Target Information
Target General Information | Top | |||||
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Target ID |
T03581
(Former ID: TTDI03539)
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Target Name |
NDR1 protein kinase (STK38)
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Synonyms |
Serine/threonine-protein kinase 38; Nuclear Dbf2-related kinase 1; NDR1
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Gene Name |
STK38
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Target Type |
Literature-reported target
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[1] | ||||
Function |
Converts MAP3K2 from its phosphorylated form to its non-phosphorylated form and inhibits autophosphorylation of MAP3K2. Negative regulator of MAP3K1/2 signaling.
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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 |
MAMTGSTPCSSMSNHTKERVTMTKVTLENFYSNLIAQHEEREMRQKKLEKVMEEEGLKDE
EKRLRRSAHARKETEFLRLKRTRLGLEDFESLKVIGRGAFGEVRLVQKKDTGHVYAMKIL RKADMLEKEQVGHIRAERDILVEADSLWVVKMFYSFQDKLNLYLIMEFLPGGDMMTLLMK KDTLTEEETQFYIAETVLAIDSIHQLGFIHRDIKPDNLLLDSKGHVKLSDFGLCTGLKKA HRTEFYRNLNHSLPSDFTFQNMNSKRKAETWKRNRRQLAFSTVGTPDYIAPEVFMQTGYN KLCDWWSLGVIMYEMLIGYPPFCSETPQETYKKVMNWKETLTFPPEVPISEKAKDLILRF CCEWEHRIGAPGVEEIKSNSFFEGVDWEHIRERPAAISIEIKSIDDTSNFDEFPESDILK PTVATSNHPETDYKNKDWVFINYTYKRFEGLTARGAIPSYMKAAK 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: AMP-PNP | Ligand Info | |||||
Structure Description | X-ray crystal structure of NDR1 kinase domain | PDB:6BXI | ||||
Method | X-ray diffraction | Resolution | 2.20 Å | Mutation | No | [2] |
PDB Sequence |
TRLGLEDFES
91 LKVIGRGAFG101 EVRLVQKKDT111 GHVYAMKILR121 KADMLEKEQV131 GHIRAERDIL 141 VEADSLWVVK151 MFYSFQDKLN161 LYLIMEFLPG171 GDMMTLLMKK181 DTLTEEETQF 191 YIAETVLAID201 SIHQLGFIHR211 DIKPDNLLLD221 SKGHVKLSDF231 GLCTGLKKAH 241 RTEFYRNLNH251 SLPSDFTFQN261 MNSKRKAETW271 KRNRRQLAFS281 TVGTPDYIAP 291 EVFMQTGYNK301 LCDWWSLGVI311 MYEMLIGYPP321 FCSETPQETY331 KKVMNWKETL 341 TFPPEVPISE351 KAKDLILRFC361 CEWEHRIGAP371 GVEEIKSNSF381 FEGVDWEHIR 391 ERPAAISIEI401 KSIDDTSNFD411 EFP
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ILE95
3.752
GLY96
3.620
ARG97
4.416
GLY98
3.148
ALA99
4.314
PHE100
4.650
GLY101
4.606
VAL103
3.367
ALA116
3.684
LYS118
3.055
LEU120
4.349
VAL150
3.667
MET166
3.528
GLU167
2.907
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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).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Tissue Distribution
Biological Network Descriptors
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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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Degree | 2 | Degree centrality | 2.15E-04 | Betweenness centrality | 6.75E-05 |
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Closeness centrality | 1.62E-01 | Radiality | 1.24E+01 | Clustering coefficient | 0.00E+00 |
Neighborhood connectivity | 6.00E+00 | Topological coefficient | 5.56E-01 | Eccentricity | 14 |
Download | Click to Download the Full PPI Network of This Target | ||||
Target Regulators | Top | |||||
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Target-interacting Proteins |
References | Top | |||||
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REF 1 | Tetrahydroisoquinoline derivatives as highly selective and potent Rho kinase inhibitors. J Med Chem. 2010 Aug 12;53(15):5727-37. | |||||
REF 2 | Structural Basis for Auto-Inhibition of the NDR1 Kinase Domain by an Atypically Long Activation Segment. Structure. 2018 Aug 7;26(8):1101-1115.e6. |
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