Pharos : Ligand Details - naltrexone

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Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.

Ligand Summary

Ligand Structure

chemical structure image

Synonyms & Links

UNII: 5S6W795CQM

PubChem: 5360515

Guide to Pharmacology: 1639

ChEMBL: CHEMBL19019

DrugCentral: 1765

LyCHI: MT269CKQJVMQ

Target Activities

OPRM1

Tclin

Mu-type opioid receptor

42 Activities

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1 – 10 of 42

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	7.81		Bioorg. Med. Chem., (2015) 23:8:1701	25783191

IC50	8.05		None, (2015) None:None:None

IC50	8.05		None, (2015) None:None:None

IC50	8.05		MedChemComm, (2013) 4:5:847	23682308

IC50	8.39		None, None:None:None

IC50	8.41		Bioorg. Med. Chem., (2013) 21:21:6405	24055076

Ki	8.57		Bioorg. Med. Chem. Lett., (2011) 21:13:4001	21621410

Ki	8.73		Bioorg. Med. Chem., (2013) 21:21:6405	24055076

Ki	8.78		None, None:None:None

Ki	8.94		Bioorg. Med. Chem. Lett., (2011) 21:13:4001	21621410

OPRD1

Tclin

Delta-type opioid receptor

40 Activities

Items per page:

1 – 10 of 40

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
Ki	7.02		J. Med. Chem., (2003) 46:10:1775	12723940

Ki	7.02		J. Med. Chem., (1998) 41:26:5188	9857089

Ki	7.02		Bioorg. Med. Chem. Lett., (2013) 23:13:3719	23721804

Ki	7.02		J. Med. Chem., (2013) 56:22:9156	24144240

Ki	7.06		None, None:None:None

Ki	7.22		Bioorg. Med. Chem. Lett., (2005) 15:8:2107	15808478

Ki	7.22		Bioorg. Med. Chem. Lett., (2009) 19:1:203	19027293

Ki	7.22		Bioorg. Med. Chem. Lett., (2009) 19:8:2289	19282177

Ki	7.42		J. Med. Chem., (2007) 50:9:2254	17407276

Ki	7.44		J. Med. Chem., (1990) 33:6:1714	2160538

OPRK1

Tclin

Kappa-type opioid receptor

26 Activities

Items per page:

1 – 10 of 26

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	7.75		None, None:None:None

Ki	8.14		None, None:None:None

Ki	8.28		Bioorg. Med. Chem. Lett., (2007) 17:19:5349	17720493

Ki	8.28		Bioorg. Med. Chem. Lett., (2007) 17:24:6841	17980586

Ki	8.29		J. Med. Chem., (2009) 52:5:1416	19199782

Ki	8.29		Bioorg. Med. Chem. Lett., (2009) 19:6:1825	19217280

Ki	8.36		J. Med. Chem., (2006) 49:25:7278	17149858

Ki	8.36		J. Med. Chem., (2006) 49:25:7290	17149859

Ki	9.05		Bioorg. Med. Chem. Lett., (2013) 23:13:3719	23721804

Ki	9.05		J. Med. Chem., (2013) 56:22:9156	24144240

CYP2D6

Tclin

Cytochrome P450 2D6

1 Activities

Items per page:

1 – 1 of 1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	6		None, None:None:None