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antitubercular agent

A substance that kills or slows the growth of Mycobacterium tuberculosis and is used in the treatment of tuberculosis.

ChEBI ID: 33231

Members (19)

MemberDefinitionClass
aminosalicylic acidAn aminobenzoic acid that is salicylic acid substituted by an amino group at position 4.4-aminosalicylic acid
azomycinAn imidazole that is 1H-imidazole substituted at position 2 by a nitro group.2-nitroimidazole
bedaquilineA quinoline-based antimycobacterial drug used (as its fumarate salt) for the treatment of pulmonary multi-drug resistant tuberculosis by inhibition of ATP synthase, an enzyme essential for the replication of the mycobacteria.bedaquiline
caribenol aA terpene lactone that is 3,4,5,5a,6,7,7a,10,10a,10b-decahydro-2H-1-oxabenzo[cd]cyclopenta[h]azulen-2-one substituted by a hydroxy group at position 10b and methyl groups at positions 3, 6, 9 and 10a. It is isolated from the West Indian gorgonian octocoral Pseudopterogorgia elisabethae and exhibits antitubercular and antimalarial activity.caribenol A
cycloserineA 4-amino-1,2-oxazolidin-3-one that has R configuration. It is an antibiotic produced by Streptomyces garyphalus or S. orchidaceus and is used as part of a multi-drug regimen for the treatment of tuberculosis when resistance to, or toxicity from, primary drugs has developed. An analogue of D-alanine, it interferes with bacterial cell wall synthesis in the cytoplasm by competitive inhibition of L-alanine racemase (which forms D-alanine from L-alanine) and D-alanine--D-alanine ligase (which incorporates D-alanine into the pentapeptide required for peptidoglycan formation and bacterial cell wall synthesis).D-cycloserine zwitterion; D-cycloserine
ethambutolAn ethylenediamine derivative that is ethane-1,2-diamine in which one hydrogen attached to each of the nitrogens is sutstituted by a 1-hydroxybutan-2-yl group (S,S-configuration). It is a bacteriostatic antimycobacterial drug, effective against Mycobacterium tuberculosis and some other mycobacteria. It is used (as the dihydrochloride salt) in combination with other antituberculous drugs in the treatment of pulmonary and extrapulmonary tuberculosis; resistant strains of M. tuberculosis are readily produced if ethambutol is used alone.ethambutol
ethambutol hydrochlorideThe dihydrchloride salt of ethambutol. A bacteriostatic antimycobacterial drug, it is effective against Mycobacterium tuberculosis and some other mycobacteria. It is used in combination with other antituberculous drugs in the treatment of pulmonary and extrapulmonary tuberculosis; resistant strains of M. tuberculosis are readily produced if ethambutol dihydrochloride is used alone.ethambutol dihydrochloride
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
hentriacontanehentriacontane
isoniazidA carbohydrazide obtained by formal condensation between pyridine-4-carboxylic acid and hydrazine.isoniazide
lomefloxacinA fluoroquinolone antibiotic, used (generally as the hydrochloride salt) to treat bacterial infections including bronchitis and urinary tract infections. It is also used to prevent urinary tract infections prior to surgery.lomefloxacin
lomefloxacin hydrochlorideThe hydrochloride salt of lomefloxacin. It is administered by mouth to treat bacterial infections including bronchitis and urinary tract infections. It is also used topically as eye drops for the treatment of bacterial conjunctivitis, and as ear drops for the treatment of otitis externa and otitis media.lomefloxacin hydrochloride
pyrazinamideA monocarboxylic acid amide resulting from the formal condensation of the carboxy group of pyrazinoic acid (pyrazine-2-carboxylic acid) with ammonia. A prodrug for pyrazinoic acid, pyrazinecarboxamide is used as part of multidrug regimens for the treatment of tuberculosis.pyrazinecarboxamide
pyrazinoic acidThe parent compound of the class of pyrazinecarboxylic acids, that is pyrazine bearing a single carboxy substituent. The active metabolite of the antitubercular drug pyrazinamide.pyrazine-2-carboxylic acid
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
rifamycin svA member of the class of rifamycins that exhibits antibiotic and antitubercular properties.rifamycin SV
rifapentinerifapentine
s-ethylcysteineA S-alkyl-L-cysteine that is L-cysteine in which the hydrogen of the thiol group is substituted by an ethyl group.S-ethyl-L-cysteine zwitterion; S-ethyl-L-cysteine
viomycinA cyclic peptide antibiotic produced by the actinomycete Streptomyces puniceus, used in the treatment of tuberculosis.viomycin

Research

Studies (47,416)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199022,619 (47.70)18.7374
1990's4,954 (10.45)18.2507
2000's6,367 (13.43)29.6817
2010's9,899 (20.88)24.3611
2020's3,577 (7.54)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials4,083 (6.17%)5.53%
Reviews3,721 (5.62%)6.00%
Case Studies6,344 (9.58%)4.05%
Observational273 (0.41%)0.25%
Other51,803 (78.22%)84.16%

Protein Targets (183)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency29.903312
15-lipoxygenase, partialHomo sapiens (human)Potency31.622811
67.9K proteinVaccinia virusPotency3.162311
acetylcholinesteraseHomo sapiens (human)Potency0.870911
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency33.205813
AR proteinHomo sapiens (human)Potency26.737444
aryl hydrocarbon receptorHomo sapiens (human)Potency10.109026
arylsulfatase AHomo sapiens (human)Potency0.021311
ATAD5 protein, partialHomo sapiens (human)Potency23.099911
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency33.807811
Bloom syndrome protein isoform 1Homo sapiens (human)Potency50.118722
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency66.896812
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency29.897517
Chain A, CruzipainTrypanosoma cruziPotency12.589311
Chain A, Ferritin light chainEquus caballus (horse)Potency39.810711
Chain A, HADH2 proteinHomo sapiens (human)Potency35.716822
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency25.118911
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency18.240612
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency17.740711
Chain B, HADH2 proteinHomo sapiens (human)Potency35.716822
chromobox protein homolog 1Homo sapiens (human)Potency46.686523
cytochrome P450 2C9 precursorHomo sapiens (human)Potency39.810713
cytochrome P450 2C9, partialHomo sapiens (human)Potency3.790811
cytochrome P450 2D6Homo sapiens (human)Potency7.563711
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency12.589311
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency17.6108212
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency33.926114
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency18.833611
DNA polymerase betaHomo sapiens (human)Potency63.095711
dopamine D1 receptorHomo sapiens (human)Potency0.009211
endonuclease IVEscherichia coliPotency5.623411
estrogen nuclear receptor alphaHomo sapiens (human)Potency20.9728712
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency1.799011
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency44.284659
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency18.3364110
EWS/FLI fusion proteinHomo sapiens (human)Potency9.572725
flap endonuclease 1Homo sapiens (human)Potency18.887611
GVesicular stomatitis virusPotency3.790811
GABA theta subunitRattus norvegicus (Norway rat)Potency17.610816
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency17.610816
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency17.610816
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency17.610816
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency17.610816
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency17.610816
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency17.610816
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency17.610816
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency17.610816
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency17.610816
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency17.610816
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency17.610816
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency17.610816
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency17.610816
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency17.610816
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency17.610816
gemininHomo sapiens (human)Potency3.653722
GLI family zinc finger 3Homo sapiens (human)Potency27.045925
GLS proteinHomo sapiens (human)Potency31.622811
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency23.149435
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency38.3220211
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency15.848911
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency3.790811
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency1.584922
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency3.790812
Interferon betaHomo sapiens (human)Potency3.790811
interleukin 8Homo sapiens (human)Potency66.824211
lamin isoform A-delta10Homo sapiens (human)Potency6.309611
LuciferasePhotinus pyralis (common eastern firefly)Potency5.011911
M-phase phosphoprotein 8Homo sapiens (human)Potency44.668411
Microtubule-associated protein tauHomo sapiens (human)Potency24.702812
mitogen-activated protein kinase 1Homo sapiens (human)Potency5.011911
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency28.183811
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency38.999936
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)Potency1.188311
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency14.125411
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency0.228211
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency125.892011
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency10.691011
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency75.686311
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency50.118711
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency20.627246
phosphopantetheinyl transferaseBacillus subtilisPotency32.983812
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency31.622811
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency35.481311
pregnane X nuclear receptorHomo sapiens (human)Potency11.703112
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency100.000011
RAR-related orphan receptor gammaMus musculus (house mouse)Potency23.903114
regulator of G-protein signaling 4Homo sapiens (human)Potency0.532311
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency21.150834
retinoid X nuclear receptor alphaHomo sapiens (human)Potency2.238711
Smad3Homo sapiens (human)Potency0.357513
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.810711
survival motor neuron protein isoform dHomo sapiens (human)Potency14.125412
TDP1 proteinHomo sapiens (human)Potency25.192526
thioredoxin glutathione reductaseSchistosoma mansoniPotency19.514712
thioredoxin reductaseRattus norvegicus (Norway rat)Potency34.833436
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency17.573412
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency0.223911
thyroid stimulating hormone receptorHomo sapiens (human)Potency8.275328
USP1 protein, partialHomo sapiens (human)Potency37.646022
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency7.526123

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
10 kDa chaperonin Escherichia coliIC50100.000022
10 kDa heat shock protein, mitochondrialHomo sapiens (human)IC50100.000011
3-oxoacyl-[acyl-carrier-protein] synthase 3 Escherichia coliIC501,000.000011
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 synthase subunit c Mycolicibacterium smegmatisIC500.011934
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50100.820015
Bile salt export pumpHomo sapiens (human)IC50325.5006718
Bile salt export pumpRattus norvegicus (Norway rat)IC50509.450014
Bile salt export pumpHomo sapiens (human)Ki31.000011
Bile salt export pumpRattus norvegicus (Norway rat)Ki7.850012
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC5056.000011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC5093.660015
Carbonic anhydrase 1Homo sapiens (human)IC50130.000011
Carbonic anhydrase 1Homo sapiens (human)Ki240.000011
Carbonic anhydrase 2Homo sapiens (human)IC50750.000011
Carbonic anhydrase 2Homo sapiens (human)Ki1,230.000011
Caspase-1Homo sapiens (human)IC508.319011
Chain A, N-methyl-D-aspartate Receptor Subunit 1Rattus norvegicus (Norway rat)Ki241.000013
Cytochrome P450 1A2Homo sapiens (human)IC5010.000011
Cytochrome P450 1A2Homo sapiens (human)Ki56.000011
Cytochrome P450 2A6Homo sapiens (human)Ki60.000011
Cytochrome P450 2C19Homo sapiens (human)IC505.800022
Cytochrome P450 2C19Homo sapiens (human)Ki10.000011
Cytochrome P450 2C8Homo sapiens (human)Ki374.000011
Cytochrome P450 2C9 Homo sapiens (human)IC5010.000011
Cytochrome P450 2D6Homo sapiens (human)IC5010.000011
Cytochrome P450 3A4Homo sapiens (human)IC5035.000044
Cytochrome P450 3A4Homo sapiens (human)Ki36.000011
D-alanine--D-alanine ligaseEnterococcus faecalis V583IC50262.000011
Dihydrofolate reductaseMycobacterium tuberculosis H37RvKi0.001011
DNA gyrase subunit AEscherichia coli K-12IC501,000.000011
DNA gyrase subunit AMycobacterium tuberculosis H37RvIC5050.000012
DNA gyrase subunit BEscherichia coli K-12IC501,000.000011
DNA gyrase subunit BMycobacterium tuberculosis H37RvIC5050.000012
DNA-directed RNA polymerase subunit betaEscherichia coli K-12IC5050.010015
DNA-directed RNA polymerase subunit betaEscherichia coli O127:H6 str. E2348/69IC50511.333333
DNA-directed RNA polymerase subunit betaMycobacterium tuberculosis H37RvIC500.010011
DNA-directed RNA polymerase subunit betaShigella sonnei Ss046IC5050.010015
Endonuclease 8-like 1Homo sapiens (human)IC5050.000011
Endonuclease III-like protein 1Homo sapiens (human)IC5050.000011
Enoyl-[acyl-carrier-protein] reductase [NADH]Mycobacterium tuberculosis H37RvIC504.160022
Formamidopyrimidine-DNA glycosylaseEscherichia coli K-12IC5050.000011
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)IC504.835022
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)IC502.300011
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)IC502.300011
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)IC502.300011
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)IC502.300011
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)IC502.300011
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)IC502.300011
Glutathione S-transferase omega-1Homo sapiens (human)IC5075.000011
Isocitrate lyaseMycobacterium tuberculosis H37RvIC50455.800011
Lanosterol 14-alpha demethylaseHomo sapiens (human)IC5030.000011
Macrophage migration inhibitory factorHomo sapiens (human)IC50400.000011
microphthalmia-associated transcription factor isoform 9Homo sapiens (human)IC502.834133
Multidrug resistance-associated protein 4Homo sapiens (human)IC5095.360015
MyeloperoxidaseHomo sapiens (human)IC504.850022
N-glycosylase/DNA lyaseHomo sapiens (human)IC5050.000044
NAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)IC50671.850012
NH(3)-dependent NAD(+) synthetaseBacillus subtilis subsp. subtilis str. 168IC501.000011
Nicotinate phosphoribosyltransferaseHomo sapiens (human)Ki0.000111
Pantothenate synthetaseMycobacterium tuberculosis H37RvIC5025.000036
Polyphenol oxidase 2Agaricus bisporusIC50502.000012
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)IC502.949011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50270.841199
Proton-coupled amino acid transporter 1Homo sapiens (human)Ki4,400.000011
Putative FAD-containing monooxygenase MymAMycobacterium tuberculosis H37RvIC504.900011
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC504.360011
Sigma intracellular receptor 2Rattus norvegicus (Norway rat)IC501.600011
Solute carrier organic anion transporter family member 1A1Rattus norvegicus (Norway rat)Ki12.400022
Solute carrier organic anion transporter family member 1A2Homo sapiens (human)Ki31.000012
Solute carrier organic anion transporter family member 1A4Rattus norvegicus (Norway rat)Ki3.386723
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)IC501.246055
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)Ki6.700023
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)IC501.500011
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)Ki3.133323
Solute carrier organic anion transporter family member 2B1 Homo sapiens (human)IC5065.000011
Solute carrier organic anion transporter family member 2B1 Homo sapiens (human)Ki33.000022
Thiosulfate sulfurtransferaseHomo sapiens (human)IC50100.000011
UDP-N-acetylmuramoyl-tripeptide--D-alanyl-D-alanine ligase Staphylococcus epidermidis RP62AIC50300.000011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
AlbuminHomo sapiens (human)Kd12.000011
ATP synthase subunit cBacillus sp. PS3Kd0.500011
B-cell lymphoma 6 proteinHomo sapiens (human)Kd1,000.000011
Cytochrome P450 2B6Homo sapiens (human)EC501.300011
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)EC502.950011
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)EC502.950011
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)EC502.950011
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)EC5010.525022
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)EC502.950011
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)EC502.950011
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)EC502.950011
Hydroxycarboxylic acid receptor 2Homo sapiens (human)EC506.300011
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC502.165699
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)EC5015.000011
Tyrosine-protein phosphatase non-receptor type 1Homo sapiens (human)Kd1,200.000044

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Arylacetamide deacetylaseHomo sapiens (human)Km200.000012
Enoyl-[acyl-carrier-protein] reductase [NADH]Mycobacterium tuberculosis H37RvMIC14.232522
Enoyl-[acyl-carrier-protein] reductase [NADH]Mycobacterium tuberculosis H37RvMIC990.070011
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