General Information of the Protein
Protein ID
PT01046
Protein Name
Serine/threonine-protein kinase SIK3
Secondarily
Protein Name
Salt-inducible kinase 3
Serine/threonine-protein kinase QSK
Gene Name
SIK3
Secondarily
Gene Name
KIAA0999
QSK
L19
Sequence
MAAAAASGAGGAAGAGTGGAGPAGRLLPPPAPGSPAAPAAVSPAAGQPRPPAPASRGPMPARIGYYEIDRTIGKGNFAVVKRATHLVTKAKVAIKIIDKTQLDEENLKKIFREVQIMKMLCHPHIIRLYQVMETERMIYLVTEYASGGEIFDHLVAHGRMAEKEARRKFKQIVTAVYFCHCRNIVHRDLKAENLLLDANLNIKIADFGFSNLFTPGQLLKTWCGSPPYAAPELFEGKEYDGPKVDIWSLGVVLYVLVCGALPFDGSTLQNLRARVLSGKFRIPFFMSTECEHLIRHMLVLDPNKRLSMEQICKHKWMKLGDADPNFDRLIAECQQLKEERQVDPLNEDVLLAMEDMGLDKEQTLQSLRSDAYDHYSAIYSLLCDRHKRHKTLRLGALPSMPRALAFQAPVNIQAEQAGTAMNISVPQVQLINPENQIVEPDGTLNLDSDEGEEPSPEALVRYLSMRRHTVGVADPRTEVMEDLQKLLPGFPGVNPQAPFLQVAPNVNFMHNLLPMQNLQPTGQLEYKEQSLLQPPTLQLLNGMGPLGRRASDGGANIQLHAQQLLKRPRGPSPLVTMTPAVPAVTPVDEESSDGEPDQEAVQSSTYKDSNTLHLPTERFSPVRRFSDGAASIQAFKAHLEKMGNNSSIKQLQQECEQLQKMYGGQIDERTLEKTQQQHMLYQQEQHHQILQQQIQDSICPPQPSPPLQAACENQPALLTHQLQRLRIQPSSPPPNHPNNHLFRQPSNSPPPMSSAMIQPHGAASSSQFQGLPSRSAIFQQQPENCSSPPNVALTCLGMQQPAQSQQVTIQVQEPVDMLSNMPGTAAGSSGRGISISPSAGQMQMQHRTNLMATLSYGHRPLSKQLSADSAEAHSLNVNRFSPANYDQAHLHPHLFSDQSRGSPSSYSPSTGVGFSPTQALKVPPLDQFPTFPPSAHQQPPHYTTSALQQALLSPTPPDYTRHQQVPHILQGLLSPRHSLTGHSDIRLPPTEFAQLIKRQQQQRQQQQQQQQQQEYQELFRHMNQGDAGSLAPSLGGQSMTERQALSYQNADSYHHHTSPQHLLQIRAQECVSQASSPTPPHGYAHQPALMHSESMEEDCSCEGAKDGFQDSKSSSTLTKGCHDSPLLLSTGGPGDPESLLGTVSHAQELGIHPYGHQPTAAFSKNKVPSREPVIGNCMDRSSPGQAVELPDHNGLGYPARPSVHEHHRPRALQRHHTIQNSDDAYVQLDNLPGMSLVAGKALSSARMSDAVLSQSSLMGSQQFQDGENEECGASLGGHEHPDLSDGSQHLNSSCYPSTCITDILLSYKHPEVSFSMEQAGV
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
CAMK protein kinase group
>
CAMK protein kinase CAMK1 family
>
CAMK protein kinase QIK subfamily
Function
Positive regulator of mTOR signaling that functions by triggering the degradation of DEPTOR, an mTOR inhibitor. Involved in the dynamic regulation of mTOR signaling in chondrocyte differentiation during skeletogenesis (PubMed:30232230). Negatively regulates cAMP signaling pathway possibly by acting on CRTC2/TORC2 and CRTC3/TORC3 (Probable). Prevents HDAC4 translocation to the nucleus (By similarity).
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Uniprot ID
Primary ID:
Q9Y2K2

Secondarily ID:
A1A5A8
H0Y494
J3KPC8
Q59FY2
Q5M9N1
Q6P3R6
Q8IYM8
Q9HA50
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Ensembl ID
ENSG00000160584
HGNC ID
HGNC:29165
Subcellular Location
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
CP0004106
 Compound Info 
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one
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C28H26N4O3
  1
1
IC50 = 460 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0568788
 Compound Info 
8-[(5-amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(3-fluoro-6-methylpyridin-2-yl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one
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C25H24ClFN6O3
  1
1
IC50 = 7000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0577426
 Compound Info 
8-[(5-amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(3-chloropyridin-2-yl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one
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C24H22Cl2N6O3
  1
1
IC50 = 9000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0550534
 Compound Info 
HG-9-91-01 (1)
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C32H37N7O3
  1
1
IC50 = 9600 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0574243
 Compound Info 
8-[(5-amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(3-methylpyridin-2-yl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one
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C25H25ClN6O3
  1
1
IC50 = 14000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0070883
 Compound Info 
8-[(5-amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methylpyridin-2-yl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one
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C25H25ClN6O3
  1
1
IC50 = 24000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0550539
 Compound Info 
8-[(5-amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-[6-(difluoromethyl)pyridin-2-yl]phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one
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C25H23ClF2N6O3
  1
1
IC50 = 50000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0579760
 Compound Info 
8-[(5-amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methoxypyridin-2-yl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one
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C25H25ClN6O4
  1
1
IC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0577014
 Compound Info 
8-[(5-amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methylpyridin-2-yl)phenyl]-2-(2-methoxyanilino)pyrido[2,3-d]pyrimidin-7-one
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C31H29ClN6O4
  1
1
IC50 = 83000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0580152
 Compound Info 
8-[(5-amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(3-methoxy-6-methylpyridin-2-yl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one
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C26H27ClN6O4
  1
1
IC50 = 84000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0004106
 Compound Info 
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one
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C28H26N4O3
  3
1 IC50 = 0.972 nM
2 IC50 = 1.24 nM
3 Kd = 0.46 nM
CP0367808
 Compound Info 
CHEMBL5090394
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C24H22ClFN6O3
  1
1 IC50 = 22 nM
Clinical Information about the Protein
Target 1 ( SIK family kinase 3 (SIK3) )
Target Type Clinical trial Target