Page last updated: 2024-08-05 15:35:21

microtubule-stabilising agent

Any substance that interacts with tubulin to promote polymerisation of microtubules.

ChEBI ID: 61950

Members (7)

MemberDefinitionClass
cabazitaxelA tetracyclic diterpenoid that is 10-deacetylbaccatin III having O-methyl groups attached at positions 7 and 10 as well as an O-(2R,3S)-3-[(tert-butoxycarbonyl)amino]-2-hydroxy-3-phenylpropanoyl group attached at position 13. Acts as a microtubule inhibitor, binds tubulin and promotes microtubule assembly and simultaneously inhibits disassembly.cabazitaxel
desoxyepothilone bAn epithilone that is epithilone C in which the hydrogen at position 13 of the oxacyclohexadec-13-ene-2,6-dione macrocycle has been replaced by a methyl group.epothilone D
epothilone aAn epithilone that is epothilone C in which the double bond in the macrocyclic lactone ring has been oxidised to the corresponding epoxide (the 13R,14S diastereoisomer).epothilone A
epothilone bAn epithilone that is epithilone D in which the double bond in the macrocyclic ring has been oxidised to the corresponding epoxide (the S,S stereoisomer).epothilone B
laulimalideA macrolide with formula C30H42O7 that is isolated from the marine sponges, Cacospongia mycofijiensis and Hyattella sp.laulimalide
paclitaxelA tetracyclic diterpenoid isolated originally from the bark of the Pacific yew tree, Taxus brevifolia. It is a mitotic inhibitor used in cancer chemotherapy. Note that the use of the former generic name 'taxol' is now limited, as Taxol is a registered trade mark.paclitaxel
tilivallineA pyrrolobenzodiazepine that is (11aS)-2,3,5,10,11,11a-hexahydro-1H-pyrrolo[2,1-c][1,4]benzodiazepine substituted by an oxo group at position 5, by a hydroxy group at position 9, and by a 1H-indol-3-yl group at position 11S. It is a natural product discovered in Klebsiella oxytoca which is the causative toxin in antibiotic associated hemorrhagic colitis. It exhibits a microtubule-stabilizing activity that leads to mitotic arrest in the host cells.tilivalline

Research

Studies (31,873)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-1990337 (1.06)18.7374
1990's3,733 (11.71)18.2507
2000's10,238 (32.12)29.6817
2010's13,214 (41.46)24.3611
2020's4,351 (13.65)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials5,982 (17.66%)5.53%
Reviews3,172 (9.36%)6.00%
Case Studies2,261 (6.68%)4.05%
Observational164 (0.48%)0.25%
Other22,292 (65.81%)84.16%

Protein Targets (90)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
67.9K proteinVaccinia virusPotency20.975223
AR proteinHomo sapiens (human)Potency0.025635
Cellular tumor antigen p53Homo sapiens (human)Potency0.012924
Chain A, Beta-lactamaseEscherichia coli K-12Potency12.589322
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency6.309611
estrogen nuclear receptor alphaHomo sapiens (human)Potency5.864845
EWS/FLI fusion proteinHomo sapiens (human)Potency0.239622
Fumarate hydrataseHomo sapiens (human)Potency5.257611
gemininHomo sapiens (human)Potency2.395725
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency0.141311
IDH1Homo sapiens (human)Potency0.007311
Interferon betaHomo sapiens (human)Potency0.010419
lamin isoform A-delta10Homo sapiens (human)Potency0.223911
LuciferasePhotinus pyralis (common eastern firefly)Potency8.492111
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency3.548111
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency35.481311
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency6.256012
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency0.192923
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency28.183811
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency44.668411
phosphopantetheinyl transferaseBacillus subtilisPotency50.118711
polyproteinZika virusPotency5.257611
PPM1D proteinHomo sapiens (human)Potency0.010416
pregnane X nuclear receptorHomo sapiens (human)Potency8.459023
pregnane X receptorRattus norvegicus (Norway rat)Potency3.548111
retinoid X nuclear receptor alphaHomo sapiens (human)Potency0.005011
TDP1 proteinHomo sapiens (human)Potency5.081427
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency0.069524
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency0.017811

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
10 kDa chaperonin Escherichia coliIC5085.000022
10 kDa heat shock protein, mitochondrialHomo sapiens (human)IC50100.000011
60 kDa chaperoninEscherichia coli K-12IC50250.000011
60 kDa chaperonin Escherichia coliIC5085.000022
60 kDa heat shock protein, mitochondrialHomo sapiens (human)IC50100.000011
Apoptosis regulator Bcl-2Homo sapiens (human)GI5010.000011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000011
ATP-dependent translocase ABCB1Homo sapiens (human)IC5036.659255
ATP-dependent translocase ABCB1Mus musculus (house mouse)IC50327.000011
Bcl-2-like protein 1Homo sapiens (human)GI5010.000011
Beta-tubulin Leishmania donovaniIC501.000011
Bile salt export pumpHomo sapiens (human)IC5022.020055
Botulinum neurotoxin type A Clostridium botulinumIC505.200011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000011
Cholecystokinin receptor type AHomo sapiens (human)IC5011.380011
Cholecystokinin receptor type AHomo sapiens (human)Ki2.276011
Delta-type opioid receptorHomo sapiens (human)IC504.202011
Delta-type opioid receptorHomo sapiens (human)Ki1.481011
Epidermal growth factor receptorHomo sapiens (human)IC5010.000011
Fibroblast growth factor receptor 1Homo sapiens (human)IC5010.000011
Genome polyprotein IC501.000011
Integrin alpha-V Homo sapiens (human)IC500.034011
Integrin beta-3Homo sapiens (human)IC500.034011
Melanocortin receptor 5Homo sapiens (human)IC5017.133011
Melanocortin receptor 5Homo sapiens (human)Ki16.072011
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000011
Nucleotide-binding oligomerization domain-containing protein 2Homo sapiens (human)IC507.943311
Proto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)IC5010.000011
Receptor tyrosine-protein kinase erbB-2Homo sapiens (human)IC5011.108011
Serum paraoxonase/arylesterase 1Homo sapiens (human)Ki16.500011
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)IC500.280011
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)Ki0.840011
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)IC500.260011
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)Ki1.800011
Substance-K receptorHomo sapiens (human)IC506.125011
Substance-K receptorHomo sapiens (human)Ki2.042011
Thiosulfate sulfurtransferaseHomo sapiens (human)IC50100.000011
Tubulin alpha-1A chainHomo sapiens (human)GI500.005333
Tubulin alpha-1A chainHomo sapiens (human)IC500.003511
Tubulin alpha-1B chainHomo sapiens (human)GI500.005333
Tubulin alpha-1B chainHomo sapiens (human)IC500.003511
Tubulin alpha-1C chainHomo sapiens (human)GI500.005333
Tubulin alpha-1C chainHomo sapiens (human)IC500.003511
Tubulin alpha-3C chainHomo sapiens (human)GI500.005333
Tubulin alpha-3C chainHomo sapiens (human)IC500.003511
Tubulin alpha-3E chainHomo sapiens (human)GI500.005333
Tubulin alpha-3E chainHomo sapiens (human)IC500.003511
Tubulin alpha-4A chainHomo sapiens (human)GI500.005333
Tubulin alpha-4A chainHomo sapiens (human)IC500.003511
Tubulin beta chainHomo sapiens (human)GI500.005333
Tubulin beta chainHomo sapiens (human)IC500.003511
Tubulin beta-1 chainHomo sapiens (human)GI500.005333
Tubulin beta-1 chainHomo sapiens (human)IC500.003511
Tubulin beta-2A chainHomo sapiens (human)GI500.005333
Tubulin beta-2A chainHomo sapiens (human)IC500.003511
Tubulin beta-2B chainHomo sapiens (human)GI500.005333
Tubulin beta-2B chainHomo sapiens (human)IC500.003511
Tubulin beta-3 chainHomo sapiens (human)GI500.005333
Tubulin beta-3 chainHomo sapiens (human)IC500.007044
Tubulin beta-4A chainHomo sapiens (human)GI500.005333
Tubulin beta-4A chainHomo sapiens (human)IC500.003511
Tubulin beta-4B chainHomo sapiens (human)GI500.005333
Tubulin beta-4B chainHomo sapiens (human)IC500.003511
Tubulin beta-6 chainHomo sapiens (human)GI500.005333
Tubulin beta-6 chainHomo sapiens (human)IC500.003511
Tubulin beta-8 chainHomo sapiens (human)GI500.005333
Tubulin beta-8 chainHomo sapiens (human)IC500.003511
Tyrosine-protein kinase ABL1Homo sapiens (human)IC5010.000011
Tyrosine-protein kinase FynHomo sapiens (human)IC5023.906011
Tyrosine-protein kinase MerHomo sapiens (human)IC504.900011
UDP-glucuronosyltransferase 1-6Homo sapiens (human)IC50139.780015
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)IC50139.780015
UDP-glucuronosyltransferase 1A4Homo sapiens (human)IC50139.780015
UDP-glucuronosyltransferase 2B10 Homo sapiens (human)IC50139.780015
UDP-glucuronosyltransferase 2B7Homo sapiens (human)IC50139.780015

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC5022.100022
Nuclear receptor subfamily 1 group I member 2Rattus norvegicus (Norway rat)EC500.010011
Similar to alpha-tubulin isoform 1 Bos taurus (cattle)EC500.830011
Tubulin alpha-1A chainHomo sapiens (human)EC500.630522
Tubulin alpha-1A chainSus scrofa (pig)EC500.520011
Tubulin alpha-1B chainHomo sapiens (human)EC500.630522
Tubulin alpha-1C chainHomo sapiens (human)EC500.630522
Tubulin alpha-3C chainHomo sapiens (human)EC500.630522
Tubulin alpha-3E chainHomo sapiens (human)EC500.630522
Tubulin alpha-4A chainHomo sapiens (human)EC500.630522
Tubulin beta chainHomo sapiens (human)EC500.630522
Tubulin beta chainSus scrofa (pig)EC500.520011
Tubulin beta-1 chainHomo sapiens (human)EC500.630522
Tubulin beta-2A chainHomo sapiens (human)EC500.630522
Tubulin beta-2B chainBos taurus (cattle)EC500.830011
Tubulin beta-2B chainHomo sapiens (human)EC500.630522
Tubulin beta-3 chainHomo sapiens (human)EC500.630522
Tubulin beta-4A chainHomo sapiens (human)EC500.630522
Tubulin beta-4B chainHomo sapiens (human)EC500.630522
Tubulin beta-6 chainHomo sapiens (human)EC500.630522
Tubulin beta-8 chainHomo sapiens (human)EC500.630522

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
ATP-dependent translocase ABCB1Homo sapiens (human)Km5.738033
ATP-dependent translocase ABCB1Homo sapiens (human)Vmax35.000011
Similar to alpha-tubulin isoform 1 Bos taurus (cattle)Activity4.200012
Similar to alpha-tubulin isoform 1 Bos taurus (cattle)ED500.700012
Tubulin alpha-1A chainHomo sapiens (human)ED500.500011
Tubulin alpha-1A chainSus scrofa (pig)ED500.576733
Tubulin alpha-1B chainHomo sapiens (human)ED500.500011
Tubulin alpha-1C chainHomo sapiens (human)ED500.500011
Tubulin alpha-3C chainHomo sapiens (human)ED500.500011
Tubulin alpha-3E chainHomo sapiens (human)ED500.500011
Tubulin alpha-4A chainHomo sapiens (human)ED500.500011
Tubulin beta chainHomo sapiens (human)ED500.500011
Tubulin beta-1 chainHomo sapiens (human)ED500.500011
Tubulin beta-2A chainHomo sapiens (human)ED500.500011
Tubulin beta-2B chainBos taurus (cattle)Activity4.200011
Tubulin beta-2B chainBos taurus (cattle)ED500.700011
Tubulin beta-2B chainHomo sapiens (human)ED500.500011
Tubulin beta-3 chainHomo sapiens (human)ED500.500011
Tubulin beta-4A chainHomo sapiens (human)ED500.500011
Tubulin beta-4B chainHomo sapiens (human)ED500.500011
Tubulin beta-6 chainHomo sapiens (human)ED500.500011
Tubulin beta-8 chainHomo sapiens (human)ED500.500011