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
Compound ID Compound Name Compound Formula
CP0138935
2-[4-(2-hydroxypropan-2-yl)anilino]-3H-benzimidazole-5-carbonitrile
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C17H16N4O
 1
1
IC50 = 700 nM
   TI
   LI
   LO
   TS
CP0249994
2-[4-(2-fluoropyridin-3-yl)anilino]-3H-benzimidazole-5-carbonitrile
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C19H12FN5
 1
1
IC50 = 1170 nM
   TI
   LI
   LO
   TS
CP0356211
2-[4-(1-methylpyrazol-4-yl)anilino]-3H-benzimidazole-5-carbonitrile
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C18H14N6
 1
1
IC50 = 1450 nM
   TI
   LI
   LO
   TS
CP0138933
2-(4-tert-butylanilino)-3H-benzimidazole-5-carbonitrile
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C18H18N4
 1
1
IC50 = 1510 nM
   TI
   LI
   LO
   TS
CP0138932
N-(4-tert-butylphenyl)-6-nitro-1H-benzimidazol-2-amine
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C17H18N4O2
 1
1
IC50 = 2340 nM
   TI
   LI
   LO
   TS
CP0295293
2-(4-tert-butylanilino)-1,3-benzothiazole-6-carbonitrile
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C18H17N3S
 1
1
IC50 = 3830 nM
   TI
   LI
   LO
   TS
CP0138934
2-(4-methylanilino)-3H-benzimidazole-5-carbonitrile
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C15H12N4
 1
1
IC50 = 4540 nM
   TI
   LI
   LO
   TS
CP0138931
2-(4-phenylanilino)-3H-benzimidazole-5-carbonitrile
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C20H14N4
 1
1
IC50 = 4890 nM
   TI
   LI
   LO
   TS
CP0134855
2-[4-[3-(trifluoromethyl)pyridin-2-yl]oxyanilino]-3H-benzimidazole-5-carbonitrile
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C20H12F3N5O
 1
1
IC50 = 6560 nM
   TI
   LI
   LO
   TS
CP0544563
2-(4-tert-butylanilino)imidazo[1,2-a]pyridine-6-carbonitrile
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C18H18N4
 1
1
IC50 = 9100 nM
   TI
   LI
   LO
   TS
CP0341911
2-(4-tert-butyl-2-fluoroanilino)-3H-benzimidazole-5-carbonitrile
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C18H17FN4
 1
1
IC50 = 10100 nM
   TI
   LI
   LO
   TS
CP0483328
2-(4-tert-butylanilino)-6-methyl-1H-benzimidazole-5-carbonitrile
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C19H20N4
 1
1
IC50 = 13000 nM
   TI
   LI
   LO
   TS
CP0134853
2-(4-tert-butylanilino)-1,3-benzoxazole-6-carbonitrile
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C18H17N3O
 1
1
IC50 = 14900 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0058653
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
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
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
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