Target Information

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Target General Information
Drug Binding Sites of Target
Different Human System Profiles of Target
Target Regulators
References
Drug Binding Sites of Target  Top
Ligand Name: Phosphonotyrosine Ligand Info
Structure Description Human raf kinase inhibitor protein (rkip) in complex with o-phosphotyrosine PDB:2QYQ
Method X-ray diffraction Resolution 1.95 Å Mutation No [2]
PDB Sequence
MPVDLSKWSG
10
PLSLQEVDEQ
20
PQHPLHVTYA
30
GAAVDELGKV
40
LTPTQVKNRP
50

TSISWDGLDS
60
GKLYTLVLTD
70
PDAPSRKDPK
80
YREWHHFLVV
90
NMKGNDISSG
100

TVLSDYVGSG
110
PPKGTGLHRY
120
VWLVYEQDRP
130
LKCDEPILSN
140
RSGDHRGKFK
150

VASFRKKYEL
160
RAPVAGTCYQ
170
AEWDDYVPKL
180
YEQLSG
Residue
Distance (Å)
ASP70
2.498
ALA73
4.446
TRP84
3.145
HIS86
2.641
GLY108
4.628
SER109
3.649
GLY110
2.710
Residue
Distance (Å)
PRO111
3.338
PRO112
3.888
HIS118
3.355
TYR120
2.525
TYR181
3.563
LEU184
3.661
Click to View More Binding Site Information of This Target with Different Ligands
Different Human System Profiles of Target  Top
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
There is no similarity protein (E value < 0.005) for this target
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.
Degree 6 Degree centrality 6.45E-04 Betweenness centrality 6.79E-05
Closeness centrality 2.20E-01 Radiality 1.39E+01 Clustering coefficient 2.00E-01
Neighborhood connectivity 3.48E+01 Topological coefficient 2.12E-01 Eccentricity 12
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