Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL129 (3'-azt, Azidothymidine, AZT, BW A509U, BW-A-509U, BW-A509U, BWA509U, COMPOUND S, COMPOUND-S, NSC-602670, Retrovir, Zidovudina, Zidovudine, Zidovudinum) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
DNA polymerase beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2392] [GtoPdb: 3231] [UniProtKB: P06746] | ||||||||
ChEMBL | Inhibition of DNA polymerase beta | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Nat Prod (1995) 58: 1024-1031 [PMID:7561895] |
Human immunodeficiency virus type 1 protease in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL243] [UniProtKB: Q72874] | ||||||||
ChEMBL | Inhibitory effect on HIV-1 RT activity using template primer,poly (rA)-oligo (dT) | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (1995) 38: 2038-2040 [PMID:7540208] |
ChEMBL | Compound is evaluated in vitro for the inhibition single mutant of HIV-1 RTS (Y181C) | B | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (1993) 36: 1291-1294 [PMID:7683725] |
ChEMBL | Compound is evaluated in vitro for the inhibition single mutant of HIV-1 RTS (K103 N) | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (1993) 36: 1291-1294 [PMID:7683725] |
ChEMBL | Inhibitory effect on HIV-1 RT activity using template primer,poly (rA)-oligo (dT) | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1995) 38: 2038-2040 [PMID:7540208] |
ChEMBL | Inhibitory activity against HIV-1 IIIB in CEM-SS infected cells (Experiment 1) | B | 6.9 | pEC50 | 126 | nM | EC50 | Bioorg Med Chem Lett (1999) 9: 803-806 [PMID:10206539] |
Human immunodeficiency virus type 1 reverse transcriptase in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL247] [UniProtKB: Q72547] | ||||||||
ChEMBL | Binding affinity to HIV1 reverse transcriptase assessed as compound incorporation into DNA by primer extension assay | B | 8.27 | pKd | 5.4 | nM | Kd | J Med Chem (2013) 56: 8765-8780 [PMID:24102161] |
ChEMBL | Compound was evaluated for enzymatic inhibitory activity against recombinant HIV reverse transcriptase | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1461-1466 [PMID:9873370] |
ChEMBL | Inhibition of HIV-1 reverse transcriptase | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 2411-2416 |
ChEMBL | Inhibition of HIV-1 reverse transcriptase. | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 2405-2410 |
ChEMBL | Inhibition of recombinant HIV-1 reverse transcriptase | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 87-90 [PMID:10636251] |
ChEMBL | Inhibition of recombinant reverse transcriptase (RT) in cell-free Quan-T-RT assay system | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3411-3416 [PMID:10617082] |
ChEMBL | Inhibition of HIV1 reverse transcriptase activity after 1 hr by ELISA | B | 4.67 | pIC50 | 21430 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 574-576 [PMID:21095125] |
ChEMBL | Inhibition of HIV1 reverse transcriptase incubated for 1 hr by colorimetric assay | B | 4.69 | pIC50 | 20520 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7041-7044 [PMID:23067552] |
ChEMBL | Inhibition of HIV1 reverse transcriptase using DIG-labeled dNTPs as substrate after 1 hr by ELISA | B | 4.7 | pIC50 | 20140 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 1738-1741 [PMID:26944616] |
ChEMBL | Inhibition of HIV-1 reverse transcriptase after 1 hr by ELISA plate reader analysis | B | 4.74 | pIC50 | 18220 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 3426-3429 [PMID:24953602] |
ChEMBL | Inhibition of HIV1 reverse transcriptase | B | 5.34 | pIC50 | 4540 | nM | IC50 | Bioorg Med Chem (2013) 21: 1964-1971 [PMID:23415084] |
ChEMBL | Inhibition of HIV1 reverse transcriptase M184V mutant-mediated viral DNA synthesis in human HOS cells assessed as luciferase activity treated 3 hrs before infection measured after 48 hrs by luminescence assay | B | 5.44 | pIC50 | 3600 | nM | IC50 | J Med Chem (2009) 52: 5356-5364 [PMID:19678643] |
ChEMBL | Inhibition of wild type HIV-1 reverse transcriptase assessed as inhibition of biotin deoxyuridine triphosphate incorporation into protein | B | 5.66 | pIC50 | 2200 | nM | IC50 | Eur J Med Chem (2023) 246: 114939-114939 [PMID:36442370] |
ChEMBL | Inhibition of HIV1 wild type reverse transcriptase-mediated viral DNA synthesis in human HOS cells assessed as luciferase activity treated 3 hrs before infection measured after 48 hrs by luminescence assay | B | 5.85 | pIC50 | 1400 | nM | IC50 | J Med Chem (2009) 52: 5356-5364 [PMID:19678643] |
ChEMBL | Inhibition of HIV-1 reverse transcriptase from peripheral blood mononuclear cells | B | 7 | pIC50 | <100 | nM | IC50 | J Med Chem (1991) 34: 3305-3309 [PMID:1720175] |
ChEMBL | Inhibition of wild type HIV 3B reverse transcriptase in MT2 cells | B | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1120-1123 [PMID:18164198] |
ChEMBL | Inhibition of HIV1 reverse transcriptase p66/p51 | B | 7.3 | pIC50 | 50 | nM | IC50 | J Nat Prod (1995) 58: 1024-1031 [PMID:7561895] |
ChEMBL | Inhibition on HIV1 reverse transcriptase p66/p51 | B | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem (2009) 17: 1739-1746 [PMID:19179082] |
ChEMBL | Inhibition of HIV1 reverse transcriptase | B | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem (2007) 15: 5519-5528 [PMID:17562366] |
ChEMBL | Concentration required to inhibit HIV reverse transcriptase | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (1992) 35: 3369-3372 [PMID:1527788] |
ChEMBL | Ability to inhibit the HIV-1 reverse transcriptase in cord blood mononuclear cells. | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1995) 38: 1-4 [PMID:7837220] |
ChEMBL | Inhibitory concentration against human immunodeficiency virus type 1 (HIV-1 strain IIIB RT) reverse transcriptase was determined by triplicate assay at high (~1 pfu/cell) multiplicity of injection (moi) | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (1998) 41: 10-23 [PMID:9438017] |
ChEMBL | antiviral activity in Human immunodeficiency virus-1 as reverse transcriptase activity in culture supernatant | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (1995) 38: 4106-4114 [PMID:7562946] |
ChEMBL | Tested for the inhibition towards HIV-reverse transcriptase | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 1819-1824 |
ChEMBL | In vitro inhibitory activity against human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1991) 34: 2231-2241 [PMID:1712395] |
ChEMBL | Antiviral activity against Human Immunodeficiency Virus by Reverse transcriptase assay in CEM-SS cells | B | 8.51 | pIC50 | 3.1 | nM | IC50 | J Med Chem (1998) 41: 1252-1262 [PMID:9548815] |
ChEMBL | Inhibitory concentration against human immunodeficiency virus type 1 (HIV-1 strain IIIB RT) reverse transcriptase was determined by triplicate assay at low (~0.1 pfu/cell) multiplicity of injection (moi) | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1998) 41: 10-23 [PMID:9438017] |
ChEMBL | Tested in vitro against HIV-1 MDR using MAGI assay | F | 4.6 | pEC50 | 24900 | nM | EC50 | J Med Chem (2000) 43: 4516-4525 [PMID:11087576] |
ChEMBL | Tested in vitro against HIV-1 LAI from MT-4 cells using MTT assay | F | 7.42 | pEC50 | 38 | nM | EC50 | J Med Chem (2000) 43: 4516-4525 [PMID:11087576] |
ChEMBL | Inhibition of HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity by MTT assay | B | 7.77 | pEC50 | 17 | nM | EC50 | ACS Med Chem Lett (2018) 9: 370-375 [PMID:29670703] |
ChEMBL | Inhibition of HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | B | 7.95 | pEC50 | 11.1 | nM | EC50 | J Med Chem (2017) 60: 4424-4443 [PMID:28481112] |
ChEMBL | Effective concentration that reduces HIV-induced cytopathic effect by 50% was determined by reverse transcriptase (RT) assay. | B | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (1993) 36: 826-830 [PMID:8385224] |
ChEMBL | Inhibition of HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | B | 8.05 | pEC50 | 8.9 | nM | EC50 | Bioorg Med Chem (2017) 25: 2491-2497 [PMID:28314514] |
ChEMBL | Antiviral activity against HIV1 IRLL98 in MT4 cells by MTT assay | F | 8.1 | pEC50 | 8 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 3541-3544 [PMID:16621553] |
ChEMBL | Inhibition of HIV1 3B reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | B | 8.14 | pEC50 | 7.3 | nM | EC50 | J Med Chem (2017) 60: 4424-4443 [PMID:28481112] |
ChEMBL | Inhibition of wild-type HIV1 3B reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytotoxicity by MTT assay | B | 8.15 | pEC50 | 7 | nM | EC50 | ACS Med Chem Lett (2018) 9: 370-375 [PMID:29670703] |
ChEMBL | Inhibition of HIV1 3B reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | B | 8.18 | pEC50 | 6.68 | nM | EC50 | J Med Chem (2017) 60: 4424-4443 [PMID:28481112] |
ChEMBL | Inhibition of HIV-1 reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | B | 8.18 | pEC50 | 6.6 | nM | EC50 | Bioorg Med Chem (2017) 25: 2491-2497 [PMID:28314514] |
ChEMBL | Inhibition of HIV1 3B reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | B | 8.2 | pEC50 | 6.34 | nM | EC50 | J Med Chem (2017) 60: 4424-4443 [PMID:28481112] |
ChEMBL | Inhibition of HIV1 3B reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | B | 8.28 | pEC50 | 5.24 | nM | EC50 | J Med Chem (2017) 60: 4424-4443 [PMID:28481112] |
ChEMBL | Inhibition of HIV1 3B reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | B | 8.32 | pEC50 | 4.79 | nM | EC50 | J Med Chem (2017) 60: 4424-4443 [PMID:28481112] |
ChEMBL | Inhibition of HIV1 3B reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | B | 8.43 | pEC50 | 3.75 | nM | EC50 | J Med Chem (2017) 60: 4424-4443 [PMID:28481112] |
ChEMBL | Effective concentration in vitro against HIV-1-infected CEM cells relative to uninfected untreated controls | F | 8.52 | pEC50 | 3 | nM | EC50 | J Med Chem (1994) 37: 4297-4306 [PMID:7996541] |
ChEMBL | Reverse transcriptase activity was measured in the culture supernatant, concentration that reduces by 50% the HIV produced in the supernatant. | B | 8.52 | pEC50 | 3 | nM | EC50 | J Med Chem (1997) 40: 1550-1558 [PMID:9154976] |
ChEMBL | Inhibition of reverse transcriptase of HIV-1 (strain RF)-infected MT-4 cells in RPMI 1640 growth medium in MTM assay | B | 8.52 | pEC50 | 3 | nM | EC50 | J Med Chem (1993) 36: 3784-3794 [PMID:7504733] |
ChEMBL | Antiviral activity against HIV1 Y188L mutant in MT4 cells by MTT assay | F | 8.52 | pEC50 | 3 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 3541-3544 [PMID:16621553] |
ChEMBL | Antiviral activity against HIV1 K103N mutant in MT4 cells by MTT assay | F | 8.52 | pEC50 | 3 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 3541-3544 [PMID:16621553] |
ChEMBL | Antiviral activity against wild type HIV1 NL4-3 in MT4 cells by MTT assay | F | 8.52 | pEC50 | 3 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 3541-3544 [PMID:16621553] |
ChEMBL | Effective concentration required to inhibit HIV-1 induced cytopathicity by 50% in CEM cells | F | 8.52 | pEC50 | 3 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 3085-3088 [PMID:11714616] |
ChEMBL | Effective concentration required to achieve 50% inhibition of HIV-1 LAI replication in human T4 lymphoblastoid CEM-SS cells. | F | 8.7 | pEC50 | 2 | nM | EC50 | J Med Chem (2000) 43: 1927-1939 [PMID:10821705] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D10 after 48 hrs | F | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem (2010) 18: 8243-8256 [PMID:21044845] |
ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 after 48 hrs | F | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem (2010) 18: 8243-8256 [PMID:21044845] |
ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 after 48 hrs by FACS analysis in presence of 10 % human serum | F | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem (2010) 18: 8243-8256 [PMID:21044845] |
ChEMBL | Antimalarial activity against Plasmodium falciparum 3D7 after 48 hrs by SYBR green assay | F | 4 | pEC50 | >100000 | nM | EC50 | Bioorg Med Chem (2010) 18: 7302-7309 [PMID:20833052] |
Thymidine kinase in Ureaplasma parvum serovar 3 (strain ATCC 700970) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075130] [UniProtKB: Q9PPP5] | ||||||||
ChEMBL | Inhibition of Ureaplasma parvum thymidine kinase by liquid scintillation counting | B | 4.9 | pIC50 | 12500 | nM | IC50 | Bioorg Med Chem (2010) 18: 3261-3269 [PMID:20378362] |
Thymidine kinase, cytosolic in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2883] [UniProtKB: P04183] | ||||||||
ChEMBL | Inhibitory affect against rabbit thymus thymidine kinase | B | 5.15 | pKi | 7000 | nM | Ki | J Med Chem (1990) 33: 258-263 [PMID:2153206] |
ChEMBL | Inhibitory affect against rabbit thymus thymidine kinase and represented as molt/4F kinase. | B | 5.54 | pKi | 2900 | nM | Ki | J Med Chem (1990) 33: 258-263 [PMID:2153206] |
ChEMBL | Inhibition of human TK1 by liquid scintillation counting | B | 5.52 | pIC50 | 3000 | nM | IC50 | Bioorg Med Chem (2010) 18: 3261-3269 [PMID:20378362] |
Thymidylate kinase in Mycobacterium tuberculosis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2361] [UniProtKB: P9WKE1] | ||||||||
ChEMBL | Inhibitory activity against thymidine monophosphate kinase (TMPK) in Mycobacterium tuberculosis | B | 4.55 | pKi | 28000 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 3045-3048 [PMID:12941330] |
ChEMBL | In Vitro inhibition of Thymidine Monophosphatase Kinase of Mycobacterium tuberculosis (TMPKm) | B | 4.55 | pKi | 28000 | nM | Ki | J Med Chem (2003) 46: 3811-3821 [PMID:12930144] |
ChEMBL | Competitive inhibition of Mycobacterium tuberculosis TMPK by Lineweaver-Burk analysis | B | 4.55 | pKi | 28000 | nM | Ki | Bioorg Med Chem (2011) 19: 7603-7611 [PMID:22061826] |
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]