Target
Mu-type opioid receptor
Ligand
BDBM21139
Substrate
BDBM21015
Meas. Tech.
Radioligand Labeled Binding Assay and [35S]GTP-gamma-S Binding Assay
pH
7.4±n/a
Temperature
298.15±n/a K
Ki
26±n/a nM
EC50
0.46±n/a nM
Citation
 Agnes, RSLee, YSDavis, PMa, SWBadghisi, HPorreca, FLai, JHruby, VJ Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors. J Med Chem 49:2868-75 (2006) [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:
BDBM21139
Synonyms:
(3S)-3-[(2S)-2-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]hexanamido]acetamido}-3-(1H-indol-3-yl)propanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid | CCK-Opioid Peptide, 9 | Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2
Type:
Peptide
Emp. Form.:
C47H61N9O10
Mol. Mass.:
912.0415
SMILES:
CCCC[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O
Structure:
Search PDB for entries with ligand similarity:
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:
Search PDB for entries with ligand similarity: