Gene Targets > vesicle transport along microtubule
Page last updated: 2024-10-24

vesicle transport along microtubule

Definition

Target type: biologicalprocess

The directed movement of a vesicle along a microtubule, mediated by motor proteins. This process begins with the attachment of a vesicle to a microtubule, and ends when the vesicle reaches its final destination. [GOC:ecd, GOC:rl]

Vesicle transport along microtubules is a fundamental process in eukaryotic cells, crucial for delivering cargo to various cellular compartments. Microtubules, long, cylindrical polymers of tubulin protein, serve as tracks for the movement of motor proteins, which bind to and carry vesicles. There are two main types of motor proteins involved: kinesins and dyneins. Kinesins generally move cargo towards the plus end of microtubules, typically extending outwards from the cell center, while dyneins move cargo towards the minus end, often located at the cell center.

The process begins with the formation of a vesicle at a donor compartment, like the endoplasmic reticulum (ER) or Golgi apparatus. This vesicle encapsulates cargo molecules, such as proteins or lipids, destined for specific destinations. The vesicle then associates with a motor protein, which binds to its surface via adaptor proteins.

The motor protein utilizes the energy from ATP hydrolysis to move along the microtubule. This movement is directional, with kinesins pulling vesicles towards the plus end and dyneins pulling towards the minus end. The movement is also highly regulated, with specific signals and regulatory proteins controlling the direction, speed, and destination of vesicle transport.

As the vesicle moves along the microtubule, it may encounter other cellular components, such as organelles or other vesicles. This interaction can lead to the fusion of the vesicle with its target compartment, releasing the cargo. This fusion event is also tightly controlled by specific protein complexes that ensure the correct targeting and delivery of the cargo.

Overall, vesicle transport along microtubules is a complex and highly regulated process involving multiple steps. It relies on the coordinated action of motor proteins, adaptor proteins, regulatory proteins, and the microtubule cytoskeleton to ensure the efficient and accurate delivery of cargo to their destinations. This process is essential for various cellular functions, including protein synthesis, secretion, cell signaling, and organelle organization.'
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Proteins (3)

ProteinDefinitionTaxonomy
Protein kinase C zeta typeA protein kinase C zeta type that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q05513]Homo sapiens (human)
HuntingtinA huntingtin that is encoded in the genome of human. [PRO:DNx, UniProtKB:P42858]Homo sapiens (human)
Kinesin-1 heavy chainA kinesin-1 heavy chain that is encoded in the genome of human. [PRO:DNx, UniProtKB:P33176]Homo sapiens (human)

Compounds (185)

CompoundDefinitionClassesRoles
edelfosine1-octadecyl-2-methylglycero-3-phosphocholine : A glycerophosphocholine that is glycero-3-phosphocholine substituted at positions 1 and 2 by octadecyl and methyl groups respectively.

edelfosine : A racemate comprising equimolar amounts of (R)- and (S)-edelfosine.

edelfosine: RN given refers to parent cpd		glycerophosphocholine
cgp 524114,5-dianilinophthalimide : Phthalimide substituted at the 4- and 5-positions by anilino groups.

4,5-dianilinophthalimide: structure given in first source		phthalimidesgeroprotector;
tyrosine kinase inhibitor
bisindolylmaleimide ibisindolylmaleimide I: a bis(indolyl)maleimide
bisindolylmaleimide ivindoles;
maleimides
n-(2-(methylamino)ethyl)-5-isoquinolinesulfonamideisoquinolines;
sulfonamide
n-(2-aminoethyl)-5-isoquinolinesulfonamide
1-(5-isoquinolinesulfonyl)piperazineisoquinolines
fasudilfasudil : An isoquinoline substituted by a (1,4-diazepan-1-yl)sulfonyl group at position 5. It is a Rho-kinase inhibitor and its hydrochloride hydrate form is approved for the treatment of cerebral vasospasm and cerebral ischemia.

fasudil: intracellular calcium antagonist; structure in first source		isoquinolines;
N-sulfonyldiazepane		antihypertensive agent;
calcium channel blocker;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
geroprotector;
neuroprotective agent;
nootropic agent;
vasodilator agent
staurosporine aglyconestaurosporine aglycone: metabolite from culture broth of Nocardiopsis sp.; a neurotrophin antag; inhibits BDNF TrkB receptor
minaprineminaprine: Agr 1240 refers to di-HCl; short-acting type A MAO inhibitor (MAOI) of mild potency; structuremorpholines;
pyridazines;
secondary amine		antidepressant;
antiparkinson drug;
cholinergic drug;
dopamine uptake inhibitor;
serotonin uptake inhibitor
imatinibaromatic amine;
benzamides;
N-methylpiperazine;
pyridines;
pyrimidines		antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor
suraminsuramin : A member of the class of phenylureas that is urea in which each of the amino groups has been substituted by a 3-({2-methyl-5-[(4,6,8-trisulfo-1-naphthyl)carbamoyl]phenyl}carbamoyl)phenyl group. An activator of both the rabbit skeletal muscle RyR1 and sheep cardiac RyR2 isoform ryanodine receptor channels, it has been used for the treatment of human African trypanosomiasis for over 100 years.

Suramin: A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties.		naphthalenesulfonic acid;
phenylureas;
secondary carboxamide		angiogenesis inhibitor;
antinematodal drug;
antineoplastic agent;
apoptosis inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
GABA antagonist;
GABA-gated chloride channel antagonist;
purinergic receptor P2 antagonist;
ryanodine receptor agonist;
trypanocidal drug
whi p180
phenidonephenidone: photographic developer; RN given refers to parent cpd; structure
tetradecanoylphorbol acetatephorbol 13-acetate 12-myristate : A phorbol ester that is phorbol in which the hydroxy groups at the cyclopropane ring juction (position 13) and the adjacent carbon (position 12) have been converted into the corresponding acetate and myristate esters. It is a major active constituent of the seed oil of Croton tiglium. It has been used as a tumour promoting agent for skin carcinogenesis in rodents and is associated with increased cell proliferation of malignant cells. However its function is controversial since a decrease in cell proliferation has also been observed in several cancer cell types.

phorbol ester : Esters of phorbol, originally found in croton oil (from Croton tiglium, of the family Euphorbiaceae). A number of phorbol esters possess activity as tumour promoters and activate the mechanisms associated with cell growth. Some of these are used in experiments as activators of protein kinase C.

Tetradecanoylphorbol Acetate: A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA.		acetate ester;
diester;
phorbol ester;
tertiary alpha-hydroxy ketone;
tetradecanoate ester		antineoplastic agent;
apoptosis inducer;
carcinogenic agent;
mitogen;
plant metabolite;
protein kinase C agonist;
reactive oxygen species generator
staurosporineindolocarbazole alkaloid;
organic heterooctacyclic compound		apoptosis inducer;
bacterial metabolite;
EC 2.7.11.13 (protein kinase C) inhibitor;
geroprotector
norharmanbeta-carboline : The parent compound of the beta-carbolines, a tricyclic structure comprising an indole ring system ortho- fused to C-3 and C-4 of a pyridine ring.

norharman: RN given refers to parent cpd		beta-carbolines;
mancude organic heterotricyclic parent		fungal metabolite;
marine metabolite
rebeccamycinrebeccamycin : An N-glycosyl compound consisting of a heteropolycyclic ring system with a glucosyl group attached to one of the indolic nitrogens.

rebeccamycin: from actinomycete strain C-38,383; structure given in first source		indolocarbazole;
N-glycosyl compound;
organic heterohexacyclic compound;
organochlorine compound
1-(5-isoquinolinesulfonyl)-2-methylpiperazine dihydrochloride1-(5-isoquinolinesulfonyl)-2-methylpiperazine dihydrochloride : A hydrochloride salt prepared from anileridine and two molar equivalents of hydrogen chloride.hydrochlorideEC 2.7.11.13 (protein kinase C) inhibitor
gefitinibaromatic ether;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
quinazolines;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
epidermal growth factor receptor antagonist
lestaurtinibindolocarbazole
vatalanibmonochlorobenzenes;
phthalazines;
pyridines;
secondary amino compound		angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
vascular endothelial growth factor receptor antagonist
ruboxistaurinruboxistaurin: inhibits protein kinase C beta; structure in first source
canertinibmonochlorobenzenes;
morpholines;
organofluorine compound;
quinazolines		antineoplastic agent;
tyrosine kinase inhibitor
cyc 202seliciclib : 2,6-Diaminopurine carrying benzylamino, (2R)-1-hydroxybutan-2-yl and isopropyl substituents at C-6, C-2-N and N-9 respectively. It is an experimental drug candidate in the family of pharmacological cyclin-dependent kinase (CDK) inhibitors.2,6-diaminopurinesantiviral drug;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
sb 203580imidazoles;
monofluorobenzenes;
pyridines;
sulfoxide		EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector;
Hsp90 inhibitor;
neuroprotective agent
enzastaurinindoles;
maleimides
erlotinibaromatic ether;
quinazolines;
secondary amino compound;
terminal acetylenic compound		antineoplastic agent;
epidermal growth factor receptor antagonist;
protein kinase inhibitor
lapatinibfurans;
organochlorine compound;
organofluorine compound;
quinazolines		antineoplastic agent;
tyrosine kinase inhibitor
sorafenib(trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
phenylureas;
pyridinecarboxamide		angiogenesis inhibitor;
anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
ferroptosis inducer;
tyrosine kinase inhibitor
7-n-butyl-6-(4'-hydroxyphenyl)-5h-pyrrolo(2,3b)pyrazine
purvalanol bpurvalanol B: protein kinase inhibitor; structure in first sourcepurvalanolprotein kinase inhibitor
h 89(E)-N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide : A N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide in which the double bond adopts a trans-configuration.

N-(2-(4-bromocinnamylamino)ethyl)-5-isoquinolinesulfonamide: structure given in first source

N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide : A member of the class of isoquinolines that is the sulfonamide obtained by formal condensation of the sulfo group of isoquinoline-5-sulfonic acid with the primary amino group of N(1)-[3-(4-bromophenyl)prop-2-en-1-yl]ethane-1,2-diamine. It is a protein kinase A inhibitor.		N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide
12-deoxyphorbol 13-acetatephorbol estermetabolite
purvalanol a6-((3-chloro)anilino)-2-(isopropyl-2-hydroxyethylamino)-9-isopropylpurine: purvalanol A is the (1R)-isomer;purvalanol
s 1033(trifluoromethyl)benzenes;
imidazoles;
pyridines;
pyrimidines;
secondary amino compound;
secondary carboxamide		anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
SMER 28SMER 28 : A member of the class of quinazolines that is quinazoline which is substituted by a prop-2-en-1-ylnitrilo group and a bromo group at positions 4 and 6, respectively. It is a modulator of mammalian autophagy.organobromine compound;
quinazolines;
secondary amino compound		autophagy inducer
xl147aromatic amine;
benzothiadiazole;
quinoxaline derivative;
sulfonamide		antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
4-[(1-methyl-5-tetrazolyl)thio]-5-phenylthieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
tamoxifenstilbenoid;
tertiary amino compound		angiogenesis inhibitor;
antineoplastic agent;
bone density conservation agent;
EC 1.2.3.1 (aldehyde oxidase) inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
estrogen antagonist;
estrogen receptor antagonist;
estrogen receptor modulator
sf 2370K-252a : A organic heterooctacyclic compound that is a potent inhibitor of protein kinase C and is isolated from Nocardiopsis sp K-252a

SF 2370: indolocarbazole isolated from Actinomadura sp. SF-2370; structure given in first source		bridged compound;
gamma-lactam;
methyl ester;
organic heterooctacyclic compound		antimicrobial agent;
bacterial metabolite;
EC 2.7.11.13 (protein kinase C) inhibitor;
tropomyosin-related kinase B receptor antagonist
tandutinibaromatic ether;
N-arylpiperazine;
N-carbamoylpiperazine;
phenylureas;
piperidines;
quinazolines;
tertiary amino compound		antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
dasatinibdasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN).

N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source		1,3-thiazoles;
aminopyrimidine;
monocarboxylic acid amide;
N-(2-hydroxyethyl)piperazine;
N-arylpiperazine;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
ha 1100HA 1100: intracellular calcium antagonist
7-epi-hydroxystaurosporine
zd 6474CH 331: structure in first sourcearomatic ether;
organobromine compound;
organofluorine compound;
piperidines;
quinazolines;
secondary amine		antineoplastic agent;
tyrosine kinase inhibitor
pd 407824
harmineharmine : A harmala alkaloid in which the harman skeleton is methoxy-substituted at C-7.

Harmine: Alkaloid isolated from seeds of PEGANUM HARMALA; ZYGOPHYLLACEAE. It is identical to banisterine, or telepathine, from Banisteria caapi and is one of the active ingredients of hallucinogenic drinks made in the western Amazon region from related plants. It has no therapeutic use, but (as banisterine) was hailed as a cure for postencephalitic PARKINSON DISEASE in the 1920's.		harmala alkaloidanti-HIV agent;
EC 1.4.3.4 (monoamine oxidase) inhibitor;
metabolite
sirolimussirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent.

Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.		antibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol		antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
ophiocordinazepinostatin: isolated from Fusarium merismoides; structure in first source; RN assigned by CAS - 63590-19-2 (ophiocordin; azepinostatin is not the same as ophiocordin)
alvocidibalvocidib : A synthetic dihydroxyflavone that is 5,7-dihydroxyflavone which is substituted by a 3-hydroxy-1-methylpiperidin-4-yl group at position 8 and by a chlorine at the 2' position (the (-)-3S,4R stereoisomer). A cyclin-dependent kinase 9 (CDK9) inhibitor, it has been studied for the treatment of acute myeloid leukaemia, arthritis and atherosclerotic plaque formation.

alvocidib: structure given in first source		dihydroxyflavone;
hydroxypiperidine;
monochlorobenzenes;
tertiary amino compound		antineoplastic agent;
antirheumatic drug;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
arcyriaflavin aarcyriaflavin A: from marine ascidian, Eudistoma sp.; structure given in first sourceindolocarbazole
pd 161570PD 161570: structure in first source
bosutinib4-((2,4-dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methyl-1-piperazinyl)propoxy)-3-quinolinecarbonitrile: a Src kinase inhibitor; structure in first sourceaminoquinoline;
aromatic ether;
dichlorobenzene;
N-methylpiperazine;
nitrile;
tertiary amino compound		antineoplastic agent;
tyrosine kinase inhibitor
orantiniborantinib : An oxindole that is 3-methyleneoxindole in which one of the hydrogens of the methylene group is substituted by a 2-(2-carboxyethyl)-3,5-dimethylpyrrol-3-yl group. It is an ATP-competitive inhibitor of the tyrosine kinase activity of fibroblast growth factor receptor 1.

orantinib: an antiangiogenic agent
su 11248monocarboxylic acid amide;
pyrroles		angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
immunomodulator;
neuroprotective agent;
vascular endothelial growth factor receptor antagonist
vx680N-arylpiperazine
cyc 1164-methyl-5-(2-(4-morpholinophenylamino)pyrimidin-4-yl)thiazol-2-amine: an aurora kinase inhibitor; structure in first source
axitinibaryl sulfide;
benzamides;
indazoles;
pyridines		antineoplastic agent;
tyrosine kinase inhibitor;
vascular endothelial growth factor receptor antagonist
a 419259
b 43RK-24466 : A member of the class of pyrrolopyrimidines that is 7H-pyrrolo[2,3-d]pyrimidine substituted by amino, 4-phenoxyphenyl, and cyclopentyl groups at positions 4, 5 and 7, respectively. It is a potent inhibitor of Lck that inhibits Lck (64-509) and LckCD isoforms (IC50 of less than 1 and 2 nM, respectively).aromatic amine;
aromatic ether;
cyclopentanes;
primary amino compound;
pyrrolopyrimidine		EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
geroprotector
cgp 533534,5-bis(4-fluoroanilino)phthalimide: structure in first sourcephthalimides
temsirolimusmacrolide lactam
pep0053-ingenyl angelate: protein kinase C agonist and antineoplastic; structure in first source
on 01910N-[2-methoxy-5-({[2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl}methyl)phenyl]glycine : A glycine derivative that is glycine in which one of the hydrogens of the amino group is substituted by a 2-methoxy-5-({[2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl}methyl)phenyl group.

ON 01910: a Plk1 inhibitor with antineoplastic activity; structure in first source

rigosertib : An N-[2-methoxy-5-({[2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl}methyl)phenyl]glycine in which the double bond has E-configuration. It is a non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM and exhibits anti-cancer properties.		N-[2-methoxy-5-({[2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl}methyl)phenyl]glycineantineoplastic agent;
apoptosis inducer;
EC 2.7.11.21 (polo kinase) inhibitor;
microtubule-destabilising agent
5-(4-chlorophenyl)-4-[(1-methyl-5-tetrazolyl)thio]thieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
a 770041aromatic amide
[4-[[4-(1-benzothiophen-2-yl)-2-pyrimidinyl]amino]phenyl]-[4-(1-pyrrolidinyl)-1-piperidinyl]methanonebenzamides;
N-acylpiperidine
av 412
edotecarin
cp 5476323-(4-bromo-2,6-difluorobenzyloxy)-5-(3-(4-pyrrolidin-1-ylbutyl)ureido)isothiazole-4-carboxylic acid amide: inhibits vascular endothelial growth factor receptor-2 tyrosine kinase; structure in first source
lenvatiniblenvatinib : A member of the class of quinolines that is the carboxamide of 4-{3-chloro-4-[(cyclopropylcarbamoyl)amino]phenoxy}-7-methoxyquinoline-6-carboxylic acid. A multi-kinase inhibitor and orphan drug used (as its mesylate salt) for the treatment of various types of thyroid cancer that do not respond to radioiodine.aromatic amide;
aromatic ether;
cyclopropanes;
monocarboxylic acid amide;
monochlorobenzenes;
phenylureas;
quinolines		antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
fibroblast growth factor receptor antagonist;
orphan drug;
vascular endothelial growth factor receptor antagonist
ripasudilisoquinolines
osi 930OSI 930: inhibits both receptor tyrosine kinase Kit and kinase insert domain receptor; structure in first sourcearomatic amide
scio-469SCIO-469: a small-molecule p38 mitogen-activated protein (MAP) kinase inhibitor for potential oral therapy for inflammatory disorders; in phase lib clinical trials for rheumatoid arthritis 4/2004

talmapimod : An indolecarboxamide obtained by formal condensation of the carboxy group of 6-chloro-3-[(dimethylamino)(oxo)acetyl]-1-methylindole-5-carboxylic acid with the secondary amino group of (2S,5R)-1-[(4-fluorophenyl)methyl]-2,5-dimethylpiperazine. It is a potent inhibitor of MAPK and exhibits anti-cancer properties.		aromatic amide;
aromatic ketone;
chloroindole;
dicarboxylic acid diamide;
indolecarboxamide;
monofluorobenzenes;
N-acylpiperazine;
N-alkylpiperazine		antineoplastic agent;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
cp 7247142-methoxy-N-(3-(4-((3-methyl-4-((6-methyl-3-pyridinyl)oxy)phenyl)amino)-6-quinazolinyl)-2-propenyl)acetamide: CP-724714 is the ((2E)-isomer, 1:1.5 succinate); structure in first source2-methoxy-N-[3-[4-[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]anilino]-6-quinazolinyl]prop-2-enyl]acetamideantineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
hepatotoxic agent
hmn-214(E)-4-(2-(2-(N-acetyl-N-(4-methoxybenzenesulfonyl)amino)stilbazole)) 1-oxide: an antineoplastic agent; structure in first source
ct52923CT52923: structure in first source
tivozanibN-(2-chloro-4-((6,7-dimethoxy-4-quinolyl)oxy)phenyl)-N'-(5-methyl-3-isoxazolyl)urea: KNR-951 is the HCl, monohydrate salt; an antineoplastic agent; structure in first sourcearomatic ether
hki 272nitrile;
quinolines		antineoplastic agent;
tyrosine kinase inhibitor
cediranibaromatic ether
ps1145PS1145: IkappaB kinase inhibitor; structure in first sourcebeta-carbolines
chir 99021CHIR 99021 : A member of the class of aminopyrimidines that is 2-aminopyrimidine substituted at positions N2, 5 and 6 by (5-cyanopyridin-2-yl)ethyl, 4-methylimidazol-2-yl and 2,4-dichlorophenyl groups respectively.

Chir 99021: structure in first source		aminopyridine;
aminopyrimidine;
cyanopyridine;
diamine;
dichlorobenzene;
imidazoles;
secondary amino compound		EC 2.7.11.26 (tau-protein kinase) inhibitor
masitinib1,3-thiazoles;
benzamides;
N-alkylpiperazine;
pyridines		antineoplastic agent;
antirheumatic drug;
tyrosine kinase inhibitor
azd 6244AZD 6244: a MEK inhibitorbenzimidazoles;
bromobenzenes;
hydroxamic acid ester;
monochlorobenzenes;
organofluorine compound;
secondary amino compound		anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
su 148135-((5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl)-N-(2-hydroxy-3-morpholin-4-ylpropyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide: has both antineoplastic and antiangiogenic activities; structure in first source
bibw 2992aromatic ether;
enamide;
furans;
monochlorobenzenes;
organofluorine compound;
quinazolines;
secondary carboxamide;
tertiary amino compound		antineoplastic agent;
tyrosine kinase inhibitor
sotrastaurinsotrastaurin : A member of the class of maleimides that is maleimide which is substituted at position 3 by an indol-3-yl group and at position 4 by a quinazolin-4-yl group, which in turn is substituted at position 2 by a 4-methylpiperazin-1-yl group. It is a potent and selective inhibitor of protein kinase C and has been investigated as an immunosuppresant in renal transplant patients.

sotrastaurin: a potent protein kinase C-selective inhibitor; structure in first source		indoles;
maleimides;
N-alkylpiperazine;
N-arylpiperazine;
quinazolines		anticoronaviral agent;
EC 2.7.11.13 (protein kinase C) inhibitor;
immunosuppressive agent
saracatinibaromatic ether;
benzodioxoles;
diether;
N-methylpiperazine;
organochlorine compound;
oxanes;
quinazolines;
secondary amino compound		anticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
autophagy inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
radiosensitizing agent
vx 702VX 702: a p38 MAP kinase inhibitorphenylpyridine
crenolanibaminopiperidine;
aromatic ether;
benzimidazoles;
oxetanes;
quinolines;
tertiary amino compound		angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
tg100-1153,3'-(2,4-diaminopteridine-6,7-diyl)diphenol: for treatment of ischemia reperfusion injury; structure in first sourcepteridines
ly 338522LY 338522: des-methyl metabolite of LY333531; structure in first source
PDGF receptor tyrosine kinase inhibitor IIIPDGF receptor tyrosine kinase inhibitor III : An N-arylpiperazine that is piperazine in which the hydrogen attached to the nitrogen at position 1 is replaced by a (4-phenoxyphenyl)aminocarbonyl group, while the hydrogen attached to the nitrogen at position 4 is replaced by a 6,7-dimethoxyquinazolin-4-yl group. It is an inhibitor of tyrosine kinases FLT3, PDGFR and KIT.aromatic ether;
N-arylpiperazine;
N-carbamoylpiperazine;
phenylureas;
quinazolines;
tertiary amino compound		EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
brivanibaromatic ether;
diether;
fluoroindole;
pyrrolotriazine;
secondary alcohol		angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
drug metabolite;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
fibroblast growth factor receptor antagonist
rgb 286638
at 75194-(2,6-dichlorobenzamido)-N-(piperidin-4-yl)-pyrazole-3-carboxamide : A member of the class of pryrazoles that is 4-amino-1H-pyrazole-3-carboxylic acid in which the primary amino group has been acylated by a 2,6-dichlorobenzoyl group and in which the carboxylic acid has been converted into a carboxamide by formal condensation with the primary amino group of 4-aminopiperidine.dichlorobenzene;
piperidines;
pyrazoles;
secondary carboxamide		antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
bms-690514
inno-406biaryl
N-[5-[[5-[(4-acetyl-1-piperazinyl)-oxomethyl]-4-methoxy-2-methylphenyl]thio]-2-thiazolyl]-4-[(3,3-dimethylbutan-2-ylamino)methyl]benzamidebenzamides
abt 869aromatic amine;
indazoles;
phenylureas		angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
azd 8931sapitinib : A member of the class of quinazolines that is 4-amino-7-methoxyquinazoline in which the amino group has been substituted by a 3-chloro-2-fluorophenyl group and in which position 6 of the quinoline ring has been substituted by a {1-[2-(methylamino)-2-oxoethyl]piperidin-4-yl}oxy group. Sapitinib is a dual tyrosine kinase inhibitor (TKI) of epithelial growth factor receptors (EGFR) HER2 and HER3.aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
piperidines;
quinazolines;
secondary amino compound;
tertiary amino compound		EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist
arq 197indoles
ridaforolimusmacrolide lactam
ch 4987655
cc-930
gw 25805-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)pyrimidine-2,4-diamine: a cFMS kinase inhibitor; structure in first source
chir-265aromatic ether
motesanibpyridinecarboxamide
fostamatinibfostamatinib: a spleen tyrosine kinase (Syk) inhibitor, metabolized to R406
trametinibacetamides;
aromatic amine;
cyclopropanes;
organofluorine compound;
organoiodine compound;
pyridopyrimidine;
ring assembly		anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector
mln8054benzazepine
pf-562,271indoles
ly2603618ureas
tg100801
dactolisibdactolisib : An imidazoquinoline that is 3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinoline substituted at position 1 by a 4-(1-cyanoisopropyl)phenyl group and at position 8 by a quinolin-3-yl group. A dual PI3K/mTOR inhibitor used in cancer treatment.

dactolisib: antineoplastic agent that inhibits both phosphatidylinositol 3-kinase and mTOR		imidazoquinoline;
nitrile;
quinolines;
ring assembly;
ureas		antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor
gsk 461364GSK 461364: an antineoplastic agent that inhibits polo-like kinase 1(trifluoromethyl)benzenes
e 7050aromatic ether
2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)-7-pyrido[2,3-d]pyrimidinonepyrazolopyridine
tak-901
buparlisibNVP-BKM120: a pan class I PI3 kinase inhibitor with antineoplastic activity; structure in first sourceaminopyridine;
aminopyrimidine;
morpholines;
organofluorine compound		antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
azd 1480
pha 848125N,1,4,4-tetramethyl-8-((4-(4-methylpiperazin-1-yl)phenyl)amino)-4,5-dihydro-1H-pyrazolo(4,3-h)quinazoline-3-carboxamide: a cyclin dependent kinase inhibitor
gsk6906931,2,5-oxadiazole;
acetylenic compound;
aromatic amine;
aromatic ether;
imidazopyridine;
piperidines;
primary amino compound;
tertiary alcohol		antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor
14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene: has antineoplastic activity; also inhibits Fms-like tyrosine kinase-3; structure in first source
pf 04217903quinolines
gdc 0941pictrelisib : A sulfonamide composed of indazole, morpholine, and methylsulfonyl-substituted piperazine rings bound to a thienopyrimidine ring.indazoles;
morpholines;
piperazines;
sulfonamide;
thienopyrimidine		EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
icotinib
4-[2-[(6-chloro-4-quinazolinyl)amino]ethyl]phenolquinazolines
kx-01
mk 5108aromatic ether
cudc 1017-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide: a histone deacetylase inhibitor; structure in first source
mln 8237MLN 8237: an aurora kinase A inhibitorbenzazepine
bms 754807BMS 754807: an IGR-1R kinase inhibitor; structure in first sourcepyrazoles;
pyridines;
pyrrolidines;
pyrrolotriazine		antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
sgi 1776SGI 1776: a Pim kinase inhibitor; structure in first sourceimidazoles
mk-1775adavosertib: a Wee1 kinase inhibitor; structure in first sourcepiperazines
dcc-2036rebastinib: an inhibitor of Tie2 tyrosine kinase receptor and antineoplastic agentorganofluorine compound;
phenylureas;
pyrazoles;
pyridinecarboxamide;
quinolines		tyrosine kinase inhibitor
cabozantinibcabozantinib : A dicarboxylic acid diamide that is N-phenyl-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide in which the hydrogen at position 4 on the phenyl ring is substituted by a (6,7-dimethoxyquinolin-4-yl)oxy group. A multi-tyrosine kinase inhibitor, used (as its malate salt) for the treatment of progressive, metastatic, medullary thyroid cancer.

cabozantinib: a multikinase inhibitor		aromatic ether;
dicarboxylic acid diamide;
organofluorine compound;
quinolines		antineoplastic agent;
tyrosine kinase inhibitor
poziotinibHM781-36B: antitumor irreversible Pan-HER inhibitor for treatment of gastric canceracrylamides;
aromatic ether;
dichlorobenzene;
diether;
monofluorobenzenes;
N-acylpiperidine;
quinazolines;
secondary amino compound;
substituted aniline		antineoplastic agent;
apoptosis inducer;
epidermal growth factor receptor antagonist
TAK-580MLN 2480: brain-penetrant RAF dimer antagonist

TAK-580 : A 1,3-thiazolecarboxamide that is 2-[(1R)-1-aminoethyl]-1,3-thiazole-5-carboxylic acid in which the carboxy group undergoes formal condensation with the amino group of 5-chloro-4-(trifluoromethyl)pyridin-2-amine and in which the amino group undergoes formal condensation with the carboxy group of 6-amino-5-chloropyrimidine-4-carboxylic acid. It is a pan-RAF kinase inhibitor which is currently in clinical development for the treatment of radiographically recurrent or progressive low-grade glioma in children and young adults.		1,3-thiazolecarboxamide;
aminopyrimidine;
chloropyridine;
organofluorine compound;
pyrimidinecarboxamide;
secondary carboxamide		antineoplastic agent;
apoptosis inducer;
B-Raf inhibitor
gsk 2126458omipalisib : A member of the class of quinolines that is quinoline which is substituted by pyridazin-4-yl and 5-[(2,4-difluorobenzene-1-sulfonyl)amino]-6-methoxypyridin-3-yl groups at positions 4 and 6, respectively. It is a highly potent inhibitor of PI3K and mTOR developed by GlaxoSmithKline and was previously in human phase 1 clinical trials for the treatment of idiopathic pulmonary fibrosis and solid tumors.

omipalisib: inhibitor of mTOR protein		aromatic ether;
difluorobenzene;
pyridazines;
pyridines;
quinolines;
sulfonamide		anticoronaviral agent;
antineoplastic agent;
autophagy inducer;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor;
radiosensitizing agent
emd1214063tepotinib: MET inhibitor
pf 3758309PF 3758309: a PAK4 p21-activated kinase inhibitor; structure in first sourceorganic heterobicyclic compound;
organonitrogen heterocyclic compound;
organosulfur heterocyclic compound
(5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol(5-(2,4-bis((3S)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol: a potent, selective, and orally bioavailable ATP-competitive mammalian target of rapamycin kinase inhibitor with in vitro and in vivo antitumor activity; structure in first sourcebenzyl alcohols;
morpholines;
pyridopyrimidine;
tertiary amino compound		antineoplastic agent;
apoptosis inducer;
mTOR inhibitor
5-(4-methoxyphenyl)-4-[(1-methyl-5-tetrazolyl)thio]thieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
5-(4-bromophenyl)-4-[(1-methyl-5-tetrazolyl)thio]thieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
gsk 1363089GSK 1363089: a multikinase inhibitor that acts on Met, RON, Axl, and VEGFR; structure in first sourcearomatic ether
kin-193pyridopyrimidine
5-(2-methoxyphenyl)-4-[(1-methyl-5-tetrazolyl)thio]thieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
5-(3-methoxyphenyl)-4-[(1-methyl-5-tetrazolyl)thio]thieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
5-(3-fluorophenyl)-4-[(1-methyl-5-tetrazolyl)thio]thieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
4-[(1-methyl-5-tetrazolyl)thio]-5-[2-(trifluoromethyl)phenyl]thieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
4-[(1-methyl-5-tetrazolyl)thio]-5-[3-(trifluoromethyl)phenyl]thieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
4-[(1-methyl-5-tetrazolyl)thio]-5-[4-(trifluoromethyl)phenyl]thieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
5-(2-bromophenyl)-4-[(1-methyl-5-tetrazolyl)thio]thieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
5-(3-bromophenyl)-4-[(1-methyl-5-tetrazolyl)thio]thieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
5-(2-chlorophenyl)-4-[(1-methyl-5-tetrazolyl)thio]thieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
4-[4-[(1-methyl-5-tetrazolyl)thio]-5-thieno[2,3-d]pyrimidinyl]benzonitrilearyl sulfide;
thienopyrimidine
4-[(1-methyl-5-tetrazolyl)thio]-5-(4-nitrophenyl)thieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
4-[(1-methyl-5-tetrazolyl)thio]-5-(4-phenylphenyl)thieno[2,3-d]pyrimidinebiphenyls;
thienopyrimidine
5-(1,3-benzodioxol-5-yl)-4-(1-methyltetrazol-5-yl)sulfanylthieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
4-[(1-methyl-5-tetrazolyl)thio]-5-(3-thiophenyl)thieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
5-(2-benzofuranyl)-4-[(1-methyl-5-tetrazolyl)thio]thieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
5-(4-dibenzothiophenyl)-4-[(1-methyl-5-tetrazolyl)thio]thieno[2,3-d]pyrimidinedibenzothiophenes;
thienopyrimidine
4-[(1-methyl-5-tetrazolyl)thio]-5-(1H-pyrrol-2-yl)thieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
1-[2-[4-[(1-methyl-5-tetrazolyl)thio]-5-thieno[2,3-d]pyrimidinyl]phenyl]ethanonearomatic ketone;
thienopyrimidine
5-(3-methylsulfonylphenyl)-4-[(1-methyl-5-tetrazolyl)thio]thieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
4-[(1-methyl-5-tetrazolyl)thio]-5-(1-naphthalenyl)thieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
5-bromo-4-[(1-methyl-5-tetrazolyl)thio]thieno[2,3-d]pyrimidinearyl sulfide;
thienopyrimidine
bay 869766
as 703026pyridinecarboxamide
dabrafenib1,3-thiazoles;
aminopyrimidine;
organofluorine compound;
sulfonamide		anticoronaviral agent;
antineoplastic agent;
B-Raf inhibitor
pki 587gedatolisib: inhibits both phosphatidylinositol 3-kinase and mTOR; structure in first source
1-[3-[4-[(1-methyl-5-tetrazolyl)thio]-5-thieno[2,3-d]pyrimidinyl]phenyl]ethanonearomatic ketone;
thienopyrimidine
abemaciclib
mk-8776
jnj38877605quinolines
dinaciclibpyrazolopyrimidine
alectinibaromatic ketone;
morpholines;
nitrile;
organic heterotetracyclic compound;
piperidines		antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
gsk2141795GSK2141795: an Akt inhibitor with antineoplastic activity; structure in first source
cep-32496agerafenib: inhibitor of RAF family kinases; structure in first source
ceritinibceritinib : A member of the class of aminopyrimidines that is 2,6-diamino-5-chloropyrimidine in which the amino groups at positions 2 and 6 are respectively carrying 2-methoxy-4-(piperidin-4-yl)-5-methylphenyl and 2-(isopropylsulfonyl)phenyl substituents. Used for the treatment of ALK-positive metastatic non-small cell lung cancer.

ceritinib: an anaplastic lymphoma kinase inhibitor		aminopyrimidine;
aromatic ether;
organochlorine compound;
piperidines;
secondary amino compound;
sulfone		antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
chir 258
osi 027OSI 027: inhibits both mTORC1 and mTORC2; structure in first source
nintedanibnintedanib : A member of the class of oxindoles that is a kinase inhibitor used (in the form of its ethylsulfonate salt) for the treatment of idiopathic pulmonary fibrosis and cancer.
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