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Target
Mu-type opioid receptor
Ligand
BDBM50178754
Substrate
n/a
Meas. Tech.
ChEMBL_326436 (CHEMBL867594)
Ki
1.68±n/a nM
Citation
 Li, T; Fujita, Y; Shiotani, K; Miyazaki, A; Tsuda, Y; Ambo, A; Sasaki, Y; Jinsmaa, Y; Marczak, E; Bryant, SD; Salvadori, S; Lazarus, LH; Okada, Y Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists. J Med Chem 48:8035-44 (2005) [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:
BDBM50178754
Synonyms:
3,6-bis-(N,N-dimethyl-Dmt-Tic-NH-propyl)-2(1H)-pyrazinone | CHEMBL261905
Type:
Small organic molecule
Emp. Form.:
C57H72N8O7
Mol. Mass.:
981.231
SMILES:
CN(C)[C@@H](Cc1c(C)cc(O)cc1C)C(=O)N1Cc2ccccc2CC1C(=O)NCCCc1[nH]c(=O)c(CCCNC(=O)C2Cc3ccccc3CN2C(=O)[C@H](Cc2c(C)cc(O)cc2C)N(C)C)nc1C
Structure:
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