Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T12119 | Target Info | |||
| Target Name | Voltage-gated sodium channel alpha Nav1.7 (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
Click to Show/Hide
|
||||
| Target Type | Clinical trial Target | ||||
| Gene Name | SCN9A | ||||
| Biochemical Class | Voltage-gated ion channel | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| 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
Click to Show/Hide
|
|||||
| Representative Drug(s) | PF-05089771 | Drug Info | IC50 = 11 nM | Click to Show More | [1] | |
| 2 | XEN-402 | Drug Info | IC50 = 84 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
Click to Show/Hide
|
|||||
| Representative Drug(s) | PF-05089771 | Drug Info | IC50 = 299 nM | [3] | ||
| 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
Click to Show/Hide
|
|||||
| Representative Drug(s) | PF-05089771 | Drug Info | IC50 = 160 nM | Click to Show More | [2] | |
| 2 | XEN-402 | Drug Info | IC50 = 170 nM | [2] | ||
| 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
Click to Show/Hide
|
|||||
| Representative Drug(s) | PF-05089771 | Drug Info | IC50 = 110 nM | Click to Show More | [2] | |
| 2 | XEN-402 | Drug Info | IC50 = 600 nM | [2] | ||
| Co-Target Name | Sodium channel protein type VII alpha (SCN7A) | Co-Target | ||||
| UniProt ID | SCN7A_HUMAN | |||||
| Gene Name | SCN7A | |||||
| Synonyms |
Sodium channel protein type 7 subunit alpha; Putative voltage-gated sodium channel subunit alpha Nax; Sodium channel protein cardiac and skeletal muscle subunit alpha; Sodium channel protein type VII subunit alpha
Click to Show/Hide
|
|||||
| Representative Drug(s) | PF-05089771 | Drug Info | IC50 = 11 nM | Click to Show More | [2] | |
| 2 | XEN-402 | Drug Info | IC50 = 54 nM | [2] | ||
| Co-Target Name | Sodium channel protein type I alpha (SCN1A) | Co-Target | ||||
| UniProt ID | SCN1A_HUMAN | |||||
| Gene Name | SCN1A | |||||
| Synonyms |
Sodium channel protein type 1 subunit alpha; Sodium channel protein brain I subunit alpha; Sodium channel protein type I subunit alpha; Voltage-gated sodium channel subunit alpha Nav1.1
Click to Show/Hide
|
|||||
| Representative Drug(s) | PF-05089771 | Drug Info | IC50 = 677 nM | [3] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Benzoxazolinone aryl sulfonamides as potent, selective Na. Bioorg Med Chem Lett. 2017 Jun 15;27(12):2683-8. | ||||
| REF 2 | Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na V 1.7. J Med Chem. 2019 Oct 10;62(19):8695-8710. | ||||
| REF 3 | Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of Na. J Med Chem. 2017 Aug 24;60(16):7029-42. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.