quinidine
An optical isomer of quinine, extracted from the bark of the CHINCHONA tree and similar plant species. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. It prolongs cellular ACTION POTENTIALS, and decreases automaticity. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.
Ligand Summary
UNII: ITX08688JL
PubChem: 5953
PubChem: 441074
Guide to Pharmacology: 2342
ChEMBL: CHEMBL21578
ChEMBL: CHEMBL1294
DrugCentral: 2346
LyCHI: TTP6PN9UM1K1
Target Activities
CYP2D6
Cytochrome P450 2D6
44 Activities
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1 – 10 of 44
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 8.7 | J. Med. Chem., (2013) 56:20:7851 | ||||
IC50 | 8.48 | J. Med. Chem., (2003) 46:1:74 | ||||
IC50 | 8.16 | Bioorg Med Chem, (2017) 25:20:5341 | ||||
IC50 | 8.14 | J Med Chem, (2020) 63:14:7721 | ||||
IC50 | 8.05 | J. Med. Chem., (2016) 59:7:3340 | ||||
Ki | 8.01 | J. Med. Chem., (2009) 52:3:626 | ||||
IC50 | 8 | J. Med. Chem., (2004) 47:22:5340 | ||||
IC50 | 8 | J. Med. Chem., (2011) 54:2:534 | ||||
IC50 | 8 | J. Nat. Prod., (2011) 74:1:102 | ||||
IC50 | 8 | MedChemComm, (2018) 9:11:1882 | ||||
KCNH2
Potassium voltage-gated channel subfamily H member 2
6 Activities
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1 – 6 of 6
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 6.52 | Cardiovasc. Res., (2011) 91:None:53 | ||||
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 | 5.84 | None, (2016) None:None:None | ||||
IC50 | 5.57 | J. Med. Chem., (2016) 59:1:264 | ||||
KCNA5
Potassium voltage-gated channel subfamily A member 5
2 Activities
SCN5A
Sodium channel protein type 5 subunit alpha
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 5.16 | J. Med. Chem., (2007) 50:12:2818 | ||||
IC50 | 5.16 | BLOCKER | ||||
ABCB1
Multidrug resistance protein 1
2 Activities
KCNT1
Potassium channel subfamily T member 1
1 Activities
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) | ||
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5.8 | ||||||
KCNH5
Potassium voltage-gated channel subfamily H member 5
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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- | 3.8 | |||||
KCNA4
Potassium voltage-gated channel subfamily A member 4
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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3.7 | ||||||
KCNA7
Potassium voltage-gated channel subfamily A member 7
1 Activities
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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4.8 | ||||||
KCND2
Potassium voltage-gated channel subfamily D 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) | ||
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- | 4.9 | |||||
SLC29A4
Equilibrative nucleoside transporter 4
1 Activities
SCN1A
Sodium channel protein type 1 subunit alpha
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 5.49 | BLOCKER | ||||
SCN2A
Sodium channel protein type 2 subunit alpha
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 5.49 | BLOCKER | ||||
SCN3A
Sodium channel protein type 3 subunit alpha
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 5.49 | BLOCKER | ||||