Target
Mu-type opioid receptor
Ligand
BDBM50393720
Substrate
n/a
Meas. Tech.
ChEMBL_856831 (CHEMBL2163096)
Ki
0.900000±n/a nM
Citation
 Breslin, HJDiamond, CJKavash, RWCai, CDyatkin, ABMiskowski, TAZhang, SPWade, PRHornby, PJHe, W Identification of a duald OR antagonist/µ OR agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d). Bioorg Med Chem Lett 22:4869-72 (2012) [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:
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:
BDBM50393720
Synonyms:
CHEMBL2159122 | CHEMBL3216329
Type:
Small organic molecule
Emp. Form.:
C32H37Cl2N5O5
Mol. Mass.:
642.573
SMILES:
Cl.Cl.COc1ccc(CN(C(C)c2nc(c[nH]2)-c2ccccc2)C(=O)C(N)Cc2c(C)cc(cc2C)C(N)=O)cc1C(O)=O
Structure:
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