duloxetine
Ligand Summary
A thiophene derivative and selective NEUROTRANSMITTER UPTAKE INHIBITOR for SEROTONIN and NORADRENALINE (SNRI). It is an ANTIDEPRESSIVE AGENT and ANXIOLYTIC, and is also used for the treatment of pain in patients with DIABETES MELLITUS and FIBROMYALGIA.
UNII: O5TNM5N07U
PubChem: 60835
Guide to Pharmacology: 202
ChEMBL: CHEMBL1175
DrugCentral: 972
LyCHI: 1UF6FFVNYYNG
Target Activities
SLC6A4
Sodium-dependent serotonin transporter
24 Activities
Items per page:
1 – 10 of 24
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 8.3 | |||||
Ki | 9.62 | ACS Med. Chem. Lett., (2013) 4:6:560 | ||||
IC50 | 9.5 | Bioorg. Med. Chem. Lett., (2013) 23:5:1456 | ||||
Ki | 9.3 | Bioorg. Med. Chem. Lett., (2009) 19:16:4630 | ||||
Ki | 9.1 | Bioorg. Med. Chem. Lett., (2003) 13:24:4477 | ||||
IC50 | 8.64 | ACS Med. Chem. Lett., (2013) 4:6:560 | ||||
IC50 | 8.52 | Bioorg. Med. Chem. Lett., (2009) 19:9:2464 | ||||
IC50 | 8.52 | Bioorg. Med. Chem. Lett., (2008) 18:18:4929 | ||||
IC50 | 8.52 | Bioorg. Med. Chem. Lett., (2010) 20:9:2809 | ||||
IC50 | 8.4 | Bioorg. Med. Chem. Lett., (2009) 19:10:2829 | ||||
SLC6A2
Sodium-dependent noradrenaline transporter
22 Activities
Items per page:
1 – 10 of 22
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 8.22 | |||||
IC50 | 8.8 | Bioorg. Med. Chem. Lett., (2013) 23:5:1456 | ||||
IC50 | 8.4 | Bioorg. Med. Chem. Lett., (2009) 19:9:2464 | ||||
IC50 | 8.4 | Bioorg. Med. Chem. Lett., (2008) 18:18:4929 | ||||
IC50 | 8.4 | Bioorg. Med. Chem. Lett., (2010) 20:9:2809 | ||||
IC50 | 8.3 | Bioorg. Med. Chem. Lett., (2009) 19:10:2829 | ||||
Ki | 8.22 | Bioorg. Med. Chem. Lett., (2012) 22:23:7219 | ||||
Ki | 8.17 | ACS Med. Chem. Lett., (2013) 4:6:560 | ||||
Ki | 8.12 | Bioorg. Med. Chem. Lett., (2003) 13:24:4477 | ||||
Ki | 8.1 | Bioorg. Med. Chem. Lett., (2009) 19:16:4630 | ||||
SLC6A3
Sodium-dependent dopamine transporter
16 Activities
Items per page:
1 – 10 of 16
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 6.62 | Bioorg. Med. Chem. Lett., (2003) 13:24:4477 | ||||
Ki | 6.6 | Bioorg. Med. Chem. Lett., (2009) 19:16:4630 | ||||
Ki | 6.5 | Bioorg. Med. Chem. Lett., (2013) 23:5:1456 | ||||
Ki | 6.43 | J. Med. Chem., (2005) 48:21:6523 | ||||
Ki | 6.36 | Bioorg. Med. Chem. Lett., (2008) 18:8:2562 | ||||
Ki | 6.36 | Bioorg. Med. Chem. Lett., (2009) 19:17:5078 | ||||
Ki | 6.36 | Bioorg. Med. Chem. Lett., (2010) 20:12:3788 | ||||
Ki | 6.32 | ACS Med. Chem. Lett., (2013) 4:6:560 | ||||
IC50 | 6.23 | Bioorg. Med. Chem. Lett., (2009) 19:10:2829 | ||||
IC50 | 6.18 | Bioorg. Med. Chem. Lett., (2008) 18:4:1346 | ||||
KCNH2
Potassium voltage-gated channel subfamily H member 2
3 Activities
Items per page:
1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 5.3 | J Pharmacol Toxicol Methods, (2014) 70:None:246 | ||||
IC50 | 5.2 | J Pharmacol Toxicol Methods, (2014) 70:None:246 | ||||
IC50 | 5 | J Pharmacol Toxicol Methods, (2014) 70:None:246 | ||||
CYP3A4
Cytochrome P450 3A4
2 Activities
HTR2A
5-hydroxytryptamine receptor 2A
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
6.3 | ||||||
HTR2C
5-hydroxytryptamine receptor 2C
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
6 | ||||||
HTR6
5-hydroxytryptamine receptor 6
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
6.4 | ||||||
SCN5A
Sodium channel protein type 5 subunit alpha
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 5.1 | J Pharmacol Toxicol Methods, (2014) 70:None:246 | ||||
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 | Bioorg. Med. Chem. Lett., (2009) 19:10:2829 | ||||