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Target
Mu-type opioid receptor
Ligand
BDBM21011
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
46±n/a nM
EC50
29±n/a nM
Citation
 Yamamoto, T; Nair, P; Vagner, J; Largent-Milnes, T; Davis, P; Ma, SW; Navratilova, E; Moye, S; Tumati, S; Lai, J; Yamamura, HI; Vanderah, TW; Porreca, F; Hruby, VJ A Structure-Activity Relationship Study and Combinatorial Synthetic Approach of C-Terminal Modified Bifunctional Peptides That Are delta/mu Opioid Receptor Agonists and Neurokinin 1 Receptor Antagonists. J Med Chem 51:1369-76 (2008) [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:
BDBM21011
Synonyms:
(2S)-2-{[(2S)-1-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-phenylpropanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-[benzyl(methyl)carbamoyl]-2-(1H-indol-3-yl)ethyl]-4-methylpentanamide | C-terminal modified bifunctional peptide, 4 | H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-Bzl
Type:
Peptide-like ligand
Emp. Form.:
C53H65N9O8
Mol. Mass.:
956.1387
SMILES:
CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N(C)Cc1ccccc1
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:
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