Target Information
| Target General Information | Top | |||||
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| Target ID |
T90961
(Former ID: TTDI03054)
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| Target Name |
BMP-2-inducible protein kinase (BMP2K)
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| Synonyms |
HRIHFB2017; BIKe
Click to Show/Hide
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| Gene Name |
BMP2K
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| Target Type |
Literature-reported target
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[1] | ||||
| Function |
May be involved in osteoblast differentiation.
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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 |
MKKFSRMPKSEGGSGGGAAGGGAGGAGAGAGCGSGGSSVGVRVFAVGRHQVTLEESLAEG
GFSTVFLVRTHGGIRCALKRMYVNNMPDLNVCKREITIMKELSGHKNIVGYLDCAVNSIS DNVWEVLILMEYCRAGQVVNQMNKKLQTGFTEPEVLQIFCDTCEAVARLHQCKTPIIHRD LKVENILLNDGGNYVLCDFGSATNKFLNPQKDGVNVVEEEIKKYTTLSYRAPEMINLYGG KPITTKADIWALGCLLYKLCFFTLPFGESQVAICDGNFTIPDNSRYSRNIHCLIRFMLEP DPEHRPDIFQVSYFAFKFAKKDCPVSNINNSSIPSALPEPMTASEAAARKSQIKARITDT IGPTETSIAPRQRPKANSATTATPSVLTIQSSATPVKVLAPGEFGNHRPKGALRPGNGPE ILLGQGPPQQPPQQHRVLQQLQQGDWRLQQLHLQHRHPHQQQQQQQQQQQQQQQQQQQQQ QQQQQQHHHHHHHHLLQDAYMQQYQHATQQQQMLQQQFLMHSVYQPQPSASQYPTMMPQY QQAFFQQQMLAQHQPSQQQASPEYLTSPQEFSPALVSYTSSLPAQVGTIMDSSYSANRSV ADKEAIANFTNQKNISNPPDMSGWNPFGEDNFSKLTEEELLDREFDLLRSNRLEERASSD KNVDSLSAPHNHPPEDPFGSVPFISHSGSPEKKAEHSSINQENGTANPIKNGKTSPASKD QRTGKKTSVQGQVQKGNDESESDFESDPPSPKSSEEEEQDDEEVLQGEQGDFNDDDTEPE NLGHRPLLMDSEDEEEEEKHSSDSDYEQAKAKYSDMSSVYRDRSGSGPTQDLNTILLTSA QLSSDVAVETPKQEFDVFGAVPFFAVRAQQPQQEKNEKNLPQHRFPAAGLEQEEFDVFTK APFSKKVNVQECHAVGPEAHTIPGYPKSVDVFGSTPFQPFLTSTSKSESNEDLFGLVPFD EITGSQQQKVKQRSLQKLSSRQRRTKQDMSKSNGKRHHGTPTSTKKTLKPTYRTPERARR HKKVGRRDSQSSNEFLTISDSKENISVALTDGKDRGNVLQPEESLLDPFGAKPFHSPDLS WHPPHQGLSDIRADHNTVLPGRPRQNSLHGSFHSADVLKMDDFGAVPFTELVVQSITPHQ SQQSQPVELDPFGAAPFPSKQ Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: Baricitinib | Ligand Info | |||||
| Structure Description | Crystal Structure of BMP-2-inducible kinase in complex with baricitinib | PDB:4W9X | ||||
| Method | X-ray diffraction | Resolution | 2.14 Å | Mutation | Yes | [2] |
| PDB Sequence |
VGVRVFAVGR
48 HQVTLEESLA58 EGGFSTVFLV68 RTHGGIRCAL78 KRMYVNNMPD88 LNVCKREITI 98 MKELSGHKNI108 VGYLDCAVNS118 ISWEVLILME131 YCRAGQVVNQ141 MNKKQTGFTE 152 PEVLQIFCDT162 CEAVARLHQC172 KTPIIHRDLK182 VENILLNDGG192 NYVLCDFGSA 202 TNKFLNPQKD212 GVNVVEEEIK222 KYTTLSYRAP232 EMINLYGGKP242 ITTKADIWAL 252 GCLLYKLCFF262 TLPFGESQVA272 ICDGNFTIPD282 NSRYSRNIHC292 LIRFMLEPDP 302 EHRPDIFQVS312 YFAFKFAAAD322 CPVSNINNSS332 IPSALPEPMT342 |
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LEU57
3.941
ALA58
3.400
GLU59
3.531
GLY60
3.367
SER63
3.292
THR64
3.936
VAL65
4.068
ALA77
3.457
LYS79
4.069
VAL109
3.686
MET130
3.659
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| Ligand Name: AZD7762 | Ligand Info | |||||
| Structure Description | Crystal Structure of BMP-2-inducible kinase in complex with small molecule AZD-7762 | PDB:4W9W | ||||
| Method | X-ray diffraction | Resolution | 1.72 Å | Mutation | Yes | [2] |
| PDB Sequence |
VGVRVFAVGR
48 HQVTLEESLA58 EGGFSTVFLV68 RTHGGIRCAL78 KRMYVNNMPD88 LNVCKREITI 98 MKELSGHKNI108 VGYLDCAVNS118 ISDNVWEVLI128 LMEYCRAGQV138 VNQMNKKLQT 148 GFTEPEVLQI158 FCDTCEAVAR168 LHQCKTPIIH178 RDLKVENILL188 NDGGNYVLCD 198 FGSATNKFLN208 PQKDGVNVVE218 EEIKKYTTLS228 YRAPEMINLY238 GGKPITTKAD 248 IWALGCLLYK258 LCFFTLPFGE268 SQVAICDGNF278 TIPDNSRYSR288 NIHCLIRFML 298 EPDPEHRPDI308 FQVSYFAFKF318 AAADCPVSNI328 NNSSIPSALP338 EPMTAS |
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LEU57
3.926
ALA58
3.753
VAL65
3.994
ALA77
3.409
VAL109
4.037
MET130
4.375
GLU131
2.890
TYR132
3.502
CYS133
2.712
ARG134
3.229
ALA135
4.690
GLY136
3.515
GLN137
3.706
ASN140
4.277
GLU184
3.499
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| 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 Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Similarity Proteins
Human Tissue Distribution
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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| Chemical Structure based Activity Landscape of Target | Top |
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| Target Regulators | Top | |||||
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| Target-regulating microRNAs | ||||||
| References | Top | |||||
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| REF 1 | Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase. Bioorg Med Chem. 2010 Jun 15;18(12):4351-62. | |||||
| REF 2 | Family-wide Structural Analysis of Human Numb-Associated Protein Kinases. Structure. 2016 Mar 1;24(3):401-11. | |||||
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