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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| 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] |
| HIV-1 protease in Human immunodeficiency virus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4296312] [UniProtKB: O90781] | ||||||||
| ChEMBL | Enzyme Inhibition of Purified HIV-1 Protease: Protease inhibitors (PI) are used to treat HIV infection by preventing viral assembly and maturation through the inhibition of HIV-1 protease activity. Biochemical assays were performed to evaluate the potential of PEG-PI conjugates to inhibit HIV-1 protease activity, relative to their respective PI parent molecules. Activity assays were performed at using the SensoLyte 520 HIV-Protease Assay Kit (Anaspec Inc., San Jose, Calif.) and recombinant HIV-1 protease. Protease activity was monitored by the formation of a fluorescent reporter product generated during HIV-1 protease-mediated digestion of a quenched, fluorimetric substrate containing the p17/p24 Prgag cleavage site. | B | 8.14 | pIC50 | 7.2 | nM | IC50 | US-10806794-B2. Protease inhibitors having enhanced features (2020) |
| 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] |
| CoV Replicase polyprotein 1ab/CoV RNA-dependent RNA polymerase/CoV Non-structural protein 15/CoV Non-structural protein 13/Replicase polyprotein 1ab in Severe acute respiratory syndrome coronavirus 2 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523582] [GtoPdb: 3125, 3139, 3206, 3261] [UniProtKB: P0DTD1] | ||||||||
| ChEMBL | Inhibition of SARS-CoV-2 MPro | B | 5.13 | pIC50 | 7380 | nM | IC50 | Eur J Med Chem (2023) 258: 115563-115563 [PMID:37329713] |
ChEMBL data shown on this page come from version 36:
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]
