zidovudine [Ligand Id: 4825] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL129 (3'-azt, Azidothymidine, AZT, BW A509U, BW-A-509U, BW-A509U, BWA509U, COMPOUND S, COMPOUND-S, NSC-602670, Retrovir, Zidovudine, Zidovudinum)
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  • Human immunodeficiency virus type 1 protease in Human immunodeficiency virus 1 [ChEMBL: CHEMBL243] [UniProtKB: Q72874]
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  • Human immunodeficiency virus type 1 reverse transcriptase in Human immunodeficiency virus 1 [ChEMBL: CHEMBL247] [UniProtKB: Q72547]
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  • Thymidine kinase in Ureaplasma parvum serovar 3 (strain ATCC 700970) [ChEMBL: CHEMBL1075130] [UniProtKB: Q9PPP5]
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  • Thymidylate kinase in Mycobacterium tuberculosis [ChEMBL: CHEMBL2361] [UniProtKB: P9WKE1]
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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 Inhibition of HIV-1 reverse transcriptase. B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (1996) 6: 2405-2410
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 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 recombinant HIV-1 reverse transcriptase B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (2000) 10: 87-90 [PMID:10636251]
ChEMBL Inhibition of HIV-1 reverse transcriptase B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (1996) 6: 2411-2416
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 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 HIV1 reverse transcriptase p66/p51 B 7.3 pIC50 50 nM IC50 J Nat Prod (1995) 58: 1024-1031 [PMID:7561895]
ChEMBL Inhibition of HIV1 reverse transcriptase B 7.3 pIC50 50 nM IC50 Bioorg Med Chem (2007) 15: 5519-5528 [PMID:17562366]
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 on HIV1 reverse transcriptase p66/p51 B 7.3 pIC50 50 nM IC50 Bioorg Med Chem (2009) 17: 1739-1746 [PMID:19179082]
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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]