Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T67952 | Target Info | |||
| Target Name | Potassium channel unspecific (KC) | ||||
| Target Type | Successful Target | ||||
| Gene Name | NO-GeName | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Opioid receptor sigma 1 (OPRS1) | Successful Target | ||||
| UniProt ID | SGMR1_HUMAN | |||||
| Gene Name | SIGMAR1 | |||||
| Synonyms |
hSigmaR1; Sigma1R; Sigma1-receptor; Sigma non-opioid intracellular receptor 1; Sigma 1-type opioid receptor; SRBP; SR31747-binding protein; SR31747 binding protein 1; SR-BP; SIG-1R; Opioid receptor, sigma 1, isoform 1; OPRS1 protein; Aging-associated gene 8 protein; AAG8
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| Representative Drug(s) | Amiodarone | Drug Info | Ki = 1 nM | [1] | ||
| Co-Target Name | Voltage-gated potassium channel Kv11.1 (KCNH2) | Successful Target | ||||
| UniProt ID | KCNH2_HUMAN | |||||
| Gene Name | KCNH2 | |||||
| Synonyms |
hERG1; hERG-1; Voltage-gated potassium channel subunit Kv11.1; Potassium voltage-gated channel subfamily H member 2; HERG K+ channel; HERG; H-ERG; Ether-a-go-go-related protein 1; Ether-a-go-go-related gene potassium channel 1; Ether-a-go-go related protein 1; Ether-a-go-go related gene potassium channel 1; Eag related protein 1; Eag homolog; ERG-1; ERG
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| Representative Drug(s) | Dofetilide | Drug Info | IC50 = 4.1 nM | Click to Show More | [2] | |
| 2 | Ibutilide | Drug Info | IC50 = 10 nM | [3] | ||
| 3 | Amiodarone | Drug Info | IC50 = 30 nM | [4] | ||
| 4 | Dronedarone | Drug Info | IC50 = 316.23 nM | [5] | ||
| Co-Target Name | Voltage-gated L-type calcium channel (L-CaC) | Successful Target | ||||
| UniProt ID | CAC1C_HUMAN; CAC1D_HUMAN; CAC1F_HUMAN; CAC1S_HUMAN | |||||
| Gene Name | NO-GeName | |||||
| Synonyms |
L-type voltage-dependent Ca(2+) channel; L-type Ca2+ channel; L-type Ca(2+) channel
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| Representative Drug(s) | Amiodarone | Drug Info | IC50 = 270 nM | [4] | ||
| Co-Target Name | Thyroid hormone receptor beta (THRB) | Successful Target | ||||
| UniProt ID | THB_HUMAN | |||||
| Gene Name | THRB | |||||
| Synonyms |
c-erbA-beta; c-erbA-2; THR1; Nuclear receptor subfamily 1 group A member 2; NR1A2; ERBA2
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| Representative Drug(s) | Amiodarone | Drug Info | IC50 = 600 nM | [6] | ||
| Co-Target Name | Thyroid hormone receptor alpha (THRA) | Successful Target | ||||
| UniProt ID | THA_HUMAN | |||||
| Gene Name | THRA | |||||
| Synonyms |
V-erbA-related protein 7; THRA2; THRA1; Nuclear receptor subfamily 1 group A member 1; NR1A1; ERBA1; EAR7; EAR-7; C-erbA-alpha; C-erbA-1
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| Representative Drug(s) | Amiodarone | Drug Info | IC50 = 650 nM | [6] | ||
| Co-Target Name | Cholestenol delta-isomerase (EBP) | Clinical trial Target | ||||
| UniProt ID | EBP_HUMAN | |||||
| Gene Name | EBP | |||||
| Synonyms |
Emopamilbinding protein; EBP; Delta(8)Delta(7) sterol isomerase; D8D7 sterol isomerase; 3betahydroxysteroidDelta(8),Delta(7)isomerase
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| Representative Drug(s) | Amiodarone | Drug Info | Ki = 25 nM | [1] | ||
| Co-Target Name | TWIK-related acid-sensitive potassium channel 1 (TASK1) | Clinical trial Target | ||||
| UniProt ID | KCNK3_HUMAN | |||||
| Gene Name | KCNK3 | |||||
| Synonyms |
Two pore potassium channel KT3.1; Two pore K(+) channel KT3.1; TWIK-related acid-sensitive K(+) channel 1; Acid-sensitive potassium channel protein TASK-1
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| Representative Drug(s) | AVE0118 | Drug Info | IC50 = 600 nM | [7] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening. J Med Chem. 2005 Jul 28;48(15):4754-64. | ||||
| REF 2 | Strategies to reduce HERG K+ channel blockade. Exploring heteroaromaticity and rigidity in novel pyridine analogues of dofetilide. J Med Chem. 2013 Apr 11;56(7):2828-40. | ||||
| REF 3 | Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods. Bioorg Med Chem Lett. 2003 Aug 18;13(16):2773-5. | ||||
| REF 4 | Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk. Cardiovasc Res. 2011 Jul 1;91(1):53-61. | ||||
| REF 5 | Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model. Eur J Med Chem. 2011 Feb;46(2):618-30. | ||||
| REF 6 | Synthesis and preliminary characterization of a novel antiarrhythmic compound (KB130015) with an improved toxicity profile compared with amiodarone. J Med Chem. 2002 Jan 31;45(3):623-30. | ||||
| REF 7 | TASK Channels Pharmacology: New Challenges in Drug Design. J Med Chem. 2019 Nov 27;62(22):10044-10058. | ||||
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