General Information of the Protein
Protein ID
PT06924
Protein Name
Fibroblast growth factor receptor 3
Secondarily
Protein Name
Heparin-binding growth factor receptor
Gene Name
FGFR3
Secondarily
Gene Name
Mfr3
Sam3
Sequence
MVVPACVLVFCVAVVAGATSEPPGPEQRVVRRAAEVPGPEPSQQEQVAFGSGDTVELSCHPPGGAPTGPTVWAKDGTGLVASHRILVGPQRLQVLNASHEDAGVYSCQHRLTRRVLCHFSVRVTDAPSSGDDEDGEDVAEDTGAPYWTRPERMDKKLLAVPAANTVRFRCPAAGNPTPSISWLKNGKEFRGEHRIGGIKLRHQQWSLVMESVVPSDRGNYTCVVENKFGSIRQTYTLDVLERSPHRPILQAGLPANQTAILGSDVEFHCKVYSDAQPHIQWLKHVEVNGSKVGPDGTPYVTVLKTAGANTTDKELEVLSLHNVTFEDAGEYTCLAGNSIGFSHHSAWLVVLPAEEELMETDEAGSVYAGVLSYGVVFFLFILVVAAVILCRLRSPPKKGLGSPTVHKVSRFPLKRQVSLESNSSMNSNTPLVRIARLSSGEGPVLANVSELELPADPKWELSRTRLTLGKPLGEGCFGQVVMAEAIGIDKDRTAKPVTVAVKMLKDDATDKDLSDLVSEMEMMKMIGKHKNIINLLGACTQGGPLYVLVEYAAKGNLREFLRARRPPGMDYSFDACRLPEEQLTCKDLVSCAYQVARGMEYLASQKCIHRDLAARNVLVTEDNVMKIADFGLARDVHNLDYYKKTTNGRLPVKWMAPEALFDRVYTHQSDVWSFGVLLWEIFTPGGPSPYPGIPVEELFKLLKEGHRMDKPASCTHDLYMIMRECWHAVPSQRPTFKQLVEDLDRILTVTSTDEYLDLSVPFEQYSPGGQDTPSSSSSGDDSVFTHDLLPPGPPSNGGPRT
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Organism
Mus musculus, Mouse
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TK protein kinase group
>
Tyrosine protein kinase FGFR family
Function
Tyrosine-protein kinase that acts as a cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of cell proliferation, differentiation and apoptosis. Plays an essential role in the regulation of chondrocyte differentiation, proliferation and apoptosis, and is required for normal skeleton development. Regulates both osteogenesis and postnatal bone mineralization by osteoblasts. Promotes apoptosis in chondrocytes, but can also promote cancer cell proliferation. Required for normal development of the inner ear. Phosphorylates PLCG1, CBL and FRS2. Ligand binding leads to the activation of several signaling cascades. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate. Phosphorylation of FRS2 triggers recruitment of GRB2, GAB1, PIK3R1 and SOS1, and mediates activation of RAS, MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. Plays a role in the regulation of vitamin D metabolism. Mutations that lead to constitutive kinase activation or impair normal FGFR3 maturation, internalization and degradation lead to aberrant signaling. Over-expressed or constitutively activated FGFR3 promotes activation of STAT1, STAT5A and STAT5B. Plays a role in postnatal lung development.
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Uniprot ID
Primary ID:
Q61851

Secondarily ID:
Q61564
Q63834
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Ensembl ID
ENSG00000068078
Subcellular Location
Cell membrane
Cytoplasmic vesicle
Endoplasmic reticulum
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
Compound ID Compound Name Compound Formula
CP0572894
N,3-dimethyl-5-[6-[(3S)-oxolan-3-yl]oxy-7-(1-propan-2-ylpyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl]benzamide
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C25H28N6O3
 1
1
IC50 = 5.4 nM
   TI
   LI
   LO
   TS
CP0952841
(S)-5-(6-(1-Isopropyl-1H-pyrazol-4-yl)-5-((tetrahydrofuran-3-yl)oxy)pyrazolo[1,5-a]pyrimidin-3-yl)-N-(methyl-d3)nicotinamide
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C23H25N7O3
 1
1
IC50 = 5.5 nM
   TI
   LI
   LO
   TS
CP0573520
US11566028, Example 63
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C23H25N7O3
 1
1
IC50 = 7.2 nM
   TI
   LI
   LO
   TS
CP0543600
4-fluoro-N,3-dimethyl-5-[7-(1-methylpyrazol-4-yl)-6-[(3S)-oxolan-3-yl]oxyimidazo[1,2-b]pyridazin-3-yl]benzamide
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C23H23FN6O3
 1
1
IC50 = 12 nM
   TI
   LI
   LO
   TS
CP0546171
3-(difluoromethyl)-4-fluoro-N-methyl-5-[7-(1-methylpyrazol-4-yl)-6-[(3S)-oxolan-3-yl]oxyimidazo[1,2-b]pyridazin-3-yl]benzamide
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C23H21F3N6O3
 1
1
IC50 = 13 nM
   TI
   LI
   LO
   TS
CP0546221
4-fluoro-3-[6-methoxy-7-(1-methylpyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl]-N-methylbenzamide
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C19H17FN6O2
 1
1
IC50 = 14 nM
   TI
   LI
   LO
   TS
CP0576753
N-methyl-3-[7-(1-methylpyrazol-4-yl)-6-[(3S)-oxolan-3-yl]oxyimidazo[1,2-b]pyridazin-3-yl]benzamide
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C22H22N6O3
 1
1
IC50 = 15 nM
   TI
   LI
   LO
   TS
CP0575470
N-ethyl-5-[6-(1-ethylpyrazol-4-yl)-5-[(3S)-oxolan-3-yl]oxypyrazolo[1,5-a]pyrimidin-3-yl]pyridine-3-carboxamide
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C23H25N7O3
 1
1
IC50 = 22 nM
   TI
   LI
   LO
   TS
CP0551969
US11566028, Example 3
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C21H21N7O3
 1
1
IC50 = 29 nM
   TI
   LI
   LO
   TS
CP0575345
N-methyl-3-[7-(1-methylpyrazol-4-yl)-6-(oxetan-3-yloxy)imidazo[1,2-b]pyridazin-3-yl]benzamide
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C21H20N6O3
 1
1
IC50 = 29 nM
   TI
   LI
   LO
   TS
CP0572978
3-[6-methoxy-7-(1-methylpyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl]-N-methylbenzamide
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C19H18N6O2
 1
1
IC50 = 33 nM
   TI
   LI
   LO
   TS
CP0550308
N-methyl-3-[7-(1-methylpyrazol-4-yl)-6-(oxolan-3-yloxy)imidazo[1,2-b]pyridazin-3-yl]benzamide
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C22H22N6O3
 1
1
IC50 = 42 nM
   TI
   LI
   LO
   TS
CP0577915
3,4-difluoro-N-methyl-5-[7-(1-methylpyrazol-4-yl)-6-[(3S)-oxolan-3-yl]oxyimidazo[1,2-b]pyridazin-3-yl]benzamide
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C22H20F2N6O3
 1
1
IC50 = 68 nM
   TI
   LI
   LO
   TS
CP0575346
N-methyl-5-[7-(1-methylpyrazol-4-yl)-6-(oxolan-3-yloxy)imidazo[1,2-b]pyridazin-3-yl]pyridine-3-carboxamide
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C21H21N7O3
 1
1
IC50 = 969 nM
   TI
   LI
   LO
   TS
CP0155468
1-[3-[[(3Z)-2-oxo-3-(1H-pyrrol-2-ylmethylidene)-1H-indol-6-yl]amino]phenyl]-3-[3-(trifluoromethyl)phenyl]urea
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C27H20F3N5O2
 1
1
IC50 = 1700 nM
   TI
   LI
   LO
   TS
CP0378059
N-[3-[[(3Z)-2-oxo-3-(1H-pyrrol-2-ylmethylidene)-1H-indol-6-yl]amino]phenyl]-3-(trifluoromethyl)benzamide
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C27H19F3N4O2
 1
1
IC50 = 6300 nM
   TI
   LI
   LO
   TS
CP0111985
3-(4-methylimidazol-1-yl)-N-[3-[[(3Z)-2-oxo-3-(1H-pyrrol-2-ylmethylidene)-1H-indol-6-yl]amino]phenyl]-5-(trifluoromethyl)benzamide
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C31H23F3N6O2
 1
1
IC50 = 7700 nM
   TI
   LI
   LO
   TS
CP0333107
1-[2-fluoro-5-(trifluoromethyl)phenyl]-3-[4-methyl-3-[[(3Z)-2-oxo-3-(1H-pyrrol-2-ylmethylidene)-1H-indol-6-yl]amino]phenyl]urea
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C28H21F4N5O2
 1
1
IC50 = 9300 nM
   TI
   LI
   LO
   TS
CP0346926
5-[(Z)-[6-[3-[[3-(4-methylpiperazin-1-yl)-5-(trifluoromethyl)benzoyl]amino]anilino]-2-oxo-1H-indol-3-ylidene]methyl]-1H-pyrrole-3-carboxylic acid
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C33H29F3N6O4
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT01411 Fibroblast growth factor receptor 3 Homo sapiens, Human