis(trifluoromethyl)benzylamino)-3-(1H-indol-3-yl)-1-oxopropan-2-ylamino)-4-methyl-1-oxopentan-2-yl)pyrrolidine-2-carboxamide | CHEMBL1214025
Type:
Small organic molecule
Emp. Form.:
C61H72F6N10O9S2
Mol. Mass.:
1267.406
SMILES:
CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(C)(C)SSC1(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(cc(c1)C(F)(F)F)C(F)(F)F |r|
Structure:
Search PDB for entries with ligand similarity: