General Information of the Protein
Protein ID
PT01115
Protein Name
Fibroblast growth factor receptor 2
Secondarily
Protein Name
K-sam
Keratinocyte growth factor receptor
Gene Name
FGFR2
Secondarily
Gene Name
BEK
KGFR
KSAM
Sequence
MVSWGRFICLVVVTMATLSLARPSFSLVEDTTLEPEEPPTKYQISQPEVYVAAPGESLEVRCLLKDAAVISWTKDGVHLGPNNRTVLIGEYLQIKGATPRDSGLYACTASRTVDSETWYFMVNVTDAISSGDDEDDTDGAEDFVSENSNNKRAPYWTNTEKMEKRLHAVPAANTVKFRCPAGGNPMPTMRWLKNGKEFKQEHRIGGYKVRNQHWSLIMESVVPSDKGNYTCVVENEYGSINHTYHLDVVERSPHRPILQAGLPANASTVVGGDVEFVCKVYSDAQPHIQWIKHVEKNGSKYGPDGLPYLKVLKAAGVNTTDKEIEVLYIRNVTFEDAGEYTCLAGNSIGISFHSAWLTVLPAPGREKEITASPDYLEIAIYCIGVFLIACMVVTVILCRMKNTTKKPDFSSQPAVHKLTKRIPLRRQVTVSAESSSSMNSNTPLVRITTRLSSTADTPMLAGVSEYELPEDPKWEFPRDKLTLGKPLGEGCFGQVVMAEAVGIDKDKPKEAVTVAVKMLKDDATEKDLSDLVSEMEMMKMIGKHKNIINLLGACTQDGPLYVIVEYASKGNLREYLRARRPPGMEYSYDINRVPEEQMTFKDLVSCTYQLARGMEYLASQKCIHRDLAARNVLVTENNVMKIADFGLARDINNIDYYKKTTNGRLPVKWMAPEALFDRVYTHQSDVWSFGVLMWEIFTLGGSPYPGIPVEELFKLLKEGHRMDKPANCTNELYMMMRDCWHAVPSQRPTFKQLVEDLDRILTLTTNEEYLDLSQPLEQYSPSYPDTRSSCSSGDDSVFSPDPMPYEPCLPQYPHINGSVKT
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Organism
Homo sapiens, Human
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, migration and apoptosis, and in the regulation of embryonic development. Required for normal embryonic patterning, trophoblast function, limb bud development, lung morphogenesis, osteogenesis and skin development. Plays an essential role in the regulation of osteoblast differentiation, proliferation and apoptosis, and is required for normal skeleton development. Promotes cell proliferation in keratinocytes and immature osteoblasts, but promotes apoptosis in differentiated osteoblasts. Phosphorylates PLCG1, FRS2 and PAK4. 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. FGFR2 signaling is down-regulated by ubiquitination, internalization and degradation. Mutations that lead to constitutive kinase activation or impair normal FGFR2 maturation, internalization and degradation lead to aberrant signaling. Over-expressed FGFR2 promotes activation of STAT1.
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Uniprot ID
Primary ID:
P21802

Secondarily ID:
B4DFC2
E7EVR6
E9PCR0
P18443
Q01742
Q12922
Q14300
Q14301
Q14302
Q14303
Q14304
Q14305
Q14672
Q14718
Q14719
Q1KHY5
Q86YI4
Q8IXC7
Q96KL9
Q96KM0
Q96KM1
Q96KM2
Q9NZU2
Q9NZU3
Q9UD01
Q9UD02
Q9UIH3
Q9UIH4
Q9UIH5
Q9UIH6
Q9UIH7
Q9UIH8
Q9UM87
Q9UMC6
Q9UNS7
Q9UQH7
Q9UQH8
Q9UQH9
Q9UQI0
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Ensembl ID
ENSG00000066468
HGNC ID
HGNC:3689
Subcellular Location
Cell membrane
Golgi apparatus
Cytoplasmic vesicle
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
CP0479968
 Compound Info 
1-[4-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]phenyl]piperidin-1-yl]prop-2-en-1-one
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C27H34N8O
  1
1
GI50 = 11.2 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0441015
 Compound Info 
N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]sulfanyl]propanamide
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C30H31F3N6OS
  1
1
GI50 = 36 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 = 2 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 = 8 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0418567
 Compound Info 
3-[4-amino-7-[3-(hydroxymethyl)cyclobutyl]pyrrolo[2,3-d]pyrimidin-5-yl]phenol
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C17H18N4O2
  1
1
IC50 = 27 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 = 190 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 = 3000 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 = 3700 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 > 2900 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000432 , KATO III
 Cell Line Info 
Cell Line ID: CL000012 , Sf21
 Cell Line Info 
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Cell Line ID: CL000431 , SNU-16
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0047214
 Compound Info 
7-(1,3,4,6,7,8,9,9a-octahydropyrido[1,2-a]pyrazin-2-yl)-N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]quinazolin-4-amine
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C29H35N7O2
  1
1 IC50 = 0.2 nM
CP0236837
 Compound Info 
N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-7-[(3R,5S)-3,4,5-trimethylpiperazin-1-yl]quinazolin-4-amine
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C28H35N7O2
  1
1 IC50 = 0.2 nM
CP0360545
 Compound Info 
N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-7-[4-(dimethylamino)piperidin-1-yl]quinazolin-4-amine
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C28H35N7O2
  1
1 IC50 = 0.3 nM
CP0549217
 Compound Info 
N-[5-[2-(2,6-dichloro-3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-7-(4-ethylpiperazin-1-yl)quinazolin-4-amine
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C27H31Cl2N7O2
  1
1 IC50 = 0.3 nM
CP0047213
 Compound Info 
N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-7-morpholin-4-ylquinazolin-4-amine
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C25H28N6O3
  1
1 IC50 = 0.4 nM
CP0121918
 Compound Info 
N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-7-[3-(dimethylamino)pyrrolidin-1-yl]quinazolin-4-amine
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C27H33N7O2
  1
1 IC50 = 0.4 nM
CP0054573
 Compound Info 
CHEBI:63453
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C26H33N5O3
  6
1 IC50 = 0.4 nM
2 IC50 = 0.6 nM
3 IC50 = 1.1 nM
4 IC50 = 1.2 nM
5 IC50 = 2.5 nM
6 IC50 = 3.2 nM
CP0182382
 Compound Info 
N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-2-ethyl-7-(4-ethylpiperazin-1-yl)quinazolin-4-amine
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C29H37N7O2
  1
1 IC50 = 0.5 nM
CP0033516
 Compound Info 
3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(morpholin-4-ylmethyl)-1,3,4,7-tetrahydro-2H-pyrrolo[3',2':5,6]pyrido[4,3-d]pyrimidin-2-one
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C24H27F2N5O4
  4
1 IC50 = 0.5 nM
2 IC50 < 0.5 nM
3 IC50 <= 1 nM
4 IC50 = 3.37 nM
CP0047216
 Compound Info 
N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-7-(4-ethylpiperazin-1-yl)-2-methylquinazolin-4-amine
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C28H35N7O2
  1
1 IC50 = 0.6 nM
CP0549218
 Compound Info 
7-(4-cyclobutylpiperazin-1-yl)-N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]quinazolin-4-amine
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C29H35N7O2
  1
1 IC50 = 0.6 nM
CP0569655
 Compound Info 
N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-7-(4-propan-2-ylpiperazin-1-yl)quinazolin-4-amine
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C28H35N7O2
  1
1 IC50 = 0.6 nM
CP0569659
 Compound Info 
2-chloro-N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-7-(4-ethylpiperazin-1-yl)quinazolin-4-amine
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C27H32ClN7O2
  1
1 IC50 = 0.6 nM
CP0133097
 Compound Info 
N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-7-(4-ethylpiperazin-1-yl)-2-propylquinazolin-4-amine
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C30H39N7O2
  1
1 IC50 = 0.7 nM
CP0569656
 Compound Info 
N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-7-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine
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C27H33N7O2
  1
1 IC50 = 0.7 nM
CP0121917
 Compound Info 
N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-7-(1-methylpiperidin-4-yl)quinazolin-4-amine
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C27H32N6O2
  1
1 IC50 = 0.8 nM
CP0122169
 Compound Info 
N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-7-(4-ethylpiperazin-1-yl)quinazolin-4-amine
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C27H33N7O2
  1
1 IC50 = 0.8 nM
CP0761938
 Compound Info 
N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-7-(4-methylpiperazin-1-yl)quinazolin-4-amine
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C26H31N7O2
  1
1 IC50 = 1 nM
CP0047221
 Compound Info 
N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-6-(4-ethylpiperazin-1-yl)isoquinolin-1-amine
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C28H34N6O2
  1
1 IC50 = 1.2 nM
CP0462436
 Compound Info 
4-N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-7-N-(2-morpholin-4-ylethyl)quinazoline-4,7-diamine
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C27H33N7O3
  1
1 IC50 = 1.3 nM
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 = 1.4 nM
CP0081362
 Compound Info 
4-fluoro-2-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-(3-methyl-2H-indazol-5-yl)pyridin-2-yl]phenol
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C27H23FN4O2
  1
1 IC50 = 1.6 nM
CP0081678
 Compound Info 
4-chloro-2-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-isoquinolin-6-ylpyridin-2-yl]phenol
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C28H22ClN3O2
  1
1 IC50 = 2 nM
CP0118715
 Compound Info 
2-fluoro-6-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-(3-methyl-2H-indazol-5-yl)pyridin-2-yl]phenol
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C27H23FN4O2
  1
1 IC50 = 2.5 nM
CP0090815
 Compound Info 
4-N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-7-N-(2-methoxyethyl)quinazoline-4,7-diamine
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C24H28N6O3
  1
1 IC50 = 2.7 nM
CP0109337
 Compound Info 
4,5-difluoro-2-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-(3-methyl-2H-indazol-5-yl)pyridin-2-yl]phenol
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C27H22F2N4O2
  1
1 IC50 = 2.8 nM
CP0099314
 Compound Info 
2-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-(3-methyl-2H-indazol-5-yl)pyridin-2-yl]phenol
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C27H24N4O2
  1
1 IC50 = 3 nM
CP0653199
 Compound Info 
N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)quinazolin-4-amine
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C21H21N5O2
  1
1 IC50 = 3.2 nM
CP0118716
 Compound Info 
2,4-difluoro-6-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-(3-methyl-2H-indazol-5-yl)pyridin-2-yl]phenol
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C27H22F2N4O2
  1
1 IC50 = 3.4 nM
CP0734490
 Compound Info 
N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-8-methoxyquinazolin-4-amine
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C22H23N5O3
  1
1 IC50 = 3.9 nM
CP0690841
 Compound Info 
N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-8-(4-ethylpiperazin-1-yl)quinazolin-4-amine
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C27H33N7O2
  1
1 IC50 = 4.3 nM
CP0109346
 Compound Info 
5-fluoro-2-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-(3-methyl-2H-indazol-5-yl)pyridin-2-yl]phenol
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C27H23FN4O2
  1
1 IC50 = 4.7 nM
CP0734491
 Compound Info 
8-Chloro-N-(5-(3,5-dimethoxyphenethyl)-1H-pyrazol-3-yl)quinazolin-4-amine
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C21H20ClN5O2
  1
1 IC50 = 4.8 nM
CP0038622
 Compound Info 
3-tert-butyl-1-(2-{[4-(diethylamino)butyl]amino}-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl)urea
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C28H41N7O3
  1
1 IC50 = 5 nM
CP0234743
 Compound Info 
4-chloro-2-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-(3-methyl-2H-pyrazolo[3,4-b]pyridin-5-yl)pyridin-2-yl]phenol
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C26H22ClN5O2
  1
1 IC50 = 6.6 nM
CP0081381
 Compound Info 
4-chloro-2-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-(3-methyl-2H-indazol-5-yl)pyridin-2-yl]phenol
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C27H23ClN4O2
  1
1 IC50 = 8.6 nM
CP0121920
 Compound Info 
4-N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-7-(4-ethylpiperazin-1-yl)-2-N-[(3-methyl-1,2-oxazol-5-yl)methyl]quinazoline-2,4-diamine
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C32H39N9O3
  1
1 IC50 < 10 nM
CP0717956
 Compound Info 
5-Chloro-N-(5-(3,5-dimethoxyphenethyl)-1H-pyrazol-3-yl)quinazolin-4-amine
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C21H20ClN5O2
  1
1 IC50 = 16.9 nM
CP0099316
 Compound Info 
3-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-(3-methyl-2H-indazol-5-yl)pyridin-2-yl]phenol
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C27H24N4O2
  1
1 IC50 = 21.4 nM
CP0109448
 Compound Info 
(2R)-2-[[5-(3-methyl-2H-indazol-5-yl)-6-phenylpyridin-3-yl]amino]-2-phenylethanol
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C27H24N4O
  1
1 IC50 = 26.3 nM
CP0961526
 Compound Info 
N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-5-methoxyquinazolin-4-amine
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C22H23N5O3
  1
1 IC50 = 100.9 nM
CP0563793
 Compound Info 
US10618902, Compound I-250
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C22H23Cl2N5O6S
  1
1 IC50 = 102 nM
CP0322325
 Compound Info 
N-[(1S,2R)-2-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)-8-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl]amino]cyclopentyl]prop-2-enamide
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C24H25Cl2N5O4
  1
1 IC50 = 247 nM
CP0558518
 Compound Info 
N-[(3R,4S)-4-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)-8-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl]amino]oxolan-3-yl]propanamide
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C23H25Cl2N5O5
  1
1 IC50 = 394 nM
CP0565334
 Compound Info 
US10189794, Compound I-241
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C23H23Cl2N5O5
  1
1 IC50 = 505 nM
CP0176348
 Compound Info 
US10618902, Compound I-279
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C23H23ClFN5O5
  1
1 IC50 = 563 nM
CP0218526
 Compound Info 
US10618902, Compound I-281
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C23H23F2N5O5
  1
1 IC50 = 672 nM
CP0229508
 Compound Info 
US10189794, Compound I-240
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C23H23Cl2N5O5
  1
1 IC50 = 776 nM
CP0322326
 Compound Info 
US10618902, Compound I-254
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C23H24ClN5O5
  1
1 IC50 = 2156 nM
CP0558520
 Compound Info 
US10618902, Compound I-294
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C25H29N5O5
  1
1 IC50 = 5132 nM
CP0486123
 Compound Info 
US10618902, Compound I-255
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C23H25N5O5
  1
1 IC50 = 10000 nM
Clinical Information about the Protein
Target 1 ( Fibroblast growth factor receptor 2 (FGFR2) )
Target Type Successful Target
Disease 4 Target-related Diseases  4
1 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
2 Cholangiocarcinoma [ICD-11: 2C12.10]
3 Alzheimer disease [ICD-11: 8A20]
4 Retinoblastoma [ICD-11: 2D02.2]
Approved Drug(s) 1 Approved Drug  1
1 Pemigatinib
 Drug Info 
Approved
Cholangiocarcinoma
Clinical Trial Drug(s) 5 Clinical Trial Drugs  5
1 E-3810
 Drug Info 
Phase 3
Solid tumour/cancer
2 LY2874455
 Drug Info 
Phase 2
Solid tumour/cancer
3 AEE-788
 Drug Info 
Phase 1/2
Solid tumour/cancer
4 Debio 1347
 Drug Info 
Phase 2
Solid tumour/cancer
5 MK-2461
 Drug Info 
Phase 1/2
Alzheimer disease
Discontinued Drug(s) 1 Discontinued Drug  1
1 PD-0183812
 Drug Info 
Terminated
Retinoblastoma
Investigative Drug(s) 1 Investigative Drug  1
1 ACTB-1003
 Drug Info 
Investigative
Solid tumour/cancer