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ChEMBL ligand: CHEMBL415324 (MK-341, NSC-758970, Rizaben, Tranilast) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]