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)

MemberDefinitionClass
clofazimine3-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
dapsoneA 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
ethionamideA 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
rifampinA 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
rifapentinerifapentine
sulfameterA 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)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19908,787 (35.46)18.7374
1990's3,420 (13.80)18.2507
2000's4,190 (16.91)29.6817
2010's6,106 (24.64)24.3611
2020's2,276 (9.19)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials2,139 (7.42%)5.53%
Reviews2,003 (6.95%)6.00%
Case Studies4,743 (16.45%)4.05%
Observational141 (0.49%)0.25%
Other19,806 (68.69%)84.16%

Protein Targets (126)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-lipoxygenase, partialHomo sapiens (human)Potency31.622811
67.9K proteinVaccinia virusPotency11.294712
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.810711
AR proteinHomo sapiens (human)Potency41.280933
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency89.125111
C-terminal-binding protein 1Homo sapiens (human)Potency3.381411
Chain A, Beta-lactamaseEscherichia coli K-12Potency0.354811
Chain A, CruzipainTrypanosoma cruziPotency12.589311
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency7.079511
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency1.778311
chromobox protein homolog 1Homo sapiens (human)Potency4.466811
cytochrome P450 2C9 precursorHomo sapiens (human)Potency0.794311
cytochrome P450 2C9, partialHomo sapiens (human)Potency2.223612
cytochrome P450 2D6Homo sapiens (human)Potency1.345011
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency2.511911
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency7.943322
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency22.671012
DNA polymerase betaHomo sapiens (human)Potency63.095711
estrogen nuclear receptor alphaHomo sapiens (human)Potency17.4774713
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency39.6916512
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency11.232212
EWS/FLI fusion proteinHomo sapiens (human)Potency20.931022
eyes absent homolog 2 isoform aHomo sapiens (human)Potency1.901511
farnesoid X nuclear receptorHomo sapiens (human)Potency4.216011
GVesicular stomatitis virusPotency2.223612
GABA theta subunitRattus norvegicus (Norway rat)Potency7.943311
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency7.943311
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency7.943311
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency7.943311
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency7.943311
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency7.943311
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency7.943311
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency7.943311
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency7.943311
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency7.943311
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency7.943311
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency7.943311
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency7.943311
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency7.943311
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency7.943311
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency7.943311
gemininHomo sapiens (human)Potency9.069523
GLI family zinc finger 3Homo sapiens (human)Potency24.336511
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency16.680646
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency4.610911
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency13.125725
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency2.223612
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency5.227624
importin subunit beta-1 isoform 1Homo sapiens (human)Potency52.305422
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency2.223614
Interferon betaHomo sapiens (human)Potency2.223612
interleukin 8Homo sapiens (human)Potency66.824212
lamin isoform A-delta10Homo sapiens (human)Potency8.075414
Microtubule-associated protein tauHomo sapiens (human)Potency31.622811
mitogen-activated protein kinase 1Homo sapiens (human)Potency3.162311
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency19.952611
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency46.393135
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency25.929011
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency0.097711
Nuclear receptor ROR-gammaHomo sapiens (human)Potency17.339912
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency33.491511
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency67.946012
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency6.911111
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency44.507022
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency39.320923
phosphopantetheinyl transferaseBacillus subtilisPotency31.622811
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency31.622811
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency7.079511
pregnane X nuclear receptorHomo sapiens (human)Potency11.703112
retinoid X nuclear receptor alphaHomo sapiens (human)Potency9.794233
Smad3Homo sapiens (human)Potency1.257513
snurportin-1Homo sapiens (human)Potency52.305422
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.810711
TDP1 proteinHomo sapiens (human)Potency16.090126
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency13.090524
thyroid stimulating hormone receptorHomo sapiens (human)Potency16.531124
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency53.138022
USP1 protein, partialHomo sapiens (human)Potency15.848911
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency11.208622
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency28.183811

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
10 kDa chaperonin Escherichia coliIC50100.000022
10 kDa heat shock protein, mitochondrialHomo sapiens (human)IC50100.000011
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.183011
6-hydroxymethyl-7,8-dihydropterin pyrophosphokinase Plasmodium bergheiIC5012.410011
60 kDa chaperonin Escherichia coliIC50100.000022
60 kDa heat shock protein, mitochondrialHomo sapiens (human)IC50100.000011
Alpha-synucleinHomo sapiens (human)IC5026.650022
Arylacetamide deacetylaseHomo sapiens (human)Ki300.000011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC5075.975014
ATP-dependent translocase ABCB1Homo sapiens (human)IC500.900033
Bile salt export pumpHomo sapiens (human)IC50244.7079714
Bile salt export pumpRattus norvegicus (Norway rat)IC50517.350012
Bile salt export pumpRattus norvegicus (Norway rat)Ki11.900011
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC5029.600012
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC5053.175014
Caspase-1Homo sapiens (human)IC508.319011
CruzipainTrypanosoma cruziIC5023.000044
Dihydrofolate reductasePneumocystis cariniiIC501.500011
DNA gyrase subunit AMycobacterium tuberculosis H37RvIC5050.000011
DNA gyrase subunit BMycobacterium tuberculosis H37RvIC5050.000011
DNA-directed RNA polymerase subunit betaEscherichia coli O127:H6 str. E2348/69IC50511.333333
DNA-directed RNA polymerase subunit betaMycobacterium tuberculosis H37RvIC500.010011
Enoyl-[acyl-carrier-protein] reductase [NADH]Mycobacterium tuberculosis H37RvIC500.030011
Glutathione S-transferase omega-1Homo sapiens (human)IC5075.000011
Lanosterol 14-alpha demethylaseHomo sapiens (human)IC5030.000011
Multidrug resistance-associated protein 4Homo sapiens (human)IC5063.825014
MyeloperoxidaseHomo sapiens (human)IC500.420011
NH(3)-dependent NAD(+) synthetaseBacillus subtilis subsp. subtilis str. 168IC501.000011
Polyphenol oxidase 2Agaricus bisporusIC504.000011
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)IC502.949011
Solute carrier organic anion transporter family member 1A1Rattus norvegicus (Norway rat)Ki18.200011
Solute carrier organic anion transporter family member 1A2Homo sapiens (human)Ki51.000011
Solute carrier organic anion transporter family member 1A4Rattus norvegicus (Norway rat)Ki1.430022
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)IC501.500044
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)Ki9.050022
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)IC501.500011
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)Ki3.200022
Solute carrier organic anion transporter family member 2B1 Homo sapiens (human)IC5065.000011
Solute carrier organic anion transporter family member 2B1 Homo sapiens (human)Ki63.000011
Thiosulfate sulfurtransferaseHomo sapiens (human)IC50100.000011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)EC5030.000011
AlbuminHomo sapiens (human)Kd12.000011
Cytochrome P450 2B6Homo sapiens (human)EC501.300011
Estrogen receptorRattus norvegicus (Norway rat)EC502.281012
Estrogen receptor betaRattus norvegicus (Norway rat)EC502.281012
mitogen-activated protein kinase kinase kinase 3 isoform 1Homo sapiens (human)EC5030.000011
mitogen-activated protein kinase kinase kinase kinase 2 isoform 1Homo sapiens (human)EC5015.155022
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC502.165699
Spike glycoproteinSevere acute respiratory syndrome coronavirus 2Kd3.820011
streptokinase A precursorStreptococcus pyogenes M1 GASEC501.762022

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Arylacetamide deacetylaseHomo sapiens (human)Km200.000012
Polyphenol oxidase 2Agaricus bisporusKic1.900011
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)Km7.250022
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)Km2.300011