Target
Mu-type opioid receptor
Ligand
BDBM21127
Substrate
BDBM21015
Meas. Tech.
Radioligand Labeled Binding Assay
pH
7.4±n/a
Temperature
298.15±n/a K
Ki
56.9±3.5 nM
Citation
 Mollica, AGuardiani, GDavis, PMa, SWPorreca, FLai, JMannina, LSobolev, APHruby, VJ Synthesis of Stable and Potent delta/mu Opioid Peptides: Analogues of H-Tyr-c[d-Cys-Gly-Phe-d-Cys]-OH by Ring-Closing Metathesis. J Med Chem 50:3138-3142 (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:
BDBM21127
Synonyms:
(5S,8R,13R)-13-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]-5-benzyl-3,6,14-trioxo-1,4,7-triazacyclotetradecane-8-carboxylic acid | rDADAE (11) | reduced bond-c[2-D-allylglycine, 5-D-allylglycine]enkephalin | single bond H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH
Type:
Cyclic Peptide
Emp. Form.:
C28H35N5O7
Mol. Mass.:
553.6068
SMILES:
N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CCCC[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O)C(O)=O
Structure:
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Substrate
Name:
BDBM21015
Synonyms:
(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]-N-methylacetamido}-N-(2-hydroxyethyl)-3-phenylpropanamide | 2-Ala-4-MePhe-5-Gly-Enkephalin | CHEMBL38874 | D-Ala2-MePhe4-Met(0)5-enkephalin-ol | DAMGO | RX 783006 | US11492374, ID 2 | [3H]DAMGO | [tyrosyl-3,5-3H(N)]-D-Ala2-Mephe4-glyol5-enkephalin
Type:
Analgesics
Emp. Form.:
C26H35N5O6
Mol. Mass.:
513.586
SMILES:
C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(C)[C@@H](Cc1ccccc1)C(=O)NCCO
Structure:
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