Target Information
| Target General Information | Top | |||||
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| Target ID |
T63851
(Former ID: TTDI03147)
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| Target Name |
Cyclin-dependent kinase-like 1 (CDKL1)
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| Synonyms |
Serine/threonine-protein kinase KKIALRE; Protein kinase p42 KKIALRE
Click to Show/Hide
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| Gene Name |
CDKL1
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| Target Type |
Literature-reported target
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[1] | ||||
| Function |
Ciliary transition zone, extracellular exosome, intracellular membrane-bounded organelle, nucleoplasm, nucleus, cyclin-dependent protein serine/threonine kinase activity, protein phosphorylation, regulation of cilium assembly.
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| BioChemical Class |
Kinase
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| UniProt ID | ||||||
| EC Number |
EC 2.7.11.22
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| Sequence |
MMEKYEKIGKIGEGSYGVVFKCRNRDTGQIVAIKKFLESEDDPVIKKIALREIRMLKQLK
HPNLVNLLEVFRRKRRLHLVFEYCDHTVLHELDRYQRGVPEHLVKSITWQTLQAVNFCHK HNCIHRDVKPENILITKHSVIKLCDFGFARLLAGPSDYYTDYVATRWYRSPELLVGDTQY GPPVDVWAIGCVFAELLSGVPLWPGKSDVDQLYLIRKTLGDLIPRHQQVFSTNQYFSGVK IPDPEDMEPLELKFPNISYPALGLLKGCLHMDPTQRLTCEQLLHHPYFENIREIEDLAKE HNKPTRKTLRKSRKHHCFTETSKLQYLPQLTGSSILPALDNKKYYCDTKKLNYRFPNI Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| 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: N-(5-{[(2s)-4-Amino-2-(3-Chlorophenyl)butanoyl]amino}-1h-Indazol-3-Yl)benzamide | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF THE HUMAN CDKL1 KINASE DOMAIN | PDB:4AGU | ||||
| Method | X-ray diffraction | Resolution | 2.40 Å | Mutation | Yes | [2] |
| PDB Sequence |
EKYEKIGKIG
11 EGSYGVVFKC21 RNRDTGQIVA31 IKKFLESEDP42 VIKKIALREI52 RMLKQLKHPN 62 LVNLLEVFRR72 KRRLHLVFEY82 CDHTVLHELD92 RYQRGVPEHL102 VKSITWQTLQ 112 AVNFCHKHNC122 IHRDVKPENI132 LITKHSVIKL142 CDFGFARLLT164 RWYRSPELLV 174 GDTQYGPPVD184 VWAIGCVFAE194 LLSGVPLWPG204 KSDVDQLYLI214 RKTLGDLIPR 224 HQQVFSTNQY234 FSGVKIPDPE244 DMEPLELKFP254 NISYPALGLL264 KGCLHMDPTE 274 RLTCEQLLHH284 PYFENIR
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ILE10
3.522
GLY11
3.438
GLU12
3.720
GLY13
3.191
TYR15
3.937
GLY16
3.499
VAL17
4.135
VAL18
3.666
ALA31
3.399
LYS33
3.879
VAL64
4.015
PHE80
3.709
GLU81
2.796
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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).
Human Similarity Proteins
Human Tissue Distribution
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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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| References | Top | |||||
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| REF 1 | Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6486-9. | |||||
| REF 2 | CDKL Family Kinases Have Evolved Distinct Structural Features and Ciliary Function. Cell Rep. 2018 Jan 23;22(4):885-894. | |||||
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