Target Information

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Target General Information
Drugs and Modes of Action
Drug Binding Sites of Target
Different Human System Profiles of Target
Target Affiliated Biological Pathways
References
Drug Binding Sites of Target  Top
Ligand Name: Ciprofloxacin Ligand Info
Structure Description Identification of small molecule inhibitors selective for apo(a) kringles KIV-7, KIV-10 and KV. PDB:4BVV
Method X-ray diffraction Resolution 1.80 Å Mutation No [5]
PDB Sequence
DCMFGNGKGY
9
RGKKATTVTG
19
TPCQEWAAQE
29
PHRHSTFIPG
39
TNKWAGLEKN
49

YCRNPDGDIN
59
GPWCYTMNPR
69
KLFDYCDIPL
79
C
Residue
Distance (Å)
ARG32
4.736
HIS33
3.701
SER34
3.471
THR35
3.263
PHE36
4.022
ASP55
2.833
Residue
Distance (Å)
ASP57
2.909
TRP62
3.370
TYR64
3.034
LEU71
3.694
PHE72
3.335
TYR74
4.544
Ligand Name: Aminocaproic acid Ligand Info
Structure Description RECOMBINANT KRINGLE IV-10/M66 VARIANT OF HUMAN APOLIPOPROTEIN(A) PDB:3KIV
Method X-ray diffraction Resolution 1.80 Å Mutation Yes [6]
PDB Sequence
QCYHGNGQSY
9
RGTFSTTVTG
19
RTCQSWSSMT
29
PHRHQRTPEN
40
YPNDGLTMNY
50

CRNPDADTGP
61
WCFTTDPSIR
71
WEYCNLTRC
Residue
Distance (Å)
HIS33
4.441
GLN34
4.667
ARG35
2.583
ASP55
2.749
ASP57
2.868
Residue
Distance (Å)
TRP62
3.446
PHE64
3.501
ARG71
2.820
TRP72
3.269
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 3.28E-06
Closeness centrality 1.78E-01 Radiality 1.29E+01 Clustering coefficient 6.00E-01
Neighborhood connectivity 1.60E+01 Topological coefficient 3.48E-01 Eccentricity 11
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