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Compile Data Set for Download or QSAR

Found 3691 hits of ic50 for UniProtKB: P22455   
Target/Host
(Institution)		LigandTarget/Host
Links		Ligand
Links		Trg + Lig
Links		Ki
nM		ΔG°
kcal/mole		IC50
nM		Kd
nM		EC50/IC50
nM		koff
s-1		kon
M-1s-1		pHTemp
°C
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM249396
PNG
(US10537571, Compound 108 | US10562888, Compound 10...)
Show SMILES CCN1CCN(CC1)c1ccc(Nc2cc(ncn2)N(C)C(=O)Nc2c(Cl)c(OC)cc(OC)c2Cl)c(NC(=O)C=C)c1
Show InChI InChI=1S/C29H34Cl2N8O4/c1-6-25(40)35-20-14-18(39-12-10-38(7-2)11-13-39)8-9-19(20)34-23-16-24(33-17-32-23)37(3)29(41)36-28-26(30)21(42-4)15-22(43-5)27(28)31/h6,8-9,14-17H,1,7,10-13H2,2-5H3,(H,35,40)(H,36,41)(H,32,33,34)
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n/an/a<0.100n/an/an/an/an/an/a



EISAI R&D MANAGEMENT CO., LTD.

US Patent


Assay Description
Recombinant FGFR1 (2.5 nM), FGFR2 (1 nM), FGFR3 (5 nM), or FGFR4 (12 nM) (Invitrogen™) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ I...

US Patent US10912774 (2021)


BindingDB Entry DOI: 10.7270/Q2PN98QH
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM249396
PNG
(US10537571, Compound 108 | US10562888, Compound 10...)
Show SMILES CCN1CCN(CC1)c1ccc(Nc2cc(ncn2)N(C)C(=O)Nc2c(Cl)c(OC)cc(OC)c2Cl)c(NC(=O)C=C)c1
Show InChI InChI=1S/C29H34Cl2N8O4/c1-6-25(40)35-20-14-18(39-12-10-38(7-2)11-13-39)8-9-19(20)34-23-16-24(33-17-32-23)37(3)29(41)36-28-26(30)21(42-4)15-22(43-5)27(28)31/h6,8-9,14-17H,1,7,10-13H2,2-5H3,(H,35,40)(H,36,41)(H,32,33,34)
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n/an/a<0.200n/an/an/an/a7.525



EISAI R&D MANAGEMENT CO., LTD.

US Patent


Assay Description
Recombinant FGFR1 (2.5 nM), or FGFR4 (12 nM) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ ID NO:1) (20 μM, FGFR1 substrate); Pol...

US Patent US9434697 (2016)


BindingDB Entry DOI: 10.7270/Q2K07351
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM249396
PNG
(US10537571, Compound 108 | US10562888, Compound 10...)
Show SMILES CCN1CCN(CC1)c1ccc(Nc2cc(ncn2)N(C)C(=O)Nc2c(Cl)c(OC)cc(OC)c2Cl)c(NC(=O)C=C)c1
Show InChI InChI=1S/C29H34Cl2N8O4/c1-6-25(40)35-20-14-18(39-12-10-38(7-2)11-13-39)8-9-19(20)34-23-16-24(33-17-32-23)37(3)29(41)36-28-26(30)21(42-4)15-22(43-5)27(28)31/h6,8-9,14-17H,1,7,10-13H2,2-5H3,(H,35,40)(H,36,41)(H,32,33,34)
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EISAI R&D Management Co., Ltd.

US Patent


Assay Description
Recombinant FGFR1 (2.5 nM), or FGFR4 (12 nM) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ ID NO:1) (20 μM, FGFR1 substrate); Pol...

US Patent US9730931 (2017)


BindingDB Entry DOI: 10.7270/Q2542QPZ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM50559106
PNG
(CHEMBL4786195)
Show SMILES COCCOc1cc(NC(=O)N2CCCc3cc(CN4C[C@@H](CC4=O)N(C)C)c(C=O)nc23)ncc1C#N |r|
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n/an/a 0.200n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEI...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c01019
BindingDB Entry DOI: 10.7270/Q2FB56MJ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM50604182
PNG
(CHEMBL5194425)
Show SMILES C[C@@H](Oc1ccc2[nH]nc(Nc3c(F)cc(cc3NC(=O)C=C)N3CCC(CC3)N3CCOCC3)c2c1)c1c(Cl)cncc1Cl |r|
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n/an/a 0.25n/an/an/an/an/an/a


TBA



Citation and Details
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM209349
PNG
(US9266883, 148)
Show SMILES COCCNc1cc(NC(=O)N2CCCc3cc(CN(C)C(=O)COC)c(C=O)nc23)ncc1C#N
Show InChI InChI=1S/C24H29N7O5/c1-30(22(33)15-36-3)13-17-9-16-5-4-7-31(23(16)28-20(17)14-32)24(34)29-21-10-19(26-6-8-35-2)18(11-25)12-27-21/h9-10,12,14H,4-8,13,15H2,1-3H3,(H2,26,27,29,34)
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TBA

Assay Description
Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEI...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c01019
BindingDB Entry DOI: 10.7270/Q2FB56MJ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM50554188
PNG
(CHEMBL4744686)
Show SMILES COc1cc(OC)c(Cl)c(Nc2ncccc2-c2cc(Nc3c(C)cccc3NC(=O)C=C)ncn2)c1Cl
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n/an/a 0.400n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of N-terminal 6x-His tagged FGFR4 catalytic domain (445-753 residues) (unknown origin) using IYGEFKKK substrate and [gamma-32P]-ATP incuba...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c00044
BindingDB Entry DOI: 10.7270/Q24Q7ZNV
More data for this
Ligand-Target Pair		3D
3D Structure (crystal)
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM604879
PNG
(N-(5-Cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-...)
Show SMILES COCCNc1cc(NC(=O)N2CCCc3cc(CN4CCCOCC4=O)c(C=O)nc23)ncc1C#N
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TBA



Citation and Details

BindingDB Entry DOI: 10.7270/Q2CJ8JDK
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM209334
PNG
(US9266883, 98)
Show SMILES COCCNc1cc(NC(=O)N2CCCc3cc(CN4CCOCC4=O)c(C=O)nc23)ncc1C#N
Show InChI InChI=1S/C24H27N7O5/c1-35-7-4-26-19-10-21(27-12-18(19)11-25)29-24(34)31-5-2-3-16-9-17(20(14-32)28-23(16)31)13-30-6-8-36-15-22(30)33/h9-10,12,14H,2-8,13,15H2,1H3,(H2,26,27,29,34)
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TBA

Assay Description
Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEI...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c01019
BindingDB Entry DOI: 10.7270/Q2FB56MJ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM50559126
PNG
(CHEMBL4796410)
Show SMILES CC(C)Nc1cc(NC(=O)N2CCCc3cc(CN(C)C(C)=O)c(C=O)nc23)ncc1C#N
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TBA

Assay Description
Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEI...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c01019
BindingDB Entry DOI: 10.7270/Q2FB56MJ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM523849
PNG
(US11136320, Compound 8)
Show SMILES CO[C@@H]1CCN(Cc2cc3CCCN(C(=O)Nc4cc(NCCSC)c(cn4)C#N)c3nc2OC)C1=O |r|
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n/an/a 0.420n/an/an/an/an/an/a


TBA

Assay Description
The FGFR4 kinase inhibition of compounds was tested by using mobility shift assay in this experiment, and the rate of FGFR4 kinase inhibition of comp...

Citation and Details

BindingDB Entry DOI: 10.7270/Q24T6NJF
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM50593531
PNG
(ASP-5878 | ASP5878 | Asp 5878 | Asp-5878 | Asp5878)
Show SMILES COc1cc(OC)c(F)c(COc2cnc(Nc3cnn(CCO)c3)nc2)c1F
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TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c01977
BindingDB Entry DOI: 10.7270/Q2R49VVS
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM161392
PNG
(US10124003, Ex. Compound 5 | US10835536, Ex. Comp ...)
Show SMILES COc1cc(OC)cc(c1)C#Cc1nn([C@H]2CCN(C2)C(=O)C#C)c2ncnc(N)c12 |r|
Show InChI InChI=1S/C22H20N6O3/c1-4-19(29)27-8-7-15(12-27)28-22-20(21(23)24-13-25-22)18(26-28)6-5-14-9-16(30-2)11-17(10-14)31-3/h1,9-11,13,15H,7-8,12H2,2-3H3,(H2,23,24,25)/t15-/m0/s1
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n/an/a 0.5n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
The inhibitory effect of the compounds on FGFR4 kinase activity was measured according to the method of Test Example 3. Purified recombinant human FG...

US Patent US10894048 (2021)


BindingDB Entry DOI: 10.7270/Q2319ZZF
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM161392
PNG
(US10124003, Ex. Compound 5 | US10835536, Ex. Comp ...)
Show SMILES COc1cc(OC)cc(c1)C#Cc1nn([C@H]2CCN(C2)C(=O)C#C)c2ncnc(N)c12 |r|
Show InChI InChI=1S/C22H20N6O3/c1-4-19(29)27-8-7-15(12-27)28-22-20(21(23)24-13-25-22)18(26-28)6-5-14-9-16(30-2)11-17(10-14)31-3/h1,9-11,13,15H,7-8,12H2,2-3H3,(H2,23,24,25)/t15-/m0/s1
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n/an/a 0.5n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Purified recombinant human FGFR4 protein was purchased from Carna Biosciences, Inc. When setting conditions for the measurement of the inhibitory ef...

US Patent US9108973 (2015)


BindingDB Entry DOI: 10.7270/Q2XW4HJV
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM50604182
PNG
(CHEMBL5194425)
Show SMILES C[C@@H](Oc1ccc2[nH]nc(Nc3c(F)cc(cc3NC(=O)C=C)N3CCC(CC3)N3CCOCC3)c2c1)c1c(Cl)cncc1Cl |r|
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TBA



Citation and Details
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM50604182
PNG
(CHEMBL5194425)
Show SMILES C[C@@H](Oc1ccc2[nH]nc(Nc3c(F)cc(cc3NC(=O)C=C)N3CCC(CC3)N3CCOCC3)c2c1)c1c(Cl)cncc1Cl |r|
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TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.2c00096
BindingDB Entry DOI: 10.7270/Q2K078BB
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM50575048
PNG
(CHEMBL4866267)
Show SMILES COc1cc(OC)c(Cl)c(c1Cl)-c1ccc2nc(Nc3c(C)cc(CCN4CCN(C)CC4)cc3NC(=O)C=C)ncc2c1
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n/an/a 0.550n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of N-terminal GST fusion tagged human FGFR4 cytoplasmic domain (460 to 802 end residues) expressed in baculovirus expression system preinc...

Citation and Details

Article DOI: 10.1016/j.ejmech.2021.113794
BindingDB Entry DOI: 10.7270/Q2Z60SWJ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM604880
PNG
(N-(5-Cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-...)
Show SMILES COCCNc1cc(NC(=O)N2CCCc3cc(CN4CCCN(C)CC4=O)c(C=O)nc23)ncc1C#N
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n/an/a 0.600n/an/an/an/an/an/a


TBA



Citation and Details

BindingDB Entry DOI: 10.7270/Q2CJ8JDK
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM50559105
PNG
(CHEMBL4754106)
Show SMILES COCCOc1cc(NC(=O)N2CCCc3cc(CN4C[C@H](CC4=O)N(C)C)c(C=O)nc23)ncc1C#N |r|
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TBA

Assay Description
Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEI...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c01019
BindingDB Entry DOI: 10.7270/Q2FB56MJ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM50559116
PNG
(CHEMBL4764394)
Show SMILES CC(C)Oc1cc(NC(=O)N2CCCc3cc(CN4CCCC4=O)c(C=O)nc23)ncc1C#N
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TBA

Assay Description
Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEI...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c01019
BindingDB Entry DOI: 10.7270/Q2FB56MJ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM209275
PNG
(US9266883, 33)
Show SMILES CC(C)Oc1cc(NC(=O)N2CCCc3ccc(C=O)nc23)ncc1C#N
Show InChI InChI=1S/C19H19N5O3/c1-12(2)27-16-8-17(21-10-14(16)9-20)23-19(26)24-7-3-4-13-5-6-15(11-25)22-18(13)24/h5-6,8,10-12H,3-4,7H2,1-2H3,(H,21,23,26)
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n/an/a 0.700n/an/an/an/an/an/a



Novartis Institutes for BioMedical Research

Curated by ChEMBL


Assay Description
Inhibition of FGFR4 (388 to 802 residues) (unknown origin) using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shif...

ACS Med Chem Lett 9: 215-220 (2018)


Article DOI: 10.1021/acsmedchemlett.7b00485
BindingDB Entry DOI: 10.7270/Q27947C7
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM50606159
PNG
(CHEMBL5186034)
Show SMILES CCn1c2cc(N[C@@H]3COCC[C@@H]3NC(=O)C=C)ncc2cc(-c2c(Cl)c(OC)cc(OC)c2Cl)c1=O |r,wU:7.6,12.13,(2,5.01,;.67,4.24,;.67,2.7,;-.67,1.93,;-2,2.7,;-3.33,1.93,;-4.67,2.7,;-6,1.93,;-7.33,2.7,;-8.67,1.93,;-8.67,.38,;-7.33,-.39,;-6,.38,;-4.67,-.39,;-4.67,-1.93,;-3.33,-2.7,;-6,-2.7,;-6,-4.24,;-3.33,.38,;-2,-.39,;-.67,.38,;.67,-.39,;2,.38,;3.34,-.39,;4.67,.38,;4.67,1.93,;6,-.39,;7.33,.38,;8.67,-.39,;6,-1.93,;4.67,-2.7,;4.67,-4.24,;6,-5.01,;3.34,-1.93,;2,-2.7,;2,1.93,;3.34,2.7,)|
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TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c01977
BindingDB Entry DOI: 10.7270/Q2R49VVS
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM209275
PNG
(US9266883, 33)
Show SMILES CC(C)Oc1cc(NC(=O)N2CCCc3ccc(C=O)nc23)ncc1C#N
Show InChI InChI=1S/C19H19N5O3/c1-12(2)27-16-8-17(21-10-14(16)9-20)23-19(26)24-7-3-4-13-5-6-15(11-25)22-18(13)24/h5-6,8,10-12H,3-4,7H2,1-2H3,(H,21,23,26)
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TBA

Assay Description
Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEI...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c01019
BindingDB Entry DOI: 10.7270/Q2FB56MJ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM50606156
PNG
(CHEMBL5202677)
Show SMILES CCn1c2cc(Nc3c(NC(=O)C=C)cccc3OC)ncc2cc(-c2c(Cl)c(OC)cc(OC)c2Cl)c1=O |(-.67,-5,;.66,-4.24,;.66,-2.7,;-.66,-1.92,;-1.99,-2.7,;-3.33,-1.92,;-4.67,-2.7,;-6,-1.92,;-6,-.38,;-4.67,.38,;-4.67,1.92,;-3.33,2.7,;-6,2.7,;-6,4.24,;-7.33,.38,;-8.67,-.38,;-8.67,-1.92,;-7.33,-2.7,;-7.33,-4.23,;-5.99,-4.99,;-3.33,-.38,;-1.99,.38,;-.66,-.38,;.66,.38,;2,-.38,;3.33,.38,;4.67,-.38,;4.67,-1.92,;6.01,.38,;7.33,-.38,;8.67,.38,;6.01,1.92,;4.67,2.7,;4.67,4.24,;6.01,5,;3.33,1.92,;2,2.7,;2,-1.92,;3.33,-2.7,)|
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n/an/a 0.700n/an/an/an/an/an/a


TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c01977
BindingDB Entry DOI: 10.7270/Q2R49VVS
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM597750
PNG
((S)—N-(5-Cyano-4-((2-methoxyethyl)amino)pyridin-2-...)
Show SMILES COCCNc1cc(NC(=O)N2CCCc3cc(CN(C)C(=O)[C@@H]4CCCO4)c(C=O)nc23)ncc1C#N |r|
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n/an/a 0.720n/an/an/an/an/an/a


TBA

Assay Description
In this experiment, the inhibitory effect of the compounds on FGFR4 kinase activity was tested by a fluorescence resonance energy transfer (TR-FRET) ...

Citation and Details

BindingDB Entry DOI: 10.7270/Q21V5JWQ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM597779
PNG
((S)—N-(5-Cyano-4-((2-methoxyethyl)amino)pyrid...)
Show SMILES COCCNc1cc(NC(=O)N2CCCc3cc(CN(C)C(=O)[C@H]4CCOC4)c(C=O)nc23)ncc1C#N |r|
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n/an/a 0.740n/an/an/an/an/an/a


TBA

Assay Description
In this experiment, the inhibitory effect of the compounds on FGFR4 kinase activity was tested by a fluorescence resonance energy transfer (TR-FRET) ...

Citation and Details

BindingDB Entry DOI: 10.7270/Q21V5JWQ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM597781
PNG
((R)—N-(5-Cyano-4-((2-methoxyethyl)amino)pyrid...)
Show SMILES COCCNc1cc(NC(=O)N2CCCc3cc(CN(C)C(=O)[C@H]4CCCN4C)c(C=O)nc23)ncc1C#N |r|
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n/an/a 0.740n/an/an/an/an/an/a


TBA

Assay Description
In this experiment, the inhibitory effect of the compounds on FGFR4 kinase activity was tested by a fluorescence resonance energy transfer (TR-FRET) ...

Citation and Details

BindingDB Entry DOI: 10.7270/Q21V5JWQ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM604845
PNG
(N-(5-Cyano-4-(((trans)-2-methoxycyclopentyl)amino)...)
Show SMILES CO[C@@H]1CCCC1Nc1cc(NC(=O)N2CCCc3cc(CN4CCOCC4=O)c(C=O)nc23)ncc1C#N |r|
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TBA



Citation and Details

BindingDB Entry DOI: 10.7270/Q2CJ8JDK
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM50559121
PNG
(CHEMBL4758832)
Show SMILES CC(C)Oc1cc(NC(=O)N2CCCc3cc(CN(C)S(C)(=O)=O)c(C=O)nc23)ncc1C#N
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TBA

Assay Description
Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEI...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c01019
BindingDB Entry DOI: 10.7270/Q2FB56MJ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM209336
PNG
(US9266883, 101)
Show SMILES COCCOc1cc(NC(=O)N2CCCc3cc(CN4CCN(C)CC4=O)c(C=O)nc23)ncc1C#N
Show InChI InChI=1S/C25H29N7O5/c1-30-6-7-31(23(34)15-30)14-18-10-17-4-3-5-32(24(17)28-20(18)16-33)25(35)29-22-11-21(37-9-8-36-2)19(12-26)13-27-22/h10-11,13,16H,3-9,14-15H2,1-2H3,(H,27,29,35)
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n/an/a 0.900n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEI...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c01019
BindingDB Entry DOI: 10.7270/Q2FB56MJ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM50559123
PNG
(CHEMBL4745780)
Show SMILES CCN(Cc1cc2CCCN(C(=O)Nc3cc(NCCOC)c(cn3)C#N)c2nc1C=O)C(C)=O
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n/an/a 0.900n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEI...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c01019
BindingDB Entry DOI: 10.7270/Q2FB56MJ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM50559128
PNG
(CHEMBL4742811)
Show SMILES COCCNc1cc(NC(=O)N2CCCc3cc(C(F)F)c(C=O)nc23)ncc1C#N
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n/an/a 0.900n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEI...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c01019
BindingDB Entry DOI: 10.7270/Q2FB56MJ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM50559108
PNG
(CHEMBL4745615)
Show SMILES COCCOc1cc(NC(=O)N2CCCc3cc(CN4CC[C@H](N(C)C)C4=O)c(C=O)nc23)ncc1C#N |r|
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n/an/a 0.900n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEI...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c01019
BindingDB Entry DOI: 10.7270/Q2FB56MJ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM597749
PNG
((R)—N-(5-Cyano-4-((2-methoxyethyl)amino)pyridin-2-...)
Show SMILES COCCNc1cc(NC(=O)N2CCCc3cc(CN(C)C(=O)[C@H]4CCCO4)c(C=O)nc23)ncc1C#N |r|
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TBA

Assay Description
In this experiment, the inhibitory effect of the compounds on FGFR4 kinase activity was tested by a fluorescence resonance energy transfer (TR-FRET) ...

Citation and Details

BindingDB Entry DOI: 10.7270/Q21V5JWQ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM50559111
PNG
(CHEMBL4791610)
Show SMILES COCCOc1cc(NC(=O)N2CCCc3cc(CN(C)C(=O)CN(C)C)c(C=O)nc23)ncc1C#N
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TBA

Assay Description
Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEI...

Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c01019
BindingDB Entry DOI: 10.7270/Q2FB56MJ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM339838
PNG
(US9757364, Compound 39)
Show SMILES COc1cc(OC)cc(c1)N(Cc1c[nH]cn1)c1ccc2ncc(cc2n1)-c1cnn(C)c1
Show InChI InChI=1S/C24H23N7O2/c1-30-13-17(11-28-30)16-6-23-22(26-10-16)4-5-24(29-23)31(14-18-12-25-15-27-18)19-7-20(32-2)9-21(8-19)33-3/h4-13,15H,14H2,1-3H3,(H,25,27)
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n/an/a 0.912n/an/an/an/an/an/a



ASTEX THERAPEUTICS LTD

US Patent


Assay Description
In a final reaction volume of 30 μL, FGFR4 (h) (60 ng/ml) was incubated with 50 mM HEPES pH 7.5, 6 mM MnCl2, 1 mM DTT, 0.1 mM Na3VO4, 0.01% Trit...

US Patent US9757364 (2017)


BindingDB Entry DOI: 10.7270/Q2SB47VT
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM50509954
PNG
(CHEMBL4446965 | US11608332, Example 46)
Show SMILES COCCNc1cc(NC(=O)N2CCCc3cc(CN4CC[C@H](OC)C4=O)c(C=O)nc23)ncc1C#N |r|
Show InChI InChI=1S/C25H29N7O5/c1-36-9-6-27-19-11-22(28-13-18(19)12-26)30-25(35)32-7-3-4-16-10-17(20(15-33)29-23(16)32)14-31-8-5-21(37-2)24(31)34/h10-11,13,15,21H,3-9,14H2,1-2H3,(H2,27,28,30,35)/t21-/m0/s1
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TBA

Assay Description
In this experiment, the inhibitory effect of the compounds on FGFR4 kinase activity was tested by a fluorescence resonance energy transfer (TR-FRET) ...

Citation and Details

BindingDB Entry DOI: 10.7270/Q21V5JWQ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM50509955
PNG
(CHEMBL4518346 | US11608332, Example 45)
Show SMILES COCCNc1cc(NC(=O)N2CCCc3cc(CN4CC[C@@H](OC)C4=O)c(C=O)nc23)ncc1C#N |r|
Show InChI InChI=1S/C25H29N7O5/c1-36-9-6-27-19-11-22(28-13-18(19)12-26)30-25(35)32-7-3-4-16-10-17(20(15-33)29-23(16)32)14-31-8-5-21(37-2)24(31)34/h10-11,13,15,21H,3-9,14H2,1-2H3,(H2,27,28,30,35)/t21-/m1/s1
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TBA

Assay Description
In this experiment, the inhibitory effect of the compounds on FGFR4 kinase activity was tested by a fluorescence resonance energy transfer (TR-FRET) ...

Citation and Details

BindingDB Entry DOI: 10.7270/Q21V5JWQ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM339850
PNG
(US9757364, Compound 49)
Show SMILES COc1cc(OC)c(F)c(N(Cc2nnc[nH]2)c2ccc3ncc(cc3n2)-c2cnn(C)c2)c1F
Show InChI InChI=1S/C23H20F2N8O2/c1-32-10-14(9-29-32)13-6-16-15(26-8-13)4-5-20(30-16)33(11-19-27-12-28-31-19)23-21(24)17(34-2)7-18(35-3)22(23)25/h4-10,12H,11H2,1-3H3,(H,27,28,31)
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n/an/a 0.933n/an/an/an/an/an/a



ASTEX THERAPEUTICS LTD

US Patent


Assay Description
In a final reaction volume of 30 μL, FGFR4 (h) (60 ng/ml) was incubated with 50 mM HEPES pH 7.5, 6 mM MnCl2, 1 mM DTT, 0.1 mM Na3VO4, 0.01% Trit...

US Patent US9757364 (2017)


BindingDB Entry DOI: 10.7270/Q2SB47VT
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM50509949
PNG
(CHEMBL4475216 | US11667631, Example 29)
Show SMILES COC[C@@H](C)Nc1cc(NC(=O)N2CCCc3cc(CN4CCCCOC4=O)c(C=O)nc23)ncc1C#N |r|
Show InChI InChI=1S/C26H31N7O5/c1-17(16-37-2)29-21-11-23(28-13-20(21)12-27)31-25(35)33-8-5-6-18-10-19(22(15-34)30-24(18)33)14-32-7-3-4-9-38-26(32)36/h10-11,13,15,17H,3-9,14,16H2,1-2H3,(H2,28,29,31,35)/t17-/m1/s1
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TBA



Citation and Details

BindingDB Entry DOI: 10.7270/Q2CJ8JDK
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM604926
PNG
(N-(5-Cyano-4-(((trans)-4-methoxytetrahydrofuran-3-...)
Show SMILES CO[C@H]1COCC1Nc1cc(NC(=O)N2CCCc3cc(CN4CCOCC4=O)c(C=O)nc23)ncc1C#N |r|
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TBA



Citation and Details

BindingDB Entry DOI: 10.7270/Q2CJ8JDK
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM597813
PNG
(N-(5-Cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-...)
Show SMILES COCCNc1cc(NC(=O)N2CCCc3cc(CN(C)C(=O)C4CCOCC4)c(C=O)nc23)ncc1C#N
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n/an/a 0.980n/an/an/an/an/an/a


TBA

Assay Description
In this experiment, the inhibitory effect of the compounds on FGFR4 kinase activity was tested by a fluorescence resonance energy transfer (TR-FRET) ...

Citation and Details

BindingDB Entry DOI: 10.7270/Q21V5JWQ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM50509963
PNG
(CHEMBL4439119 | US11667631, Example 60)
Show SMILES CO[C@@H]1CCC[C@H]1Nc1cc(NC(=O)N2CCCc3cc(CN4CCOCC4=O)c(C=O)nc23)ncc1C#N |r|
Show InChI InChI=1S/C27H31N7O5/c1-38-23-6-2-5-20(23)30-21-11-24(29-13-19(21)12-28)32-27(37)34-7-3-4-17-10-18(22(15-35)31-26(17)34)14-33-8-9-39-16-25(33)36/h10-11,13,15,20,23H,2-9,14,16H2,1H3,(H2,29,30,32,37)/t20-,23-/m1/s1
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TBA



Citation and Details

BindingDB Entry DOI: 10.7270/Q2CJ8JDK
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM249401
PNG
(US10537571, Compound 114 | US10912774, Compound 11...)
Show SMILES COc1cc(OC)c(Cl)c(NC(=O)N(C)c2cc(Nc3ccccc3NC(=O)C#C)ncn2)c1Cl
Show InChI InChI=1S/C23H20Cl2N6O4/c1-5-19(32)29-14-9-7-6-8-13(14)28-17-11-18(27-12-26-17)31(2)23(33)30-22-20(24)15(34-3)10-16(35-4)21(22)25/h1,6-12H,2-4H3,(H,29,32)(H,30,33)(H,26,27,28)
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n/an/a<1n/an/an/an/a7.525



EISAI R&D MANAGEMENT CO., LTD.

US Patent


Assay Description
Compounds were profiled for FGFR inhibition activity at Reaction Biology Corporation (Malvern, Pa.) with their Kinase HotSpot assay. See, Anastassiad...

US Patent US9434697 (2016)


BindingDB Entry DOI: 10.7270/Q2K07351
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM249403
PNG
(US10537571, Compound 120 | US10912774, Compound 12...)
Show SMILES COc1cc(OC)c(Cl)c(NC(=O)N(CCCN(C)C)c2cc(Nc3ccccc3NC(=O)C=C)ncn2)c1Cl
Show InChI InChI=1S/C27H31Cl2N7O4/c1-6-23(37)33-18-11-8-7-10-17(18)32-21-15-22(31-16-30-21)36(13-9-12-35(2)3)27(38)34-26-24(28)19(39-4)14-20(40-5)25(26)29/h6-8,10-11,14-16H,1,9,12-13H2,2-5H3,(H,33,37)(H,34,38)(H,30,31,32)
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n/an/a<1n/an/an/an/a7.525



EISAI R&D MANAGEMENT CO., LTD.

US Patent


Assay Description
Compounds were profiled for FGFR inhibition activity at Reaction Biology Corporation (Malvern, Pa.) with their Kinase HotSpot assay. See, Anastassiad...

US Patent US9434697 (2016)


BindingDB Entry DOI: 10.7270/Q2K07351
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM249404
PNG
(US10537571, Compound 121 | US10912774, Compound 12...)
Show SMILES COc1cc(OC)c(Cl)c(NC(=O)N(CCCN2CCN(C)CC2)c2cc(Nc3ccccc3NC(=O)C=C)ncn2)c1Cl
Show InChI InChI=1S/C30H36Cl2N8O4/c1-5-26(41)36-21-10-7-6-9-20(21)35-24-18-25(34-19-33-24)40(12-8-11-39-15-13-38(2)14-16-39)30(42)37-29-27(31)22(43-3)17-23(44-4)28(29)32/h5-7,9-10,17-19H,1,8,11-16H2,2-4H3,(H,36,41)(H,37,42)(H,33,34,35)
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n/an/a<1n/an/an/an/a7.525



EISAI R&D MANAGEMENT CO., LTD.

US Patent


Assay Description
Compounds were profiled for FGFR inhibition activity at Reaction Biology Corporation (Malvern, Pa.) with their Kinase HotSpot assay. See, Anastassiad...

US Patent US9434697 (2016)


BindingDB Entry DOI: 10.7270/Q2K07351
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM249405
PNG
(US10537571, Compound 122 | US10912774, Compound 12...)
Show SMILES COc1cc(OC)c(Cl)c(NC(=O)N(C)c2cc(Nc3ccc(cc3NC(=O)C=C)C3CCNCC3)ncn2)c1Cl
Show InChI InChI=1S/C28H31Cl2N7O4/c1-5-24(38)35-19-12-17(16-8-10-31-11-9-16)6-7-18(19)34-22-14-23(33-15-32-22)37(2)28(39)36-27-25(29)20(40-3)13-21(41-4)26(27)30/h5-7,12-16,31H,1,8-11H2,2-4H3,(H,35,38)(H,36,39)(H,32,33,34)
PDB

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UniProtKB/SwissProt

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UniChem
US Patent
n/an/a<1n/an/an/an/a7.525



EISAI R&D MANAGEMENT CO., LTD.

US Patent


Assay Description
Compounds were profiled for FGFR inhibition activity at Reaction Biology Corporation (Malvern, Pa.) with their Kinase HotSpot assay. See, Anastassiad...

US Patent US9434697 (2016)


BindingDB Entry DOI: 10.7270/Q2K07351
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM249406
PNG
(US10537571, Compound 123 | US10912774, Compound 12...)
Show SMILES COc1cc(OC)c(Cl)c(NC(=O)N(C)c2cc(Nc3ccc(cc3NC(=O)C=C)N3CCOCC3)ncn2)c1Cl
Show InChI InChI=1S/C27H29Cl2N7O5/c1-5-23(37)33-18-12-16(36-8-10-41-11-9-36)6-7-17(18)32-21-14-22(31-15-30-21)35(2)27(38)34-26-24(28)19(39-3)13-20(40-4)25(26)29/h5-7,12-15H,1,8-11H2,2-4H3,(H,33,37)(H,34,38)(H,30,31,32)
PDB

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UniProtKB/SwissProt

DrugBank
antibodypedia
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PC cid
PC sid
UniChem
US Patent
n/an/a<1n/an/an/an/a7.525



EISAI R&D MANAGEMENT CO., LTD.

US Patent


Assay Description
Compounds were profiled for FGFR inhibition activity at Reaction Biology Corporation (Malvern, Pa.) with their Kinase HotSpot assay. See, Anastassiad...

US Patent US9434697 (2016)


BindingDB Entry DOI: 10.7270/Q2K07351
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM249407
PNG
(US10537571, Compound 124 | US10912774, Compound 12...)
Show SMILES COc1cc(OC)c(Cl)c(NC(=O)N(C)c2cc(Nc3ccc(cc3NC(=O)C=C)N3C[C@H](C)N[C@H](C)C3)ncn2)c1Cl |r|
Show InChI InChI=1S/C29H34Cl2N8O4/c1-7-25(40)36-20-10-18(39-13-16(2)34-17(3)14-39)8-9-19(20)35-23-12-24(33-15-32-23)38(4)29(41)37-28-26(30)21(42-5)11-22(43-6)27(28)31/h7-12,15-17,34H,1,13-14H2,2-6H3,(H,36,40)(H,37,41)(H,32,33,35)/t16-,17+
PDB

KEGG

UniProtKB/SwissProt

DrugBank
antibodypedia
GoogleScholar
AffyNet 
PC cid
PC sid
UniChem
US Patent
n/an/a<1n/an/an/an/a7.525



EISAI R&D MANAGEMENT CO., LTD.

US Patent


Assay Description
Compounds were profiled for FGFR inhibition activity at Reaction Biology Corporation (Malvern, Pa.) with their Kinase HotSpot assay. See, Anastassiad...

US Patent US9434697 (2016)


BindingDB Entry DOI: 10.7270/Q2K07351
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(Homo sapiens (Human))		BDBM249408
PNG
(US10537571, Compound 125 | US10912774, Compound 12...)
Show SMILES COc1cc(OC)c(Cl)c(NC(=O)N(C)c2cc(Nc3ccc(cc3NC(=O)C=C)N3CCN(CC3)S(C)(=O)=O)ncn2)c1Cl
Show InChI InChI=1S/C28H32Cl2N8O6S/c1-6-24(39)34-19-13-17(37-9-11-38(12-10-37)45(5,41)42)7-8-18(19)33-22-15-23(32-16-31-22)36(2)28(40)35-27-25(29)20(43-3)14-21(44-4)26(27)30/h6-8,13-16H,1,9-12H2,2-5H3,(H,34,39)(H,35,40)(H,31,32,33)
PDB

KEGG

UniProtKB/SwissProt

DrugBank
antibodypedia
GoogleScholar
AffyNet 
PC cid
PC sid
UniChem
US Patent
n/an/a<1n/an/an/an/a7.525



EISAI R&D MANAGEMENT CO., LTD.

US Patent


Assay Description
Compounds were profiled for FGFR inhibition activity at Reaction Biology Corporation (Malvern, Pa.) with their Kinase HotSpot assay. See, Anastassiad...

US Patent US9434697 (2016)


BindingDB Entry DOI: 10.7270/Q2K07351
More data for this
Ligand-Target Pair
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