General Information of the Protein
Protein ID
PT01061
Protein Name
Proto-oncogene tyrosine-protein kinase ROS
Secondarily
Protein Name
Proto-oncogene c-Ros
Proto-oncogene c-Ros-1
Receptor tyrosine kinase c-ros oncogene 1
c-Ros receptor tyrosine kinase
Gene Name
ROS1
Secondarily
Gene Name
MCF3
ROS
Sequence
MKNIYCLIPKLVNFATLGCLWISVVQCTVLNSCLKSCVTNLGQQLDLGTPHNLSEPCIQGCHFWNSVDQKNCALKCRESCEVGCSSAEGAYEEEVLENADLPTAPFASSIGSHNMTLRWKSANFSGVKYIIQWKYAQLLGSWTYTKTVSRPSYVVKPLHPFTEYIFRVVWIFTAQLQLYSPPSPSYRTHPHGVPETAPLIRNIESSSPDTVEVSWDPPQFPGGPILGYNLRLISKNQKLDAGTQRTSFQFYSTLPNTIYRFSIAAVNEVGEGPEAESSITTSSSAVQQEEQWLFLSRKTSLRKRSLKHLVDEAHCLRLDAIYHNITGISVDVHQQIVYFSEGTLIWAKKAANMSDVSDLRIFYRGSGLISSISIDWLYQRMYFIMDELVCVCDLENCSNIEEITPPSISAPQKIVADSYNGYVFYLLRDGIYRADLPVPSGRCAEAVRIVESCTLKDFAIKPQAKRIIYFNDTAQVFMSTFLDGSASHLILPRIPFADVKSFACENNDFLVTDGKVIFQQDALSFNEFIVGCDLSHIEEFGFGNLVIFGSSSQLHPLPGRPQELSVLFGSHQALVQWKPPALAIGANVILISDIIELFELGPSAWQNWTYEVKVSTQDPPEVTHIFLNISGTMLNVPELQSAMKYKVSVRASSPKRPGPWSEPSVGTTLVPASEPPFIMAVKEDGLWSKPLNSFGPGEFLSSDIGNVSDMDWYNNSLYYSDTKGDVFVWLLNGTDISENYHLPSIAGAGALAFEWLGHFLYWAGKTYVIQRQSVLTGHTDIVTHVKLLVNDMVVDSVGGYLYWTTLYSVESTRLNGESSLVLQTQPWFSGKKVIALTLDLSDGLLYWLVQDSQCIHLYTAVLRGQSTGDTTITEFAAWSTSEISQNALMYYSGRLFWINGFRIITTQEIGQKTSVSVLEPARFNQFTIIQTSLKPLPGNFSFTPKVIPDSVQESSFRIEGNASSFQILWNGPPAVDWGVVFYSVEFSAHSKFLASEQHSLPVFTVEGLEPYALFNLSVTPYTYWGKGPKTSLSLRAPETVPSAPENPRIFILPSGKCCNKNEVVVEFRWNKPKHENGVLTKFEIFYNISNQSITNKTCEDWIAVNVTPSVMSFQLEGMSPRCFIAFQVRAFTSKGPGPYADVVKSTTSEINPFPHLITLLGNKIVFLDMDQNQVVWTFSAERVISAVCYTADNEMGYYAEGDSLFLLHLHNRSSSELFQDSLVFDITVITIDWISRHLYFALKESQNGMQVFDVDLEHKVKYPREVKIHNRNSTIISFSVYPLLSRLYWTEVSNFGYQMFYYSIISHTLHRILQPTATNQQNKRNQCSCNVTEFELSGAMAIDTSNLEKPLIYFAKAQEIWAMDLEGCQCWRVITVPAMLAGKTLVSLTVDGDLIYWIITAKDSTQIYQAKKGNGAIVSQVKALRSRHILAYSSVMQPFPDKAFLSLASDTVEPTILNATNTSLTIRLPLAKTNLTWYGITSPTPTYLVYYAEVNDRKNSSDLKYRILEFQDSIALIEDLQPFSTYMIQIAVKNYYSDPLEHLPPGKEIWGKTKNGVPEAVQLINTTVRSDTSLIISWRESHKPNGPKESVRYQLAISHLALIPETPLRQSEFPNGRLTLLVTRLSGGNIYVLKVLACHSEEMWCTESHPVTVEMFNTPEKPYSLVPENTSLQFNWKAPLNVNLIRFWVELQKWKYNEFYHVKTSCSQGPAYVCNITNLQPYTSYNVRVVVVYKTGENSTSLPESFKTKAGVPNKPGIPKLLEGSKNSIQWEKAEDNGCRITYYILEIRKSTSNNLQNQNLRWKMTFNGSCSSVCTWKSKNLKGIFQFRVVAANNLGFGEYSGISENIILVGDDFWIPETSFILTIIVGIFLVVTIPLTFVWHRRLKNQKSAKEGVTVLINEDKELAELRGLAAGVGLANACYAIHTLPTQEEIENLPAFPREKLTLRLLLGSGAFGEVYEGTAVDILGVGSGEIKVAVKTLKKGSTDQEKIEFLKEAHLMSKFNHPNILKQLGVCLLNEPQYIILELMEGGDLLTYLRKARMATFYGPLLTLVDLVDLCVDISKGCVYLERMHFIHRDLAARNCLVSVKDYTSPRIVKIGDFGLARDIYKNDYYRKRGEGLLPVRWMAPESLMDGIFTTQSDVWSFGILIWEILTLGHQPYPAHSNLDVLNYVQTGGRLEPPRNCPDDLWNLMTQCWAQEPDQRPTFHRIQDQLQLFRNFFLNSIYKSRDEANNSGVINESFEGEDGDVICLNSDDIMPVALMETKNREGLNYMVLATECGQGEEKSEGPLGSQESESCGLRKEEKEPHADKDFCQEKQVAYCPSGKPEGLNYACLTHSGYGDGSD
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TK protein kinase group
>
Tyrosine protein kinase Sev family
Function
Receptor tyrosine kinase (RTK) that plays a role in epithelial cell differentiation and regionalization of the proximal epididymal epithelium. NELL2 is an endogenous ligand for ROS1. Upon endogenous stimulation by NELL2, ROS1 activates the intracellular signaling pathway and triggers epididymal epithelial differentiation and subsequent sperm maturation (By similarity). May activate several downstream signaling pathways related to cell differentiation, proliferation, growth and survival including the PI3 kinase-mTOR signaling pathway. Mediates the phosphorylation of PTPN11, an activator of this pathway. May also phosphorylate and activate the transcription factor STAT3 to control anchorage-independent cell growth. Mediates the phosphorylation and the activation of VAV3, a guanine nucleotide exchange factor regulating cell morphology. May activate other downstream signaling proteins including AKT1, MAPK1, MAPK3, IRS1 and PLCG2.
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Uniprot ID
Primary ID:
P08922

Secondarily ID:
Q15368
Q5TDB5
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Ensembl ID
ENSG00000047936
HGNC ID
HGNC:10261
Subcellular Location
Cell membrane
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: CL000077 , Ba/F3
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0019908
 Compound Info 
BDBM50242742
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C30H40ClN7O3S
  1
1
IC50 = 2 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0043052
 Compound Info 
FORETINIB
   Show/Hide
C34H34F2N4O6
  1
1
IC50 = 10 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0061016
 Compound Info 
3-(4-Amino-7-cyclopentyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-phenol
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C17H18N4O
  1
1
IC50 = 42 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0385508
 Compound Info 
2-[4-[4-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperazin-1-yl]acetic acid
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C27H28FN7O2
  1
1
IC50 = 60 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0385511
 Compound Info 
1-[4-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperidin-4-ol
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C26H27FN6O
  1
1
IC50 = 210 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0388864
 Compound Info 
4-[6-(benzylamino)imidazo[1,2-b]pyridazin-3-yl]benzonitrile
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C20H15N5
  1
1
IC50 = 300 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0395047
 Compound Info 
6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]-3-pyridin-2-ylimidazo[1,2-b]pyridazine
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C21H18FN5
  1
1
IC50 = 600 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0661487
 Compound Info 
3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea monophosphate
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C26H34Cl2N7O7P
  1
1
IC50 = 3263 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0388620
 Compound Info 
methyl N-[4-[7-amino-3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxypyrazolo[1,5-a]pyrimidin-6-yl]phenyl]carbamate
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C28H32N6O5
  1
1
IC50 = 5500 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0388615
 Compound Info 
3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxy-6-(1,3-thiazol-2-yl)pyrazolo[1,5-a]pyrimidin-7-amine
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C23H26N6O3S
  1
1
IC50 > 11000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0388616
 Compound Info 
3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxy-6-phenylpyrazolo[1,5-a]pyrimidin-7-amine
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C26H29N5O3
  1
1
IC50 > 11000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0138866
 Compound Info 
1-[4-[3-[4-amino-5-(2-fluoro-5-hydroxyphenyl)pyrrolo[2,3-d]pyrimidin-7-yl]cyclobutyl]piperazin-1-yl]ethanone
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C22H25FN6O2
  1
1
IC50 > 11000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000310 , HCC78
 Cell Line Info 
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0020453
 Compound Info 
US10081622, Compound 11
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C31H34F2N6O2
  3
1 IC50 = 0.2 nM
2 IC50 = 7 nM
3 IC50 = 12 nM
CP0025347
 Compound Info 
(S)-2-(3-(3-hydroxy-5-methylphenyl)-4-(6-(2-hydroxypropylamino)-2-(pyridin-3-yl)pyrimidin-4-yl)-1H-pyrazol-1-yl)acetonitrile
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C24H23N7O2
  2
1 IC50 = 1.7 nM
2 IC50 = 199 nM
CP0258438
 Compound Info 
2-[4-[6-(4-hydroxybutylamino)-2-pyridin-3-ylpyrimidin-4-yl]-3-(3-hydroxy-5-methylphenyl)pyrazol-1-yl]acetonitrile
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C25H25N7O2
  1
1 IC50 = 24 nM
CP0053320
 Compound Info 
2-[4-[6-(4-hydroxybutylamino)-2-pyridin-3-ylpyrimidin-4-yl]-3-(3-methoxy-5-methylphenyl)pyrazol-1-yl]acetonitrile
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C26H27N7O2
  1
1 IC50 = 56 nM
CP0068418
 Compound Info 
2-[3-(3-methoxy-5-methylphenyl)-4-[6-(3-morpholin-4-ylpropylamino)-2-pyridin-3-ylpyrimidin-4-yl]pyrazol-1-yl]acetonitrile
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C29H32N8O2
  1
1 IC50 = 88 nM
CP0068432
 Compound Info 
2-[3-(3-hydroxy-5-methylphenyl)-4-[6-(3-hydroxypropylamino)-2-pyridin-3-ylpyrimidin-4-yl]pyrazol-1-yl]acetonitrile
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C24H23N7O2
  1
1 IC50 = 108 nM
CP0051407
 Compound Info 
2-[4-[6-(3-hydroxypropylamino)-2-pyridin-3-ylpyrimidin-4-yl]-3-(3-methoxy-5-methylphenyl)pyrazol-1-yl]acetonitrile
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C25H25N7O2
  1
1 IC50 = 119 nM
CP0068430
 Compound Info 
2-[3-(3-methoxy-5-methylphenyl)-4-[6-(2-morpholin-4-ylethylamino)-2-pyridin-3-ylpyrimidin-4-yl]pyrazol-1-yl]acetonitrile
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C28H30N8O2
  1
1 IC50 = 148 nM
CP0053366
 Compound Info 
2-[3-(3-hydroxy-5-methylphenyl)-4-[6-(3-morpholin-4-ylpropylamino)-2-pyridin-3-ylpyrimidin-4-yl]pyrazol-1-yl]acetonitrile
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C28H30N8O2
  1
1 IC50 = 183 nM
CP0053365
 Compound Info 
2-[3-(3-hydroxy-5-methylphenyl)-4-[6-(2-morpholin-4-ylethylamino)-2-pyridin-3-ylpyrimidin-4-yl]pyrazol-1-yl]acetonitrile
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C27H28N8O2
  1
1 IC50 = 478 nM
CP0019908
 Compound Info 
BDBM50242742
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C30H40ClN7O3S
  1
1 Kd = 0.49 nM
CP0043052
 Compound Info 
FORETINIB
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C34H34F2N4O6
  4
1 Kd = 14 nM
2 Ki = 8.2 nM
3 Ki = 16 nM
4 Ki = 20 nM
Clinical Information about the Protein
Target 1 ( Proto-oncogene c-Ros (ROS1) )
Target Type Successful Target
Disease 3 Target-related Diseases  3
1 Non-small-cell lung cancer [ICD-11: 2C25.Y]
2 Non-small-cell lung cancer [ICD-11: 2C25]
3 Brain metastases [ICD-11: 2D50]
Approved Drug(s) 4 Approved Drugs  4
1 Crizotinib
 Drug Info 
Approved
Non-small-cell lung cancer
2 Lorlatinib
 Drug Info 
Approved
Non-small-cell lung cancer
3 Entrectinib
 Drug Info 
Approved
Non-small-cell lung cancer
4 Repotrectinib
 Drug Info 
Approved
Non-small-cell lung cancer
Patented Agent(s) 1 Patented Agent  1
1 PMID28270010-Compound-Figure21-b
 Drug Info 
Patented
Brain metastases
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT06680 Proto-oncogene tyrosine-protein kinase ROS Mus musculus, Mouse
 Protein Info