Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T20178 Target Info
Target Name Tumor necrosis factor (TNF)
Synonyms
Tumour necrosis factor alpha; Tumour necrosis factor; Tumor necrosis factor ligand superfamily member 2; TNFalpha; TNFSF2; TNFA; TNF-alpha; TNF-a; TNF alpha; Cachectin
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Target Type Successful Target
Gene Name TNF
Biochemical Class Cytokine: tumor necrosis factor
UniProt ID
TNFA_HUMAN
Co-Targets of This Target  Top
Co-Target Name Cannabinoid receptor 1 (CB1) Successful Target
UniProt ID CNR1_HUMAN
Gene Name CNR1
Synonyms
Cannabinoid CB1 receptor; CNR; CB-R; CANN6
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Representative Drug(s) CPL-7075 Drug Info Ki = 5.7 nM [1]
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 [2]
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 [3]
Co-Target Name Cannabinoid receptor 2 (CB2) Successful Target
UniProt ID CNR2_HUMAN
Gene Name CNR2
Synonyms
hCB2; Cannabinoid CB2 receptor; CX5; CB2B; CB2A; CB-2
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Representative Drug(s) CPL-7075 Drug Info Ki = 170.5 nM [4]
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 [5]
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 [5]
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 [6]
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 [6]
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 [7]
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 [5]
Co-Target Name Protein cereblon-DNA-binding protein Ikaros (CRBN-IKZF1) Co-Target
UniProt ID CRBN_HUMAN-IKZF1_HUMAN
Gene Name CRBN-IKZF1
Representative Drug(s) Lenalidomide Drug Info EC50 = 67 nM [8]
Co-Target Name Protein cereblon-Zinc finger protein Aiolos complex (CRBN-IKZF3) Co-Target
UniProt ID CRBN_HUMAN-IKZF3_HUMAN
Gene Name CRBN-IKZF3
Representative Drug(s) Lenalidomide Drug Info EC50 = 87 nM [8]
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 [3]
References  Top
REF 1 The cannabinoid acids, analogs and endogenous counterparts. Bioorg Med Chem. 2014 May 15;22(10):2830-43.
REF 2 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 3 Chemical Approaches to Modulating Complement-Mediated Diseases. J Med Chem. 2018 Apr 26;61(8):3253-3276.
REF 4 Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists. J Med Chem. 2013 Nov 14;56(21):8224-56.
REF 5 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 6 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 7 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.
REF 8 A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos. J Med Chem. 2018 Jan 25;61(2):535-542.

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