naltrexone
Ligand Summary
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.
UNII: 5S6W795CQM
PubChem: 5360515
Guide to Pharmacology: 1639
ChEMBL: CHEMBL19019
DrugCentral: 1765
LyCHI: MT269CKQJVMQ
Target Activities
OPRD1
Delta-type opioid receptor
54 Activities
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1 – 10 of 54
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
- | 8 | |||||
6.8 | ||||||
Kd | 8.8 | J. Med. Chem., (2008) 51:6:1913 | ||||
EC50 | 8.36 | J. Med. Chem., (2013) 56:22:9156 | ||||
EC50 | 8.26 | J. Med. Chem., (2003) 46:14:3174 | ||||
IC50 | 8.26 | J. Med. Chem., (2006) 49:20:6104 | ||||
EC50 | 8.26 | Bioorg. Med. Chem., (2014) 22:15:4067 | ||||
Ki | 8.2 | ACS Med Chem Lett, (2019) 10:12:1641 | ||||
Ki | 8.19 | J. Med. Chem., (2006) 49:20:6104 | ||||
Ki | 8.18 | J. Med. Chem., (1985) 28:7:974 | ||||
OPRM1
Mu-type opioid receptor
52 Activities
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1 – 10 of 52
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 10.3 | J. Med. Chem., (2008) 51:6:1913 | ||||
Ki | 10.15 | Bioorg. Med. Chem. Lett., (2011) 21:13:4001 | ||||
Ki | 9.96 | Bioorg. Med. Chem. Lett., (2005) 15:8:2107 | ||||
Ki | 9.96 | Bioorg. Med. Chem. Lett., (2009) 19:1:203 | ||||
Ki | 9.96 | Bioorg. Med. Chem. Lett., (2009) 19:8:2289 | ||||
Ki | 9.8 | ACS Med Chem Lett, (2019) 10:12:1641 | ||||
Ki | 9.7 | J. Med. Chem., (2003) 46:8:1563 | ||||
Ki | 9.7 | J. Med. Chem., (2003) 46:14:3174 | ||||
Ki | 9.7 | J. Med. Chem., (2004) 47:21:5069 | ||||
Ki | 9.7 | J. Med. Chem., (2006) 49:17:5333 | ||||
OPRK1
Kappa-type opioid receptor
33 Activities
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1 – 10 of 33
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
9.2 | ||||||
Ki | 10.38 | Bioorg. Med. Chem., (2009) 17:18:6671 | ||||
Ki | 9.72 | Bioorg. Med. Chem. Lett., (2005) 15:8:2107 | ||||
Ki | 9.72 | Bioorg. Med. Chem. Lett., (2009) 19:1:203 | ||||
Ki | 9.72 | Bioorg. Med. Chem. Lett., (2009) 19:8:2289 | ||||
Ki | 9.6 | J. Med. Chem., (2007) 50:9:2254 | ||||
Ki | 9.4 | J. Med. Chem., (2003) 46:8:1563 | ||||
Ki | 9.4 | J. Med. Chem., (2003) 46:14:3174 | ||||
Ki | 9.4 | J. Med. Chem., (2004) 47:21:5069 | ||||
Ki | 9.4 | J. Med. Chem., (2006) 49:17:5333 | ||||
CYP2D6
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 | ||||