General Information of the Protein
Protein ID
PT01351
Protein Name
Casein kinase I isoform delta
Secondarily
Protein Name
Tau-protein kinase CSNK1D
Gene Name
CSNK1D
Secondarily
Gene Name
HCKID
Sequence
MELRVGNRYRLGRKIGSGSFGDIYLGTDIAAGEEVAIKLECVKTKHPQLHIESKIYKMMQGGVGIPTIRWCGAEGDYNVMVMELLGPSLEDLFNFCSRKFSLKTVLLLADQMISRIEYIHSKNFIHRDVKPDNFLMGLGKKGNLVYIIDFGLAKKYRDARTHQHIPYRENKNLTGTARYASINTHLGIEQSRRDDLESLGYVLMYFNLGSLPWQGLKAATKRQKYERISEKKMSTPIEVLCKGYPSEFATYLNFCRSLRFDDKPDYSYLRQLFRNLFHRQGFSYDYVFDWNMLKFGASRAADDAERERRDREERLRHSRNPATRGLPSTASGRLRGTQEVAPPTPLTPTSHTANTSPRPVSGMERERKVSMRLHRGAPVNISSSDLTGRQDTSRMSTSQIPGRVASSGLQSVVHR
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
CK1 protein kinase group
>
CK1 protein kinase CK1 family
Function
Essential serine/threonine-protein kinase that regulates diverse cellular growth and survival processes including Wnt signaling, DNA repair and circadian rhythms. It can phosphorylate a large number of proteins. Casein kinases are operationally defined by their preferential utilization of acidic proteins such as caseins as substrates. Phosphorylates connexin-43/GJA1, MAP1A, SNAPIN, MAPT/TAU, TOP2A, DCK, HIF1A, EIF6, p53/TP53, DVL2, DVL3, ESR1, AIB1/NCOA3, DNMT1, PKD2, YAP1, PER1 and PER2. Central component of the circadian clock. In balance with PP1, determines the circadian period length through the regulation of the speed and rhythmicity of PER1 and PER2 phosphorylation. Controls PER1 and PER2 nuclear transport and degradation. YAP1 phosphorylation promotes its SCF(beta-TRCP) E3 ubiquitin ligase-mediated ubiquitination and subsequent degradation. DNMT1 phosphorylation reduces its DNA-binding activity. Phosphorylation of ESR1 and AIB1/NCOA3 stimulates their activity and coactivation. Phosphorylation of DVL2 and DVL3 regulates WNT3A signaling pathway that controls neurite outgrowth. Phosphorylates NEDD9/HEF1 (By similarity). EIF6 phosphorylation promotes its nuclear export. Triggers down-regulation of dopamine receptors in the forebrain. Activates DCK in vitro by phosphorylation. TOP2A phosphorylation favors DNA cleavable complex formation. May regulate the formation of the mitotic spindle apparatus in extravillous trophoblast. Modulates connexin-43/GJA1 gap junction assembly by phosphorylation. Probably involved in lymphocyte physiology. Regulates fast synaptic transmission mediated by glutamate.
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Uniprot ID
Primary ID:
P48730

Secondarily ID:
A2I2P2
Q96KZ6
Q9BTN5
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Ensembl ID
ENSG00000141551
HGNC ID
HGNC:2452
Subcellular Location
Cytoplasm
Nucleus
Cytoplasm
Cytoskeleton
Microtubule organizing center
Centrosome
Cytoplasm
Perinuclear region
Cell membrane
Cytoplasm
Cytoskeleton
Spindle
Golgi apparatus
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000053 , COS-7
Compound ID Compound Name Compound Formula
CP0087982
9-[3-(4-fluorophenyl)-1-methylpyrazol-4-yl]-2,3,4,5-tetrahydropyrido[2,3-f][1,4]oxazepine
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C18H17FN4O
 1
1
IC50 = 42.1 nM
   TI
   LI
   LO
   TS
CP0087984
1-[4-[3-(4-fluorophenyl)-1-methylpyrazol-4-yl]pyridin-2-yl]-N-methylmethanamine
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C17H17FN4
 1
1
IC50 = 63.8 nM
   TI
   LI
   LO
   TS
CP0070395
4-[3-cyclohexyl-5-(4-fluorophenyl)imidazol-4-yl]pyrimidin-2-amine
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C19H20FN5
 1
1
IC50 = 80.5 nM
   TI
   LI
   LO
   TS
CP0088115
3-[4-[3-(4-fluorophenyl)-1-methylpyrazol-4-yl]pyridin-2-yl]morpholine
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C19H19FN4O
 1
1
IC50 = 90 nM
   TI
   LI
   LO
   TS
CP0233986
[4-[3-(4-fluorophenyl)-1-methylpyrazol-4-yl]pyridin-2-yl]methanol
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C16H14FN3O
 1
1
IC50 = 237 nM
   TI
   LI
   LO
   TS
CP0067567
4-[3-(4-fluorophenyl)-1-methylpyrazol-4-yl]pyridine
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C15H12FN3
 1
1
IC50 = 545 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0087982
9-[3-(4-fluorophenyl)-1-methylpyrazol-4-yl]-2,3,4,5-tetrahydropyrido[2,3-f][1,4]oxazepine
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C18H17FN4O
 1
1 IC50 = 6 nM
CP0088115
3-[4-[3-(4-fluorophenyl)-1-methylpyrazol-4-yl]pyridin-2-yl]morpholine
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C19H19FN4O
 1
1 IC50 = 6.6 nM
CP0070395
4-[3-cyclohexyl-5-(4-fluorophenyl)imidazol-4-yl]pyrimidin-2-amine
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C19H20FN5
 4
1 IC50 = 7.8 nM
2 IC50 = 13 nM
3 IC50 = 32 nM
4 IC50 = 80 nM
CP0087984
1-[4-[3-(4-fluorophenyl)-1-methylpyrazol-4-yl]pyridin-2-yl]-N-methylmethanamine
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C17H17FN4
 1
1 IC50 = 12.9 nM
CP0233986
[4-[3-(4-fluorophenyl)-1-methylpyrazol-4-yl]pyridin-2-yl]methanol
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C16H14FN3O
 1
1 IC50 = 14.2 nM
CP0007305
N-[(4,5-difluoro-1H-benzimidazol-2-yl)methyl]-9-(3-fluorophenyl)-2-morpholin-4-ylpurin-6-amine
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C23H19F3N8O
 1
1 IC50 = 44 nM
CP0067567
4-[3-(4-fluorophenyl)-1-methylpyrazol-4-yl]pyridine
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C15H12FN3
 1
1 IC50 = 48.1 nM
CP0003337
IC261
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C18H17NO4
 2
1 IC50 = 1000 nM
2 IC50 = 2570 nM
Clinical Information about the Protein
Target 1 ( Casein kinase I delta (CSNK1D) )
Target Type Preclinical Target
Disease 2 Target-related Diseases  2
1 Chronic lymphocytic leukaemia [ICD-11: 2A82.0]
2 Pancreatic cancer [ICD-11: 2C10]
Preclinical Drug(s) 3 Preclinical Drugs  3
1 D-4476 Preclinical
Chronic lymphocytic leukaemia
2 IC261 Preclinical
Pancreatic cancer
3 PF-4800567 Preclinical
Chronic lymphocytic leukaemia