Page last updated: 2024-08-05 15:16:37
leprostatic drug
A substance that suppresses Mycobacterium leprae, ameliorates the clinical manifestations of leprosy, and/or reduces the incidence and severity of leprous reactions.
ChEBI ID: 35816
Members (6)
| Member | Definition | Class |
|---|---|---|
| clofazimine | 3-Isopropylimino-3,5-dihydro-phenazine in which the hydrogen at position 5 is substituted substituted by a 4-chlorophenyl group, and that at position 2 is substituted by a (4-chlorophenyl)amino group. A dark red crystalline solid, clofazimine is an antimycobacterial and is one of the main drugs used for the treatment of multi-bacillary leprosy. However, it can cause red/brown discolouration of the skin, so other treatments are often preferred in light-skinned patients. | clofazimine |
| dapsone | A sulfone that is diphenylsulfone in which the hydrogen atom at the 4 position of each of the phenyl groups is substituted by an amino group. It is active against a wide range of bacteria, but is mainly employed for its actions against Mycobacterium leprae, being used as part of multidrug regimens in the treatment of all forms of leprosy. | dapsone |
| ethionamide | A thiocarboxamide that is pyridine-4-carbothioamide substituted by an ethyl group at position 2. A prodrug that undergoes metabolic activation by conversion to the corresponding S-oxide. | ethionamide |
| rifampin | A member of the class of rifamycins that is a a semisynthetic antibiotic derived from Amycolatopsis rifamycinica (previously known as Amycolatopsis mediterranei and Streptomyces mediterranei). | rifampicin zwitterion; rifampicin |
| rifapentine | rifapentine | |
| sulfameter | A sulfonamide consisting of pyrimidine having a methoxy substituent at the 5-position and a 4-aminobenzenesulfonamido group at the 2-position. | sulfamethoxydiazine |
Research
Studies (24,779)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 8,787 (35.46) | 18.7374 |
| 1990's | 3,420 (13.80) | 18.2507 |
| 2000's | 4,190 (16.91) | 29.6817 |
| 2010's | 6,106 (24.64) | 24.3611 |
| 2020's | 2,276 (9.19) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 2,139 (7.42%) | 5.53% |
| Reviews | 2,003 (6.95%) | 6.00% |
| Case Studies | 4,743 (16.45%) | 4.05% |
| Observational | 141 (0.49%) | 0.25% |
| Other | 19,806 (68.69%) | 84.16% |
Protein Targets (126)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 15-lipoxygenase, partial | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| 67.9K protein | Vaccinia virus | Potency | 11.2947 | 1 | 2 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| AR protein | Homo sapiens (human) | Potency | 41.2809 | 3 | 3 |
| bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 89.1251 | 1 | 1 |
| C-terminal-binding protein 1 | Homo sapiens (human) | Potency | 3.3814 | 1 | 1 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 0.3548 | 1 | 1 |
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 12.5893 | 1 | 1 |
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 7.0795 | 1 | 1 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 1.7783 | 1 | 1 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 4.4668 | 1 | 1 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 0.7943 | 1 | 1 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 2.2236 | 1 | 2 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 1.3450 | 1 | 1 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 2.5119 | 1 | 1 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 7.9433 | 2 | 2 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 22.6710 | 1 | 2 |
| DNA polymerase beta | Homo sapiens (human) | Potency | 63.0957 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 17.4774 | 7 | 13 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 39.6916 | 5 | 12 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 11.2322 | 1 | 2 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 20.9310 | 2 | 2 |
| eyes absent homolog 2 isoform a | Homo sapiens (human) | Potency | 1.9015 | 1 | 1 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 4.2160 | 1 | 1 |
| G | Vesicular stomatitis virus | Potency | 2.2236 | 1 | 2 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| geminin | Homo sapiens (human) | Potency | 9.0695 | 2 | 3 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 24.3365 | 1 | 1 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 16.6806 | 4 | 6 |
| GTP-binding nuclear protein Ran isoform 1 | Homo sapiens (human) | Potency | 4.6109 | 1 | 1 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 13.1257 | 2 | 5 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 2.2236 | 1 | 2 |
| hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) | Homo sapiens (human) | Potency | 5.2276 | 2 | 4 |
| importin subunit beta-1 isoform 1 | Homo sapiens (human) | Potency | 52.3054 | 2 | 2 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 2.2236 | 1 | 4 |
| Interferon beta | Homo sapiens (human) | Potency | 2.2236 | 1 | 2 |
| interleukin 8 | Homo sapiens (human) | Potency | 66.8242 | 1 | 2 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 8.0754 | 1 | 4 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 3.1623 | 1 | 1 |
| muscleblind-like protein 1 isoform 1 | Homo sapiens (human) | Potency | 19.9526 | 1 | 1 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 46.3931 | 3 | 5 |
| nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 25.9290 | 1 | 1 |
| nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 0.0977 | 1 | 1 |
| Nuclear receptor ROR-gamma | Homo sapiens (human) | Potency | 17.3399 | 1 | 2 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 33.4915 | 1 | 1 |
| parathyroid hormone/parathyroid hormone-related peptide receptor precursor | Homo sapiens (human) | Potency | 67.9460 | 1 | 2 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 6.9111 | 1 | 1 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 44.5070 | 2 | 2 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 39.3209 | 2 | 3 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 31.6228 | 1 | 1 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 7.0795 | 1 | 1 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 11.7031 | 1 | 2 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 9.7942 | 3 | 3 |
| Smad3 | Homo sapiens (human) | Potency | 1.2575 | 1 | 3 |
| snurportin-1 | Homo sapiens (human) | Potency | 52.3054 | 2 | 2 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 16.0901 | 2 | 6 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 13.0905 | 2 | 4 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 16.5311 | 2 | 4 |
| transcriptional regulator ERG isoform 3 | Homo sapiens (human) | Potency | 53.1380 | 2 | 2 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 15.8489 | 1 | 1 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 11.2086 | 2 | 2 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 28.1838 | 1 | 1 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 10 kDa chaperonin | Escherichia coli | IC50 | 100.0000 | 2 | 2 |
| 10 kDa heat shock protein, mitochondrial | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| 5-hydroxytryptamine receptor 6 | Homo sapiens (human) | Ki | 0.1830 | 1 | 1 |
| 6-hydroxymethyl-7,8-dihydropterin pyrophosphokinase | Plasmodium berghei | IC50 | 12.4100 | 1 | 1 |
| 60 kDa chaperonin | Escherichia coli | IC50 | 100.0000 | 2 | 2 |
| 60 kDa heat shock protein, mitochondrial | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Alpha-synuclein | Homo sapiens (human) | IC50 | 26.6500 | 2 | 2 |
| Arylacetamide deacetylase | Homo sapiens (human) | Ki | 300.0000 | 1 | 1 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 75.9750 | 1 | 4 |
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | IC50 | 0.9000 | 3 | 3 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 244.7079 | 7 | 14 |
| Bile salt export pump | Rattus norvegicus (Norway rat) | IC50 | 517.3500 | 1 | 2 |
| Bile salt export pump | Rattus norvegicus (Norway rat) | Ki | 11.9000 | 1 | 1 |
| Broad substrate specificity ATP-binding cassette transporter ABCG2 | Homo sapiens (human) | IC50 | 29.6000 | 1 | 2 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 53.1750 | 1 | 4 |
| Caspase-1 | Homo sapiens (human) | IC50 | 8.3190 | 1 | 1 |
| Cruzipain | Trypanosoma cruzi | IC50 | 23.0000 | 4 | 4 |
| Dihydrofolate reductase | Pneumocystis carinii | IC50 | 1.5000 | 1 | 1 |
| DNA gyrase subunit A | Mycobacterium tuberculosis H37Rv | IC50 | 50.0000 | 1 | 1 |
| DNA gyrase subunit B | Mycobacterium tuberculosis H37Rv | IC50 | 50.0000 | 1 | 1 |
| DNA-directed RNA polymerase subunit beta | Escherichia coli O127:H6 str. E2348/69 | IC50 | 511.3333 | 3 | 3 |
| DNA-directed RNA polymerase subunit beta | Mycobacterium tuberculosis H37Rv | IC50 | 0.0100 | 1 | 1 |
| Enoyl-[acyl-carrier-protein] reductase [NADH] | Mycobacterium tuberculosis H37Rv | IC50 | 0.0300 | 1 | 1 |
| Glutathione S-transferase omega-1 | Homo sapiens (human) | IC50 | 75.0000 | 1 | 1 |
| Lanosterol 14-alpha demethylase | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 63.8250 | 1 | 4 |
| Myeloperoxidase | Homo sapiens (human) | IC50 | 0.4200 | 1 | 1 |
| NH(3)-dependent NAD(+) synthetase | Bacillus subtilis subsp. subtilis str. 168 | IC50 | 1.0000 | 1 | 1 |
| Polyphenol oxidase 2 | Agaricus bisporus | IC50 | 4.0000 | 1 | 1 |
| Polyunsaturated fatty acid lipoxygenase ALOX15 | Oryctolagus cuniculus (rabbit) | IC50 | 2.9490 | 1 | 1 |
| Solute carrier organic anion transporter family member 1A1 | Rattus norvegicus (Norway rat) | Ki | 18.2000 | 1 | 1 |
| Solute carrier organic anion transporter family member 1A2 | Homo sapiens (human) | Ki | 51.0000 | 1 | 1 |
| Solute carrier organic anion transporter family member 1A4 | Rattus norvegicus (Norway rat) | Ki | 1.4300 | 2 | 2 |
| Solute carrier organic anion transporter family member 1B1 | Homo sapiens (human) | IC50 | 1.5000 | 4 | 4 |
| Solute carrier organic anion transporter family member 1B1 | Homo sapiens (human) | Ki | 9.0500 | 2 | 2 |
| Solute carrier organic anion transporter family member 1B3 | Homo sapiens (human) | IC50 | 1.5000 | 1 | 1 |
| Solute carrier organic anion transporter family member 1B3 | Homo sapiens (human) | Ki | 3.2000 | 2 | 2 |
| Solute carrier organic anion transporter family member 2B1 | Homo sapiens (human) | IC50 | 65.0000 | 1 | 1 |
| Solute carrier organic anion transporter family member 2B1 | Homo sapiens (human) | Ki | 63.0000 | 1 | 1 |
| Thiosulfate sulfurtransferase | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
Activation Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | EC50 | 30.0000 | 1 | 1 |
| Albumin | Homo sapiens (human) | Kd | 12.0000 | 1 | 1 |
| Cytochrome P450 2B6 | Homo sapiens (human) | EC50 | 1.3000 | 1 | 1 |
| Estrogen receptor | Rattus norvegicus (Norway rat) | EC50 | 2.2810 | 1 | 2 |
| Estrogen receptor beta | Rattus norvegicus (Norway rat) | EC50 | 2.2810 | 1 | 2 |
| mitogen-activated protein kinase kinase kinase 3 isoform 1 | Homo sapiens (human) | EC50 | 30.0000 | 1 | 1 |
| mitogen-activated protein kinase kinase kinase kinase 2 isoform 1 | Homo sapiens (human) | EC50 | 15.1550 | 2 | 2 |
| Nuclear receptor subfamily 1 group I member 2 | Homo sapiens (human) | EC50 | 2.1656 | 9 | 9 |
| Spike glycoprotein | Severe acute respiratory syndrome coronavirus 2 | Kd | 3.8200 | 1 | 1 |
| streptokinase A precursor | Streptococcus pyogenes M1 GAS | EC50 | 1.7620 | 2 | 2 |
Other Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Arylacetamide deacetylase | Homo sapiens (human) | Km | 200.0000 | 1 | 2 |
| Polyphenol oxidase 2 | Agaricus bisporus | Kic | 1.9000 | 1 | 1 |
| Solute carrier organic anion transporter family member 1B1 | Homo sapiens (human) | Km | 7.2500 | 2 | 2 |
| Solute carrier organic anion transporter family member 1B3 | Homo sapiens (human) | Km | 2.3000 | 1 | 1 |