naloxone
Ligand Summary
A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.
UNII: 36B82AMQ7N
PubChem: 44666320
PubChem: 5284596
Guide to Pharmacology: 1638
Guide to Pharmacology: 1676
ChEMBL: CHEMBL1718
ChEMBL: CHEMBL80
DrugCentral: 1878
LyCHI: DPQP2SH7AKWH
Target Activities
OPRM1
Mu-type opioid receptor
40 Activities
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1 – 10 of 40
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
- | 8.9 | |||||
9 | ||||||
9 | ||||||
Kd | 9.66 | J. Med. Chem., (2007) 50:3:512 | ||||
Kd | 9.66 | Bioorg. Med. Chem. Lett., (2008) 18:4:1350 | ||||
Ki | 9.64 | Bioorg. Med. Chem., (2011) 19:9:2808 | ||||
Ki | 9.25 | Bioorg. Med. Chem., (2009) 17:14:5080 | ||||
Ki | 9.24 | Bioorg. Med. Chem. Lett., (2011) 21:13:4001 | ||||
Ki | 9.18 | Bioorg. Med. Chem. Lett., (2009) 19:1:203 | ||||
Ki | 9.1 | J. Med. Chem., (2007) 50:9:2254 | ||||
OPRD1
Delta-type opioid receptor
22 Activities
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1 – 10 of 22
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
7.8 | ||||||
- | 7.2 | |||||
6.2 | ||||||
Ki | 7.72 | J. Med. Chem., (1994) 37:19:3121 | ||||
Ki | 7.67 | Bioorg. Med. Chem., (2009) 17:14:5080 | ||||
Ki | 7.52 | J. Nat. Prod., (2015) 78:6:1461 | ||||
Ki | 7.48 | Bioorg. Med. Chem. Lett., (2003) 13:24:4459 | ||||
Ki | 7.48 | J. Med. Chem., (2006) 49:25:7290 | ||||
Ki | 7.48 | J. Med. Chem., (2006) 49:25:7278 | ||||
Ki | 7.48 | Bioorg. Med. Chem. Lett., (2008) 18:6:2006 | ||||
OPRK1
Kappa-type opioid receptor
20 Activities
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1 – 10 of 20
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
8.3 | ||||||
Ki | 9.6 | Bioorg. Med. Chem., (2011) 19:9:2808 | ||||
Ki | 8.96 | J. Med. Chem., (2007) 50:9:2254 | ||||
Ki | 8.92 | Bioorg. Med. Chem. Lett., (2000) 10:6:523 | ||||
Ki | 8.92 | Bioorg. Med. Chem. Lett., (2009) 19:1:203 | ||||
IC50 | 8.82 | J. Med. Chem., (2001) 44:21:3378 | ||||
Ki | 8.52 | J. Med. Chem., (2010) 53:3:1392 | ||||
Ki | 8.35 | Bioorg. Med. Chem., (2009) 17:14:5080 | ||||
EC50 | 8.18 | J. Med. Chem., (2003) 46:11:2104 | ||||
Ki | 8.04 | Bioorg. Med. Chem. Lett., (2003) 13:24:4459 | ||||
ADORA3
Adenosine receptor A3
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.8 | |||||