clozapine
A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.
Ligand Summary
Target Activities
DRD4
D(4) dopamine receptor
60 Activities
Items per page:
1 – 10 of 60
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7 | MedChemComm, (2012) 3:5:580 | ||||
Ki | 7.14 | Bioorg. Med. Chem. Lett., (1997) 7:9:1207 | ||||
Ki | 7.15 | J. Med. Chem., (1995) 38:25:4950 | ||||
Ki | 7.16 | J. Med. Chem., (1997) 40:1:1 | ||||
Ki | 7.22 | Eur. J. Med. Chem., (2013) 62:None:214 | ||||
Ki | 7.22 | Eur. J. Med. Chem., (2013) 66:None:122 | ||||
IC50 | 7.24 | J. Med. Chem., (1996) 39:20:4044 | ||||
Ki | 7.27 | Bioorg. Med. Chem. Lett., (2003) 13:21:3779 | ||||
Ki | 7.27 | Bioorg. Med. Chem. Lett., (2003) 13:21:3779 | ||||
Ki | 7.27 | Bioorg. Med. Chem., (2008) 16:15:7291 | ||||
DRD2
D(2) dopamine receptor
38 Activities
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1 – 10 of 38
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7.04 | J. Med. Chem., (1997) 40:17:2688 | ||||
Ki | 7.04 | J. Med. Chem., (1997) 40:25:4026 | ||||
Ki | 7.05 | Eur. J. Med. Chem., (2014) 77:None:91 | ||||
Ki | 7.05 | Eur. J. Med. Chem., (2014) 77:None:91 | ||||
Ki | 7.08 | Bioorg. Med. Chem. Lett., (2009) 19:2:538 | ||||
Ki | 7.11 | Bioorg. Med. Chem. Lett., (2004) 14:16:4263 | ||||
Ki | 7.13 | J. Med. Chem., (1996) 39:10:1941 | ||||
Ki | 7.13 | J. Med. Chem., (1996) 39:10:1943 | ||||
Ki | 7.13 | J. Med. Chem., (1997) 40:15:2374 | ||||
Ki | 7.13 | Bioorg. Med. Chem. Lett., (1999) 9:9:1285 | ||||
HTR2A
5-hydroxytryptamine receptor 2A
34 Activities
Items per page:
1 – 10 of 34
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7.44 | J. Med. Chem., (2013) 56:3:1211 | ||||
Ki | 7.44 | J. Med. Chem., (2013) 56:3:1211 | ||||
Ki | 7.75 | J. Nat. Prod., (2015) 78:4:722 | ||||
Ki | 7.82 | MedChemComm, (2015) 6:4:601 | ||||
Ki | 7.82 | Bioorg. Med. Chem. Lett., (2016) 26:14:3216 | ||||
IC50 | 7.92 | J. Med. Chem., (1996) 39:20:4044 | ||||
Ki | 8 | MedChemComm, (2012) 3:5:580 | ||||
Ki | 8 | J. Med. Chem., (2014) 57:22:9578 | ||||
Ki | 8.02 | None, (2013) None:None:None | ||||
Ki | 8.02 | None, (2013) None:None:None | ||||
HTR2C
5-hydroxytryptamine receptor 2C
27 Activities
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1 – 10 of 27
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7 | MedChemComm, (2012) 3:5:580 | ||||
Ki | 7.62 | Eur. J. Med. Chem., (2013) 62:None:214 | ||||
Ki | 7.64 | Eur. J. Med. Chem., (2013) 66:None:122 | ||||
Ki | 7.68 | J. Med. Chem., (2005) 48:6:1709 | ||||
Ki | 7.77 | Bioorg. Med. Chem., (2008) 16:15:7291 | ||||
Ki | 7.8 | J. Med. Chem., (1999) 42:15:2774 | ||||
Ki | 7.8 | J. Med. Chem., (2002) 45:1:54 | ||||
Ki | 7.82 | Bioorg. Med. Chem. Lett., (2010) 20:18:5431 | ||||
Ki | 7.89 | None, (2013) None:None:None | ||||
Ki | 7.89 | None, (2013) None:None:None | ||||
HTR6
5-hydroxytryptamine receptor 6
16 Activities
Items per page:
1 – 10 of 16
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7 | MedChemComm, (2012) 3:5:580 | ||||
Ki | 7.77 | Bioorg. Med. Chem. Lett., (2010) 20:18:5431 | ||||
Ki | 7.77 | J. Med. Chem., (2012) 55:12:5704 | ||||
IC50 | 7.77 | Bioorg. Med. Chem., (2014) 22:5:1782 | ||||
IC50 | 7.96 | None, None:None:None | ||||
Ki | 7.96 | Bioorg. Med. Chem., (2008) 16:15:7291 | ||||
Ki | 8 | J. Med. Chem., (2000) 43:5:1011 | ||||
Ki | 8.02 | J. Med. Chem., (2003) 46:14:2795 | ||||
Ki | 8.1 | J. Med. Chem., (2007) 50:21:5103 | ||||
Ki | 8.21 | Bioorg. Med. Chem. Lett., (2014) 24:2:576 | ||||
HTR7
5-hydroxytryptamine receptor 7
16 Activities
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1 – 10 of 16
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7 | MedChemComm, (2012) 3:5:580 | ||||
Ki | 7.32 | J. Med. Chem., (2005) 48:6:1709 | ||||
Ki | 7.4 | J. Med. Chem., (2003) 46:14:2795 | ||||
Ki | 7.4 | Bioorg. Med. Chem. Lett., (2010) 20:8:2465 | ||||
Ki | 7.43 | J. Nat. Prod., (2015) 78:4:722 | ||||
Ki | 7.6 | Eur. J. Med. Chem., (2014) 78:None:324 | ||||
Ki | 7.7 | J. Med. Chem., (2007) 50:21:5103 | ||||
Ki | 7.75 | Eur. J. Med. Chem., (2012) 56:None:348 | ||||
Ki | 7.75 | Bioorg. Med. Chem. Lett., (2013) 23:15:4419 | ||||
Ki | 7.75 | Bioorg. Med. Chem., (2015) 23:1:212 | ||||
HRH1
Histamine H1 receptor
13 Activities
Items per page:
1 – 10 of 13
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7.77 | J. Med. Chem., (2001) 44:4:477 | ||||
Ki | 8 | MedChemComm, (2012) 3:5:580 | ||||
IC50 | 8.31 | None, None:None:None | ||||
Kd | 8.51 | J. Med. Chem., (2011) 54:1:26 | ||||
Ki | 8.62 | Bioorg. Med. Chem. Lett., (2009) 19:2:538 | ||||
Ki | 8.68 | J. Med. Chem., (2004) 47:6:1303 | ||||
Ki | 8.74 | Bioorg. Med. Chem., (2012) 20:3:1291 | ||||
Ki | 8.74 | Bioorg. Med. Chem., (2008) 16:15:7291 | ||||
Ki | 8.96 | J. Med. Chem., (2005) 48:6:1709 | ||||
Ki | 9 | J. Med. Chem., (2014) 57:6:2670 | ||||
KCNH2
Potassium voltage-gated channel subfamily H member 2
12 Activities
Items per page:
1 – 10 of 12
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 5.06 | None, None:None:None | ||||
Ki | 5.39 | J. Med. Chem., (2007) 50:13:2931 | ||||
IC50 | 5.4 | Eur. J. Med. Chem., (2011) 46:2:618 | ||||
Ki | 5.51 | J. Med. Chem., (2007) 50:13:2931 | ||||
IC50 | 6.04 | MedChemComm, (2015) 6:5:831 | ||||
IC50 | 6.19 | J. Med. Chem., (2013) 56:11:4671 | ||||
IC50 | 6.49 | Bioorg. Med. Chem. Lett., (2003) 13:16:2773 | ||||
IC50 | 6.49 | Bioorg. Med. Chem. Lett., (2005) 15:11:2886 | ||||
IC50 | 6.49 | Bioorg. Med. Chem., (2008) 16:11:6252 | ||||
IC50 | 6.5 | J. Med. Chem., (2009) 52:14:4266 | ||||
CHRM1
Muscarinic acetylcholine receptor M1
11 Activities
Items per page:
1 – 10 of 11
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7 | MedChemComm, (2012) 3:5:580 | ||||
IC50 | 8 | None, None:None:None | ||||
IC50 | 8.03 | J. Med. Chem., (1997) 40:25:4146 | ||||
IC50 | 8.03 | J. Med. Chem., (1999) 42:12:2235 | ||||
Ki | 8.2 | J. Med. Chem., (2007) 50:21:5103 | ||||
Ki | 8.61 | None, None:None:None | ||||
Ki | 8.74 | Bioorg. Med. Chem., (2012) 20:3:1291 | ||||
Ki | 8.74 | Bioorg. Med. Chem., (2008) 16:15:7291 | ||||
Ki | 9.01 | J. Med. Chem., (2001) 44:4:477 | ||||
7.9 | ||||||
DRD1
D(1A) dopamine receptor
7 Activities
Items per page:
1 – 7 of 7
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7.05 | Bioorg. Med. Chem. Lett., (2009) 19:2:538 | ||||
Ki | 7.28 | J. Med. Chem., (2001) 44:4:477 | ||||
Ki | 7.28 | None, None:None:None | ||||
Ki | 7.5 | Bioorg. Med. Chem. Lett., (2004) 14:16:4263 | ||||
Ki | 7.67 | Bioorg. Med. Chem. Lett., (2009) 19:21:6059 | ||||
Ki | 8.12 | Med Chem Res, (2013) 22:2:520 | ||||
6.9 | ||||||
HRH4
Histamine H4 receptor
6 Activities
Items per page:
1 – 6 of 6
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.15 | J. Med. Chem., (2006) 49:15:4512 | ||||
Kd | 7.68 | J. Med. Chem., (2006) 49:15:4512 | ||||
Kd | 7.84 | J. Med. Chem., (2006) 49:15:4512 | ||||
Kd | 7.92 | J. Med. Chem., (2006) 49:15:4512 | ||||
5.7 | ||||||
5.5 | ||||||
ADRA1A
Alpha-1A adrenergic receptor
6 Activities
Items per page:
1 – 6 of 6
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.43 | J. Med. Chem., (1984) 27:4:495 | ||||
Ki | 7.72 | None, (2013) None:None:None | ||||
Ki | 7.72 | None, (2013) None:None:None | ||||
Ki | 7.72 | J. Med. Chem., (2014) 57:6:2670 | ||||
Ki | 8 | MedChemComm, (2012) 3:5:580 | ||||
8.1 | ||||||
HTR2B
5-hydroxytryptamine receptor 2B
5 Activities
Items per page:
1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
|---|---|---|---|---|
EC50 | 7.7 | |||