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
62 Activities
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1 – 10 of 62
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
7.5 | ||||||
Ki | 8.05 | Bioorg. Med. Chem. Lett., (2002) 12:21:3105 | ||||
Ki | 8 | J. Med. Chem., (1996) 39:10:1941 | ||||
Ki | 8 | J. Med. Chem., (1997) 40:15:2374 | ||||
Ki | 8 | J. Med. Chem., (1999) 42:14:2706 | ||||
Ki | 8 | J. Med. Chem., (1996) 39:20:4044 | ||||
Ki | 8 | J. Med. Chem., (1996) 39:10:1943 | ||||
Ki | 8 | Bioorg. Med. Chem. Lett., (1999) 9:9:1285 | ||||
Ki | 8 | J Med Chem, (2017) 60:17:7233 | ||||
Ki | 7.89 | Bioorg. Med. Chem. Lett., (1997) 7:10:1327 | ||||
DRD2
D(2) dopamine receptor
41 Activities
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1 – 10 of 41
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
6.2 | ||||||
Ki | 8.15 | Med Chem Res, (2013) 22:2:520 | ||||
IC50 | 8.05 | J. Med. Chem., (2005) 48:21:6523 | ||||
Ki | 7.55 | Bioorg. Med. Chem. Lett., (2002) 12:15:1937 | ||||
Ki | 7.55 | Bioorg. Med. Chem. Lett., (2002) 12:4:633 | ||||
Ki | 7.55 | Bioorg. Med. Chem. Lett., (1999) 9:14:1969 | ||||
Ki | 7.55 | J. Med. Chem., (2001) 44:17:2691 | ||||
Ki | 7.55 | J. Med. Chem., (2000) 43:23:4563 | ||||
Ki | 7.55 | Bioorg. Med. Chem. Lett., (2000) 10:17:2041 | ||||
Ki | 7.55 | Bioorg. Med. Chem. Lett., (1999) 9:21:3143 | ||||
HTR2A
5-hydroxytryptamine receptor 2A
39 Activities
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1 – 10 of 39
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
8.9 | ||||||
Ki | 8.92 | None, None:None:None | ||||
Ki | 8.57 | Bioorg. Med. Chem. Lett., (2004) 14:16:4263 | ||||
Ki | 8.52 | Bioorg Med Chem, (2020) 28:15:115578 | ||||
Ki | 8.52 | Bioorg Med Chem Lett, (2020) 30:8:127053 | ||||
Ki | 8.48 | J. Med. Chem., (2004) 47:6:1303 | ||||
Ki | 8.4 | J. Med. Chem., (2001) 44:4:477 | ||||
IC50 | 8.38 | None, None:None:None | ||||
Ki | 8.31 | J. Med. Chem., (2012) 55:4:1572 | ||||
Ki | 8.3 | J. Med. Chem., (1996) 39:20:4044 | ||||
HTR2C
5-hydroxytryptamine receptor 2C
28 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 8.54 | Bioorg. Med. Chem. Lett., (2004) 14:16:4263 | ||||
Ki | 8.54 | Med Chem Res, (2013) 22:2:520 | ||||
Ki | 8.5 | None, None:None:None | ||||
Ki | 8.32 | J. Med. Chem., (2014) 57:22:9578 | ||||
Ki | 8.3 | J. Med. Chem., (2001) 44:4:477 | ||||
Ki | 8.3 | J. Med. Chem., (2000) 43:24:4678 | ||||
IC50 | 8.22 | None, None:None:None | ||||
Ki | 8.1 | J. Med. Chem., (2007) 50:21:5103 | ||||
Ki | 8.03 | J. Med. Chem., (2013) 56:3:1211 | ||||
Ki | 8.03 | J. Med. Chem., (2013) 56:3:1211 | ||||
HTR7
5-hydroxytryptamine receptor 7
27 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
7.4 | ||||||
Ki | 8.26 | Bioorg. Med. Chem. Lett., (2014) 24:2:576 | ||||
Ki | 8.23 | Bioorg. Med. Chem. Lett., (2014) 24:2:576 | ||||
Ki | 8.05 | J. Med. Chem., (2000) 43:5:1011 | ||||
Ki | 7.94 | Bioorg Med Chem, (2020) 28:15:115578 | ||||
Ki | 7.9 | J. Med. Chem., (2003) 46:26:5638 | ||||
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 | ||||
Ki | 7.75 | Eur. J. Med. Chem., (2016) 112:None:258 | ||||
HTR6
5-hydroxytryptamine receptor 6
19 Activities
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1 – 10 of 19
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 8.4 | J. Med. Chem., (2003) 46:14:2795 | ||||
Ki | 8.4 | Eur. J. Med. Chem., (2012) 56:None:348 | ||||
Ki | 8.4 | Bioorg. Med. Chem. Lett., (2013) 23:15:4419 | ||||
Ki | 8.4 | Eur J Med Chem, (2018) 145:None:790 | ||||
Ki | 8.4 | Bioorg Med Chem, (2020) 28:15:115578 | ||||
Ki | 8.32 | Bioorg. Med. Chem. Lett., (2000) 10:20:2295 | ||||
Ki | 8.3 | None, None:None:None | ||||
Ki | 8.22 | Bioorg. Med. Chem. Lett., (2014) 24:2:576 | ||||
Ki | 8.21 | Bioorg. Med. Chem. Lett., (2014) 24:2:576 | ||||
Ki | 8.1 | J. Med. Chem., (2007) 50:21:5103 | ||||
KCNH2
Potassium voltage-gated channel subfamily H member 2
14 Activities
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1 – 10 of 14
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.72 | J. Med. Chem., (2002) 45:18:3844 | ||||
IC50 | 6.72 | Eur. J. Med. Chem., (2009) 44:5:1926 | ||||
IC50 | 6.5 | J. Med. Chem., (2009) 52:14:4266 | ||||
IC50 | 6.5 | J. Med. Chem., (2009) 52:14:4266 | ||||
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 | 6.19 | J. Med. Chem., (2013) 56:11:4671 | ||||
IC50 | 6.04 | MedChemComm, (2015) 6:5:831 | ||||
Ki | 5.51 | J. Med. Chem., (2007) 50:13:2931 | ||||
HRH1
Histamine H1 receptor
13 Activities
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1 – 10 of 13
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
EC50 | 9.4 | None, (2004) None:None:None | ||||
EC50 | 9.4 | |||||
Ki | 9.24 | None, None:None:None | ||||
Ki | 9 | J. Med. Chem., (2014) 57:6:2670 | ||||
Ki | 8.96 | J. Med. Chem., (2005) 48:6:1709 | ||||
Ki | 8.74 | Bioorg. Med. Chem., (2008) 16:15:7291 | ||||
Ki | 8.74 | Bioorg. Med. Chem., (2012) 20:3:1291 | ||||
Ki | 8.68 | J. Med. Chem., (2004) 47:6:1303 | ||||
Ki | 8.62 | Bioorg. Med. Chem. Lett., (2009) 19:2:538 | ||||
Kd | 8.51 | J. Med. Chem., (2011) 54:1:26 | ||||
CHRM1
Muscarinic acetylcholine receptor M1
11 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
7.9 | ||||||
7.7 | ||||||
Ki | 9.01 | J. Med. Chem., (2001) 44:4:477 | ||||
Ki | 8.74 | Bioorg. Med. Chem., (2008) 16:15:7291 | ||||
Ki | 8.74 | Bioorg. Med. Chem., (2012) 20:3:1291 | ||||
Ki | 8.61 | None, None:None:None | ||||
Ki | 8.2 | J. Med. Chem., (2007) 50:21:5103 | ||||
IC50 | 8.03 | J. Med. Chem., (1999) 42:12:2235 | ||||
IC50 | 8.03 | J. Med. Chem., (1997) 40:25:4146 | ||||
IC50 | 8 | None, None:None:None | ||||
DRD1
D(1A) dopamine receptor
7 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
6.9 | ||||||
Ki | 8.12 | Med Chem Res, (2013) 22:2:520 | ||||
Ki | 7.67 | Bioorg. Med. Chem. Lett., (2009) 19:21:6059 | ||||
Ki | 7.5 | Bioorg. Med. Chem. Lett., (2004) 14:16:4263 | ||||
Ki | 7.28 | J. Med. Chem., (2001) 44:4:477 | ||||
Ki | 7.28 | None, None:None:None | ||||
Ki | 7.05 | Bioorg. Med. Chem. Lett., (2009) 19:2:538 | ||||
HRH4
Histamine H4 receptor
6 Activities
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1 – 6 of 6
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
5.7 | ||||||
5.5 | ||||||
Kd | 7.92 | J. Med. Chem., (2006) 49:15:4512 | ||||
Kd | 7.84 | J. Med. Chem., (2006) 49:15:4512 | ||||
Kd | 7.68 | J. Med. Chem., (2006) 49:15:4512 | ||||
Kd | 7.15 | J. Med. Chem., (2006) 49:15:4512 | ||||
ADRA1A
Alpha-1A adrenergic receptor
5 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
8.1 | ||||||
Ki | 8 | MedChemComm, (2012) 3:5:580 | ||||
Ki | 7.72 | J. Med. Chem., (2014) 57:6:2670 | ||||
Ki | 7.72 | None, (2013) None:None:None | ||||
Kd | 7.43 | J. Med. Chem., (1984) 27:4:495 | ||||
HTR2B
5-hydroxytryptamine receptor 2B
5 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 8.5 | J. Med. Chem., (2007) 50:21:5103 | ||||
Ki | 8.14 | None, None:None:None | ||||
IC50 | 7.96 | None, None:None:None | ||||
EC50 | 7.7 | None, (2004) None:None:None | ||||
EC50 | 7.7 | |||||
DRD3
D(3) dopamine receptor
4 Activities
CHRM4
Muscarinic acetylcholine receptor M4
4 Activities
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1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 8.2 | None, None:None:None | ||||
Ki | 7.9 | J. Med. Chem., (2007) 50:21:5103 | ||||
IC50 | 7.35 | None, None:None:None | ||||
Ki | 7 | MedChemComm, (2012) 3:5:580 | ||||
ADRA2C
Alpha-2C adrenergic receptor
4 Activities
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1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 8.94 | None, None:None:None | ||||
Ki | 8.54 | J. Med. Chem., (2005) 48:6:1709 | ||||
IC50 | 8.1 | None, None:None:None | ||||
Ki | 7 | MedChemComm, (2012) 3:5:580 | ||||
ADRA1D
Alpha-1D adrenergic receptor
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
7.7 | ||||||
Ki | 7.77 | None, None:None:None | ||||
IC50 | 7.46 | None, None:None:None | ||||
CHRM3
Muscarinic acetylcholine receptor M3
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7.77 | None, None:None:None | ||||
IC50 | 7.11 | None, None:None:None | ||||
Ki | 7 | MedChemComm, (2012) 3:5:580 | ||||
ADRA2A
Alpha-2A adrenergic receptor
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7.62 | J. Med. Chem., (2005) 48:6:1709 | ||||
Ki | 7.47 | None, None:None:None | ||||
IC50 | 7.05 | None, None:None:None | ||||
HTR3A
5-hydroxytryptamine receptor 3A
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 6.73 | Bioorg. Med. Chem. Lett., (2004) 14:16:4263 | ||||
Ki | 6.73 | Med Chem Res, (2013) 22:2:520 | ||||
Ki | 6 | MedChemComm, (2012) 3:5:580 | ||||
ADRA2B
Alpha-2B adrenergic receptor
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7.96 | None, None:None:None | ||||
IC50 | 7.64 | None, None:None:None | ||||
Ki | 7 | MedChemComm, (2012) 3:5:580 | ||||
HTR1A
5-hydroxytryptamine receptor 1A
3 Activities
CHRM5
Muscarinic acetylcholine receptor M5
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 8.02 | None, None:None:None | ||||
IC50 | 7.89 | None, None:None:None | ||||
Ki | 7 | MedChemComm, (2012) 3:5:580 | ||||
ADRA1B
Alpha-1B adrenergic receptor
2 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
8.2 | ||||||
Ki | 8 | MedChemComm, (2012) 3:5:580 | ||||
SLC6A4
Sodium-dependent serotonin transporter
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 6.54 | None, None:None:None | ||||
IC50 | 6.26 | None, None:None:None | ||||
H1F0
Histone H1.0
2 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 9 | None, (2013) None:None:None | ||||
Ki | 9 | |||||
HTR1B
5-hydroxytryptamine receptor 1B
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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6.2 | ||||||
HTR1D
5-hydroxytryptamine receptor 1D
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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6.4 | ||||||
HTR1E
5-hydroxytryptamine receptor 1E
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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6.4 | ||||||
HTR1F
5-hydroxytryptamine receptor 1F
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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6.9 | ||||||
HTR5A
5-hydroxytryptamine receptor 5A
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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5.3 | ||||||
DRD5
D(1B) dopamine receptor
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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6.6 | ||||||
HRH3
Histamine H3 receptor
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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5.8 | ||||||
KCNJ6
G protein-activated inward rectifier potassium channel 2
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
- | 3.8 | |||||
CHRM2
Muscarinic acetylcholine receptor M2
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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Ki | 7 | MedChemComm, (2012) 3:5:580 | ||||