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Patent code US10251892

Compile Data Set for Download or QSAR

Found 856 hits of Enzyme Inhibition Constant Data   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM262002
PNG
(3-(2,6-difluoro-3,5- dimethoxyphenyl)-7-(1,3- dime...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3N(Cc3cn(C)nc3C)C2=O)-c2cn(C)nc2C)c1F
Show InChI InChI=1S/C26H27F2N7O3/c1-14-17(10-32(3)30-14)12-34-20-7-19(18-13-33(4)31-15(18)2)29-9-16(20)11-35(26(34)36)25-23(27)21(37-5)8-22(38-6)24(25)28/h7-10,13H,11-12H2,1-6H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM262021
PNG
(3-(2,6-difluoro-3,5-dimethoxyphenyl)-7-(1,3-dimeth...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3N(c3cn[nH]c3)C2=O)-c2cn(C)nc2C)c1F
Show InChI InChI=1S/C23H21F2N7O3/c1-12-15(11-30(2)29-12)16-5-17-13(7-26-16)10-31(23(33)32(17)14-8-27-28-9-14)22-20(24)18(34-3)6-19(35-4)21(22)25/h5-9,11H,10H2,1-4H3,(H,27,28)
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM262031
PNG
(1-(4-(2'-(2,6-difluoro-3,5- dimethoxyphenyl)-3'-ox...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3C3(CC3)C2=O)-c2cnn(c2C)C2(CCC2)C#N)c1F
Show InChI InChI=1S/C27H25F2N5O3/c1-15-17(12-32-34(15)26(14-30)5-4-6-26)19-9-18-16(11-31-19)13-33(25(35)27(18)7-8-27)24-22(28)20(36-2)10-21(37-3)23(24)29/h9-12H,4-8,13H2,1-3H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM262032
PNG
(6'-(1-(1-acetylpyrrolidin-3-yl)- 1H-pyrazol-4-yl)-...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3C3(CC3)C2=O)-c2cnn(c2)C2CCN(C2)C(C)=O)c1F
Show InChI InChI=1S/C27H27F2N5O4/c1-15(35)32-7-4-18(14-32)34-13-17(11-31-34)20-8-19-16(10-30-20)12-33(26(36)27(19)5-6-27)25-23(28)21(37-2)9-22(38-3)24(25)29/h8-11,13,18H,4-7,12,14H2,1-3H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM262032
PNG
(6'-(1-(1-acetylpyrrolidin-3-yl)- 1H-pyrazol-4-yl)-...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3C3(CC3)C2=O)-c2cnn(c2)C2CCN(C2)C(C)=O)c1F
Show InChI InChI=1S/C27H27F2N5O4/c1-15(35)32-7-4-18(14-32)34-13-17(11-31-34)20-8-19-16(10-30-20)12-33(26(36)27(19)5-6-27)25-23(28)21(37-2)9-22(38-3)24(25)29/h8-11,13,18H,4-7,12,14H2,1-3H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM262033
PNG
(2'-(2,6-difluoro-3,5- dimethoxyphenyl)-6'-(1-(3- m...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3C3(CC3)C2=O)-c2cnn(CCCN3CCOCC3)c2)c1F
Show InChI InChI=1S/C28H31F2N5O4/c1-37-22-13-23(38-2)25(30)26(24(22)29)35-17-18-14-31-21(12-20(18)28(4-5-28)27(35)36)19-15-32-34(16-19)7-3-6-33-8-10-39-11-9-33/h12-16H,3-11,17H2,1-2H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM262040
PNG
(2'-(2,6-difluoro-3,5- dimethoxyphenyl)-6'-(1-ethyl...)
Show SMILES CCn1cc(c(C)n1)-c1cc2c(CN(C(=O)C22CC2)c2c(F)c(OC)cc(OC)c2F)cn1
Show InChI InChI=1S/C24H24F2N4O3/c1-5-29-12-15(13(2)28-29)17-8-16-14(10-27-17)11-30(23(31)24(16)6-7-24)22-20(25)18(32-3)9-19(33-4)21(22)26/h8-10,12H,5-7,11H2,1-4H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM262044
PNG
(2'-(2,6-difluoro-3,5- dimethoxyphenyl)-6'-{1-[(1,1...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3C3(CC3)C2=O)-c2cnn(CC3CCCS(=O)(=O)N3)c2)c1F
Show InChI InChI=1S/C26H27F2N5O5S/c1-37-20-9-21(38-2)23(28)24(22(20)27)33-13-15-10-29-19(8-18(15)26(5-6-26)25(33)34)16-11-30-32(12-16)14-17-4-3-7-39(35,36)31-17/h8-12,17,31H,3-7,13-14H2,1-2H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))
BDBM262053
PNG
(5-(2′-(2,6-difluoro-3,5-dimethoxyphenyl)-3&#...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3C3(CC3)C2=O)-c2[nH]ncc2C#N)c1F
Show InChI InChI=1S/C22H17F2N5O3/c1-31-15-6-16(32-2)18(24)20(17(15)23)29-10-12-8-26-14(19-11(7-25)9-27-28-19)5-13(12)22(3-4-22)21(29)30/h5-6,8-9H,3-4,10H2,1-2H3,(H,27,28)
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM262057
PNG
(5-(3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-2-...)
Show SMILES CCNC(=O)c1ccc(cn1)-c1cc2N(CC)C(=O)N(Cc2cn1)c1c(F)c(OC)cc(OC)c1F
Show InChI InChI=1S/C25H25F2N5O4/c1-5-28-24(33)16-8-7-14(11-29-16)17-9-18-15(12-30-17)13-32(25(34)31(18)6-2)23-21(26)19(35-3)10-20(36-4)22(23)27/h7-12H,5-6,13H2,1-4H3,(H,28,33)
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM262064
PNG
(3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-7-(6-...)
Show SMILES CCN1C(=O)N(Cc2cnc(cc12)-c1ccc(nc1)N1CCOCC1)c1c(F)c(OC)cc(OC)c1F
Show InChI InChI=1S/C26H27F2N5O4/c1-4-32-19-11-18(16-5-6-22(30-13-16)31-7-9-37-10-8-31)29-14-17(19)15-33(26(32)34)25-23(27)20(35-2)12-21(36-3)24(25)28/h5-6,11-14H,4,7-10,15H2,1-3H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM262066
PNG
(5-(3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-2-...)
Show SMILES CCN1C(=O)N(Cc2cnc(cc12)-c1ccc(nc1)C(N)=O)c1c(F)c(OC)cc(OC)c1F
Show InChI InChI=1S/C23H21F2N5O4/c1-4-29-16-7-15(12-5-6-14(22(26)31)27-9-12)28-10-13(16)11-30(23(29)32)21-19(24)17(33-2)8-18(34-3)20(21)25/h5-10H,4,11H2,1-3H3,(H2,26,31)
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM262069
PNG
(1-(5-{3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-[(5-m...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3N(Cc3nnc(C)o3)C2=O)-c2ccc(nc2)C2(CCC2)C#N)c1F
Show InChI InChI=1S/C29H25F2N7O4/c1-16-35-36-24(42-16)14-37-20-9-19(17-5-6-23(34-11-17)29(15-32)7-4-8-29)33-12-18(20)13-38(28(37)39)27-25(30)21(40-2)10-22(41-3)26(27)31/h5-6,9-12H,4,7-8,13-14H2,1-3H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))
BDBM261900
PNG
(2′-(2,6-difluoro-3,5-dimethoxyphenyl)-6̸...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3C3(CC3)C2=O)-c2cncc(c2)N2CCOCC2)c1F
Show InChI InChI=1S/C27H26F2N4O4/c1-35-21-11-22(36-2)24(29)25(23(21)28)33-15-17-13-31-20(10-19(17)27(3-4-27)26(33)34)16-9-18(14-30-12-16)32-5-7-37-8-6-32/h9-14H,3-8,15H2,1-2H3
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US Patent


Assay Description
In the FGFR Enzymatic Assay after dilution in assay buffer, added to the plate and pre-incubated for 5 to 10 minutes.


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))
BDBM261911
PNG
(2′-(2,6-difluoro-3,5-dimethoxyphenyl)-6̸...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3C3(CC3)C2=O)-c2cncc(c2)C(=O)N2CCOCC2)c1F
Show InChI InChI=1S/C28H26F2N4O5/c1-37-21-11-22(38-2)24(30)25(23(21)29)34-15-18-14-32-20(10-19(18)28(3-4-28)27(34)36)16-9-17(13-31-12-16)26(35)33-5-7-39-8-6-33/h9-14H,3-8,15H2,1-2H3
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Incyte Corporation

US Patent


Assay Description
In the FGFR Enzymatic Assay after dilution in assay buffer, added to the plate and pre-incubated for 5 to 10 minutes.


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM262011
PNG
(3-(2,6-difluoro-3,5- dimethoxyphenyl)-7-(1,3- dime...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3N(C2=O)c2ccccc2F)-c2cn(C)nc2C)c1F
Show InChI InChI=1S/C26H22F3N5O3/c1-14-16(13-32(2)31-14)18-9-20-15(11-30-18)12-33(26(35)34(20)19-8-6-5-7-17(19)27)25-23(28)21(36-3)10-22(37-4)24(25)29/h5-11,13H,12H2,1-4H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM262013
PNG
(3-(2,6-difluoro-3,5- dimethoxyphenyl)-7-(1,3- dime...)
Show SMILES COc1cnc(cn1)N1C(=O)N(Cc2cnc(cc12)-c1cn(C)nc1C)c1c(F)c(OC)cc(OC)c1F
Show InChI InChI=1S/C25H23F2N7O4/c1-13-15(12-32(2)31-13)16-6-17-14(8-28-16)11-33(24-22(26)18(36-3)7-19(37-4)23(24)27)25(35)34(17)20-9-30-21(38-5)10-29-20/h6-10,12H,11H2,1-5H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM262019
PNG
(1-((1-cyclopropyl-1H-pyrazol-4-yl)methyl)-3-(2,6-d...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3N(Cc3cnn(c3)C3CC3)C2=O)-c2cn(C)nc2C)c1F
Show InChI InChI=1S/C27H27F2N7O3/c1-15-19(14-33(2)32-15)20-7-21-17(10-30-20)13-35(26-24(28)22(38-3)8-23(39-4)25(26)29)27(37)34(21)11-16-9-31-36(12-16)18-5-6-18/h7-10,12,14,18H,5-6,11,13H2,1-4H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM262025
PNG
(3-(2,6-difluoro-3,5-dimethoxyphenyl)-7-(1,3-dimeth...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3N(C2=O)c2ccc3cn[nH]c3c2)-c2cn(C)nc2C)c1F
Show InChI InChI=1S/C27H23F2N7O3/c1-14-18(13-34(2)33-14)20-8-21-16(10-30-20)12-35(26-24(28)22(38-3)9-23(39-4)25(26)29)27(37)36(21)17-6-5-15-11-31-32-19(15)7-17/h5-11,13H,12H2,1-4H3,(H,31,32)
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Incyte Corporation

US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM262027
PNG
(1-(5-(3-(2,6-difluoro-3,5-dimethoxyphenyl)-2-oxo-1...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3N(C2=O)c2ccncn2)-c2ccc(nc2)C2(CCC2)C#N)c1F
Show InChI InChI=1S/C29H23F2N7O3/c1-40-21-11-22(41-2)26(31)27(25(21)30)37-14-18-13-34-19(10-20(18)38(28(37)39)24-6-9-33-16-36-24)17-4-5-23(35-12-17)29(15-32)7-3-8-29/h4-6,9-13,16H,3,7-8,14H2,1-2H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM262032
PNG
(6'-(1-(1-acetylpyrrolidin-3-yl)- 1H-pyrazol-4-yl)-...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3C3(CC3)C2=O)-c2cnn(c2)C2CCN(C2)C(C)=O)c1F
Show InChI InChI=1S/C27H27F2N5O4/c1-15(35)32-7-4-18(14-32)34-13-17(11-31-34)20-8-19-16(10-30-20)12-33(26(36)27(19)5-6-27)25-23(28)21(37-2)9-22(38-3)24(25)29/h8-11,13,18H,4-7,12,14H2,1-3H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))
BDBM262032
PNG
(6'-(1-(1-acetylpyrrolidin-3-yl)- 1H-pyrazol-4-yl)-...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3C3(CC3)C2=O)-c2cnn(c2)C2CCN(C2)C(C)=O)c1F
Show InChI InChI=1S/C27H27F2N5O4/c1-15(35)32-7-4-18(14-32)34-13-17(11-31-34)20-8-19-16(10-30-20)12-33(26(36)27(19)5-6-27)25-23(28)21(37-2)9-22(38-3)24(25)29/h8-11,13,18H,4-7,12,14H2,1-3H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM262042
PNG
(2'-(2,6-difluoro-3,5- dimethoxyphenyl)-6'-(2- (dim...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3C3(CC3)C2=O)-c2csc(n2)N(C)C)c1F
Show InChI InChI=1S/C23H22F2N4O3S/c1-28(2)22-27-15(11-33-22)14-7-13-12(9-26-14)10-29(21(30)23(13)5-6-23)20-18(24)16(31-3)8-17(32-4)19(20)25/h7-9,11H,5-6,10H2,1-4H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))
BDBM262044
PNG
(2'-(2,6-difluoro-3,5- dimethoxyphenyl)-6'-{1-[(1,1...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3C3(CC3)C2=O)-c2cnn(CC3CCCS(=O)(=O)N3)c2)c1F
Show InChI InChI=1S/C26H27F2N5O5S/c1-37-20-9-21(38-2)23(28)24(22(20)27)33-13-15-10-29-19(8-18(15)26(5-6-26)25(33)34)16-11-30-32(12-16)14-17-4-3-7-39(35,36)31-17/h8-12,17,31H,3-7,13-14H2,1-2H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM262045
PNG
(2'-(2,6-difluoro-3,5- dimethoxyphenyl)-6'-(3-methy...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3C3(CC3)C2=O)-c2cn(nc2C)C2CCN(C)C2)c1F
Show InChI InChI=1S/C27H29F2N5O3/c1-15-18(14-34(31-15)17-5-8-32(2)13-17)20-9-19-16(11-30-20)12-33(26(35)27(19)6-7-27)25-23(28)21(36-3)10-22(37-4)24(25)29/h9-11,14,17H,5-8,12-13H2,1-4H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM262049
PNG
(6'-(1-((1-acetylazetidin-3- yl)methyl)-1H-pyrazol-...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3C3(CC3)C2=O)-c2cnn(CC3CN(C3)C(C)=O)c2)c1F
Show InChI InChI=1S/C27H27F2N5O4/c1-15(35)32-10-16(11-32)12-33-13-18(9-31-33)20-6-19-17(8-30-20)14-34(26(36)27(19)4-5-27)25-23(28)21(37-2)7-22(38-3)24(25)29/h6-9,13,16H,4-5,10-12,14H2,1-3H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM262049
PNG
(6'-(1-((1-acetylazetidin-3- yl)methyl)-1H-pyrazol-...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3C3(CC3)C2=O)-c2cnn(CC3CN(C3)C(C)=O)c2)c1F
Show InChI InChI=1S/C27H27F2N5O4/c1-15(35)32-10-16(11-32)12-33-13-18(9-31-33)20-6-19-17(8-30-20)14-34(26(36)27(19)4-5-27)25-23(28)21(37-2)7-22(38-3)24(25)29/h6-9,13,16H,4-5,10-12,14H2,1-3H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM262052
PNG
(3-(2,6-difluoro-3,5- dimethoxyphenyl)-7-(1,3-dimet...)
Show SMILES CCN1C(=O)N(Cc2cnc(cc12)-c1cn(C)nc1C)c1c(F)c(OC)cc(OC)c1F
Show InChI InChI=1S/C22H23F2N5O3/c1-6-28-16-7-15(14-11-27(3)26-12(14)2)25-9-13(16)10-29(22(28)30)21-19(23)17(31-4)8-18(32-5)20(21)24/h7-9,11H,6,10H2,1-5H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM262067
PNG
(2′-(2,6-difluoro-3,5-dimethoxyphenyl)-6̸...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3C3(CC3)C2=O)-c2ccncc2)c1F
Show InChI InChI=1S/C23H19F2N3O3/c1-30-17-10-18(31-2)20(25)21(19(17)24)28-12-14-11-27-16(13-3-7-26-8-4-13)9-15(14)23(5-6-23)22(28)29/h3-4,7-11H,5-6,12H2,1-2H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM261969
PNG
(US10251892, Example 69 | US10632126, Example 69 | ...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3N(Cc3ccncc3)C2=O)-c2cn(C)nc2C)c1F
Show InChI InChI=1S/C26H24F2N6O3/c1-15-18(14-32(2)31-15)19-9-20-17(11-30-19)13-34(26(35)33(20)12-16-5-7-29-8-6-16)25-23(27)21(36-3)10-22(37-4)24(25)28/h5-11,14H,12-13H2,1-4H3
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Incyte Corporation

US Patent


Assay Description
In the FGFR Enzymatic Assay after dilution in assay buffer, added to the plate and pre-incubated for 5 to 10 minutes.


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM262071
PNG
(3-(2,6-difluoro-3,5- dimethoxyphenyl)-7-(1,3- dime...)
Show SMILES CCOc1cc(CN2C(=O)N(Cc3cnc(cc23)-c2cn(C)nc2C)c2c(F)c(OC)cc(OC)c2F)ccn1
Show InChI InChI=1S/C28H28F2N6O4/c1-6-40-24-9-17(7-8-31-24)13-35-21-10-20(19-15-34(3)33-16(19)2)32-12-18(21)14-36(28(35)37)27-25(29)22(38-4)11-23(39-5)26(27)30/h7-12,15H,6,13-14H2,1-5H3
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US Patent


Assay Description
In the FGFR Enzymatic Assay after dilution in assay buffer, added to the plate and pre-incubated for 5 to 10 minutes.


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM262079
PNG
(3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-((1-(2,2-di...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3N(Cc3cnn(CC(F)F)c3)C2=O)-c2cn(C)nc2C)c1F
Show InChI InChI=1S/C26H25F4N7O3/c1-14-17(12-34(2)33-14)18-5-19-16(8-31-18)11-37(25-23(29)20(39-3)6-21(40-4)24(25)30)26(38)36(19)10-15-7-32-35(9-15)13-22(27)28/h5-9,12,22H,10-11,13H2,1-4H3
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Incyte Corporation

US Patent


Assay Description
In the FGFR Enzymatic Assay after dilution in assay buffer, added to the plate and pre-incubated for 5 to 10 minutes.


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM262051
PNG
(3-(2,6-difluoro-3,5- dimethoxyphenyl)-1-ethyl-7-(1...)
Show SMILES CCN1C(=O)N(Cc2cnc(cc12)-c1cnn(C)c1)c1c(F)c(OC)cc(OC)c1F
Show InChI InChI=1S/C21H21F2N5O3/c1-5-27-15-6-14(12-9-25-26(2)10-12)24-8-13(15)11-28(21(27)29)20-18(22)16(30-3)7-17(31-4)19(20)23/h6-10H,5,11H2,1-4H3
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Incyte Corporation

US Patent


Assay Description
In the FGFR Enzymatic Assay after dilution in assay buffer, added to the plate and pre-incubated for 5 to 10 minutes.


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM262052
PNG
(3-(2,6-difluoro-3,5- dimethoxyphenyl)-7-(1,3-dimet...)
Show SMILES CCN1C(=O)N(Cc2cnc(cc12)-c1cn(C)nc1C)c1c(F)c(OC)cc(OC)c1F
Show InChI InChI=1S/C22H23F2N5O3/c1-6-28-16-7-15(14-11-27(3)26-12(14)2)25-9-13(16)10-29(22(28)30)21-19(23)17(31-4)8-18(32-5)20(21)24/h7-9,11H,6,10H2,1-5H3
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Incyte Corporation

US Patent


Assay Description
In the FGFR Enzymatic Assay after dilution in assay buffer, added to the plate and pre-incubated for 5 to 10 minutes.


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))
BDBM261904
PNG
(2′-(2,6-difluoro-3,5-dimethoxyphenyl)-6̸...)
Show SMILES COc1cncc(c1)-c1cc2c(CN(C(=O)C22CC2)c2c(F)c(OC)cc(OC)c2F)cn1
Show InChI InChI=1S/C24H21F2N3O4/c1-31-15-6-13(9-27-11-15)17-7-16-14(10-28-17)12-29(23(30)24(16)4-5-24)22-20(25)18(32-2)8-19(33-3)21(22)26/h6-11H,4-5,12H2,1-3H3
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Incyte Corporation

US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM262057
PNG
(5-(3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-2-...)
Show SMILES CCNC(=O)c1ccc(cn1)-c1cc2N(CC)C(=O)N(Cc2cn1)c1c(F)c(OC)cc(OC)c1F
Show InChI InChI=1S/C25H25F2N5O4/c1-5-28-24(33)16-8-7-14(11-29-16)17-9-18-15(12-30-17)13-32(25(34)31(18)6-2)23-21(26)19(35-3)10-20(36-4)22(23)27/h7-12H,5-6,13H2,1-4H3,(H,28,33)
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Incyte Corporation

US Patent


Assay Description
In the FGFR Enzymatic Assay after dilution in assay buffer, added to the plate and pre-incubated for 5 to 10 minutes.


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM262068
PNG
(2′-(2,6-difluoro-3,5-dimethoxyphenyl)-6̸...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3C3(CC3)C2=O)-c2cnn(C)c2)c1F
Show InChI InChI=1S/C22H20F2N4O3/c1-27-10-13(9-26-27)15-6-14-12(8-25-15)11-28(21(29)22(14)4-5-22)20-18(23)16(30-2)7-17(31-3)19(20)24/h6-10H,4-5,11H2,1-3H3
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Incyte Corporation

US Patent


Assay Description
In the FGFR Enzymatic Assay after dilution in assay buffer, added to the plate and pre-incubated for 5 to 10 minutes.


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM261917
PNG
(4-(2′-(2,6-difluoro-3,5-dimethoxyphenyl)-3&#...)
Show SMILES CNC(=O)c1ccc(cc1)-c1cc2c(CN(C(=O)C22CC2)c2c(F)c(OC)cc(OC)c2F)cn1
Show InChI InChI=1S/C26H23F2N3O4/c1-29-24(32)15-6-4-14(5-7-15)18-10-17-16(12-30-18)13-31(25(33)26(17)8-9-26)23-21(27)19(34-2)11-20(35-3)22(23)28/h4-7,10-12H,8-9,13H2,1-3H3,(H,29,32)
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM261929
PNG
(3-(2,6-difluoro-3,5-dimethoxyphenyl)-7-(1,3-dimeth...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3N(Cc3cc(C)on3)C2=O)-c2cn(C)nc2C)c1F
Show InChI InChI=1S/C25H24F2N6O4/c1-13-6-16(30-37-13)11-32-19-7-18(17-12-31(3)29-14(17)2)28-9-15(19)10-33(25(32)34)24-22(26)20(35-4)8-21(36-5)23(24)27/h6-9,12H,10-11H2,1-5H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM261929
PNG
(3-(2,6-difluoro-3,5-dimethoxyphenyl)-7-(1,3-dimeth...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3N(Cc3cc(C)on3)C2=O)-c2cn(C)nc2C)c1F
Show InChI InChI=1S/C25H24F2N6O4/c1-13-6-16(30-37-13)11-32-19-7-18(17-12-31(3)29-14(17)2)28-9-15(19)10-33(25(32)34)24-22(26)20(35-4)8-21(36-5)23(24)27/h6-9,12H,10-11H2,1-5H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM261933
PNG
(3-(2,6-difluoro-3,5-dimethoxyphenyl)-7-(1,3-dimeth...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3N(Cc3cc(C)no3)C2=O)-c2cn(C)nc2C)c1F
Show InChI InChI=1S/C25H24F2N6O4/c1-13-6-16(37-30-13)11-32-19-7-18(17-12-31(3)29-14(17)2)28-9-15(19)10-33(25(32)34)24-22(26)20(35-4)8-21(36-5)23(24)27/h6-9,12H,10-11H2,1-5H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM261954
PNG
(2′-(2,6-difluoro-3,5-dimethoxyphenyl)-6̸...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3C3(CC3)C2=O)-c2cn(nc2C)C2CCS(=O)(=O)C2)c1F
Show InChI InChI=1S/C26H26F2N4O5S/c1-14-17(12-32(30-14)16-4-7-38(34,35)13-16)19-8-18-15(10-29-19)11-31(25(33)26(18)5-6-26)24-22(27)20(36-2)9-21(37-3)23(24)28/h8-10,12,16H,4-7,11,13H2,1-3H3
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Incyte Corporation

US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM261980
PNG
(6-(3-(2,6-difluoro-3,5- dimethoxyphenyl)-7-(1,3- d...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3N(C2=O)c2ccc(cn2)C#N)-c2cn(C)nc2C)c1F
Show InChI InChI=1S/C26H21F2N7O3/c1-14-17(13-33(2)32-14)18-7-19-16(11-30-18)12-34(25-23(27)20(37-3)8-21(38-4)24(25)28)26(36)35(19)22-6-5-15(9-29)10-31-22/h5-8,10-11,13H,12H2,1-4H3
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Incyte Corporation

US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM261989
PNG
(3-(2,6-difluoro-3,5- dimethoxyphenyl)-7-(1,3- dime...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3N(Cc3cccnn3)C2=O)-c2cn(C)nc2C)c1F
Show InChI InChI=1S/C25H23F2N7O3/c1-14-17(13-32(2)31-14)18-8-19-15(10-28-18)11-34(25(35)33(19)12-16-6-5-7-29-30-16)24-22(26)20(36-3)9-21(37-4)23(24)27/h5-10,13H,11-12H2,1-4H3
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Incyte Corporation

US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))
BDBM261989
PNG
(3-(2,6-difluoro-3,5- dimethoxyphenyl)-7-(1,3- dime...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3N(Cc3cccnn3)C2=O)-c2cn(C)nc2C)c1F
Show InChI InChI=1S/C25H23F2N7O3/c1-14-17(13-32(2)31-14)18-8-19-15(10-28-18)11-34(25(35)33(19)12-16-6-5-7-29-30-16)24-22(26)20(36-3)9-21(37-4)23(24)27/h5-10,13H,11-12H2,1-4H3
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Incyte Corporation

US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM262012
PNG
(3-(3-(2,6-difluoro-3,5- dimethoxyphenyl)-7-(1,3- d...)
Show SMILES CNS(=O)(=O)c1cccc(c1)N1C(=O)N(Cc2cnc(cc12)-c1cn(C)nc1C)c1c(F)c(OC)cc(OC)c1F
Show InChI InChI=1S/C27H26F2N6O5S/c1-15-19(14-33(3)32-15)20-10-21-16(12-31-20)13-34(26-24(28)22(39-4)11-23(40-5)25(26)29)27(36)35(21)17-7-6-8-18(9-17)41(37,38)30-2/h6-12,14,30H,13H2,1-5H3
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Incyte Corporation

US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM262019
PNG
(1-((1-cyclopropyl-1H-pyrazol-4-yl)methyl)-3-(2,6-d...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3N(Cc3cnn(c3)C3CC3)C2=O)-c2cn(C)nc2C)c1F
Show InChI InChI=1S/C27H27F2N7O3/c1-15-19(14-33(2)32-15)20-7-21-17(10-30-20)13-35(26-24(28)22(38-3)8-23(39-4)25(26)29)27(37)34(21)11-16-9-31-36(12-16)18-5-6-18/h7-10,12,14,18H,5-6,11,13H2,1-4H3
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM262020
PNG
(2-(4-((3-(2,6-difluoro-3,5-dimethoxyphenyl)-7-(1,3...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3N(Cc3cnn(CC#N)c3)C2=O)-c2cn(C)nc2C)c1F
Show InChI InChI=1S/C26H24F2N8O3/c1-15-18(14-33(2)32-15)19-7-20-17(10-30-19)13-36(25-23(27)21(38-3)8-22(39-4)24(25)28)26(37)35(20)12-16-9-31-34(11-16)6-5-29/h7-11,14H,6,12-13H2,1-4H3
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Incyte Corporation

US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM262021
PNG
(3-(2,6-difluoro-3,5-dimethoxyphenyl)-7-(1,3-dimeth...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3N(c3cn[nH]c3)C2=O)-c2cn(C)nc2C)c1F
Show InChI InChI=1S/C23H21F2N7O3/c1-12-15(11-30(2)29-12)16-5-17-13(7-26-16)10-31(23(33)32(17)14-8-27-28-9-14)22-20(24)18(34-3)6-19(35-4)21(22)25/h5-9,11H,10H2,1-4H3,(H,27,28)
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US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))
BDBM262033
PNG
(2'-(2,6-difluoro-3,5- dimethoxyphenyl)-6'-(1-(3- m...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc(cc3C3(CC3)C2=O)-c2cnn(CCCN3CCOCC3)c2)c1F
Show InChI InChI=1S/C28H31F2N5O4/c1-37-22-13-23(38-2)25(30)26(24(22)29)35-17-18-14-31-21(12-20(18)28(4-5-28)27(35)36)19-15-32-34(16-19)7-3-6-33-8-10-39-11-9-33/h12-16H,3-11,17H2,1-2H3
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Incyte Corporation

US Patent


Assay Description
The inhibitor potency of the exemplified compounds was measured in an enzyme assay that measures peptide phosphorylation using FRET measurements to d...


US Patent US10251892 (2019)


BindingDB Entry DOI: 10.7270/Q2MC9298
More data for this
Ligand-Target Pair
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* indicates data uncertainty>20%