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Target
Mu-type opioid receptor
Ligand
BDBM21014
Substrate
n/a
Meas. Tech.
ChEMBL_1437484 (CHEMBL3387855)
Ki
2.6±n/a nM
Citation
 Mollica, A; Carotenuto, A; Novellino, E; Limatola, A; Costante, R; Pinnen, F; Stefanucci, A; Pieretti, S; Borsodi, A; Samavati, R; Zador, F; Benyhe, S; Davis, P; Porreca, F; Hruby, VJ Novel cyclic biphalin analogue with improved antinociceptive properties. ACS Med Chem Lett 5:1032-6 (2014) [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:
BDBM21014
Synonyms:
(2S)-2-amino-N-[(1R)-1-[({[(1S)-1-{N'-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-phenylpropanoyl]hydrazinecarbonyl}-2-phenylethyl]carbamoyl}methyl)carbamoyl]ethyl]-3-(4-hydroxyphenyl)propanamide | (Tyr-Ala-Gly-Phe-NH2)2 | Biphalin | CHEMBL200199 | bis(Tyr-Ala-Gly-PheNH2)hydrazide | enkephalin dimer
Type:
Analgesics
Emp. Form.:
C46H56N10O10
Mol. Mass.:
908.9978
SMILES:
C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1
Structure:
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