General Information of the Protein
Protein ID
PT01667
Protein Name
MAP/microtubule affinity-regulating kinase 4
Secondarily
Protein Name
MAP/microtubule affinity-regulating kinase-like 1
Gene Name
MARK4
Secondarily
Gene Name
KIAA1860
MARKL1
Sequence
MSSRTVLAPGNDRNSDTHGTLGSGRSSDKGPSWSSRSLGARCRNSIASCPEEQPHVGNYRLLRTIGKGNFAKVKLARHILTGREVAIKIIDKTQLNPSSLQKLFREVRIMKGLNHPNIVKLFEVIETEKTLYLVMEYASAGEVFDYLVSHGRMKEKEARAKFRQIVSAVHYCHQKNIVHRDLKAENLLLDAEANIKIADFGFSNEFTLGSKLDTFCGSPPYAAPELFQGKKYDGPEVDIWSLGVILYTLVSGSLPFDGHNLKELRERVLRGKYRVPFYMSTDCESILRRFLVLNPAKRCTLEQIMKDKWINIGYEGEELKPYTEPEEDFGDTKRIEVMVGMGYTREEIKESLTSQKYNEVTATYLLLGRKTEEGGDRGAPGLALARVRAPSDTTNGTSSSKGTSHSKGQRSSSSTYHRQRRHSDFCGPSPAPLHPKRSPTSTGEAELKEERLPGRKASCSTAGSGSRGLPPSSPMVSSAHNPNKAEIPERRKDSTSTPNNLPPSMMTRRNTYVCTERPGAERPSLLPNGKENSSGTPRVPPASPSSHSLAPPSGERSRLARGSTIRSTFHGGQVRDRRAGGGGGGGVQNGPPASPTLAHEAAPLPAGRPRPTTNLFTKLTSKLTRRVADEPERIGGPEVTSCHLPWDQTETAPRLLRFPWSVKLTSSRPPEALMAALRQATAAARCRCRQPQPFLLACLHGGAGGPEPLSHFEVEVCQLPRPGLRGVLFRRVAGTALAFRTLVTRISNDLEL
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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 MARK subfamily
Function
Serine/threonine-protein kinase (PubMed:15009667, PubMed:14594945, PubMed:23666762, PubMed:23184942). Phosphorylates the microtubule-associated protein MAPT/TAU (PubMed:14594945, PubMed:23666762). Also phosphorylates the microtubule-associated proteins MAP2 and MAP4 (PubMed:14594945). Involved in regulation of the microtubule network, causing reorganization of microtubules into bundles (PubMed:14594945, PubMed:25123532). Required for the initiation of axoneme extension during cilium assembly (PubMed:23400999). Regulates the centrosomal location of ODF2 and phosphorylates ODF2 in vitro (PubMed:23400999). Plays a role in cell cycle progression, specifically in the G1/S checkpoint (PubMed:25123532). Reduces neuronal cell survival (PubMed:15009667). Plays a role in energy homeostasis by regulating satiety and metabolic rate (By similarity). Promotes adipogenesis by activating JNK1 and inhibiting the p38MAPK pathway, and triggers apoptosis by activating the JNK1 pathway (By similarity). Phosphorylates mTORC1 complex member RPTOR and acts as a negative regulator of the mTORC1 complex, probably due to disruption of the interaction between phosphorylated RPTOR and the RRAGA/RRAGC heterodimer which is required for mTORC1 activation (PubMed:23184942). Involved in NLRP3 positioning along microtubules by mediating NLRP3 recruitment to microtubule organizing center (MTOC) upon inflammasome activation (PubMed:28656979).
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Uniprot ID
Primary ID:
Q96L34

Secondarily ID:
Q8NG37
Q96JG7
Q96SQ2
Q9BYD8
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Ensembl ID
ENSG00000007047
HGNC ID
HGNC:13538
Subcellular Location
Cytoplasm
Cytoskeleton
Microtubule organizing center
Centrosome
Cytoplasm
Cytoskeleton
Microtubule organizing center
Cytoplasm
Cytoskeleton
Cilium basal body
Cytoplasm
Cytoskeleton
Cilium axoneme
Cytoplasm
Cell projection
Dendrite
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: CL000025 , HEK-293T
Compound ID Compound Name Compound Formula
CP0382546
2-anilino-7-[(1S)-4-hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethylpyrrolo[2,3-d]pyrimidin-6-one
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C23H22N4O2
 1
1
IC50 = 21 nM
   TI
   LI
   LO
   TS
CP0060100
N-[(1S)-1-(2-anilino-5,5-dimethyl-6-oxopyrrolo[2,3-d]pyrimidin-7-yl)-2,3-dihydro-1H-inden-4-yl]methanesulfonamide
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C24H25N5O3S
 1
1
IC50 = 180 nM
   TI
   LI
   LO
   TS
CP0382544
7-[(1S)-1-(3-hydroxyphenyl)ethyl]-5,5-dimethyl-2-(pyridin-3-ylamino)pyrrolo[2,3-d]pyrimidin-6-one
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C21H21N5O2
 1
1
IC50 = 270 nM
   TI
   LI
   LO
   TS
CP0307932
7-[(1S)-4-amino-2,3-dihydro-1H-inden-1-yl]-2-anilino-5,5-dimethylpyrrolo[2,3-d]pyrimidin-6-one
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C23H23N5O
 1
1
IC50 = 450 nM
   TI
   LI
   LO
   TS
CP0323244
7-[(1S)-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-2-(pyridin-3-ylamino)pyrrolo[2,3-d]pyrimidin-6-one
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C22H21N5O
 1
1
IC50 = 520 nM
   TI
   LI
   LO
   TS
CP0366861
7-cyclohexyl-5,5-dimethyl-2-(3-piperazin-1-ylanilino)pyrrolo[2,3-d]pyrimidin-6-one
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C24H32N6O
 1
1
IC50 = 920 nM
   TI
   LI
   LO
   TS
CP0191016
5,5-dimethyl-7-[(1S)-1-phenylethyl]-2-(pyridin-3-ylamino)pyrrolo[2,3-d]pyrimidin-6-one
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C21H21N5O
 1
1
IC50 = 2750 nM
   TI
   LI
   LO
   TS
CP0382542
5,5-dimethyl-7-(2-phenylpropan-2-yl)-2-(pyridin-3-ylamino)pyrrolo[2,3-d]pyrimidin-6-one
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C22H23N5O
 1
1
IC50 = 3760 nM
   TI
   LI
   LO
   TS
CP0228585
7-[(2R)-butan-2-yl]-5,5-dimethyl-2-(pyridin-3-ylamino)pyrrolo[2,3-d]pyrimidin-6-one
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C17H21N5O
 1
1
IC50 = 5910 nM
   TI
   LI
   LO
   TS
CP0307950
7-cyclohexyl-5,5-dimethyl-2-(pyridin-3-ylamino)pyrrolo[2,3-d]pyrimidin-6-one
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C19H23N5O
 1
1
IC50 = 5990 nM
   TI
   LI
   LO
   TS
CP0267285
2-anilino-7-cyclohexyl-5,5-dimethylpyrrolo[2,3-d]pyrimidin-6-one
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C20H24N4O
 1
1
IC50 = 8600 nM
   TI
   LI
   LO
   TS
CP0180469
2-anilino-7-[(1R)-2,2-difluoro-1-phenylethyl]-5,5-dimethylpyrrolo[2,3-d]pyrimidin-6-one
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C22H20F2N4O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0202678
2-anilino-5,5-dimethyl-7-phenylpyrrolo[2,3-d]pyrimidin-6-one
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C20H18N4O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0228586
2-anilino-5,5-dimethyl-6-(1-methylpyrazol-4-yl)pyrrolo[3,4-d]pyrimidin-7-one
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C18H18N6O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0254997
7-cyclohexyl-5,5-dimethyl-N-phenyl-6H-pyrrolo[2,3-d]pyrimidin-2-amine
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C20H26N4
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0302978
7-[(1S)-1-(4-fluorophenyl)ethyl]-5,5-dimethyl-2-(pyridin-3-ylamino)pyrrolo[2,3-d]pyrimidin-6-one
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C21H20FN5O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0307949
2-anilino-5,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-6-one
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C14H14N4O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0382541
2-anilino-5,5-dimethyl-7-[(2S)-3-methylbutan-2-yl]pyrrolo[2,3-d]pyrimidin-6-one
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C19H24N4O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS