| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T83145 | ||||
| Target Name | Nuclear factor NF-kappa-B (NFKB) | ||||
| Type of Target |
Successful |
||||
| Drug Potency against Target | Sulfasalazine | Drug Info | IC50 = 89 nM | [5] | |
| 15-ACETOXY-EREMANTHOLIDE B | Drug Info | IC100 = 5000 nM | [2] | ||
| 15-ACETOXY-EREMANTHOLIDE B | Drug Info | IC100 = 5000 nM | [1] | ||
| 15-DEOXYBUDLEIN A | Drug Info | IC100 = 5000 nM | [2] | ||
| 15-DEOXYBUDLEIN A | Drug Info | IC100 = 5000 nM | [1] | ||
| 15-deoxygoiazensolide | Drug Info | IC100 = 10000 nM | [2] | ||
| 15-isobutyrylmiguanin | Drug Info | IC100 = 12500 nM | [2] | ||
| 1beta-methoxy-miller-9Z-enolide | Drug Info | IC100 = 10000 nM | [2] | ||
| 2-amino-N-(quinolin-8-yl)benzenesulfonamide | Drug Info | IC50 = 2000 nM | [3] | ||
| 2-nitro-N-(quinolin-8-yl)benzenesulfonamide | Drug Info | IC50 = 3200 nM | [3] | ||
| 2-oxoguaia-1,4(15), 11(13)-trien-12,8beta-olide | Drug Info | IC100 = 5000 nM | [2] | ||
| 2-oxoguaia-1,4,11(13)-trien-12,8alpha-olide | Drug Info | IC100 = 10000 nM | [2] | ||
| 2beta-methoxy-2-deethoxyphantomolin | Drug Info | IC100 = 10000 nM | [2] | ||
| 3,4-epoxydehydroleucodin | Drug Info | IC100 = 5000 nM | [2] | ||
| 4,5-ISOBUDLEIN A | Drug Info | IC100 = 10000 nM | [2] | ||
| 4-nitro-N-(quinolin-8-yl)benzenesulfonamide | Drug Info | IC50 = 1500 nM | [3] | ||
| 4beta,15-epoxy-miller-9E-enolide | Drug Info | IC100 = 5000 nM | [2] | ||
| 4beta,15-epoxy-miller-9Z-enolide | Drug Info | IC100 = 5000 nM | [2] | ||
| 5-bromo-N-(quinolin-8-yl)thiophene-2-sulfonamide | Drug Info | IC50 = 1100 nM | [3] | ||
| 5-chloro-N-(quinolin-8-yl)thiophene-2-sulfonamide | Drug Info | IC50 = 1300 nM | [3] | ||
| 5H-6-thia-4,5-diaza-chrysene 6,6-dioxide | Drug Info | IC50 = 1000 nM | [3] | ||
| 7-hydroxycostunolide | Drug Info | IC100 = 10000 nM | [2] | ||
| 9-chloro-5H-6-thia-4,5-diaza-chrysene 6,6-dioxide | Drug Info | IC50 = 1100 nM | [3] | ||
| 9-fluoro-5H-6-thia-4,5-diaza-chrysene 6,6-dioxide | Drug Info | IC50 = 1700 nM | [3] | ||
| 9-methyl-5H-6-thia-4,5-diaza-chrysene 6,6-dioxide | Drug Info | IC50 = 600 nM | [3] | ||
| 9alpha-acetoxy-miller-1(10)Z-enolide | Drug Info | IC100 = 10000 nM | [2] | ||
| ARTOBILOXANTHONE | Drug Info | IC50 = 3700 nM | [4] | ||
| ARTORIGIDIN A | Drug Info | IC50 = 2000 nM | [4] | ||
| ATRIPLICIOLIDTIGLATE | Drug Info | IC100 = 5000 nM | [2] | ||
| ATRIPLICIOLIDTIGLATE | Drug Info | IC100 = 5000 nM | [1] | ||
| BUDLEIN A | Drug Info | IC100 = 5000 nM | [2] | ||
| BUDLEIN A | Drug Info | IC100 = 5000 nM | [1] | ||
| Centratherin | Drug Info | IC100 = 5000 nM | [2] | ||
| ENHYDRIN | Drug Info | IC100 = 10000 nM | [2] | ||
| HELENALIN | Drug Info | IC100 = 10000 nM | [2] | ||
| HELENALIN | Drug Info | IC100 = 10000 nM | [1] | ||
| Helenalin-2-methylbutyrate | Drug Info | IC100 = 10000 nM | [2] | ||
| HELENALINMETHACRYLATE | Drug Info | IC100 = 5000 nM | [2] | ||
| ISOGOIAZENSOLIDE | Drug Info | IC100 = 10000 nM | [2] | ||
| ISOGOIAZENSOLIDE | Drug Info | IC100 = 10000 nM | [1] | ||
| Miller-9E-enolide | Drug Info | IC100 = 5000 nM | [2] | ||
| Miller-9Z-enolide | Drug Info | IC100 = 10000 nM | [2] | ||
| MOLEPHANTIN | Drug Info | IC100 = 10000 nM | [2] | ||
| MOLEPHANTIN | Drug Info | IC100 = 10000 nM | [1] | ||
| MOLEPHANTININ | Drug Info | IC100 = 10000 nM | [2] | ||
| MOLEPHANTININ | Drug Info | IC100 = 10000 nM | [1] | ||
| N-(quinolin-8-yl)thiophene-2-sulfonamide | Drug Info | IC50 = 3600 nM | [3] | ||
| ROCAGLAMIDE | Drug Info | IC50 = 4000 nM | [4] | ||
| SCANDENOLIDE | Drug Info | IC100 = 10000 nM | [2] | ||
| SCANDENOLIDE | Drug Info | IC100 = 10000 nM | [1] | ||
| Action against Disease Model | Omtriptolide | Drug Info | Triptolide significantly impairs DC-mediated chemoattraction of neutrophils and T cells both in vitro and in vivo by suppressing DC production of CC and CXC chemokines includingMIP-1alpha, MIP-1beta, MCP-1, RANTES, TARC, and IP-10 in response to LPS. triptolide-mediated inhibition of NF-kappaB activation, Stat3 phosphorylation and increase of SOCS1 expression in DC may be involved in the inhibitory effect of triptolide | [6] | |
| References | |||||
| REF 1 | Quantitative structure-activity relationship of sesquiterpene lactones as inhibitors of the transcription factor NF-kappaB. J Med Chem. 2004 Nov 18;47(24):6042-54. | ||||
| REF 2 | Development of a structural model for NF-kappaB inhibition of sesquiterpene lactones using self-organizing neural networks. J Med Chem. 2006 Apr 6;49(7):2241-52. | ||||
| REF 3 | Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFkappaB activity within two separate high-throughput s... Bioorg Med Chem Lett. 2008 Jan 1;18(1):329-35. | ||||
| REF 4 | Cytotoxic and NF-kappaB inhibitory constituents of Artocarpus rigida. J Nat Prod. 2010 May 28;73(5):949-55. | ||||
| REF 5 | Novel sulfasalazine analogues with enhanced NF-kB inhibitory and apoptosis promoting activity. Apoptosis. 2005 May;10(3):481-91. | ||||
| REF 6 | Immunosuppressant triptolide inhibits dendritic cell-mediated chemoattraction of neutrophils and T cells through inhibiting Stat3 phosphorylation a... Biochem Biophys Res Commun. 2006 Jul 7;345(3):1122-30. | ||||
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