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Identification
NameStaurosporine
Accession NumberDB02010  (EXPT02970, EXPT02972)
TypeSmall Molecule
GroupsExperimental
DescriptionAn indolocarbazole that is a potent protein kinase C inhibitor which enhances cAMP-mediated responses in human neuroblastoma cells. (Biochem Biophys Res Commun 1995;214(3):1114-20)
Structure
Thumb
SynonymsNot Available
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIH88EPA0A3N
CAS number62996-74-1
WeightAverage: 466.531
Monoisotopic: 466.200490718
Chemical FormulaC28H26N4O3
InChI KeyInChIKey=HKSZLNNOFSGOKW-UCBFMKAXSA-N
InChI
InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20+,26-,28-/m1/s1
IUPAC Name
(2R,3R,4R,6S)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1²,⁶.0⁷,²⁸.0⁸,¹³.0¹⁵,¹⁹.0²⁰,²⁷.0²¹,²⁶]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one
SMILES
CN[C@@H]1C[C@@H]2O[C@](C)([C@@H]1OC)N1C3=C(C=CC=C3)C3=C1C1=C(C4=C(C=CC=C4)N21)C1=C3CNC1=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as indolocarbazoles. These are polycyclic aromatic compounds containing an indole fused to a carbazole.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassIndoles and derivatives
Sub ClassCarbazoles
Direct ParentIndolocarbazoles
Alternative Parents
Substituents
  • Indolocarbazole
  • Pyrroloindole
  • Isoindolone
  • Isoindole or derivatives
  • Isoindoline
  • Indole
  • Benzenoid
  • Oxane
  • Heteroaromatic compound
  • Pyrrole
  • Secondary carboxylic acid amide
  • Lactam
  • Carboxamide group
  • Oxacycle
  • Azacycle
  • Secondary amine
  • Ether
  • Secondary aliphatic amine
  • Dialkyl ether
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationNot Available
PharmacodynamicsNot Available
Mechanism of actionNot Available
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organismsNot Available
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9737
Blood Brain Barrier-0.5243
Caco-2 permeable-0.5213
P-glycoprotein substrateSubstrate0.7192
P-glycoprotein inhibitor IInhibitor0.6683
P-glycoprotein inhibitor IINon-inhibitor0.6315
Renal organic cation transporterNon-inhibitor0.7748
CYP450 2C9 substrateNon-substrate0.7682
CYP450 2D6 substrateNon-substrate0.7667
CYP450 3A4 substrateSubstrate0.7987
CYP450 1A2 substrateNon-inhibitor0.563
CYP450 2C9 inhibitorNon-inhibitor0.6732
CYP450 2D6 inhibitorNon-inhibitor0.8232
CYP450 2C19 inhibitorNon-inhibitor0.6896
CYP450 3A4 inhibitorNon-inhibitor0.5634
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5897
Ames testNon AMES toxic0.6318
CarcinogenicityNon-carcinogens0.8573
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.6695 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9986
hERG inhibition (predictor II)Inhibitor0.5198
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.0439 mg/mLALOGPS
logP3.14ALOGPS
logP3.97ChemAxon
logS-4ALOGPS
pKa (Strongest Acidic)14.14ChemAxon
pKa (Strongest Basic)9.55ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area69.45 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity132.37 m3·mol-1ChemAxon
Polarizability51.38 Å3ChemAxon
Number of Rings8ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Chikara Murakata, Toshimitsu Takiguchi, Shigeo Katsumata, Akira Mihara, Keiichi Takahashi, Hiromitsu Saito, Shiro Akinaga, Masami Okabe, Yutaka Saito, “Process for producing staurosporine derivatives.” U.S. Patent US5344926, issued December, 1990.

US5344926
General ReferencesNot Available
External Links
ATC CodesNot Available
AHFS CodesNot Available
PDB Entries
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Staurosporine.
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Staurosporine.
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Staurosporine.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Staurosporine.
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Staurosporine.
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Staurosporine.
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Staurosporine.
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Staurosporine.
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Staurosporine.
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Staurosporine.
AtazanavirThe serum concentration of Atazanavir can be increased when it is combined with Staurosporine.
AtenololThe serum concentration of Atenolol can be increased when it is combined with Staurosporine.
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Staurosporine.
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Staurosporine.
BoceprevirThe serum concentration of Boceprevir can be increased when it is combined with Staurosporine.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Staurosporine.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Staurosporine.
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Staurosporine.
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Staurosporine.
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Staurosporine.
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Staurosporine.
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Staurosporine.
CarbamazepineThe serum concentration of Carbamazepine can be increased when it is combined with Staurosporine.
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Staurosporine.
CeritinibThe serum concentration of Ceritinib can be increased when it is combined with Staurosporine.
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Staurosporine.
ChlorpromazineThe serum concentration of Chlorpromazine can be increased when it is combined with Staurosporine.
CimetidineThe serum concentration of Cimetidine can be increased when it is combined with Staurosporine.
CiprofloxacinThe serum concentration of Ciprofloxacin can be increased when it is combined with Staurosporine.
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Staurosporine.
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Staurosporine.
ClarithromycinThe serum concentration of Clarithromycin can be increased when it is combined with Staurosporine.
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Staurosporine.
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Staurosporine.
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Staurosporine.
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Staurosporine.
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Staurosporine.
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Staurosporine.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Staurosporine.
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Staurosporine.
CrizotinibThe serum concentration of Crizotinib can be increased when it is combined with Staurosporine.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Staurosporine.
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be increased when it is combined with Staurosporine.
DabrafenibThe serum concentration of Dabrafenib can be increased when it is combined with Staurosporine.
DactinomycinThe serum concentration of Dactinomycin can be increased when it is combined with Staurosporine.
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Staurosporine.
DasatinibThe serum concentration of Dasatinib can be increased when it is combined with Staurosporine.
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Staurosporine.
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Staurosporine.
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Staurosporine.
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Staurosporine.
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Staurosporine.
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Staurosporine.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Staurosporine.
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Staurosporine.
DiltiazemThe serum concentration of Diltiazem can be increased when it is combined with Staurosporine.
DipyridamoleThe serum concentration of Dipyridamole can be increased when it is combined with Staurosporine.
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Staurosporine.
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Staurosporine.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Staurosporine.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Staurosporine.
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Staurosporine.
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Staurosporine.
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Staurosporine.
ErythromycinThe serum concentration of Erythromycin can be increased when it is combined with Staurosporine.
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Staurosporine.
EstriolThe serum concentration of Estriol can be increased when it is combined with Staurosporine.
EstroneThe serum concentration of Estrone can be increased when it is combined with Staurosporine.
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Staurosporine.
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Staurosporine.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Staurosporine.
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Staurosporine.
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Staurosporine.
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Staurosporine.
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Staurosporine.
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Staurosporine.
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Staurosporine.
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Staurosporine.
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Staurosporine.
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Staurosporine.
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Staurosporine.
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Staurosporine.
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Staurosporine.
IdelalisibThe serum concentration of Idelalisib can be increased when it is combined with Staurosporine.
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Staurosporine.
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Staurosporine.
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Staurosporine.
IndinavirThe serum concentration of Indinavir can be increased when it is combined with Staurosporine.
IndomethacinThe serum concentration of Indomethacin can be increased when it is combined with Staurosporine.
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Staurosporine.
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Staurosporine.
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Staurosporine.
KetoconazoleThe serum concentration of Ketoconazole can be increased when it is combined with Staurosporine.
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Staurosporine.
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Staurosporine.
LansoprazoleThe serum concentration of Lansoprazole can be increased when it is combined with Staurosporine.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Staurosporine.
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Staurosporine.
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Staurosporine.
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Staurosporine.
LevofloxacinThe serum concentration of Levofloxacin can be increased when it is combined with Staurosporine.
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Staurosporine.
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Staurosporine.
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Staurosporine.
LosartanThe serum concentration of Losartan can be increased when it is combined with Staurosporine.
MannitolThe serum concentration of Mannitol can be increased when it is combined with Staurosporine.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Staurosporine.
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Staurosporine.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Staurosporine.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Staurosporine.
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Staurosporine.
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Staurosporine.
MorphineThe serum concentration of Morphine can be increased when it is combined with Staurosporine.
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Staurosporine.
NadololThe serum concentration of Nadolol can be increased when it is combined with Staurosporine.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Staurosporine.
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Staurosporine.
NelfinavirThe serum concentration of Nelfinavir can be increased when it is combined with Staurosporine.
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Staurosporine.
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Staurosporine.
NilotinibThe serum concentration of Nilotinib can be increased when it is combined with Staurosporine.
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Staurosporine.
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Staurosporine.
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Staurosporine.
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Staurosporine.
OsimertinibThe serum concentration of Osimertinib can be increased when it is combined with Staurosporine.
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Staurosporine.
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Staurosporine.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Staurosporine.
PhenobarbitalThe serum concentration of Phenobarbital can be increased when it is combined with Staurosporine.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Staurosporine.
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Staurosporine.
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Staurosporine.
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Staurosporine.
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Staurosporine.
PrazosinThe serum concentration of Prazosin can be increased when it is combined with Staurosporine.
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Staurosporine.
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Staurosporine.
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Staurosporine.
PropranololThe serum concentration of Propranolol can be increased when it is combined with Staurosporine.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Staurosporine.
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Staurosporine.
QuinidineThe serum concentration of Quinidine can be increased when it is combined with Staurosporine.
QuinineThe serum concentration of Quinine can be increased when it is combined with Staurosporine.
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Staurosporine.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Staurosporine.
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Staurosporine.
RifampicinThe serum concentration of Rifampicin can be increased when it is combined with Staurosporine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Staurosporine.
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Staurosporine.
RitonavirThe serum concentration of Ritonavir can be increased when it is combined with Staurosporine.
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Staurosporine.
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Staurosporine.
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Staurosporine.
SaquinavirThe serum concentration of Saquinavir can be increased when it is combined with Staurosporine.
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Staurosporine.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Staurosporine.
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Staurosporine.
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Staurosporine.
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Staurosporine.
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Staurosporine.
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Staurosporine.
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Staurosporine.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Staurosporine.
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Staurosporine.
Taurocholic AcidThe serum concentration of Taurocholic Acid can be increased when it is combined with Staurosporine.
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Staurosporine.
TelaprevirThe serum concentration of Telaprevir can be increased when it is combined with Staurosporine.
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Staurosporine.
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Staurosporine.
TimololThe serum concentration of Timolol can be increased when it is combined with Staurosporine.
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Staurosporine.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Staurosporine.
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Staurosporine.
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Staurosporine.
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Staurosporine.
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Staurosporine.
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Staurosporine.
VenlafaxineThe serum concentration of Venlafaxine can be increased when it is combined with Staurosporine.
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Staurosporine.
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Staurosporine.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Staurosporine.
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Staurosporine.
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Staurosporine.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Sh2 domain binding
Specific Function:
Non-receptor tyrosine-protein kinase that plays an essential role in the selection and maturation of developing T-cells in the thymus and in the function of mature T-cells. Plays a key role in T-cell antigen receptor (TCR)-linked signal transduction pathways. Constitutively associated with the cytoplasmic portions of the CD4 and CD8 surface receptors. Association of the TCR with a peptide antig...
Gene Name:
LCK
Uniprot ID:
P06239
Molecular Weight:
58000.15 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Transcription factor binding
Specific Function:
Proto-oncogene with serine/threonine kinase activity involved in cell survival and cell proliferation and thus providing a selective advantage in tumorigenesis. Exerts its oncogenic activity through: the regulation of MYC transcriptional activity, the regulation of cell cycle progression and by phosphorylation and inhibition of proapoptotic proteins (BAD, MAP3K5, FOXO3). Phosphorylation of MYC ...
Gene Name:
PIM1
Uniprot ID:
P11309
Molecular Weight:
45411.905 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Non-membrane spanning protein tyrosine kinase activity
Specific Function:
Tyrosine kinase that plays an essential role in regulation of the adaptive immune response. Regulates the development, function and differentiation of conventional T-cells and nonconventional NKT-cells. When antigen presenting cells (APC) activate T-cell receptor (TCR), a series of phosphorylation lead to the recruitment of ITK to the cell membrane, in the vicinity of the stimulated TCR recepto...
Gene Name:
ITK
Uniprot ID:
Q08881
Molecular Weight:
71830.405 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Receptor signaling protein tyrosine kinase activity
Specific Function:
Non-receptor tyrosine kinase which mediates signal transduction downstream of a variety of transmembrane receptors including classical immunoreceptors like the B-cell receptor (BCR). Regulates several biological processes including innate and adaptive immunity, cell adhesion, osteoclast maturation, platelet activation and vascular development. Assembles into signaling complexes with activated r...
Gene Name:
SYK
Uniprot ID:
P43405
Molecular Weight:
72065.76 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Signal transducer activity
Specific Function:
Stress-activated serine/threonine-protein kinase involved in cytokines production, endocytosis, reorganization of the cytoskeleton, cell migration, cell cycle control, chromatin remodeling, DNA damage response and transcriptional regulation. Following stress, it is phosphorylated and activated by MAP kinase p38-alpha/MAPK14, leading to phosphorylation of substrates. Phosphorylates serine in the...
Gene Name:
MAPKAPK2
Uniprot ID:
P49137
Molecular Weight:
45567.415 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Ubiquitin protein ligase binding
Specific Function:
Constitutively active protein kinase that acts as a negative regulator in the hormonal control of glucose homeostasis, Wnt signaling and regulation of transcription factors and microtubules, by phosphorylating and inactivating glycogen synthase (GYS1 or GYS2), EIF2B, CTNNB1/beta-catenin, APC, AXIN1, DPYSL2/CRMP2, JUN, NFATC1/NFATC, MAPT/TAU and MACF1. Requires primed phosphorylation of the majo...
Gene Name:
GSK3B
Uniprot ID:
P49841
Molecular Weight:
46743.865 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Receptor binding
Specific Function:
Non-receptor tyrosine-protein kinase that plays an important role in the regulation of cell growth, differentiation, migration and immune response. Phosphorylates tyrosine residues located in the C-terminal tails of Src-family kinases (SFKs) including LCK, SRC, HCK, FYN, LYN or YES1. Upon tail phosphorylation, Src-family members engage in intramolecular interactions between the phosphotyrosine ...
Gene Name:
CSK
Uniprot ID:
P41240
Molecular Weight:
50703.975 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Metal ion binding
Specific Function:
Serine/threonine-protein kinase involved in the control of the cell cycle; essential for meiosis, but dispensable for mitosis. Phosphorylates CTNNB1, USP37, p53/TP53, NPM1, CDK7, RB1, BRCA2, MYC, NPAT, EZH2. Interacts with cyclins A, B1, B3, D, or E. Triggers duplication of centrosomes and DNA. Acts at the G1-S transition to promote the E2F transcriptional program and the initiation of DNA synt...
Gene Name:
CDK2
Uniprot ID:
P24941
Molecular Weight:
33929.215 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Protein serine/threonine kinase activity
Specific Function:
Phosphoinositide-3-kinase (PI3K) that phosphorylates PtdIns(4,5)P2 (Phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 plays a key role by recruiting PH domain-containing proteins to the membrane, including AKT1 and PDPK1, activating signaling cascades involved in cell growth, survival, proliferation, motility and morphology. Links G-protein...
Gene Name:
PIK3CG
Uniprot ID:
P48736
Molecular Weight:
126452.625 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Protein serine/threonine kinase activity
Specific Function:
Serine/threonine kinase which acts as a master kinase, phosphorylating and activating a subgroup of the AGC family of protein kinases. Its targets include: protein kinase B (PKB/AKT1, PKB/AKT2, PKB/AKT3), p70 ribosomal protein S6 kinase (RPS6KB1), p90 ribosomal protein S6 kinase (RPS6KA1, RPS6KA2 and RPS6KA3), cyclic AMP-dependent protein kinase (PRKACA), protein kinase C (PRKCD and PRKCZ), ser...
Gene Name:
PDPK1
Uniprot ID:
O15530
Molecular Weight:
63151.305 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Ubiquitin-protein transferase activity
Specific Function:
Calcium-independent, phospholipid- and diacylglycerol (DAG)-dependent serine/threonine-protein kinase that mediates non-redundant functions in T-cell receptor (TCR) signaling, including T-cells activation, proliferation, differentiation and survival, by mediating activation of multiple transcription factors such as NF-kappa-B, JUN, NFATC1 and NFATC2. In TCR-CD3/CD28-co-stimulated T-cells, is re...
Gene Name:
PRKCQ
Uniprot ID:
Q04759
Molecular Weight:
81864.145 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Receptor binding
Specific Function:
Tyrosine kinase that plays an essential role in regulation of the adaptive immune response. Regulates motility, adhesion and cytokine expression of mature T-cells, as well as thymocyte development. Contributes also to the development and activation of primary B-lymphocytes. When antigen presenting cells (APC) activate T-cell receptor (TCR), a serie of phosphorylations lead to the recruitment of...
Gene Name:
ZAP70
Uniprot ID:
P43403
Molecular Weight:
69871.63 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Budworth J, Davies R, Malkhandi J, Gant TW, Ferry DR, Gescher A: Comparison of staurosporine and four analogues: their effects on growth, rhodamine 123 retention and binding to P-glycoprotein in multidrug-resistant MCF-7/Adr cells. Br J Cancer. 1996 May;73(9):1063-8. [PubMed:8624264 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23