Target Information
| Target General Information | Top | |||||
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| Target ID |
T16596
(Former ID: TTDI02151)
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| Target Name |
PIM-3 protein kinase (PIM3)
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| Synonyms |
Serine/threonine-protein kinase pim-3
Click to Show/Hide
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| Gene Name |
PIM3
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| Target Type |
Patented-recorded target
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[1] | ||||
| Function |
May contribute to tumorigenesis through: the delivery of survival signaling through phosphorylation of BAD which induces release of the anti-apoptotic protein Bcl-X(L), the regulation of cell cycle progression, protein synthesis and by regulation of MYC transcriptional activity. Additionally to this role on tumorigenesis, can also negatively regulate insulin secretion by inhibiting the activation of MAPK1/3 (ERK1/2), through SOCS6. Involved also in the control of energy metabolism and regulation of AMPK activity in modulating MYC and PPARGC1A protein levels and cell growth. Proto-oncogene with serine/threonine kinase activity that can prevent apoptosis, promote cell survival and protein translation.
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| BioChemical Class |
Kinase
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| UniProt ID | ||||||
| EC Number |
EC 2.7.11.1
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| Sequence |
MLLSKFGSLAHLCGPGGVDHLPVKILQPAKADKESFEKAYQVGAVLGSGGFGTVYAGSRI
ADGLPVAVKHVVKERVTEWGSLGGATVPLEVVLLRKVGAAGGARGVIRLLDWFERPDGFL LVLERPEPAQDLFDFITERGALDEPLARRFFAQVLAAVRHCHSCGVVHRDIKDENLLVDL RSGELKLIDFGSGALLKDTVYTDFDGTRVYSPPEWIRYHRYHGRSATVWSLGVLLYDMVC GDIPFEQDEEILRGRLLFRRRVSPECQQLIRWCLSLRPSERPSLDQIAAHPWMLGADGGV PESCDLRLCTLDPDDVASTTSSSESL Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| HIT2.0 ID | T07F6I | |||||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Similarity Proteins
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| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "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 Regulators | Top | |||||
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| Target-regulating microRNAs | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| References | Top | |||||
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| REF 1 | 7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: a novel class of Pim kinase inhibitors with potent cell antiproliferative activity. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6687-92. | |||||
| REF 2 | Azole compounds as PIM inhibitors. US9321756. | |||||
| REF 3 | Kinase inhibitors and methods of their use. US8592455. | |||||
| REF 4 | Pyrrolo[2,3-a] carbazoles and use thereof as PIM kinase inhibitors. US8481586. | |||||
| REF 5 | Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use. US9573943. | |||||
| REF 6 | Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use. US8669361. | |||||
| REF 7 | Heterocyclic kinase inhibitors. US8759338. | |||||
| REF 8 | PIM kinase inhibitors and methods of their use. US8829193. | |||||
| REF 9 | Substituted pyrido[2,3-d]pyrimidin-7(8H)-ones and therapeutic uses thereof. US8889696. | |||||
| REF 10 | Ring-substituted N-pyridinyl amides as kinase inhibitors. US8987457. | |||||
| REF 11 | 5-azaindazole compounds and methods of use. US9434725. | |||||
| REF 12 | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors. US9580418. | |||||
| REF 13 | Tricyclic compounds for use as kinase inhibitors. US9682991. | |||||
| REF 14 | 7,8-dichloro-1-oxo-beta-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes. J Med Chem. 2012 Jan 12;55(1):403-13. | |||||
| REF 15 | Structure and Property Based Design of Pyrazolo[1,5-a]pyrimidine Inhibitors of CK2 Kinase with Activity in Vivo. ACS Med Chem Lett. 2013 Jul 3;4(8):800-5. | |||||
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