Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T43739 | Target Info | |||
| Target Name | Voltage-gated sodium channel alpha Nav1.8 (SCN10A) | ||||
| Synonyms |
hPN3; Voltage-gated sodium channel subunit alpha Nav1.8; Sodium channel protein type X subunit alpha; Sodium channel protein type 10 subunit alpha; Peripheral nerve sodium channel 3; PN3
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| Target Type | Successful Target | ||||
| Gene Name | SCN10A | ||||
| Biochemical Class | Voltage-gated ion channel | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Human immunodeficiency virus Reverse transcriptase (HIV RT) | Successful Target | ||||
| UniProt ID | POL_HV1B1 | |||||
| Gene Name | HIV RT | |||||
| Synonyms |
HIV p66 RT; HIV Exoribonuclease H
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| Representative Drug(s) | Rilpivirine | Drug Info | IC50 = 0.68 nM | [1] | ||
| Co-Target Name | Voltage-gated sodium channel alpha Nav1.5 (SCN5A) | Successful Target | ||||
| UniProt ID | SCN5A_HUMAN | |||||
| Gene Name | SCN5A | |||||
| Synonyms |
Voltage-gated sodium channel subunit alpha Nav1.5; Sodium channel protein type V subunit alpha; Sodium channel protein type 5 subunit alpha; Sodium channel protein cardiac muscle subunit alpha; HH1
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| Representative Drug(s) | Tetracaine | Drug Info | IC50 = 200 nM | [2] | ||
| Co-Target Name | S-mephenytoin 4-hydroxylase (CYP2C9) | Successful Target | ||||
| UniProt ID | CP2C9_HUMAN | |||||
| Gene Name | CYP2C9 | |||||
| Synonyms |
Cytochrome P450 PB-1; Cytochrome P450 MP-8; Cytochrome P450 MP-4; Cytochrome P450 2C9; Cytochrome P-450MP; Cholesterol 25-hydroxylase; CYPIIC9; CYP2C10; (S)-limonene 7-monooxygenase; (S)-limonene 6-monooxygenase; (R)-limonene 6-monooxygenase
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| Representative Drug(s) | Rilpivirine | Drug Info | IC50 = 346 nM | [3] | ||
| 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) | Rilpivirine | Drug Info | IC50 = 500 nM | [3] | ||
| Co-Target Name | Voltage-gated sodium channel alpha Nav1.3 (SCN3A) | Successful Target | ||||
| UniProt ID | SCN3A_HUMAN | |||||
| Gene Name | SCN3A | |||||
| Synonyms |
Voltage-gated sodium channel subunit alpha Nav1.3; Voltage-gated sodium channel subtype III; Sodium channel protein, brain III subunit alpha; Sodium channel protein type III subunit alpha; Sodium channel protein type 3 subunit alpha; Sodium channel protein brain III subunit alpha; NAC3; KIAA1356
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| Representative Drug(s) | Tetracaine | Drug Info | IC50 = 740 nM | [4] | ||
| Co-Target Name | Voltage-gated sodium channel alpha Nav1.7 (SCN9A) | Clinical trial Target | ||||
| UniProt ID | SCN9A_HUMAN | |||||
| Gene Name | SCN9A | |||||
| Synonyms |
hNE-Na; Voltage-gated sodium channel subunit alpha Nav1.7; Sodium channel proteintype IX subunit alpha; Sodium channel proteintype 9 subunit alpha; Sodium channel protein type IX subunit alpha; Sodium channel protein type 9 subunit alpha; Peripheral sodium channel 1; PN1; Neuroendocrine sodium channel; NENA
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| Representative Drug(s) | Tetracaine | Drug Info | IC50 = 56 nM | [4] | ||
| Co-Target Name | Voltage-gated sodium channel alpha Nav1.6 (SCN8A) | Clinical trial Target | ||||
| UniProt ID | SCN8A_HUMAN | |||||
| Gene Name | SCN8A | |||||
| Synonyms |
Voltage-gated sodium channel subunit alpha Nav1.6; Sodium channel protein type VIII subunit alpha; Sodium channel protein type 8 subunit alpha; SCN8A
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| Representative Drug(s) | Tetracaine | Drug Info | IC50 = 520 nM | [4] | ||
| Co-Target Name | Voltage-gated sodium channel alpha Nav1.2 (SCN2A) | Literature-reported Target | ||||
| UniProt ID | SCN2A_HUMAN | |||||
| Gene Name | SCN2A | |||||
| Synonyms |
Voltage-gated sodium channelsubunit alpha Nav1.2; Sodium channel protein type II subunit alpha; Sodium channel protein brainII subunit alpha; SCN2A; HBSC II
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| Representative Drug(s) | Tetracaine | Drug Info | IC50 = 490 nM | [4] | ||
| Co-Target Name | Cytochrome P450 2C19 (CYP2C19) | Co-Target | ||||
| UniProt ID | CP2CJ_HUMAN | |||||
| Gene Name | CYP2C19 | |||||
| Synonyms |
Fenbendazole monooxygenase (4'-hydroxylating); (R)-limonene 6-monooxygenase; (S)-limonene 6-monooxygenase; (S)-limonene 7-monooxygenase; CYPIIC17; CYPIIC19; Cytochrome P450-11A; Cytochrome P450-254C; Mephenytoin 4-hydroxylase
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| Representative Drug(s) | Rilpivirine | Drug Info | IC50 = 335 nM | [3] | ||
| References | Top | ||||
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| REF 1 | Molecular and cellular studies evaluating a potent 2-cyanoindolizine catechol diether NNRTI targeting wildtype and Y181C mutant HIV-1 reverse transcriptase. Bioorg Med Chem Lett. 2019 Aug 15;29(16):2182-2188. | ||||
| REF 2 | Discovery of aminocyclohexene analogues as selective and orally bioavailable hNav1.7 inhibitors for analgesia. Bioorg Med Chem Lett. 2017 Nov 15;27(22):4979-4984. | ||||
| REF 3 | Structure-Based Bioisosterism Yields HIV-1 NNRTIs with Improved Drug-Resistance Profiles and Favorable Pharmacokinetic Properties. J Med Chem. 2020 May 14;63(9):4837-4848. | ||||
| REF 4 | Substituted Indazoles as Nav1.7 Blockers for the Treatment of Pain. J Med Chem. 2016 Apr 14;59(7):3373-91. | ||||
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