Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T88595 | Target Info | |||
Target Name | MERS-CoV spike glycoprotein (S) | ||||
Synonyms |
MERS-CoV S glycoprotein; MERS-CoV E2; MERS-CoV Peplomer protein
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Gene Name | MERS-CoV S | ||||
Biochemical Class | Betacoronaviruses spike protein family | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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Co-Target Name | Cationic trypsinogen (PRSS1) | Successful Target | ||||
UniProt ID | TRY1_HUMAN | |||||
Gene Name | PRSS1 | |||||
Synonyms |
Trypsin-1; Trypsin I; TRYP1; TRY1; TRP1; Serine protease 1; Beta-trypsin
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Representative Drug(s) | Nafamostat | Drug Info | IC50 = 17 nM | [1] | ||
Co-Target Name | Complement C1s component (C1S) | Successful Target | ||||
UniProt ID | C1S_HUMAN | |||||
Gene Name | C1S | |||||
Synonyms |
Complement component 1 subcomponent s; Complement C1s subcomponent; C1-esterase; C1 esterase
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Representative Drug(s) | Nafamostat | Drug Info | IC50 = 29 nM | [2] | ||
Co-Target Name | Plasminogen (PLG) | Successful Target | ||||
UniProt ID | PLMN_HUMAN | |||||
Gene Name | PLG | |||||
Synonyms |
Plasmin
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Representative Drug(s) | Nafamostat | Drug Info | IC50 = 240 nM | [3] | ||
Co-Target Name | Coagulation factor IIa (F2) | Successful Target | ||||
UniProt ID | THRB_HUMAN | |||||
Gene Name | F2 | |||||
Synonyms |
Prothrombin; Coagulation factor II
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Representative Drug(s) | Nafamostat | Drug Info | IC50 = 290 nM | [3] | ||
Co-Target Name | Suppressor of tumorigenicity 14 protein (ST14) | Patented-recorded Target | ||||
UniProt ID | ST14_HUMAN | |||||
Gene Name | ST14 | |||||
Synonyms |
Tumor-associated differentially-expressed gene 15 protein; Tumor associated differentially-expressed gene-15 protein; TADG15; Serine protease TADG-15; Serine protease 14; SNC19; Prostamin; PRSS14; Membrane-type serine protease 1; Membrane type serine protease 1; Matriptase; MT-SP1
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Representative Drug(s) | Nafamostat | Drug Info | Ki = 0.02 nM | [4] | ||
Co-Target Name | Serine protease hepsin (HPN) | Patented-recorded Target | ||||
UniProt ID | HEPS_HUMAN | |||||
Gene Name | HPN | |||||
Synonyms |
Transmembrane protease, serine 1; HPN; HEPSIN
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Representative Drug(s) | Nafamostat | Drug Info | Ki = 0.53 nM | [4] | ||
Co-Target Name | Hepatocyte growth factor activator (HGFAC) | Literature-reported Target | ||||
UniProt ID | HGFA_HUMAN | |||||
Gene Name | HGFAC | |||||
Synonyms |
Hepatocyte growth factor activator long chain; HGFAC; HGFA; HGF activator
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Representative Drug(s) | Nafamostat | Drug Info | Ki = 25 nM | [5] | ||
Co-Target Name | Tissue kallikrein (KLK1) | Literature-reported Target | ||||
UniProt ID | KLK1_HUMAN | |||||
Gene Name | KLK1 | |||||
Synonyms |
Kidney/pancreas/salivary gland kallikrein; Kallikrein1; Kallikrein-1
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Representative Drug(s) | Nafamostat | Drug Info | IC50 = 650 nM | [3] | ||
Co-Target Name | Complement C1r (C1R) | Co-Target | ||||
UniProt ID | C1R_HUMAN | |||||
Gene Name | C1R | |||||
Synonyms |
Complement C1r subcomponent; Complement component 1 subcomponent r
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Representative Drug(s) | Nafamostat | Drug Info | IC50 = 800 nM | [2] |
References | Top | ||||
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REF 1 | Benzenesulfonamide derivatives of 2-substituted 4H-3,1-benzoxazin-4-ones and benzthiazin-4-ones as inhibitors of complement C1r protease. Bioorg Med Chem Lett. 1999 Mar 22;9(6):815-20. | ||||
REF 2 | Chemical Approaches to Modulating Complement-Mediated Diseases. J Med Chem. 2018 Apr 26;61(8):3253-3276. | ||||
REF 3 | Synthesis and evaluation of 2-aryl-4H-3,1-benzoxazin-4-ones as C1r serine protease inhibitors. Bioorg Med Chem Lett. 1996 Mar 19;6(6):679-82. | ||||
REF 4 | Structure-based discovery of small molecule hepsin and HGFA protease inhibitors: Evaluation of potency and selectivity derived from distinct binding pockets. Bioorg Med Chem. 2015 May 15;23(10):2328-43. | ||||
REF 5 | Inhibitors of HGFA, Matriptase, and Hepsin Serine Proteases: A Nonkinase Strategy to Block Cell Signaling in Cancer. ACS Med Chem Lett. 2014 Oct 9;5(11):1219-24. |
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