haloperidol
A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279)
Ligand Summary
UNII: J6292F8L3D
PubChem: 3559
Guide to Pharmacology: 86
ChEMBL: CHEMBL54
DrugCentral: 1353
LyCHI: GKRULT6FAR97
Target Activities
DRD2
D(2) dopamine receptor
101 Activities
Items per page:
1 – 10 of 101
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
8.3 | ||||||
Ki | 9.92 | J. Med. Chem., (2002) 45:26:5727 | ||||
Ki | 9.8 | Bioorg. Med. Chem. Lett., (1999) 9:15:2167 | ||||
Ki | 9.8 | J. Med. Chem., (1996) 39:22:4421 | ||||
IC50 | 9.8 | J. Med. Chem., (2014) 57:16:7042 | ||||
IC50 | 9.8 | J Med Chem, (2019) 62:10:5132 | ||||
Ki | 9.6 | Bioorg Med Chem, (2017) 25:19:5084 | ||||
Ki | 9.38 | Bioorg Med Chem, (2017) 25:19:5084 | ||||
Ki | 9.36 | J. Med. Chem., (1993) 36:24:3929 | ||||
Ki | 9.36 | Bioorg. Med. Chem. Lett., (1999) 9:15:2167 | ||||
SIGMAR1
Sigma non-opioid intracellular receptor 1
59 Activities
Items per page:
1 – 10 of 59
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 9.7 | J. Med. Chem., (2005) 48:15:4754 | ||||
Ki | 9.68 | Bioorg Med Chem Lett, (2017) 27:10:2216 | ||||
Ki | 9.48 | J. Med. Chem., (1993) 36:24:3929 | ||||
Ki | 9.36 | Bioorg. Med. Chem. Lett., (1997) 7:17:2303 | ||||
Ki | 9.22 | J. Med. Chem., (1994) 37:13:1964 | ||||
Ki | 9.22 | Bioorg. Med. Chem. Lett., (1994) 4:18:2185 | ||||
Ki | 8.96 | Bioorg. Med. Chem., (2016) 24:9:2060 | ||||
Ki | 8.92 | Bioorg. Med. Chem. Lett., (2014) 24:2:576 | ||||
Ki | 8.82 | J. Med. Chem., (1998) 41:27:5402 | ||||
Ki | 8.82 | J. Med. Chem., (2001) 44:11:1815 | ||||
DRD3
D(3) dopamine receptor
50 Activities
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1 – 10 of 50
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
7 | ||||||
IC50 | 10.22 | J. Med. Chem., (2014) 57:16:7042 | ||||
IC50 | 9.6 | J Med Chem, (2019) 62:10:5132 | ||||
Ki | 9.16 | J. Med. Chem., (1994) 37:21:3523 | ||||
Ki | 9.05 | J. Med. Chem., (2009) 52:1:151 | ||||
Ki | 9.02 | J. Med. Chem., (1993) 36:24:3929 | ||||
Ki | 8.8 | J. Med. Chem., (2007) 50:21:5103 | ||||
Ki | 8.7 | J. Med. Chem., (1996) 39:10:1943 | ||||
Ki | 8.7 | J. Med. Chem., (1996) 39:10:1941 | ||||
Ki | 8.7 | J. Med. Chem., (1997) 40:15:2374 | ||||
DRD4
D(4) dopamine receptor
45 Activities
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1 – 10 of 45
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 9.13 | J. Med. Chem., (2002) 45:26:5727 | ||||
Ki | 9 | J. Med. Chem., (1996) 39:20:4044 | ||||
Ki | 9 | J. Med. Chem., (2000) 43:2:270 | ||||
IC50 | 8.89 | J. Med. Chem., (1998) 41:24:4903 | ||||
Ki | 8.85 | Bioorg. Med. Chem. Lett., (2004) 14:20:5095 | ||||
Ki | 8.8 | Bioorg. Med. Chem. Lett., (2001) 11:10:1313 | ||||
Ki | 8.72 | Bioorg. Med. Chem. Lett., (2004) 14:20:5095 | ||||
Ki | 8.7 | J. Med. Chem., (2000) 43:21:3923 | ||||
Ki | 8.68 | J. Med. Chem., (1996) 39:14:2764 | ||||
Ki | 8.66 | J. Med. Chem., (1997) 40:25:4026 | ||||
KCNH2
Potassium voltage-gated channel subfamily H member 2
18 Activities
Items per page:
1 – 10 of 18
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8 | J. Med. Chem., (2013) 56:22:8955 | ||||
IC50 | 7.57 | J. Med. Chem., (2009) 52:14:4266 | ||||
IC50 | 7.57 | J. Med. Chem., (2009) 52:14:4266 | ||||
IC50 | 7.57 | Eur. J. Med. Chem., (2011) 46:2:618 | ||||
IC50 | 7.57 | Cardiovasc. Res., (2011) 91:None:53 | ||||
IC50 | 7.55 | J. Med. Chem., (2002) 45:18:3844 | ||||
IC50 | 7.55 | Bioorg. Med. Chem. Lett., (2005) 15:6:1737 | ||||
IC50 | 7.55 | Eur. J. Med. Chem., (2009) 44:5:1926 | ||||
IC50 | 7.52 | Bioorg. Med. Chem. Lett., (2003) 13:16:2773 | ||||
IC50 | 7.52 | Bioorg. Med. Chem. Lett., (2005) 15:11:2886 | ||||
HTR2A
5-hydroxytryptamine receptor 2A
7 Activities
Items per page:
1 – 7 of 7
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
7.4 | ||||||
Ki | 7.68 | None, None:None:None | ||||
Ki | 7.6 | J. Med. Chem., (2004) 47:6:1303 | ||||
IC50 | 7.12 | None, None:None:None | ||||
Ki | 7.05 | Eur J Med Chem, (2018) 145:None:790 | ||||
Ki | 7 | J. Med. Chem., (2007) 50:21:5103 | ||||
Ki | 7 | None, (2013) None:None:None | ||||
DRD1
D(1A) dopamine receptor
5 Activities
Items per page:
1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 8.21 | Bioorg. Med. Chem. Lett., (2009) 19:21:6059 | ||||
Ki | 7.6 | Bioorg. Med. Chem. Lett., (2011) 21:12:3622 | ||||
Ki | 7.31 | J. Med. Chem., (1996) 39:14:2764 | ||||
Ki | 7.26 | None, None:None:None | ||||
Ki | 7.09 | J. Med. Chem., (2004) 47:17:4155 | ||||
DRD5
D(1B) dopamine 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) | ||
|---|---|---|---|---|---|---|
6.3 | ||||||
Ki | 7.42 | J. Med. Chem., (2011) 54:8:2529 | ||||
Ki | 7.32 | Bioorg. Med. Chem. Lett., (2011) 21:12:3622 | ||||
Ki | 7.24 | J. Med. Chem., (2004) 47:17:4155 | ||||
TMEM97
Sigma intracellular receptor 2
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 | 7.8 | J Med Chem, (2017) 60:23:9531 | ||||
Ki | 7.8 | ACS Med Chem Lett, (2020) 11:5:889 | ||||
Ki | 7.75 | Eur J Med Chem, (2019) 174:None:226 | ||||
Ki | 7.8 | |||||
ADRA1D
Alpha-1D adrenergic receptor
2 Activities
Items per page:
1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7.39 | None, None:None:None | ||||
IC50 | 7.08 | None, None:None:None | ||||
HTR1D
5-hydroxytryptamine receptor 1D
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
6.6 | ||||||
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) | ||
|---|---|---|---|---|---|---|
6.3 | ||||||
KCNJ6
G protein-activated inward rectifier potassium channel 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) | ||
|---|---|---|---|---|---|---|
4.1 | ||||||
KCNH1
Potassium voltage-gated channel subfamily H member 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) | ||
|---|---|---|---|---|---|---|
6.2 | ||||||
ADRA1A
Alpha-1A adrenergic receptor
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7.96 | None, (2013) None:None:None | ||||
ABCB1
Multidrug resistance protein 1
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 6.7 | J. Med. Chem., (2002) 45:26:5671 | ||||
EBP
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 6.72 | J. Med. Chem., (2005) 48:15:4754 | ||||
H1F0
Histone H1.0
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 6.11 | None, (2013) None:None:None | ||||
KCNK2
Potassium channel subfamily K member 2
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 5.26 | J. Med. Chem., (2016) 59:11:5149 | ||||