Reaction Details Report a problem with these data
Target
Mu-type opioid receptor
Ligand
BDBM50139013
Substrate
n/a
Meas. Tech.
ChEMBL_2145911 (CHEMBL5030191)
Ki
6.1±n/a nM
Citation
Zhang, YZ; Wang, MM; Wang, SY; Wang, XF; Yang, WJ; Zhao, YN; Han, FT; Zhang, Y; Gu, N; Wang, CL Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. J Med Chem 64:16801-16819 (2021) [PubMed] Article
More Info.:
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:
BDBM50139013
Synonyms:
(S)-1-[(S)-2-Amino-3-(4-hydroxy-phenyl)-propionyl]-pyrrolidine-2-carboxylic acid [(S)-1-((S)-1-carbamoyl-2-phenyl-ethylcarbamoyl)-2-phenyl-ethyl]-amide | (S)-N-((S)-1-((S)-1-amino-1-oxo-3-phenylpropan-2-ylamino)-1-oxo-3-phenylpropan-2-yl)-1-((S)-2-amino-3-(4-hydroxyphenyl)propanoyl)pyrrolidine-2-carboxamide | 1-[(S)-2-Amino-3-(4-hydroxy-phenyl)-propionyl]-pyrrolidine-2-carboxylicacid[1-((S)-(S)-1-carbamoyl-2-phenyl-ethylcarbamoyl)-2-phenyl-ethyl]-amide | CHEMBL333357 | H-Tyr-Pro-Phe-Phe-NH2 | Tyr-Pro-Phe-Phe-NH2 | endomorphin-2
Type:
Small organic molecule
Emp. Form.:
C32H37N5O5
Mol. Mass.:
571.6667
SMILES:
N[C@@H](Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O |r|