Target Information

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Target General Information
Drug Binding Sites of Target
Different Human System Profiles of Target
Chemical Structure based Activity Landscape of Target
Target Poor or Non Binders
Target Regulators
References
Drug Binding Sites of Target  Top
Ligand Name: GSK2801 Ligand Info
Structure Description BAZ2A bromodomain in complex with GSK2801 chemical probe PDB:7BL9
Method X-ray diffraction Resolution 1.30 Å Mutation No [3]
PDB Sequence
SMHSDLTFCE
1803
IILMEMESHD
1813
AAWPFLEPVN
1823
PRLVSGYRRI
1833
IKNPMDFSTM
1843

RERLLRGGYT
1853
SSEEFAADAL
1863
LVFDNCQTFN
1873
EDDSEVGKAG
1883
HIMRRFFESR
1893

WEEFY
Residue
Distance (Å)
TRP1816
2.328
PRO1817
2.387
PHE1818
2.541
LEU1819
3.857
GLU1820
2.423
PRO1821
3.008
VAL1822
2.545
ASN1823
3.938
Residue
Distance (Å)
LEU1826
2.520
VAL1827
2.085
TYR1830
3.255
VAL1865
4.955
CYS1869
3.470
PHE1872
2.385
ASN1873
2.114
VAL1879
3.007
Ligand Name: BAZ2-ICR Ligand Info
Structure Description BAZ2A bromodomain in complex with the chemical probe BAZ2-ICR PDB:7BL8
Method X-ray diffraction Resolution 2.50 Å Mutation No [4]
PDB Sequence
MHSDLTFCEI
1804
ILMEMESHDA
1814
AWPFLEPVNP
1824
RLVSGYRRII
1834
KNPMDFSTMR
1844

ERLLRGGYTS
1854
SEEFAADALL
1864
VFDNCQTFNE
1874
DDSEVGKAGH
1884
IMRRFFESRW
1894

EEFY
Residue
Distance (Å)
TRP1816
3.263
PRO1817
3.284
PHE1818
3.487
LEU1819
3.057
GLU1820
2.870
PRO1821
3.384
VAL1822
3.402
ASN1823
2.825
Residue
Distance (Å)
LEU1826
3.847
VAL1827
3.595
TYR1830
4.214
CYS1869
4.814
PHE1872
4.564
ASN1873
3.435
VAL1879
3.614
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
Protein Name Pfam ID Percentage of Identity (%) E value
Protein Jade-3 (JADE3)
PF10513 ; 
PF13831 ; 
PF13832
More >>
 36.765 (25/68) 2.00E-03
E3 ubiquitin-protein ligase Jade-2 (JADE2)
PF10513 ; 
PF13831 ; 
PF13832
More >>
 29.762 (25/84) 5.00E-03
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 2 Degree centrality 2.15E-04 Betweenness centrality 2.02E-04
Closeness centrality 1.80E-01 Radiality 1.30E+01 Clustering coefficient 0.00E+00
Neighborhood connectivity 8.50E+00 Topological coefficient 5.00E-01 Eccentricity 13
Download Click to Download the Full PPI Network of This Target

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