A DNA polymerase inhibitor that interferes with the activity of reverse transcriptase, EC 2.7.7.49, a viral DNA polymerase enzyme that retroviruses need in order to reproduce.
ChEBI ID: 59897
| Member | Definition | Class |
|---|---|---|
| entecavir | Guanine substituted at the 9 position by a 4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl group. A synthetic analogue of 2'-deoxyguanosine, it is a nucleoside reverse transcriptase inhibitor with selective antiviral activity against hepatitis B virus. Entecavir is phosphorylated intracellularly to the active triphosphate form, which competes with deoxyguanosine triphosphate, the natural substrate of hepatitis B virus reverse transcriptase, inhibiting every stage of the enzyme's activity, although it has no activity against HIV. It is used for the treatment of chronic hepatitis B. | entecavir (anhydrous) |
| lamivudine | A monothioacetal that consists of cytosine having a (2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl moiety attached at position 1. An inhibitor of HIV-1 reverse transcriptase, it is used as an antiviral in the treatment of AIDS and hepatitis B. | lamivudine |
| ribavirin | A 1-ribosyltriazole that is the 1-ribofuranosyl derivative of 1,2,4-triazole-3-carboxamide. A synthetic guanosine analogue, it is an inhibitor of HCV polymerase and possesses a broad spectrum of activity against DNA and RNA viruses. | ribavirin |
| rilpivirine | An aminopyrimidine that is pyrimidine-2,4-diamine in which the amino groups at positions 2 and 4 are substituted by 4-cyanophenyl and 4-[(E)-2-cyanovinyl]-2,6-dimethylphenyl groups respectively. Used for treatment of HIV. | rilpivirine |
| stavudine | A nucleoside analogue obtained by formal dehydration across positions 2 and 3 of thymidine. An inhibitor of HIV-1 reverse transcriptase | stavudine |
| telbivudine | A pyrimidine 2'-deoxyribonucleoside that is the L-enantiomer of thymine. A synthetic thymidine nucleoside analogue with activity against HBV DNA polymerase. | telbivudine |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 613 (2.91) | 18.7374 |
| 1990's | 1,825 (8.65) | 18.2507 |
| 2000's | 8,174 (38.74) | 29.6817 |
| 2010's | 8,891 (42.14) | 24.3611 |
| 2020's | 1,598 (7.57) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 4,078 (16.87%) | 5.53% |
| Reviews | 3,356 (13.89%) | 6.00% |
| Case Studies | 2,388 (9.88%) | 4.05% |
| Observational | 366 (1.51%) | 0.25% |
| Other | 13,978 (57.84%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 32.4648 | 1 | 2 |
| alpha-galactosidase | Homo sapiens (human) | Potency | 50.1187 | 1 | 1 |
| AR protein | Homo sapiens (human) | Potency | 10.0848 | 2 | 2 |
| arylsulfatase A | Homo sapiens (human) | Potency | 16.9441 | 1 | 1 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 18.3489 | 1 | 1 |
| Ataxin-2 | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 0.6012 | 1 | 1 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 0.7943 | 2 | 2 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 37.4338 | 3 | 5 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 25.1459 | 1 | 2 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 80.4486 | 1 | 3 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 0.7943 | 2 | 2 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 7.7619 | 1 | 1 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 3.8874 | 1 | 3 |
| DNA polymerase beta | Homo sapiens (human) | Potency | 79.4328 | 1 | 1 |
| endonuclease IV | Escherichia coli | Potency | 0.0001 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 21.0690 | 4 | 8 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 1.9740 | 10 | 16 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 0.0631 | 1 | 1 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 14.2558 | 3 | 5 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 28.7486 | 2 | 2 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 0.7079 | 1 | 1 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 0.7943 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 0.7943 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 0.7943 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 0.7943 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 0.7943 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 0.7943 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 0.7943 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 0.7943 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 0.7943 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 0.7943 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 0.7943 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 0.7943 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 0.7943 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 0.7943 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 0.7943 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 0.7943 | 1 | 1 |
| geminin | Homo sapiens (human) | Potency | 11.8846 | 2 | 5 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 7.0795 | 1 | 1 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 26.6032 | 1 | 1 |
| Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 27.9015 | 2 | 9 |
| interleukin 8 | Homo sapiens (human) | Potency | 70.9011 | 1 | 2 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 23.6555 | 1 | 3 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 3.5481 | 1 | 1 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 1.4342 | 2 | 2 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 58.7322 | 3 | 4 |
| nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 8.0636 | 1 | 2 |
| Nuclear receptor ROR-gamma | Homo sapiens (human) | Potency | 9.4228 | 1 | 2 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 17.1044 | 2 | 7 |
| peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 23.9341 | 1 | 1 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 50.1187 | 1 | 1 |
| plasminogen precursor | Mus musculus (house mouse) | Potency | 7.0795 | 1 | 1 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 9.1024 | 1 | 1 |
| Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) | Potency | 89.1251 | 1 | 1 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 4.8831 | 2 | 4 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 51.1478 | 2 | 3 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 17.3739 | 2 | 2 |
| Smad3 | Homo sapiens (human) | Potency | 14.1254 | 1 | 1 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 31.0990 | 1 | 2 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 21.1699 | 1 | 2 |
| TDP1 protein | Homo sapiens (human) | Potency | 0.8034 | 2 | 6 |
| Thrombopoietin | Homo sapiens (human) | Potency | 12.5893 | 2 | 2 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 20.2735 | 2 | 4 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 0.0035 | 1 | 1 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 15.8489 | 2 | 2 |
| urokinase plasminogen activator surface receptor precursor | Mus musculus (house mouse) | Potency | 7.0795 | 1 | 1 |
| urokinase-type plasminogen activator precursor | Mus musculus (house mouse) | Potency | 7.0795 | 1 | 1 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 26.6032 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Adenosine receptor A1 | Homo sapiens (human) | Ki | 7.4100 | 2 | 2 |
| Adenosine receptor A1 | Mus musculus (house mouse) | Ki | 4.4300 | 1 | 1 |
| Adenosine receptor A2a | Homo sapiens (human) | Ki | 7.4100 | 1 | 1 |
| Adenosine receptor A3 | Homo sapiens (human) | Ki | 7.4100 | 1 | 1 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 5 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 133.0000 | 1 | 5 |
| Broad substrate specificity ATP-binding cassette transporter ABCG2 | Homo sapiens (human) | IC50 | 1.5000 | 1 | 1 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 5 |
| Capsid protein | Hepatitis B virus | IC50 | 50.0500 | 2 | 2 |
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 | 6.1612 | 6 | 6 |
| Cytochrome P450 2C19 | Homo sapiens (human) | IC50 | 0.3363 | 4 | 4 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 | 0.2818 | 5 | 5 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 | 2.3635 | 6 | 6 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 | 1.7406 | 5 | 5 |
| exodeoxyribonuclease V subunit RecB | Escherichia coli str. K-12 substr. MG1655 | IC50 | 62.7110 | 1 | 2 |
| exodeoxyribonuclease V subunit RecC | Escherichia coli str. K-12 substr. MG1655 | IC50 | 62.7110 | 1 | 2 |
| exodeoxyribonuclease V subunit RecD | Escherichia coli str. K-12 substr. MG1655 | IC50 | 62.7110 | 1 | 2 |
| Gag-Pol polyprotein | HIV-1 M:B_HXB2R | IC50 | 0.0680 | 1 | 1 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 5 |
| Potassium voltage-gated channel subfamily E member 1 | Homo sapiens (human) | IC50 | 251.1890 | 1 | 1 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 | 23,357.6243 | 7 | 7 |
| Potassium voltage-gated channel subfamily KQT member 1 | Homo sapiens (human) | IC50 | 251.1890 | 1 | 1 |
| Reverse transcriptase | Moloney murine leukemia virus | IC50 | 10.0000 | 1 | 1 |
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | IC50 | 0.9592 | 21 | 22 |
| Sodium channel protein type 5 subunit alpha | Homo sapiens (human) | IC50 | 3,162.2800 | 1 | 1 |
| Thymidine kinase 2 | Rattus norvegicus (Norway rat) | Ki | 3,250.0000 | 1 | 1 |
| Thymidine kinase, cytosolic | Homo sapiens (human) | Ki | 597.5000 | 2 | 2 |
| Thymidine kinase, cytosolic | Rattus norvegicus (Norway rat) | Ki | 1,700.0000 | 1 | 1 |
| Voltage-dependent L-type calcium channel subunit alpha-1C | Homo sapiens (human) | IC50 | 463.5333 | 3 | 3 |
| Voltage-dependent L-type calcium channel subunit alpha-1D | Homo sapiens (human) | IC50 | 463.5333 | 3 | 3 |
| Voltage-dependent L-type calcium channel subunit alpha-1F | Homo sapiens (human) | IC50 | 463.5333 | 3 | 3 |
| Voltage-dependent L-type calcium channel subunit alpha-1S | Homo sapiens (human) | IC50 | 463.5333 | 3 | 3 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Albumin | Homo sapiens (human) | Kd | 44.0000 | 1 | 2 |
| Angiotensin-converting enzyme 2 | Homo sapiens (human) | EC50 | 109.5000 | 1 | 1 |
| Capsid protein | Hepatitis B virus | EC50 | 4.2379 | 3 | 5 |
| Genome polyprotein | Human enterovirus 71 (strain BRCR) | EC50 | 100.0000 | 1 | 1 |
| glycogen synthase kinase-3 beta isoform 1 | Homo sapiens (human) | EC50 | 300.0000 | 1 | 1 |
| Hsf1 protein | Mus musculus (house mouse) | EC50 | 0.2870 | 1 | 1 |
| NS5 | Zika virus | EC50 | 20.8000 | 1 | 1 |
| Polymerase acidic protein | Influenza A virus (A/Puerto Rico/8/1934(H1N1)) | EC50 | 21.2667 | 3 | 3 |
| Polymerase basic protein 2 | Influenza A virus (A/Puerto Rico/8/1934(H1N1)) | EC50 | 20.0000 | 2 | 2 |
| Procathepsin L | Homo sapiens (human) | EC50 | 109.5000 | 1 | 1 |
| Replicase polyprotein 1a | Severe acute respiratory syndrome-related coronavirus | EC50 | 109.5000 | 1 | 1 |
| Replicase polyprotein 1ab | Betacoronavirus England 1 | EC50 | 109.5000 | 1 | 1 |
| Replicase polyprotein 1ab | Human coronavirus 229E | EC50 | 109.5000 | 1 | 1 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | EC50 | 109.5000 | 1 | 1 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome-related coronavirus | EC50 | 109.5000 | 1 | 1 |
| Reverse transcriptase | Human immunodeficiency virus 1 | EC50 | 0.0010 | 4 | 4 |
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | EC50 | 6.3808 | 6 | 8 |
| RNA-directed RNA polymerase catalytic subunit | Influenza A virus (A/Puerto Rico/8/1934(H1N1)) | EC50 | 21.2667 | 3 | 3 |
| Spike glycoprotein | Betacoronavirus England 1 | EC50 | 109.5000 | 1 | 1 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | EC50 | 109.5000 | 1 | 1 |
| Transmembrane protease serine 2 | Homo sapiens (human) | EC50 | 109.5000 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Adenosylhomocysteinase | Homo sapiens (human) | Kinact | 266.0000 | 1 | 1 |
| Adenosylhomocysteinase | Homo sapiens (human) | KR | 407.0000 | 1 | 1 |
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | IC90 | 0.1000 | 1 | 1 |
| Thymidine kinase, cytosolic | Homo sapiens (human) | Km | 133.0000 | 1 | 1 |