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
Chemical Structure based Activity Landscape of Target
Target Poor or Non Binders
Target Affiliated Biological Pathways
References
Drug Binding Sites of Target  Top
Ligand Name: Nalpha-[(4-Methylpiperazin-1-Yl)carbonyl]-N-[(3s)-1-Phenyl-5-(Phenylsulfonyl)pentan-3-Yl]-L-Phenylalaninamide Ligand Info
Structure Description CRYSTAL STRUCTURE OF HUMAN CATHEPSIN V COMPLEXED WITH AN IRREVERSIBLE VINYL SULFONE INHIBITOR PDB:1FH0
Method X-ray diffraction Resolution 1.60 Å Mutation Yes [3]
PDB Sequence
LPKSVDWRKK
10
GYVTPVKNQK
20
QCGSCWAFSA
30
TGALEGQMFR
40
KTGKLVSLSE
50

QNLVDCSRPQ
60
GNQGCNGGFM
70
ARAFQYVKEN
80
GGLDSEESYP
90
YVAVDEICKY
100

RPENSVAQDT
110
GFTVVAPGKE
119
KALMKAVATV
129
GPISVAMDAG
139
HSSFQFYKSG
149

IYFEPDCSSK
159
NLDHGVLVVG
169
YGFEGANSDN
179
SKYWLVKNSW
189
GPEWGSNGYV
199

KIAKDKNNHC
209
GIATAASYPN
219
V
Residue
Distance (Å)
GLN19
2.887
CYS22
4.618
GLY23
3.500
SER24
4.765
CYS25
1.793
TRP26
3.148
GLY61
3.738
GLN63
3.596
CYS65
3.457
ASN66
3.417
GLY67
3.126
GLY68
2.896
Residue
Distance (Å)
PHE69
3.350
MET70
4.009
ALA135
3.416
ALA138
3.839
GLY139
4.261
LEU161
3.795
ASP162
3.156
HIS163
3.132
GLY164
4.073
TRP189
2.966
ALA214
4.599
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).
Human Pathway Affiliation of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes (Pharmacol Rev, 58: 259-279, 2006).
Human Similarity Proteins
Human Tissue Distribution
Human Pathway Affiliation
Protein Name Pfam ID Percentage of Identity (%) E value
Putative inactive cathepsin L-like protein CTSL3P (CTSL3P) 61.818 (68/110) 1.40E-36
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.
 Download Picture         KEGG Link      
 Download Picture         KEGG Link      
KEGG Pathway Pathway ID Affiliated Target Pathway Map
Lysosome hsa04142 Affiliated Target
  Class: Cellular Processes => Transport and catabolism Pathway Hierarchy
Apoptosis hsa04210 Affiliated Target
  Class: Cellular Processes => Cell growth and death Pathway Hierarchy

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