tranilast [Ligand Id: 6326] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL415324 (MK-341, NSC-758970, Rizaben, Tranilast)
  • H-PGDS/Hematopoietic prostaglandin D synthase in Human [ChEMBL: CHEMBL5879] [GtoPdb: 1381] [UniProtKB: O60760]
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  • NLRP3/NACHT, LRR and PYD domains-containing protein 3 in Mouse [ChEMBL: CHEMBL3779755] [GtoPdb: 1770] [UniProtKB: Q8R4B8]
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  • TRPV2/Transient receptor potential cation channel subfamily V member 2 in Human [ChEMBL: CHEMBL5051] [GtoPdb: 508] [UniProtKB: Q9Y5S1]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
H-PGDS/Hematopoietic prostaglandin D synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5879] [GtoPdb: 1381] [UniProtKB: O60760]
ChEMBL Inhibition of glutathione-S-transferase activity of prostaglandin D2 synthase B 4.94 pIC50 11600 nM IC50 J Med Chem (2008) 51: 2178-2186 [PMID:18341273]
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-primed C57BL/6 mouse bone marrow derived macrophages incubated for 30 mins in presence of ATP by immunoblotting analysis B 4.6 pIC50 25000 nM IC50 Bioorg Med Chem Lett (2021) 44: 128101-128101 [PMID:33984476]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
TRPV2/Transient receptor potential cation channel subfamily V member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5051] [GtoPdb: 508] [UniProtKB: Q9Y5S1]
GtoPdb - - 5 pIC50 10000 nM IC50 Cell Calcium (1997) 22: 75-82 [PMID:9292225]
ChEMBL Antagonist activity at TRPV2 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2019) 62: 1373-1384 [PMID:30620187]

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]