Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T13075 | Target Info | |||
| Target Name | Casein kinase I alpha (CSNK1A1) | ||||
| Synonyms | Casein kinase I isoform alpha; CKI-alpha; CK1 | ||||
| Target Type | Clinical trial Target | ||||
| Gene Name | CSNK1A1 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: S-Lenalidomide | Ligand Info | |||||
| Structure Description | Structural basis of Lenalidomide induced CK1a degradation by the crl4crbn ubiquitin ligase | PDB:5FQD | ||||
| Method | X-ray diffraction | Resolution | 2.45 Å | Mutation | No | [1] |
| PDB Sequence |
EFIVGGKYKL
19 VRKIGSGSFG29 DIYLAINITN39 GEEVAVKLES49 QKARHPQLLY59 ESKLYKILQG 69 GVGIPHIRWY79 GQEKDYNVLV89 MDLLGPSLED99 LFNFCSRRFT109 MKTVLMLADQ 119 MISRIEYVHT129 KNFIHRDIKP139 DNFLMGIGRH149 CNKLFLIDFG159 LAKKYRDNRT 169 RQHIPYREDK179 NLTGTARYAS189 INAHLGIEQS199 RRDDMESLGY209 VLMYFNRTSL 219 PWQGLKAATK229 KQKYEKISEK239 KMSTPVEVLC249 KGFPAEFAMY259 LNYCRGLRFE 269 EAPDYMYLRQ279 LFRILFRTLN289 HQYDYTFDWT299 MLKQ
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| Ligand Name: Casein Kinase inhibitor A86 | Ligand Info | |||||
| Structure Description | Crystal structure of Human CSNK1A1 with A86 | PDB:6GZD | ||||
| Method | X-ray diffraction | Resolution | 2.28 Å | Mutation | No | [2] |
| PDB Sequence |
AEFIVGGKYK
18 LGRKIGSGSF28 GDIYLATNIT38 NGEEVAVKLE48 SQKARHPQLH58 YESKLYKILQ 68 GGVGIPHIRW78 YGQEKDYNVL88 VMDLLGPSLE98 DLFNFCSRRF108 TMKTVLMLAD 118 QMISRIEYVH128 TKNFIHRDIK138 PDNFLMGIGR148 HCNKLFLIDF158 GLAKKYRDNR 168 TRQHIPYRED178 KNLTGTARYA188 SINAHLGIEQ198 SRRDDMESLG208 YVLMYFNRTS 218 LPWQGLKAAT228 KKQKYEKISE238 KKMSTPVEVL248 CKGFPAEFAM258 YLNYCRGLRF 268 EEAPDYMYLR278 QLFRILFRTL288 NHQYDYTFDW298 TMLKQKA
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| Ligand Name: Tris(2-carboxyethyl)phosphine | Ligand Info | |||||
| Structure Description | Crystal structure of Human CSNK1A1 with A86 | PDB:6GZD | ||||
| Method | X-ray diffraction | Resolution | 2.28 Å | Mutation | No | [2] |
| PDB Sequence |
AEFIVGGKYK
18 LGRKIGSGSF28 GDIYLATNIT38 NGEEVAVKLE48 SQKARHPQLH58 YESKLYKILQ 68 GGVGIPHIRW78 YGQEKDYNVL88 VMDLLGPSLE98 DLFNFCSRRF108 TMKTVLMLAD 118 QMISRIEYVH128 TKNFIHRDIK138 PDNFLMGIGR148 HCNKLFLIDF158 GLAKKYRDNR 168 TRQHIPYRED178 KNLTGTARYA188 SINAHLGIEQ198 SRRDDMESLG208 YVLMYFNRTS 218 LPWQGLKAAT228 KKQKYEKISE238 KKMSTPVEVL248 CKGFPAEFAM258 YLNYCRGLRF 268 EEAPDYMYLR278 QLFRILFRTL288 NHQYDYTFDW298 TMLKQKA
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Click to Show 3D Structure of This Binding Site
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Structural basis of lenalidomide-induced CK1Alpha degradation by the CRL4(CRBN) ubiquitin ligase. Nature. 2016 Apr 7;532(7597):127-30. | ||||
| REF 2 | Small Molecules Co-targeting CKIAlpha and the Transcriptional Kinases CDK7/9 Control AML in Preclinical Models. Cell. 2018 Sep 20;175(1):171-185.e25. | ||||
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