Co-Target(s) Information
| 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 | |||||
| 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) | 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) | 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) | 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) | 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) | 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) | 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) | 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) | 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) | 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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