General Information of the Protein
Protein ID
PT03251
Protein Name
Serine/threonine-protein kinase A-Raf
Secondarily
Protein Name
Proto-oncogene A-Raf
Proto-oncogene A-Raf-1
Proto-oncogene Pks
Gene Name
ARAF
Secondarily
Gene Name
ARAF1
PKS
PKS2
Sequence
MEPPRGPPANGAEPSRAVGTVKVYLPNKQRTVVTVRDGMSVYDSLDKALKVRGLNQDCCVVYRLIKGRKTVTAWDTAIAPLDGEELIVEVLEDVPLTMHNFVRKTFFSLAFCDFCLKFLFHGFRCQTCGYKFHQHCSSKVPTVCVDMSTNRQQFYHSVQDLSGGSRQHEAPSNRPLNELLTPQGPSPRTQHCDPEHFPFPAPANAPLQRIRSTSTPNVHMVSTTAPMDSNLIQLTGQSFSTDAAGSRGGSDGTPRGSPSPASVSSGRKSPHSKSPAEQRERKSLADDKKKVKNLGYRDSGYYWEVPPSEVQLLKRIGTGSFGTVFRGRWHGDVAVKVLKVSQPTAEQAQAFKNEMQVLRKTRHVNILLFMGFMTRPGFAIITQWCEGSSLYHHLHVADTRFDMVQLIDVARQTAQGMDYLHAKNIIHRDLKSNNIFLHEGLTVKIGDFGLATVKTRWSGAQPLEQPSGSVLWMAAEVIRMQDPNPYSFQSDVYAYGVVLYELMTGSLPYSHIGCRDQIIFMVGRGYLSPDLSKISSNCPKAMRRLLSDCLKFQREERPLFPQILATIELLQRSLPKIERSASEPSLHRTQADELPACLLSAARLVP
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TKL protein kinase group
>
TKL protein kinase RAF family
Function
Involved in the transduction of mitogenic signals from the cell membrane to the nucleus. May also regulate the TOR signaling cascade. Phosphorylates PFKFB2 (PubMed:36402789).
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Uniprot ID
Primary ID:
P10398

Secondarily ID:
P07557
Q5H9B2
Q5H9B3
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Ensembl ID
ENSG00000078061
HGNC ID
HGNC:646
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: CL000045 , A-375
Compound ID Compound Name Compound Formula
CP0095082
DABRAFENIB
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C23H20F3N5O2S2
 1
1
IC50 = 26 nM
   TI
   LI
   LO
   TS
CP0672877
1-(3,3-Dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea
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C23H29FN6O
 1
1
IC50 = 44 nM
   TI
   LI
   LO
   TS
CP0006321
PLX-4032
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C23H18ClF2N3O3S
 1
1
IC50 = 950 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0672877
1-(3,3-Dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea
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C23H29FN6O
 1
1 IC50 = 1.2 nM
CP0006321
PLX-4032
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C23H18ClF2N3O3S
 1
1 IC50 = 2.1 nM
CP0145292
4-methyl-N-[4-[(1-methylpiperidin-4-yl)methoxy]-3-(trifluoromethyl)phenyl]-3-[[1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)cyclopropanecarbonyl]amino]benzamide
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C32H33F3N6O3
 1
1 IC50 = 35.7 nM
Clinical Information about the Protein
Target 1 ( A-Raf messenger RNA (ARAF mRNA) )
Target Type Clinical trial Target