Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T63986
(Former ID: TTDC00339)
|
|||||
| Target Name |
Kinesin spindle messenger RNA (KIF11 mRNA)
|
|||||
| Synonyms |
Thyroid receptor-interacting protein 5 (mRNA); TRIP5 (mRNA); TRIP-5 (mRNA); TR-interacting protein 5 (mRNA); Kinesin-related motor protein Eg5 (mRNA); Kinesin-like spindle protein HKSP (mRNA); Kinesin-like protein KIF11 (mRNA); Kinesin-like protein 1 (mRNA); KNSL1 (mRNA); EG5 (mRNA)
Click to Show/Hide
|
|||||
| Gene Name |
KIF11
|
|||||
| Target Type |
Clinical trial target
|
[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Liver cancer [ICD-11: 2C12] | |||||
| 2 | Malignant haematopoietic neoplasm [ICD-11: 2B33] | |||||
| Function |
Required in non-mitotic cells for transport of secretory proteins from the Golgi complex to the cell surface. Motor protein required for establishing a bipolar spindle during mitosis.
Click to Show/Hide
|
|||||
| BioChemical Class |
mRNA target
|
|||||
| UniProt ID | ||||||
| Sequence |
MASQPNSSAKKKEEKGKNIQVVVRCRPFNLAERKASAHSIVECDPVRKEVSVRTGGLADK
SSRKTYTFDMVFGASTKQIDVYRSVVCPILDEVIMGYNCTIFAYGQTGTGKTFTMEGERS PNEEYTWEEDPLAGIIPRTLHQIFEKLTDNGTEFSVKVSLLEIYNEELFDLLNPSSDVSE RLQMFDDPRNKRGVIIKGLEEITVHNKDEVYQILEKGAAKRTTAATLMNAYSSRSHSVFS VTIHMKETTIDGEELVKIGKLNLVDLAGSENIGRSGAVDKRAREAGNINQSLLTLGRVIT ALVERTPHVPYRESKLTRILQDSLGGRTRTSIIATISPASLNLEETLSTLEYAHRAKNIL NKPEVNQKLTKKALIKEYTEEIERLKRDLAAAREKNGVYISEENFRVMSGKLTVQEEQIV ELIEKIGAVEEELNRVTELFMDNKNELDQCKSDLQNKTQELETTQKHLQETKLQLVKEEY ITSALESTEEKLHDAASKLLNTVEETTKDVSGLHSKLDRKKAVDQHNAEAQDIFGKNLNS LFNNMEELIKDGSSKQKAMLEVHKTLFGNLLSSSVSALDTITTVALGSLTSIPENVSTHV SQIFNMILKEQSLAAESKTVLQELINVLKTDLLSSLEMILSPTVVSILKINSQLKHIFKT SLTVADKIEDQKKELDGFLSILCNNLHELQENTICSLVESQKQCGNLTEDLKTIKQTHSQ ELCKLMNLWTERFCALEEKCENIQKPLSSVQENIQQKSKDIVNKMTFHSQKFCADSDGFS QELRNFNQEGTKLVEESVKHSDKLNGNLEKISQETEQRCESLNTRTVYFSEQWVSSLNER EQELHNLLEVVSQCCEASSSDITEKSDGRKAAHEKQHNIFLDQMTIDEDKLIAQNLELNE TIKIGLTKLNCFLEQDLKLDIPTGTTPQRKSYLYPSTLVRTEPREHLLDQLKRKQPELLM MLNCSENNKEETIPDVDVEEAVLGQYTEEPLSQEPSVDAGVDCSSIGGVPFFQHKKSHGK DKENRGINTLERSKVEETTEHLVTKSRLPLRAQINL Click to Show/Hide
|
|||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Clinical Trial Drug(s) | [+] 2 Clinical Trial Drugs | + | ||||
| 1 | ALN-VSP | Drug Info | Phase 1 | Liver cancer | [1] | |
| 2 | EMD-534085 | Drug Info | Phase 1 | Haematological malignancy | [2] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 50 Inhibitor drugs | + | ||||
| 1 | EMD-534085 | Drug Info | [3] | |||
| 2 | (S)-dimethylenastron | Drug Info | [4] | |||
| 3 | (S)-enastron | Drug Info | [4] | |||
| 4 | 1-(7-methyl-9H-carbazol-3-yl)ethanone | Drug Info | [5] | |||
| 5 | 1-(trifluoromethyl)-9H-carbazole | Drug Info | [5] | |||
| 6 | 1-tert-butyl-9H-carbazole | Drug Info | [5] | |||
| 7 | 11H-benzo[a]carbazole | Drug Info | [5] | |||
| 8 | 2,3,4,11-tetrahydro-1H-benzo[a]carbazole | Drug Info | [5] | |||
| 9 | 2-(difluoromethyl)-9H-carbazole | Drug Info | [5] | |||
| 10 | 2-(trifluoromethoxy)-9H-carbazole | Drug Info | [5] | |||
| 11 | 2-(trifluoromethyl)-9H-carbazole | Drug Info | [5] | |||
| 12 | 2-ethyl-9H-carbazole | Drug Info | [5] | |||
| 13 | 2-isopropyl-9H-carbazole | Drug Info | [5] | |||
| 14 | 2-methyl-6-(trifluoromethyl)-9H-carbazole | Drug Info | [5] | |||
| 15 | 2-methyl-9H-carbazole | Drug Info | [5] | |||
| 16 | 2-tert-butoxy-9H-carbazole | Drug Info | [5] | |||
| 17 | 2-tert-butyl-7-(trifluoromethyl)-9H-carbazole | Drug Info | [5] | |||
| 18 | 2-tert-butyl-9H-carbazole | Drug Info | [5] | |||
| 19 | 3-(trifluoromethyl)-9H-carbazole | Drug Info | [5] | |||
| 20 | 3-methyl-6-(trifluoromethyl)-9H-carbazole | Drug Info | [5] | |||
| 21 | 3-tert-butyl-9H-carbazole | Drug Info | [5] | |||
| 22 | 4'-(trifluoromethyl)-4-biphenylol | Drug Info | [6] | |||
| 23 | 4'-(trifluoromethyl)-4-biphenylsulfonamide | Drug Info | [6] | |||
| 24 | 4'-(trifluoromethyl)-4-biphenylyl carbamate | Drug Info | [6] | |||
| 25 | 4'-(trifluoromethyl)-4-biphenylyl sulfamate | Drug Info | [6] | |||
| 26 | 4'-trifluoromethyl-biphenyl-4-ylamine | Drug Info | [6] | |||
| 27 | 4-(trifluoromethyl)biphenyl | Drug Info | [6] | |||
| 28 | 6-fluoro-2-methyl-9H-carbazole | Drug Info | [5] | |||
| 29 | 7-tert-butyl-9H-carbazole-3-carboxylic acid | Drug Info | [5] | |||
| 30 | 9-methyl-2-(trifluoromethyl)-9H-carbazole | Drug Info | [5] | |||
| 31 | 9H-carbazole-2-carbaldehyde | Drug Info | [5] | |||
| 32 | 9H-carbazole-3-carbaldehyde | Drug Info | [5] | |||
| 33 | Adociasulfate-2 | Drug Info | [7] | |||
| 34 | Methyl 7-tert-butyl-9H-carbazole-3-carboxylate | Drug Info | [5] | |||
| 35 | Methyl 9H-carbazole-2-carboxylate | Drug Info | [5] | |||
| 36 | Methyl[4'-(trifluoromethyl)-4-biphenylyl]amine | Drug Info | [6] | |||
| 37 | N-(4'-bromo-3,3'-difluoro-4-biphenylyl)urea | Drug Info | [6] | |||
| 38 | N-(4'-chloro-4-biphenylyl)methanesulfonamide | Drug Info | [6] | |||
| 39 | N-(4'-isopropyl-4-biphenylyl)urea | Drug Info | [6] | |||
| 40 | N-(4'-methyl-4-biphenylyl)urea | Drug Info | [6] | |||
| 41 | N-(4'-t-butyl-4-biphenylyl)urea | Drug Info | [6] | |||
| 42 | N-[3'-(trifluoromethyl)-4-biphenylyl]urea | Drug Info | [6] | |||
| 43 | N-[4'-(ethylsulfonyl)-3-fluoro-4-biphenylyl]urea | Drug Info | [6] | |||
| 44 | N-[4'-(trifluoromethyl)-4-biphenylyl]sulfamide | Drug Info | [6] | |||
| 45 | N-[4'-(trifluoromethyl)-4-biphenylyl]thiourea | Drug Info | [6] | |||
| 46 | N-[4'-(trifluoromethyl)-4-biphenylyl]urea | Drug Info | [6] | |||
| 47 | N-[4-(1,3-benzodioxol-5-yl)phenyl]sulfamide | Drug Info | [6] | |||
| 48 | N-{4'-[(trifluoromethyl)sulfonyl]-4-biphenyl}urea | Drug Info | [6] | |||
| 49 | N-{4'-[(trifluoromethyl)thio]-4-biphenyl}urea | Drug Info | [6] | |||
| 50 | SB-731489 | Drug Info | [6] | |||
| Cell-based Target Expression Variations | Top | |||||
|---|---|---|---|---|---|---|
| Cell-based Target Expression Variations | ||||||
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
|
|
||
| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
|
|
||
| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
|
|
||
| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | MHC class II antigen presentation | |||||
| 2 | Kinesins | |||||
| WikiPathways | [+] 2 WikiPathways | + | ||||
| 1 | MHC class II antigen presentation | |||||
| 2 | Kinesins | |||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Clinical pipeline report, company report or official report of Alnylam Pharmaceuticals, Inc (2011). | |||||
| REF 2 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027260) | |||||
| REF 3 | The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1491-5. | |||||
| REF 4 | Structural basis for inhibition of Eg5 by dihydropyrimidines: stereoselectivity of antimitotic inhibitors enastron, dimethylenastron and fluorastrol. J Med Chem. 2010 Aug 12;53(15):5676-83. | |||||
| REF 5 | Kinesin spindle protein (KSP) inhibitors with 2,3-fused indole scaffolds. J Med Chem. 2010 Jul 8;53(13):5054-8. | |||||
| REF 6 | Novel ATP-competitive kinesin spindle protein inhibitors. J Med Chem. 2007 Oct 4;50(20):4939-52. | |||||
| REF 7 | Inhibition of kinesin motor proteins by adociasulfate-2. J Med Chem. 2006 Aug 10;49(16):4857-60. | |||||
| REF 8 | US patent application no. 7,407,943, Antisense modulation of apolipoprotein B expression. | |||||
| REF 9 | US patent application no. 7,163,927, Antisense modulation of kinesin-like 1 expression. | |||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.