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 inflammasome activation in LPS/nigericin-treated C57BL/6 mouse bone marrow-derived macrophages assessed as reduction in IL-1beta secretion preincubated for 3 hrs with LPS and for 30 mins with compound prior to nigericin addition and measured after 30 mins by ELISA B 5.64 pIC50 2310 nM IC50 Eur J Med Chem (2022) 236: 114357-114357 [PMID:35428012]
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]