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Name | Mu-type opioid receptor |
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Species | Mus musculus (Mouse) |
Gene | Oprm1 |
Synonym | opioid receptor, mu 1 opioid receptor OP3 Mu receptor MOR-1 [ Show all ] |
Disease | N/A for non-human GPCRs |
Length | 398 |
Amino acid sequence | MDSSAGPGNISDCSDPLAPASCSPAPGSWLNLSHVDGNQSDPCGPNRTGLGGSHSLCPQTGSPSMVTAITIMALYSIVCVVGLFGNFLVMYVIVRYTKMKTATNIYIFNLALADALATSTLPFQSVNYLMGTWPFGNILCKIVISIDYYNMFTSIFTLCTMSVDRYIAVCHPVKALDFRTPRNAKIVNVCNWILSSAIGLPVMFMATTKYRQGSIDCTLTFSHPTWYWENLLKICVFIFAFIMPVLIITVCYGLMILRLKSVRMLSGSKEKDRNLRRITRMVLVVVAVFIVCWTPIHIYVIIKALITIPETTFQTVSWHFCIALGYTNSCLNPVLYAFLDENFKRCFREFCIPTSSTIEQQNSARIRQNTREHPSTANTVDRTNHQLENLEAETAPLP |
UniProt | P42866 |
Protein Data Bank | 4dkl, 5c1m, 6dde, 6ddf |
GPCR-HGmod model | N/A |
3D structure model | This structure is from PDB ID 4dkl. |
BioLiP | BL0416752, BL0416751, BL0321492, BL0224753, BL0224754, BL0224755,BL0224756, BL0321491 |
Therapeutic Target Database | N/A |
ChEMBL | CHEMBL2858 |
IUPHAR | 319 |
DrugBank | N/A |
Name | naltrexone |
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Molecular formula | C20H23NO4 |
IUPAC name | (4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-one |
Molecular weight | 341.407 |
Hydrogen bond acceptor | 5 |
Hydrogen bond donor | 2 |
XlogP | 1.9 |
Synonyms | HS-0002 Morphinan-6-one, 17-(cyclopropylmethyl)-4,5-alpha-epoxy-3,14-dihydroxy- Naltrexona (1S,5R,13R,17S)-4-(cyclopropylmethyl)-10,17-dihydroxy-12-oxa-4-azapentacyclo[9.6.1.0^{1,13}.0^{5,17}.0^{7,18}]octadeca-7,9,11(18)-trien-14-one Naltrexone (sustained release), elbion [ Show all ] |
Inchi Key | DQCKKXVULJGBQN-XFWGSAIBSA-N |
Inchi ID | InChI=1S/C20H23NO4/c22-13-4-3-12-9-15-20(24)6-5-14(23)18-19(20,16(12)17(13)25-18)7-8-21(15)10-11-1-2-11/h3-4,11,15,18,22,24H,1-2,5-10H2/t15-,18+,19+,20-/m1/s1 |
PubChem CID | 5360515 |
ChEMBL | CHEMBL19019 |
IUPHAR | 1639 |
BindingDB | 60212, 50000787 |
DrugBank | DB00704 |
Structure | |
Lipinski's druglikeness | This ligand satisfies Lipinski's rule of five. |
Parameter | Value | Reference | Database source |
---|---|---|---|
AD50 | 0.05 mg kg-1 | PMID8410998, PMID8410999 | ChEMBL |
Dose ratio | 50.2 - | PMID2409281 | ChEMBL |
EC50 | 0.16 nM | PMID23948248, PMID25783191 | ChEMBL |
EC50 | 0.16 nM | PMID25783191 | BindingDB |
Emax | 5.4 % | PMID23948248, PMID25783191 | ChEMBL |
Kd | 1.738 nM | PMID17962026 | ChEMBL |
Ke | 0.09 nM | PMID18062664 | ChEMBL |
Ke | 0.21 nM | PMID14736254 | ChEMBL |
Ke | 0.24 nM | PMID18062664 | ChEMBL |
Ke | 0.44 nM | PMID19253983 | ChEMBL |
Ke | 0.57 nM | PMID18062664 | ChEMBL |
Ki | 0.265 nM | PMID21889335 | ChEMBL |
Ki | 0.33 nM | PMID25783191 | BindingDB |
Ki | 0.33 nM | PMID23948248, PMID25783191 | ChEMBL |
Ki | 0.6457 nM | PMID23585918 | ChEMBL |
Ki | 0.646 nM | PMID23585918 | BindingDB |
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