Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T20297 Target Info
Target Name Serine protease unspecific (SP)
Target Type Successful Target
Gene Name NO-GeName
UniProt ID
NOUNIPROTAC
Co-Targets of This Target  Top
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 Click to Show More [1]
2 Camostat Drug Info IC50 = 50.6 nM [3]
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 [4]
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 Click to Show More [4]
2 Gabexate Drug Info IC50 = 687 nM [5]
3 Camostat Drug Info IC50 = 780 nM [7]
Co-Target Name Urokinase-type plasminogen activator (PLAU) Successful Target
UniProt ID UROK_HUMAN
Gene Name PLAU
Synonyms
UPA; U-plasminogen activator
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Representative Drug(s) Gabexate Drug Info IC50 = 431 nM [5]
Co-Target Name Solute carrier family 47 member 1 (SLC47A1) Successful Target
UniProt ID S47A1_HUMAN
Gene Name SLC47A1
Synonyms
hMATE-1; Multidrug and toxin extrusion protein 1; MATE1; MATE-1
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Representative Drug(s) Gabexate Drug Info IC50 = 500 nM [6]
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 [8]
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 [9]
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 [4]
Co-Target Name Trypsin (TRY) Co-Target
UniProt ID TRY1_HUMAN; TRY2_HUMAN; TRY3_HUMAN
Gene Name PRSS1; PRSS2; PRSS3
Representative Drug(s) Camostat Drug Info IC50 = 3.5 nM [7]
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]
Co-Target Name Solute carrier family 22 member 2 (SLC22A2) Co-Target
UniProt ID S22A2_HUMAN
Gene Name SLC22A2
Synonyms
Organic cation transporter 2; hOCT2
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Representative Drug(s) Gabexate Drug Info IC50 = 900 nM [6]
References  Top
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 New orally active serine protease inhibitors. J Med Chem. 1995 Jul 7;38(14):2521-3.
REF 4 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 5 Discovery and SAR of Novel and Selective Inhibitors of Urokinase Plasminogen Activator (uPA) with an Imidazo[1,2-a]pyridine Scaffold. J Med Chem. 2015 Dec 10;58(23):9238-57.
REF 6 Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. J Med Chem. 2013 Feb 14;56(3):781-795.
REF 7 Synthesis and structure-activity relationships of small-molecular di-basic esters, amides and carbamates as flaviviral protease inhibitors. Eur J Med Chem. 2019 Aug 15;176:187-194.
REF 8 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 9 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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