tipranavir [Ligand Id: 12685] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL222559 (Aptivus, Tipranavir, U-140690)
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  • Human immunodeficiency virus type 1 protease in Human immunodeficiency virus 1 [ChEMBL: CHEMBL243] [UniProtKB: Q72874]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CAAX prenyl protease 1 homolog in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075286] [UniProtKB: Q80W54]
ChEMBL Inhibition of mouse ZMPSTE24 expressed n delta ste24 delta rce1 yeast B 5.92 pIC50 1200 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 13432-13437 [PMID:17652517]
cathepsin D/Cathepsin D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2581] [GtoPdb: 2345] [UniProtKB: P07339]
ChEMBL Compound was tested for inhibition human Cathepsin D B 4.82 pKi 15000 nM Ki J Med Chem (1996) 39: 4349-4353 [PMID:8893827]
cathepsin E/Cathepsin E in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3092] [GtoPdb: 2346] [UniProtKB: P14091]
ChEMBL Compound was tested for inhibition human Cathepsin E B 5.05 pKi 9000 nM Ki J Med Chem (1996) 39: 4349-4353 [PMID:8893827]
Human immunodeficiency virus type 1 protease in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL243] [UniProtKB: Q72874]
ChEMBL Compound was tested for inhibition of HIV protease triple mutant (Q7K/L33I/L63I) B 9 pKi <1 nM Ki J Med Chem (1996) 39: 4349-4353 [PMID:8893827]
ChEMBL Tested for inhibition of HIV protease B 7.52 pIC50 30 nM IC50 J Med Chem (1996) 39: 4349-4353 [PMID:8893827]
ChEMBL Inhibition of HIV-1 protease in a cell culture assay using HIV-1 IIIB infected H9 cells. F 7.52 pIC50 30 nM IC50 J Med Chem (1998) 41: 3467-3476 [PMID:9719600]
pepsinogen A5/Pepsin A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3295] [GtoPdb: 2390] [UniProtKB: P0DJD9]
ChEMBL Inhibition of human pepsin B 5.7 pKi 2000 nM Ki J Med Chem (1996) 39: 4349-4353 [PMID:8893827]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimicrobial activity against chloroquine-resistant Plasmodium falciparum Dd2 after 48 hrs F 4.68 pEC50 21000 nM EC50 Antimicrob Agents Chemother (2010) 54: 1334-1337 [PMID:20028821]
ChEMBL Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 48 hrs F 4.7 pEC50 20000 nM EC50 Antimicrob Agents Chemother (2010) 54: 1334-1337 [PMID:20028821]
ChEMBL Antimicrobial activity against Plasmodium falciparum harboring HFP-tagged Pfs16 protein after 48 hrs F 4.74 pEC50 18000 nM EC50 Antimicrob Agents Chemother (2010) 54: 1334-1337 [PMID:20028821]
ChEMBL Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum D10 after 48 hrs F 4.92 pEC50 12000 nM EC50 Antimicrob Agents Chemother (2010) 54: 1334-1337 [PMID:20028821]

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]