pimozide
A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to HALOPERIDOL for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403)
Ligand Summary
UNII: 1HIZ4DL86F
PubChem: 16362
Guide to Pharmacology: 90
ChEMBL: CHEMBL1423
DrugCentral: 2172
LyCHI: QC4NBYGR69YF
Target Activities
KCNH2
Potassium voltage-gated channel subfamily H member 2
15 Activities
Items per page:
1 – 10 of 15
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.52 | Eur. J. Med. Chem., (2008) 43:11:2479 | ||||
IC50 | 7.75 | J. Med. Chem., (2002) 45:18:3844 | ||||
IC50 | 7.75 | Bioorg. Med. Chem. Lett., (2003) 13:10:1829 | ||||
IC50 | 7.75 | J. Med. Chem., (2003) 46:11:2017 | ||||
IC50 | 7.74 | Bioorg. Med. Chem. Lett., (2005) 15:6:1737 | ||||
IC50 | 7.74 | Eur. J. Med. Chem., (2009) 44:5:1926 | ||||
IC50 | 7.7 | Cardiovasc. Res., (2011) 91:None:53 | ||||
Ki | 7.38 | Bioorg. Med. Chem. Lett., (2006) 16:20:5303 | ||||
IC50 | 7.3 | Bioorg. Med. Chem. Lett., (2003) 13:16:2773 | ||||
IC50 | 7.3 | Bioorg. Med. Chem. Lett., (2005) 15:11:2886 | ||||
DRD2
D(2) dopamine receptor
5 Activities
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1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
7.6 | ||||||
Ki | 7.93 | J. Med. Chem., (2012) 55:22:9735 | ||||
Ki | 7.92 | J. Med. Chem., (2003) 46:11:2017 | ||||
Kd | 7.54 | Bioorg. Med. Chem., (2010) 18:16:5938 | ||||
Ki | 8.86 | ANTAGONIST | ||||
HTR6
5-hydroxytryptamine receptor 6
2 Activities
CACNA1G
Voltage-dependent T-type calcium channel subunit alpha-1G
2 Activities
HTR1A
5-hydroxytryptamine receptor 1A
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
6.8 | ||||||
HTR7
5-hydroxytryptamine receptor 7
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
- | 9.3 | |||||
CACNA1H
Voltage-dependent T-type calcium channel subunit alpha-1H
1 Activities
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7.3 | ||||||
CACNA1I
Voltage-dependent T-type calcium channel subunit alpha-1I
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
7.5 | ||||||
DRD3
D(3) dopamine receptor
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
7.4 | ||||||
HRH1
Histamine H1 receptor
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
6.2 | ||||||
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) | ||
|---|---|---|---|---|---|---|
- | 5.5 | |||||
KCNA10
Potassium voltage-gated channel subfamily A member 10
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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6.5 | ||||||
ABCB1
Multidrug resistance protein 1
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.1 | J. Med. Chem., (2003) 46:9:1716 | ||||
GLRA1
Glycine receptor subunit alpha-1
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
EC50 | 5.77 | J. Med. Chem., (2015) 58:7:2958 | ||||
KCNK2
Potassium channel subfamily K member 2
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 5.75 | J. Med. Chem., (2016) 59:11:5149 | ||||