Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T07279 | Target Info | |||
| Target Name | Serine/threonine-protein kinase pim-2 (PIM2) | ||||
| Synonyms | Pim-2h; PIM2 | ||||
| Target Type | Clinical trial Target | ||||
| Gene Name | PIM2 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: 2-(2,6-Difluorophenyl)-N-{4-[(3s)-Pyrrolidin-3-Yloxy]pyridin-3-Yl}-1,3-Thiazole-4-Carboxamide | Ligand Info | |||||
| Structure Description | PIM2 kinase in complex with Compound 1s | PDB:4X7Q | ||||
| Method | X-ray diffraction | Resolution | 2.33 Å | Mutation | No | [1] |
| PDB Sequence |
AFEAEYRLGP
36 LLGKGFGTVF47 AGHRLTDRLQ57 VAIKVIPRCP81 LEVALLWKVG91 AGGGHPGVIR 101 LLDWFETFML114 VLERPLPAQD124 LFDYITEKGP134 LGEGPSRCFF144 GQVVAAIQHC 154 HSRGVVHRDI164 KDENILIDLR174 RGCAKLIDFG184 SGALLHDEPY194 TDFDGTRVYS 204 PPEWISRHQY214 HALPATVWSL224 GILLYDMVCG234 DIPFERDQEI244 LEAELHFPAH 254 VSPDCCALIR264 RCLAPKPSSR274 PSLEEILLDP284 WMQ
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| Ligand Name: Ruthenium-pyridocarbazole-1 | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF THE HUMAN PIM2 IN COMPLEX WITH A RUTHENIUM ORGANOMETALLIC LIGAND RU1 | PDB:2IWI | ||||
| Method | X-ray diffraction | Resolution | 2.80 Å | Mutation | No | [2] |
| PDB Sequence |
YRLGPLLGKG
41 GFGTVFAGHR51 LTDRLQVAIK61 VIPRNRVLVT79 CPLEVALLWK89 VGAGGGHPGV 99 IRLLDWFFML114 VLERPLPAQD124 LFDYITEKGP134 LGEGPSRCFF144 GQVVAAIQHC 154 HSRGVVHRDI164 KDENILIDLR174 RGCAKLIDFG184 SGALLHDEPY194 TDFDGTRVYS 204 PPEWISRHQY214 HALPATVWSL224 GILLYDMVCG234 DIPFERDQEI244 LEAELHFPAH 254 VSPDCCALIR264 RCLAPKPSSR274 PSLEEILLDP284 WMQT
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Structure-based design of low-nanomolar PIM kinase inhibitors. Bioorg Med Chem Lett. 2015 Feb 1;25(3):474-80. | ||||
| REF 2 | Crystal structure of the PIM2 kinase in complex with an organoruthenium inhibitor. PLoS One. 2009 Oct 20;4(10):e7112. | ||||
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