Syk inhibitor III [Ligand Id: 6048] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL596380 (3,4-Methylenedioxyb-Nitrostyrene)
  • NLRP3/NACHT, LRR and PYD domains-containing protein 3 in Mouse [ChEMBL: CHEMBL3779755] [GtoPdb: 1770] [UniProtKB: Q8R4B8]
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  • Transitional endoplasmic reticulum ATPase in Human [ChEMBL: CHEMBL1075145] [UniProtKB: P55072]
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  • SRC proto-oncogene, non-receptor tyrosine kinase in Human [GtoPdb: 2206] [UniProtKB: P12931]
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  • spleen associated tyrosine kinase in Human [GtoPdb: 2230] [UniProtKB: P43405]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
NLRP3/NACHT, LRR and PYD domains-containing protein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3779755] [GtoPdb: 1770] [UniProtKB: Q8R4B8]
ChEMBL Inhibition of NLRP3 inflammasome activation in LPS-stimulated mouse bone marrow-derived macrophages assessed as reduction in IL-1beta secretion preincubated for 30 mins followed by nigericin addition and measured after 30 mins by ELISA B 5.64 pIC50 2310 nM IC50 J Med Chem (2021) 64: 13633-13657 [PMID:34506712]
ChEMBL Inhibition of NLRP3 in LPS stimulated mouse BMDM cells after 15 mins followed by addition of ATP by ELISA analysis B 5.7 pIC50 2000 nM IC50 J Med Chem (2016) 59: 1691-1710 [PMID:26422006]
ChEMBL Inhibition of NLRP3 inflammasome activation in LPS-primed mouse bone marrow derived macrophages preincubated for 15 mins followed by addition of ATP and measured after 30 mins by ELISA method B 5.7 pIC50 2000 nM IC50 Eur J Med Chem (2020) 185: 111822-111822 [PMID:31699536]
Transitional endoplasmic reticulum ATPase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075145] [UniProtKB: P55072]
ChEMBL Inhibition of His6-tagged p97 (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as reduction in ATPase activity measured after 60 mins by biomol green reagent based assay B 5.77 pIC50 1700 nM IC50 Eur J Med Chem (2021) 213: 113148-113148 [PMID:33476933]
ChEMBL Inhibition of p97 in human HeLa cells assessed as reduction in proteasomal turnover of p97-dependent reporter substrate UbG76V-GFP incubated for 120 mins by luciferase reporter gene assay B 5.8 pIC50 1600 nM IC50 Eur J Med Chem (2021) 213: 113148-113148 [PMID:33476933]
SRC proto-oncogene, non-receptor tyrosine kinase in Human [GtoPdb: 2206] [UniProtKB: P12931]
GtoPdb - - 4.56 pIC50 27300 nM IC50 Biochem Pharmacol (2007) 74: 601-11 [PMID:17601492]
spleen associated tyrosine kinase in Human [GtoPdb: 2230] [UniProtKB: P43405]
GtoPdb - - 5.55 pIC50 2800 nM IC50 Biochem Pharmacol (2007) 74: 601-11 [PMID:17601492]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]