flunarizine
Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. It is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy.
Ligand Summary
UNII: R7PLA2DM0J
PubChem: 941361
ChEMBL: CHEMBL30008
DrugCentral: 1200
LyCHI: FH1AY465SJH3
Target Activities
CYP2J2
Cytochrome P450 2J2
5 Activities
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1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7 | Drug Metab. Dispos., (2013) 41:1:60 | ||||
Ki | 6.89 | Drug Metab. Dispos., (2013) 41:1:60 | ||||
IC50 | 6.12 | Drug Metab. Dispos., (2013) 41:1:60 | ||||
IC50 | 6.03 | Drug Metab. Dispos., (2013) 41:1:60 | ||||
IC50 | 6.02 | Drug Metab. Dispos., (2013) 41:1:60 | ||||
CACNA1G
Voltage-dependent T-type calcium channel subunit alpha-1G
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 6.28 | Bioorg. Med. Chem., (2010) 18:16:5938 | ||||
Kd | 6.28 | Bioorg. Med. Chem. Lett., (2011) 21:1:215 | ||||
Kd | 6.28 | BLOCKER | ||||
CACNA1I
Voltage-dependent T-type calcium channel subunit alpha-1I
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 6.08 | Bioorg. Med. Chem., (2010) 18:16:5938 | ||||
Kd | 6.08 | Bioorg. Med. Chem. Lett., (2011) 21:1:215 | ||||
Kd | 6.08 | BLOCKER | ||||
DRD3
D(3) dopamine receptor
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 | 7.48 | None, None:None:None | ||||
IC50 | 7.01 | None, None:None:None | ||||
CACNA1H
Voltage-dependent T-type calcium channel subunit alpha-1H
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 5.44 | Bioorg. Med. Chem., (2010) 18:16:5938 | ||||
Kd | 5.44 | BLOCKER | ||||
SIGMAR1
Sigma non-opioid intracellular receptor 1
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 | 8 | None, None:None:None | ||||
IC50 | 7.6 | None, None:None:None | ||||
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 | 6.58 | None, None:None:None | ||||
IC50 | 6.3 | None, None:None:None | ||||
KCNH2
Potassium voltage-gated channel subfamily H member 2
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 | 6.3 | None, None:None:None | ||||
IC50 | 6.22 | None, None:None:None | ||||
SLC6A3
Sodium-dependent dopamine 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 | 6.33 | None, None:None:None | ||||
IC50 | 6.23 | None, None:None:None | ||||
HRH1
Histamine H1 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) | ||
|---|---|---|---|---|---|---|
Ki | 7.75 | None, None:None:None | ||||
CACNA1B
Voltage-dependent N-type calcium channel subunit alpha-1B
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 | 5.78 | Bioorg. Med. Chem. Lett., (2007) 17:3:662 | ||||
ADRA2C
Alpha-2C adrenergic 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) | ||
|---|---|---|---|---|---|---|
Ki | 7.5 | None, None:None:None | ||||