Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
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
SCNBA_HUMAN
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) 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) 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
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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