Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T34123 | Target Info | |||
Target Name | Voltage-gated sodium channel alpha Nav1.9 (SCN11A) | ||||
Synonyms |
hNaN; Sodium channel protein type XIsubunit alpha; Sodium channel protein type 11subunit alpha; Sensory neuron sodium channel 2; SNS2; SCN12A; SCN11A; Peripheral nerve sodium channel 5; PN5
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Target Type | Successful Target | ||||
Gene Name | SCN11A | ||||
Biochemical Class | Voltage-gated ion channel | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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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) | Tolperisone | Drug Info | Ki = 5.587 nM | [1] | ||
Co-Target Name | Human immunodeficiency virus Protease (HIV PR) | Successful Target | ||||
UniProt ID | POL_HV1B1 | |||||
Gene Name | HIV PR | |||||
Synonyms |
HIV Retropepsin; HIV PR
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Representative Drug(s) | Iboctadekin + rituximab | Drug Info | Ki = 16.98 nM | [2] | ||
Co-Target Name | Angiotensinogenase renin (REN) | Successful Target | ||||
UniProt ID | RENI_HUMAN | |||||
Gene Name | REN | |||||
Synonyms |
Renin; Angiotensinogenase
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Representative Drug(s) | Iboctadekin + rituximab | Drug Info | Ki = 100 nM | [3] | ||
Co-Target Name | Carbonic anhydrase II (CA-II) | Successful Target | ||||
UniProt ID | CAH2_HUMAN | |||||
Gene Name | CA2 | |||||
Synonyms |
Carbonic anhydrase C; Carbonic anhydrase 2; Carbonate dehydratase II; CAC
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Representative Drug(s) | Lacosamide | Drug Info | Ki = 331 nM | [4] | ||
Co-Target Name | Carbonic anhydrase I (CA-I) | Successful Target | ||||
UniProt ID | CAH1_HUMAN | |||||
Gene Name | CA1 | |||||
Synonyms |
Carbonic anhydrase B; Carbonic anhydrase 1; Carbonate dehydratase I; CAB
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Representative Drug(s) | Lacosamide | Drug Info | Ki = 362 nM | [4] | ||
Co-Target Name | Carbonic anhydrase VI (CA-VI) | Successful Target | ||||
UniProt ID | CAH6_HUMAN | |||||
Gene Name | CA6 | |||||
Synonyms |
Secreted carbonic anhydrase; Salivary carbonic anhydrase; Carbonic anhydrase 6; Carbonate dehydratase VI
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Representative Drug(s) | Lacosamide | Drug Info | Ki = 412 nM | [4] | ||
Co-Target Name | Adrenergic receptor alpha-2B (ADRA2B) | Successful Target | ||||
UniProt ID | ADA2B_HUMAN | |||||
Gene Name | ADRA2B | |||||
Synonyms |
Subtype C2; Alpha-2BAR; Alpha-2B adrenoreceptor; Alpha-2B adrenoceptor; Alpha-2B adrenergic receptor; Alpha-2 adrenergic receptor subtype C2; ADRA2RL1; ADRA2L1
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Representative Drug(s) | Tolperisone | Drug Info | Ki = 456 nM | [1] | ||
Co-Target Name | Carbonic anhydrase XIV (CA-XIV) | Successful Target | ||||
UniProt ID | CAH14_HUMAN | |||||
Gene Name | CA14 | |||||
Synonyms |
UNQ690/PRO1335; Carbonic anhydrase 14; Carbonate dehydratase XIV
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Representative Drug(s) | Lacosamide | Drug Info | Ki = 473 nM | [4] | ||
Co-Target Name | Carbonic anhydrase IV (CA-IV) | Successful Target | ||||
UniProt ID | CAH4_HUMAN | |||||
Gene Name | CA4 | |||||
Synonyms |
Carbonic anhydrase 4; Carbonate dehydratase IV; CAIV
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Representative Drug(s) | Lacosamide | Drug Info | Ki = 525 nM | [4] | ||
Co-Target Name | Cathepsin D (CTSD) | Clinical trial Target | ||||
UniProt ID | CATD_HUMAN | |||||
Gene Name | CTSD | |||||
Synonyms |
CPSD; CD
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Representative Drug(s) | Iboctadekin + rituximab | Drug Info | IC50 = 0.0016 ug.mL-1 | [5] | ||
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) | Lacosamide | Drug Info | IC50 = 182 nM | [6] | ||
Co-Target Name | Carbonic anhydrase IX (CA-IX) | Clinical trial Target | ||||
UniProt ID | CAH9_HUMAN | |||||
Gene Name | CA9 | |||||
Synonyms |
Renal cell carcinoma-associated antigen G250; RCC-associated antigen G250; PMW1; P54/58N; Membrane antigen MN; MN; G250 antigen (MN/CA IX/G250); G250; Carbonic anhydrase 9; Carbonate dehydratase IX; CAIX
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Representative Drug(s) | Lacosamide | Drug Info | Ki = 353 nM | [4] | ||
Co-Target Name | Cathepsin L (CTSL) | Clinical trial Target | ||||
UniProt ID | CATL1_HUMAN | |||||
Gene Name | CTSL | |||||
Synonyms |
Major excreted protein; MEP; Cathepsin L1; CTSL1
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Representative Drug(s) | Iboctadekin + rituximab | Drug Info | IC50 = 800 nM | [7] | ||
Co-Target Name | Plasmodium Plasmepsin 2 (Malaria PLA2) | Patented-recorded Target | ||||
UniProt ID | PLM2_PLAFA | |||||
Gene Name | Malaria PLA2 | |||||
Synonyms |
Plasmepsin-2; PFAPD; Aspartic hemoglobinase II
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Representative Drug(s) | Iboctadekin + rituximab | Drug Info | IC50 = 0.42 nM | [8] | ||
Co-Target Name | Cathepsin E (CTSE) | Literature-reported Target | ||||
UniProt ID | CATE_HUMAN | |||||
Gene Name | CTSE | |||||
Synonyms |
Cathepsin E
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Representative Drug(s) | Iboctadekin + rituximab | Drug Info | IC50 = 0.08 nM | [9] | ||
Co-Target Name | Plasmodium Plasmepsin 1 (Malaria PLA1) | Literature-reported Target | ||||
UniProt ID | PLM1_PLAFA | |||||
Gene Name | Malaria PLA1 | |||||
Synonyms |
Plasmepsin I; PFAPG; Aspartic hemoglobinase I
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Representative Drug(s) | Iboctadekin + rituximab | Drug Info | IC50 = 0.9 nM | [8] | ||
Co-Target Name | Pepsinogen-5 (PGA5) | Literature-reported Target | ||||
UniProt ID | PEPA5_HUMAN | |||||
Gene Name | PGA5 | |||||
Synonyms |
Pepsin A-5
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Representative Drug(s) | Iboctadekin + rituximab | Drug Info | IC50 = 59 nM | [10] | ||
Co-Target Name | Disintegrin and metalloproteinase domain-containing protein 9 (ADAM9) | Co-Target | ||||
UniProt ID | ADAM9_HUMAN | |||||
Gene Name | ADAM9 | |||||
Synonyms |
ADAM 9; Cellular disintegrin-related protein; Meltrin-gamma; Metalloprotease/disintegrin/cysteine-rich protein 9; Myeloma cell metalloproteinase
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Representative Drug(s) | Iboctadekin + rituximab | Drug Info | IC50 = 56.3 nM | [11] | ||
Co-Target Name | Carbonic anhydrase VB (CA5B) | Co-Target | ||||
UniProt ID | CAH5B_HUMAN | |||||
Gene Name | CA5B | |||||
Synonyms |
Carbonic anhydrase 5B, mitochondrial; Carbonate dehydratase VB; Carbonic anhydrase VB; CA-VB
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Representative Drug(s) | Lacosamide | Drug Info | Ki = 341 nM | [4] | ||
Co-Target Name | Carbonic anhydrase III (CA3) | Co-Target | ||||
UniProt ID | CAH3_HUMAN | |||||
Gene Name | CA3 | |||||
Synonyms |
Carbonic anhydrase 3; Carbonate dehydratase III; CA-III
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Representative Drug(s) | Lacosamide | Drug Info | Ki = 374 nM | [4] |
References | Top | ||||
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REF 1 | DrugMatrix in vitro pharmacology data. National Toxicology Program | ||||
REF 2 | Three-dimensional pharmacophores from binding data. J Med Chem. 1994 Jun 10;37(12):1769-78. | ||||
REF 3 | Inhibition of the renin-angiotensin system. A new approach to the therapy of hypertension. J Med Chem. 1981 Apr;24(4):355-61. | ||||
REF 4 | The coumarin-binding site in carbonic anhydrase accommodates structurally diverse inhibitors: the antiepileptic lacosamide as an example and lead molecule for novel classes of carbonic anhydrase inhibitors. J Med Chem. 2010 Jan 28;53(2):850-4. | ||||
REF 5 | Inhibition of Cathepsin D protease activity by. Med Chem Res. 2012 Dec 18;22:3953-8. | ||||
REF 6 | Ion channels as therapeutic targets: a drug discovery perspective. J Med Chem. 2013 Feb 14;56(3):593-624. | ||||
REF 7 | Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity. J Med Chem. 2009 May 14;52(9):3093-7. | ||||
REF 8 | 2-Aminoquinazolin-4(3H)-one based plasmepsin inhibitors with improved hydrophilicity and selectivity. Bioorg Med Chem. 2018 May 15;26(9):2488-2500. | ||||
REF 9 | Tasiamide F, a potent inhibitor of cathepsins D and E from a marine cyanobacterium. Bioorg Med Chem. 2016 Aug 1;24(15):3276-82. | ||||
REF 10 | Auxiliary agents for the peroral administration of peptide and protein drugs: synthesis and evaluation of novel pepstatin analogues. J Med Chem. 1998 Jun 18;41(13):2339-44. | ||||
REF 11 | Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. J Med Chem. 2009 Sep 24;52(18):5732-47. |
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