Page last updated: 2024-08-05 15:21:04
HIV-1 reverse transcriptase inhibitor
An entity which inhibits the activity of HIV-1 reverse transcriptase.
ChEBI ID: 53756
Members (25)
| Member | Definition | Class |
|---|---|---|
| 1-((2-hydroxyethoxy)methyl)-6-(phenylthio)thymine | A pyrimidone that is thymine which is substituted at positions 1 and 6 by a (2-hydroxyethoxy)methyl group and a phenylsulfanyl group, respectively. | 1-[(2-hydroxyethoxy)methyl]-6-(phenylsulfanyl)thymine |
| abacavir | A 2,6-diaminopurine that is (1S)-cyclopent-2-en-1-ylmethanol in which the pro-R hydrogen at the 4-position is substituted by a 2-amino-6-(cyclopropylamino)-9H-purin-9-yl group. A nucleoside analogue reverse transcriptase inhibitor (NRTI) with antiretroviral activity against HIV, it is used (particularly as the sulfate) with other antiretrovirals in combination therapy of HIV infection. | abacavir |
| adefovir | A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens has been replaced by a 2-(6-amino-9H-purin-9-yl)ethoxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(t-butoxycarbonyloxymethyl) ester (dipivoxil ester) prodrug is used to treat chronic hepatitis B viral infection. | adefovir |
| adefovir dipivoxil | An organic phosphonate that is the dipivoxil ester of adefovir. A prodrug for adefovir, an HIV-1 reverse transcriptase inhibitor, adefovir pivoxil is used to treat chronic hepatitis B viral infection. | adefovir pivoxil |
| calanolide a | An organic heterotetracyclic compound that is 11,12-dihydro-2H,6H,10H-dipyrano[2,3-f:2',3'-h]chromen-2-one substituted by a hydroxy group at position 12, methyl groups at positions 6, 6, 10 and 11 and a propyl group at position 4 (the 10R,11S,12S stereoisomer). Isolated from Calophyllum lanigerum var austrocoriaceum and Calophyllum brasiliense, it exhibits potent activity against HIV-1 reverse transcriptase. | (+)-calanolide A |
| costatolide | An organic heterotetracyclic compound that is 11,12-dihydro-2H,6H,10H-dipyrano[2,3-f:2',3'-h]chromen-2-one substituted by a hydroxy group at position 12, methyl groups at positions 6, 6, 10 and 11 and a propyl group at position 4 (the 10S,11R,12S stereoisomer). Isolated from Calophyllum lanigerum var austrocoriaceum and Calophyllum brasiliense, it exhibits potent activity against HIV-1 reverse transcriptase. | (-)-calanolide B |
| delavirdine | The amide resulting from the formal condensation of 5-[(methylsulfonyl)amino]-1H-indole-2-carboxylic acid and 4-amino group of 1-[3-(isopropylamino)pyridin-2-yl]piperazine, delavirdine is a non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1. Viral resistance emerges rapidly when delavirdine is used alone, so it is therefore used (as the methanesulfonic acid salt) with other antiretrovirals for combination therapy of HIV infection. | delavirdine |
| delavirdine mesylate | The monomethanesulfonic acid salt of delavirdine, a non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1. Viral resistance emerges rapidly when delavirdine is used alone, so it is therefore used (as the methanesulfonic acid salt) with other antiretrovirals for combination therapy of HIV infection. | delavirdine mesylate |
| didanosine | A purine 2',3'-dideoxyribonucleoside that is inosine in which the hydroxy groups at both the 2' and the 3' positions on the sugar moiety have been replaced by hydrogen. An antiviral drug, it is used as a medication to treat HIV/AIDS. | didanosine |
| efavirenz | 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection. | efavirenz |
| emivirine | A pyrimidone that is uracil which is substituted at positions 1, 5 and 6 by ethoxymethyl, isopropyl, and benzyl groups, respectively. A non-nucleoside inhibitor of HIV-1 reverse transcriptase, emivirine was an unsuccessful experimental agent for the treatment of HIV. | emivirine |
| emtricitabine | An organofluorine compound that is 5-fluorocytosine substituted at the 1 position by a 2-(hydroxymethyl)-1,3-oxathiolan-5-yl group (2R,5S configuration). It is used in combination therapy for the treatment of HIV-1 infection. | emtricitabine |
| etravirine | An aminopyrimidine that consists of 2,6-diaminopyrimidine bearing a bromo substituent at position 5, a 4-cyano-2,6-dimethylphenoxy substituent at position 4 and having a 4-cyanophenyl substituent attached to the 2-amino group. NNRTI of HIV-1, binds directly to RT and blocks RNA-dependent and DNA-dependent DNA polymerase activities | etravirine |
| foscarnet | Phosphoric acid in which one of the hydroxy groups is replaced by a carboxylic acid group. It is used as the trisodium salt as an antiviral agent in the treatment of cytomegalovirus retinitis (CMV retinitis, an inflamation of the retina that can lead to blindness) and as an alternative to ganciclovir for AIDS patients who require concurrent antiretroviral therapy but are unable to tolerate ganciclovir due to haematological toxicity. | phosphonoformic acid |
| gs-7340 | An L-alanine derivative that is isopropyl L-alaninate in which one of the amino hydrogens is replaced by an (S)-({[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy}methyl)(phenoxy)phosphoryl group. A prodrug for tenofovir, it is used (as the fumarate salt) in combination therapy for the treatment of HIV-1 infection. | tenofovir alafenamide |
| 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 |
| maprounic acid | A pentacyclic triterpenoid isolated from Maprounea africana and has been shown to exhibit inhibitory activity against HIV-1 reverse transcriptase. | maprounic acid |
| nevirapine | A dipyridodiazepine that is 5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepine which is substituted by methyl, oxo, and cyclopropyl groups at positions 4, 6, and 11, respectively. A non-nucleoside reverse transcriptase inhibitor with activity against HIV-1, it is used in combination with other antiretrovirals for the treatment of HIV infection. | nevirapine |
| nigranoic acid | A tetracyclic triterpenoid that is 3,4-secocycloarta-4(28),24-(Z)-diene substituted by carboxy groups at positions 3 and 26. Isolated from Schisandra henryi and Schisandra propinqua, it exhibits cytotoxic and anti-HIV activities. | nigranoic acid |
| nsc 614846 | The (active) (-)-enantiomer of the carbocyclic analogue of 2',3'-dideoxy-2',3'-didehydroguanosine. | (-)-carbovir |
| 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 |
| tenofovir | A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens is replaced by a [(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(isopropyloxycarbonyloxymethyl) ester (disoproxil ester) prodrug is used as the fumaric acid salt in combination therapy for the treatment of HIV infection. | tenofovir (anhydrous) |
| tenofovir disoproxil fumarate | A fumarate salt prepared from equimolar amounts of tenofovir disoproxil and fumaric acid. It is used in combination therapy for the treatment of HIV infection. | tenofovir disoproxil fumarate |
| zalcitabine | A pyrimidine 2',3'-dideoxyribonucleoside compound having cytosine as the nucleobase. | zalcitabine |
| zidovudine | A pyrimidine 2',3'-dideoxyribonucleoside compound having a 3'-azido substituent and thymine as the nucleobase. | zidovudine |
Research
Studies (27,443)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 969 (3.53) | 18.7374 |
| 1990's | 7,270 (26.49) | 18.2507 |
| 2000's | 8,709 (31.73) | 29.6817 |
| 2010's | 8,118 (29.58) | 24.3611 |
| 2020's | 2,377 (8.66) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 6,895 (16.99%) | 5.53% |
| Reviews | 3,940 (9.71%) | 6.00% |
| Case Studies | 3,335 (8.22%) | 4.05% |
| Observational | 483 (1.19%) | 0.25% |
| Other | 25,939 (63.90%) | 84.16% |
Protein Targets (203)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 67.9K protein | Vaccinia virus | Potency | 22.3872 | 1 | 1 |
| acetylcholinesterase | Homo sapiens (human) | Potency | 27.8685 | 3 | 3 |
| activating transcription factor 6 | Homo sapiens (human) | Potency | 0.0674 | 1 | 1 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 33.5520 | 1 | 2 |
| AR protein | Homo sapiens (human) | Potency | 21.2988 | 7 | 12 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 68.5896 | 1 | 1 |
| Ataxin-2 | Homo sapiens (human) | Potency | 29.8493 | 1 | 1 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 12.9840 | 2 | 2 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 29.8493 | 1 | 1 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 199.5260 | 2 | 2 |
| caspase 7, apoptosis-related cysteine protease | Homo sapiens (human) | Potency | 50.1983 | 1 | 2 |
| caspase-3 | Cricetulus griseus (Chinese hamster) | Potency | 15.7936 | 1 | 1 |
| caspase-3 | Homo sapiens (human) | Potency | 50.1983 | 1 | 2 |
| Caspase-7 | Cricetulus griseus (Chinese hamster) | Potency | 15.7936 | 1 | 1 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 34.9248 | 2 | 4 |
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 31.6228 | 1 | 1 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 20.9624 | 1 | 5 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 89.1251 | 1 | 2 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 9.6632 | 1 | 2 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 17.6838 | 1 | 4 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 8.8023 | 2 | 7 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 26.9073 | 1 | 4 |
| DNA polymerase beta | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 89.1251 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 26.8391 | 8 | 13 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 23.7101 | 1 | 1 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 25.3607 | 5 | 16 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 15.7142 | 1 | 2 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 13.9080 | 4 | 10 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 26.0529 | 2 | 3 |
| G | Vesicular stomatitis virus | Potency | 9.6632 | 1 | 2 |
| GALC protein | Homo sapiens (human) | Potency | 0.7079 | 1 | 1 |
| geminin | Homo sapiens (human) | Potency | 14.7297 | 2 | 6 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 15.2639 | 2 | 8 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 18.2701 | 2 | 5 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 21.1317 | 1 | 1 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 33.4889 | 2 | 2 |
| Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 0.3192 | 2 | 2 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 9.6632 | 1 | 2 |
| hypothetical protein, conserved | Trypanosoma brucei | Potency | 35.4813 | 1 | 1 |
| hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 26.8325 | 1 | 1 |
| importin subunit beta-1 isoform 1 | Homo sapiens (human) | Potency | 5.6234 | 1 | 1 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 9.6632 | 1 | 4 |
| Interferon beta | Homo sapiens (human) | Potency | 30.3102 | 2 | 11 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 12.0515 | 1 | 4 |
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 11.4239 | 1 | 1 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 1.8370 | 1 | 2 |
| mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 14.6762 | 2 | 5 |
| neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 10.0000 | 1 | 1 |
| NFKB1 protein, partial | Homo sapiens (human) | Potency | 0.7943 | 2 | 2 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 17.4109 | 3 | 7 |
| nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 20.9608 | 1 | 2 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 13.3574 | 2 | 2 |
| nuclear receptor subfamily 1, group I, member 2 | Rattus norvegicus (Norway rat) | Potency | 31.8326 | 1 | 2 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 1.9786 | 2 | 8 |
| peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Potency | 37.9330 | 1 | 1 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 17.3898 | 1 | 4 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 41.8038 | 2 | 2 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 73.7420 | 3 | 4 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 9.0063 | 1 | 3 |
| PPM1D protein | Homo sapiens (human) | Potency | 34.8984 | 1 | 6 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 42.1119 | 3 | 6 |
| progesterone receptor | Homo sapiens (human) | Potency | 21.5665 | 2 | 3 |
| pyruvate kinase PKM isoform a | Homo sapiens (human) | Potency | 39.8107 | 2 | 2 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 14.1983 | 2 | 7 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 32.3509 | 3 | 13 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 32.4165 | 2 | 7 |
| serine/threonine-protein kinase mTOR isoform 1 | Homo sapiens (human) | Potency | 28.9633 | 1 | 1 |
| serine/threonine-protein kinase PLK1 | Homo sapiens (human) | Potency | 29.9349 | 1 | 1 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 34.9761 | 2 | 2 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 34.9761 | 2 | 2 |
| snurportin-1 | Homo sapiens (human) | Potency | 5.6234 | 1 | 1 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 12.6414 | 2 | 11 |
| TAR DNA-binding protein 43 | Homo sapiens (human) | Potency | 5.6234 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 15.0762 | 2 | 25 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 10.4558 | 3 | 4 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 17.5614 | 3 | 13 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 11.2006 | 2 | 2 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 12.2352 | 2 | 2 |
| tyrosine-protein kinase Yes | Homo sapiens (human) | Potency | 43.4320 | 1 | 1 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 0.6310 | 1 | 1 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 15.5961 | 2 | 2 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 16.3729 | 2 | 3 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 56.2341 | 1 | 1 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 21.1317 | 1 | 1 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Adenosine deaminase | Bos taurus (cattle) | Ki | 800.0000 | 1 | 1 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 120.2100 | 2 | 10 |
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | IC50 | 376.9000 | 4 | 4 |
| Beta-lactamase | Escherichia coli K-12 | IC50 | 90.0000 | 1 | 1 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 139.9636 | 3 | 11 |
| Broad substrate specificity ATP-binding cassette transporter ABCG2 | Homo sapiens (human) | IC50 | 86.3600 | 3 | 5 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 120.4800 | 2 | 10 |
| Cannabinoid receptor 1 | Mus musculus (house mouse) | Ki | 3.6050 | 1 | 2 |
| Capsid protein | Hepatitis B virus | IC50 | 50.0500 | 2 | 2 |
| Carbonic anhydrase 2 | Homo sapiens (human) | Ki | 14,200.0000 | 1 | 1 |
| Carbonic anhydrase 4 | Homo sapiens (human) | Ki | 820.0000 | 1 | 1 |
| Carbonic anhydrase 5A, mitochondrial | Homo sapiens (human) | Ki | 41,700.0000 | 1 | 1 |
| Carbonic anhydrase 9 | Homo sapiens (human) | Ki | 2,210.0000 | 1 | 1 |
| Cardiac ryanodine receptor 2 | Canis lupus familiaris (dog) | Ki | 7.0000 | 1 | 1 |
| Chain A, Hiv-1 Reverse Transcriptase | Human immunodeficiency virus 1 | IC50 | 6.4070 | 1 | 8 |
| Chain A, POL POLYPROTEIN | Human immunodeficiency virus 1 | IC50 | 0.2612 | 1 | 8 |
| Chain A, Reverse transcriptase/ribonuclease H | HIV-1 M:B_HXB2R | IC50 | 0.0021 | 1 | 2 |
| Chain A, Reverse transcriptase/ribonuclease H | Human immunodeficiency virus 1 | IC50 | 1.1650 | 1 | 1 |
| Chain B, HIV-1 REVERSE TRANSCRIPTASE | Human immunodeficiency virus 1 | IC50 | 6.8336 | 1 | 5 |
| Chain B, p51 RT | HIV-1 M:B_HXB2R | IC50 | 0.0021 | 1 | 2 |
| Chain B, POL POLYPROTEIN | Human immunodeficiency virus 1 | IC50 | 0.2612 | 1 | 6 |
| Chymotrypsinogen A | Bos taurus (cattle) | IC50 | 225.0000 | 1 | 1 |
| Cruzipain | Trypanosoma cruzi | IC50 | 131.5000 | 2 | 4 |
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 | 5.2846 | 6 | 7 |
| Cytochrome P450 2C19 | Homo sapiens (human) | IC50 | 0.3363 | 4 | 4 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 | 0.2296 | 6 | 7 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 | 8.0266 | 7 | 8 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 | 6.8379 | 7 | 8 |
| Deoxycytidine kinase | Homo sapiens (human) | Ki | 680.0000 | 2 | 2 |
| Disintegrin and metalloproteinase domain-containing protein 17 | Homo sapiens (human) | IC50 | 0.0920 | 1 | 2 |
| DNA polymerase alpha catalytic subunit | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| DNA polymerase beta | Homo sapiens (human) | IC50 | 112.5000 | 2 | 2 |
| DNA polymerase catalytic subunit | Human herpesvirus 3 strain Dumas | IC50 | 0.2800 | 1 | 1 |
| DNA polymerase catalytic subunit | Human herpesvirus 5 strain AD169 | IC50 | 2.5000 | 2 | 2 |
| DNA polymerase delta catalytic subunit | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| Envelope glycoprotein gp160 [Cleaved into: Surface protein gp120 | Human immunodeficiency virus 1 | IC50 | 0.0035 | 1 | 1 |
| Exoribonuclease H | Human immunodeficiency virus 2 | IC50 | 20.0000 | 1 | 1 |
| Gag-Pol polyprotein | HIV-1 M:B_HXB2R | IC50 | 10.7417 | 34 | 79 |
| Gag-Pol polyprotein | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | IC50 | 0.3600 | 2 | 3 |
| Gag-Pol polyprotein | Human immunodeficiency virus type 1 BH10 | IC50 | 17.2958 | 6 | 11 |
| Gag-Pol polyprotein | Human immunodeficiency virus type 2 (ISOLATE ROD) | IC50 | 11.0250 | 1 | 4 |
| Gag-Pol polyprotein | HIV-1 M:B_HXB2R | Ki | 5.9557 | 1 | 14 |
| Glutamate receptor ionotropic, NMDA 1 | Rattus norvegicus (Norway rat) | IC50 | 0.0100 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2A | Rattus norvegicus (Norway rat) | IC50 | 0.0100 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2B | Rattus norvegicus (Norway rat) | IC50 | 0.0100 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2C | Rattus norvegicus (Norway rat) | IC50 | 0.0100 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2D | Rattus norvegicus (Norway rat) | IC50 | 0.0100 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 3A | Rattus norvegicus (Norway rat) | IC50 | 0.0100 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 3B | Rattus norvegicus (Norway rat) | IC50 | 0.0100 | 1 | 1 |
| Imidazoleglycerol-phosphate dehydratase | Saccharomyces cerevisiae S288C | IC50 | 59.6333 | 1 | 3 |
| Integrase | Human immunodeficiency virus 1 | IC50 | 100.0000 | 1 | 1 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | IC50 | 0.2717 | 1 | 3 |
| Malate dehydrogenase, cytoplasmic | Homo sapiens (human) | IC50 | 85.0000 | 1 | 1 |
| Microsomal triglyceride transfer protein large subunit | Homo sapiens (human) | IC50 | 2.9020 | 1 | 2 |
| Multidrug resistance-associated protein 1 | Homo sapiens (human) | IC50 | 8.5000 | 1 | 1 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 9 |
| Phosphoribosyl pyrophosphate synthase-associated protein 2 | Homo sapiens (human) | Ki | 3,000.0000 | 1 | 1 |
| Potassium voltage-gated channel subfamily D member 3 | Homo sapiens (human) | IC50 | 3,162.2800 | 1 | 1 |
| Potassium voltage-gated channel subfamily E member 1 | Homo sapiens (human) | IC50 | 1,258.9300 | 1 | 1 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 | 73.0269 | 8 | 8 |
| Potassium voltage-gated channel subfamily KQT member 1 | Homo sapiens (human) | IC50 | 1,258.9300 | 1 | 1 |
| Protease | Human immunodeficiency virus 1 | IC50 | 26.1372 | 9 | 12 |
| Protein kinase C beta type | Homo sapiens (human) | IC50 | 150.0000 | 1 | 1 |
| Protein kinase C epsilon type | Homo sapiens (human) | IC50 | 150.0000 | 1 | 1 |
| Prothrombin | Bos taurus (cattle) | IC50 | 0.5860 | 1 | 2 |
| Renin | Homo sapiens (human) | Ki | 7.0000 | 1 | 1 |
| Replicase polyprotein 1ab | Betacoronavirus England 1 | IC50 | 10.0000 | 1 | 1 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | IC50 | 13.4420 | 2 | 5 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome-related coronavirus | IC50 | 15.8050 | 1 | 4 |
| Reverse transcriptase | Human immunodeficiency virus 1 | IC50 | 66.2510 | 7 | 21 |
| Reverse transcriptase | Moloney murine leukemia virus | IC50 | 10.0000 | 1 | 1 |
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | IC50 | 16.6678 | 362 | 599 |
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | Ki | 179.2006 | 44 | 72 |
| Ryanodine receptor 1 | Homo sapiens (human) | Ki | 7.0000 | 1 | 1 |
| Sodium channel protein type 5 subunit alpha | Homo sapiens (human) | IC50 | 2,241.1285 | 2 | 2 |
| Solute carrier family 22 member 6 | Homo sapiens (human) | IC50 | 20.7500 | 2 | 2 |
| Thymidine kinase | Ureaplasma parvum serovar 3 str. ATCC 700970 | IC50 | 12.5000 | 1 | 1 |
| Thymidine kinase | Staphylococcus aureus | Ki | 944.0000 | 1 | 1 |
| Thymidine kinase, cytosolic | Homo sapiens (human) | IC50 | 3.0000 | 1 | 1 |
| Thymidine kinase, cytosolic | Homo sapiens (human) | Ki | 4.9500 | 2 | 2 |
| Thymidylate kinase | Mycobacterium tuberculosis H37Rv | Ki | 28.0000 | 3 | 3 |
| Voltage-dependent L-type calcium channel subunit alpha-1C | Homo sapiens (human) | IC50 | 54.2000 | 1 | 1 |
| Voltage-dependent L-type calcium channel subunit alpha-1D | Homo sapiens (human) | IC50 | 54.2000 | 1 | 1 |
| Voltage-dependent L-type calcium channel subunit alpha-1F | Homo sapiens (human) | IC50 | 54.2000 | 1 | 1 |
| Voltage-dependent L-type calcium channel subunit alpha-1S | Homo sapiens (human) | IC50 | 54.2000 | 1 | 1 |
Activation Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Albumin | Homo sapiens (human) | Kd | 44.0000 | 1 | 6 |
| C-X-C chemokine receptor type 4 | Homo sapiens (human) | EC50 | 0.0880 | 1 | 1 |
| Capsid protein | Hepatitis B virus | EC50 | 2.6736 | 3 | 4 |
| Chain A, probable fosfomycin resistance protein | Pseudomonas aeruginosa PAO1 | Kd | 0.2000 | 1 | 1 |
| Chain B, probable fosfomycin resistance protein | Pseudomonas aeruginosa PAO1 | Kd | 0.2000 | 1 | 1 |
| Cholesterol 24-hydroxylase | Homo sapiens (human) | Kd | 5.3333 | 3 | 3 |
| Hsf1 protein | Mus musculus (house mouse) | EC50 | 0.2870 | 1 | 1 |
| Protease | Human immunodeficiency virus 1 | EC50 | 0.1260 | 1 | 1 |
| Reverse transcriptase | Human immunodeficiency virus 1 | EC50 | 72.9280 | 14 | 34 |
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | EC50 | 2.7749 | 62 | 130 |
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | Kd | 4.3764 | 4 | 4 |
Other Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | ID50 | 10.2000 | 1 | 2 |
| Acetylcholinesterase | Rattus norvegicus (Norway rat) | ID50 | 17.5400 | 1 | 2 |
| Adenosine deaminase | Bos taurus (cattle) | Km | 430.0000 | 1 | 1 |
| Adenylate kinase 2, mitochondrial | Homo sapiens (human) | Km | 4,500.0000 | 1 | 2 |
| Adenylate kinase isoenzyme 1 | Homo sapiens (human) | Km | 4,500.0000 | 1 | 2 |
| Carbonic anhydrase 1 | Homo sapiens (human) | KA | 12.0000 | 1 | 1 |
| Cytochrome P450 2B6 | Homo sapiens (human) | Km | 0.4500 | 1 | 1 |
| Ectonucleoside triphosphate diphosphohydrolase 1 | Bos taurus (cattle) | Km | 2.9000 | 1 | 1 |
| Fructose-1,6-bisphosphatase 1 | Mus musculus (house mouse) | ID50 | 4.2000 | 1 | 2 |
| Lysosomal protective protein | Homo sapiens (human) | Km | 610.0000 | 1 | 1 |
| Phosphoribosyl pyrophosphate synthase-associated protein 2 | Homo sapiens (human) | Km | 1,500.0000 | 1 | 1 |
| Protease | Human immunodeficiency virus 1 | IC90 | 3.7260 | 4 | 4 |
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | Activity | 1.7652 | 6 | 11 |
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | C90 | 7.3000 | 1 | 1 |
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | CC50 | 67.0000 | 1 | 2 |
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | CD50 | 129.0000 | 1 | 2 |
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | ED50 | 1.0176 | 7 | 16 |
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | IC90 | 0.0493 | 13 | 13 |
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | ID50 | 7.0164 | 39 | 74 |
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | Km | 1,112.5000 | 4 | 4 |
| Solute carrier family 22 member 11 | Homo sapiens (human) | Km | 151.8000 | 1 | 1 |
| Solute carrier family 22 member 6 | Homo sapiens (human) | Km | 31.4600 | 4 | 5 |
| Solute carrier family 22 member 6 | Rattus norvegicus (Norway rat) | Km | 169.0000 | 2 | 2 |
| Solute carrier family 22 member 7 | Homo sapiens (human) | Km | 26.8000 | 1 | 1 |
| Solute carrier family 22 member 7 | Rattus norvegicus (Norway rat) | Km | 1,513.0000 | 1 | 2 |
| Solute carrier family 22 member 8 | Homo sapiens (human) | Km | 711.7000 | 2 | 3 |
| Solute carrier organic anion transporter family member 1A3 | Rattus norvegicus (Norway rat) | Km | 70.3000 | 2 | 2 |
| Thymidine kinase | Ureaplasma parvum serovar 3 str. ATCC 700970 | Km | 2.7000 | 1 | 1 |
| Thymidine kinase | Staphylococcus aureus | Km | 11.6000 | 1 | 1 |
| Thymidine kinase, cytosolic | Homo sapiens (human) | Km | 3.1333 | 3 | 3 |
| Thymidine kinase, cytosolic | Rattus norvegicus (Norway rat) | Phosphorylation rate | 4.0000 | 1 | 1 |
| UDP-glucuronosyltransferase 2B7 | Homo sapiens (human) | Km | 770.0000 | 1 | 1 |