General Information of the Protein
Protein ID
PT01421
Protein Name
Casein kinase I isoform gamma-2
Gene Name
CSNK1G2
Secondarily
Gene Name
CK1G2
Sequence
MDFDKKGGKGETEEGRRMSKAGGGRSSHGIRSSGTSSGVLMVGPNFRVGKKIGCGNFGELRLGKNLYTNEYVAIKLEPIKSRAPQLHLEYRFYKQLSATEGVPQVYYFGPCGKYNAMVLELLGPSLEDLFDLCDRTFTLKTVLMIAIQLITRMEYVHTKSLIYRDVKPENFLVGRPGTKRQHAIHIIDFGLAKEYIDPETKKHIPYREHKSLTGTARYMSINTHLGKEQSRRDDLEALGHMFMYFLRGSLPWQGLKADTLKERYQKIGDTKRATPIEVLCENFPEEMATYLRYVRRLDFFEKPDYDYLRKLFTDLFDRSGFVFDYEYDWAGKPLPTPIGTVHTDLPSQPQLRDKTQPHSKNQALNSTNGELNADDPTAGHSNAPITAPAEVEVADETKCCCFFKRRKRKSLQRHK
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
CK1 protein kinase group
>
CK1 protein kinase CK1 family
Function
Serine/threonine-protein kinase. Casein kinases are operationally defined by their preferential utilization of acidic proteins such as caseins as substrates. It can phosphorylate a large number of proteins. Participates in Wnt signaling (By similarity). Phosphorylates COL4A3BP/CERT, MTA1 and SMAD3. SMAD3 phosphorylation promotes its ligand-dependent ubiquitination and subsequent proteasome degradation, thus inhibiting SMAD3-mediated TGF-beta responses. Hyperphosphorylation of the serine-repeat motif of COL4A3BP/CERT leads to its inactivation by dissociation from the Golgi complex, thus down-regulating ER-to-Golgi transport of ceramide and sphingomyelin synthesis. Triggers PER1 proteasomal degradation probably through phosphorylation (PubMed:15077195, PubMed:15917222, PubMed:18794808, PubMed:19005213). Involved in brain development and vesicular trafficking and neurotransmitter releasing from small synaptic vesicles. Regulates fast synaptic transmission mediated by glutamate (By similarity). Involved in regulation of reactive oxygen species (ROS) levels (PubMed:37099597).
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Uniprot ID
Primary ID:
P78368

Secondarily ID:
B5BU42
O00704
Q8WUB1
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Ensembl ID
ENSG00000133275
HGNC ID
HGNC:2455
Subcellular Location
Cytoplasm
Cell cortex
Cytoplasm
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: CL000006 , HEK293
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0138935
 Compound Info 
2-[4-(2-hydroxypropan-2-yl)anilino]-3H-benzimidazole-5-carbonitrile
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C17H16N4O
  1
1
IC50 = 700 nM
 Bioactivity Info 
   TI
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CP0249994
 Compound Info 
2-[4-(2-fluoropyridin-3-yl)anilino]-3H-benzimidazole-5-carbonitrile
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C19H12FN5
  1
1
IC50 = 1170 nM
 Bioactivity Info 
   TI
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CP0356211
 Compound Info 
2-[4-(1-methylpyrazol-4-yl)anilino]-3H-benzimidazole-5-carbonitrile
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C18H14N6
  1
1
IC50 = 1450 nM
 Bioactivity Info 
   TI
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CP0138933
 Compound Info 
2-(4-tert-butylanilino)-3H-benzimidazole-5-carbonitrile
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C18H18N4
  1
1
IC50 = 1510 nM
 Bioactivity Info 
   TI
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CP0138932
 Compound Info 
N-(4-tert-butylphenyl)-6-nitro-1H-benzimidazol-2-amine
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C17H18N4O2
  1
1
IC50 = 2340 nM
 Bioactivity Info 
   TI
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CP0295293
 Compound Info 
2-(4-tert-butylanilino)-1,3-benzothiazole-6-carbonitrile
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C18H17N3S
  1
1
IC50 = 3830 nM
 Bioactivity Info 
   TI
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CP0138934
 Compound Info 
2-(4-methylanilino)-3H-benzimidazole-5-carbonitrile
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C15H12N4
  1
1
IC50 = 4540 nM
 Bioactivity Info 
   TI
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CP0138931
 Compound Info 
2-(4-phenylanilino)-3H-benzimidazole-5-carbonitrile
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C20H14N4
  1
1
IC50 = 4890 nM
 Bioactivity Info 
   TI
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CP0134855
 Compound Info 
2-[4-[3-(trifluoromethyl)pyridin-2-yl]oxyanilino]-3H-benzimidazole-5-carbonitrile
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C20H12F3N5O
  1
1
IC50 = 6560 nM
 Bioactivity Info 
   TI
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CP0544563
 Compound Info 
2-(4-tert-butylanilino)imidazo[1,2-a]pyridine-6-carbonitrile
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C18H18N4
  1
1
IC50 = 9100 nM
 Bioactivity Info 
   TI
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CP0341911
 Compound Info 
2-(4-tert-butyl-2-fluoroanilino)-3H-benzimidazole-5-carbonitrile
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C18H17FN4
  1
1
IC50 = 10100 nM
 Bioactivity Info 
   TI
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CP0483328
 Compound Info 
2-(4-tert-butylanilino)-6-methyl-1H-benzimidazole-5-carbonitrile
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C19H20N4
  1
1
IC50 = 13000 nM
 Bioactivity Info 
   TI
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CP0134853
 Compound Info 
2-(4-tert-butylanilino)-1,3-benzoxazole-6-carbonitrile
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C18H17N3O
  1
1
IC50 = 14900 nM
 Bioactivity Info 
   TI
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0058653
 Compound Info 
2-[2-[(4,5-difluoro-2-methylphenoxy)methyl]-5-methoxypyridin-4-yl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one
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C21H19F2N3O3
  2
1 IC50 = 4 nM
2 IC50 = 44 nM
CP0114180
 Compound Info 
2-[2-[(3,4-difluorophenoxy)methyl]-5-methoxypyridin-4-yl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one
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C20H17F2N3O3
  2
1 IC50 = 5 nM
2 IC50 = 254 nM
CP0204066
 Compound Info 
2-(5-methoxy-2-quinolin-3-ylpyrimidin-4-yl)-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one
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C21H17N5O2
  2
1 IC50 = 8 nM
2 IC50 > 3333 nM
CP0058652
 Compound Info 
2-[2-[2-(4-fluorophenyl)ethyl]-5-methoxypyridin-4-yl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one
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C21H20FN3O2
  2
1 IC50 = 26 nM
2 IC50 = 1300 nM
Clinical Information about the Protein
Target 1 ( Casein kinase I gamma-2 (CSNK1G2) )
Target Type Literature-reported Target