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Compile Data Set for Download or QSAR

Found 1728 hits Enz. Inhib. hit(s) with Target = 'Fibroblast growth factor receptor 2'   
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))
BDBM50198782
PNG
(([7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]tri...)
Show SMILES Cc1cc(cc2nnc(Nc3ccc(OCCN4CCCC4)cc3)nc12)-c1c(Cl)cccc1Cl
Show InChI InChI=1S/C26H25Cl2N5O/c1-17-15-18(24-21(27)5-4-6-22(24)28)16-23-25(17)30-26(32-31-23)29-19-7-9-20(10-8-19)34-14-13-33-11-2-3-12-33/h4-10,15-16H,2-3,11-14H2,1H3,(H,29,30,32)
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493n/an/an/an/an/an/an/an/a



TargeGen, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR2


Bioorg Med Chem Lett 17: 602-8 (2007)


Article DOI: 10.1016/j.bmcl.2006.11.006
BindingDB Entry DOI: 10.7270/Q29024MW
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50237710
PNG
(4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifl...)
Show SMILES Cc1cn(cn1)-c1cc(NC(=O)c2ccc(C)c(Nc3nccc(n3)-c3cccnc3)c2)cc(c1)C(F)(F)F
Show InChI InChI=1S/C28H22F3N7O/c1-17-5-6-19(10-25(17)37-27-33-9-7-24(36-27)20-4-3-8-32-14-20)26(39)35-22-11-21(28(29,30)31)12-23(13-22)38-15-18(2)34-16-38/h3-16H,1-2H3,(H,35,39)(H,33,36,37)
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7.22E+3n/an/an/an/an/an/an/an/a



Genomics Institute of the Novartis Research Foundation

Curated by PDSP Ki Database




Proc Natl Acad Sci U S A 103: 3153-8 (2006)


Article DOI: 10.1073/pnas.0511292103
BindingDB Entry DOI: 10.7270/Q21Z430B
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM13530
PNG
(4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[...)
Show SMILES CN1CCN(Cc2ccc(cc2)C(=O)Nc2ccc(C)c(Nc3nccc(n3)-c3cccnc3)c2)CC1
Show InChI InChI=1S/C29H31N7O/c1-21-5-10-25(18-27(21)34-29-31-13-11-26(33-29)24-4-3-12-30-19-24)32-28(37)23-8-6-22(7-9-23)20-36-16-14-35(2)15-17-36/h3-13,18-19H,14-17,20H2,1-2H3,(H,32,37)(H,31,33,34)
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>1.00E+4n/an/an/an/an/an/an/an/a



Genomics Institute of the Novartis Research Foundation

Curated by PDSP Ki Database




Proc Natl Acad Sci U S A 103: 3153-8 (2006)


Article DOI: 10.1073/pnas.0511292103
BindingDB Entry DOI: 10.7270/Q21Z430B
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166749
PNG
(CHEMBL3799403)
Show SMILES COc1cc(CCc2cc(Nc3ncnc4cc(ccc34)N3CCN(CC3)C(C)C)n[nH]2)cc(OC)c1
Show InChI InChI=1S/C28H35N7O2/c1-19(2)34-9-11-35(12-10-34)22-7-8-25-26(16-22)29-18-30-28(25)31-27-15-21(32-33-27)6-5-20-13-23(36-3)17-24(14-20)37-4/h7-8,13-19H,5-6,9-12H2,1-4H3,(H2,29,30,31,32,33)
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n/an/a<0.100n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 in human SNU16 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166744
PNG
(CHEMBL3798625)
Show SMILES COc1cc(CCc2cc(Nc3ncnc4cc(ccc34)N3C[C@H](C)N(C)[C@H](C)C3)n[nH]2)cc(OC)c1
Show InChI InChI=1S/C28H35N7O2/c1-18-15-35(16-19(2)34(18)3)22-8-9-25-26(13-22)29-17-30-28(25)31-27-12-21(32-33-27)7-6-20-10-23(36-4)14-24(11-20)37-5/h8-14,17-19H,6-7,15-16H2,1-5H3,(H2,29,30,31,32,33)/t18-,19+
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n/an/a<0.100n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 in human SNU16 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166748
PNG
(CHEMBL3799426)
Show SMILES COc1cc(CCc2cc(Nc3ncnc4cc(ccc34)N3CCN(CC3)C3CCC3)n[nH]2)cc(OC)c1
Show InChI InChI=1S/C29H35N7O2/c1-37-24-14-20(15-25(18-24)38-2)6-7-21-16-28(34-33-21)32-29-26-9-8-23(17-27(26)30-19-31-29)36-12-10-35(11-13-36)22-4-3-5-22/h8-9,14-19,22H,3-7,10-13H2,1-2H3,(H2,30,31,32,33,34)
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n/an/a<0.100n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 in human SNU16 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM339807
PNG
(US9757364, Compound 11)
Show SMILES COc1cc(OC)cc(c1)N(CCCO)c1ccc2ncc(-c3cnn(C)c3)c(Cl)c2n1
Show InChI InChI=1S/C23H24ClN5O3/c1-28-14-15(12-26-28)19-13-25-20-5-6-21(27-23(20)22(19)24)29(7-4-8-30)16-9-17(31-2)11-18(10-16)32-3/h5-6,9-14,30H,4,7-8H2,1-3H3
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US Patent
n/an/a 0.126n/an/an/an/an/an/a



ASTEX THERAPEUTICS LTD

US Patent


Assay Description
In a final reaction volume of 30 μL, FGFR2 (h) (150 ng/ml) was incubated with 50 mM HEPES pH 7.5, 6 mM MnCl2, 1 mM DTT, 0.1 mM Na3VO4, 0.01% Tri...


US Patent US9757364 (2017)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166610
PNG
(CHEMBL3800526)
Show SMILES COc1cc(CCc2cc(Nc3ncnc4cc(ccc34)N3CCN4CCCCC4C3)n[nH]2)cc(OC)c1
Show InChI InChI=1S/C29H35N7O2/c1-37-24-13-20(14-25(17-24)38-2)6-7-21-15-28(34-33-21)32-29-26-9-8-22(16-27(26)30-19-31-29)36-12-11-35-10-4-3-5-23(35)18-36/h8-9,13-17,19,23H,3-7,10-12,18H2,1-2H3,(H2,30,31,32,33,34)
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n/an/a 0.200n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166744
PNG
(CHEMBL3798625)
Show SMILES COc1cc(CCc2cc(Nc3ncnc4cc(ccc34)N3C[C@H](C)N(C)[C@H](C)C3)n[nH]2)cc(OC)c1
Show InChI InChI=1S/C28H35N7O2/c1-18-15-35(16-19(2)34(18)3)22-8-9-25-26(13-22)29-17-30-28(25)31-27-12-21(32-33-27)7-6-20-10-23(36-4)14-24(11-20)37-5/h8-14,17-19H,6-7,15-16H2,1-5H3,(H2,29,30,31,32,33)/t18-,19+
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n/an/a 0.200n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM161453
PNG
(US10124003, Ex. Compound 66 | US9108973, 66)
Show SMILES COC(=O)[C@@H]1C[C@@H](CN1C(=O)C=C)n1cc(C#Cc2cc(OC)cc(OC)c2)c2c(N)ncnc12
Show InChI InChI=1S/C25H25N5O5/c1-5-21(31)30-13-17(10-20(30)25(32)35-4)29-12-16(22-23(26)27-14-28-24(22)29)7-6-15-8-18(33-2)11-19(9-15)34-3/h5,8-9,11-12,14,17,20H,1,10,13H2,2-4H3,(H2,26,27,28)/t17-,20-/m0/s1
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n/an/a<0.300n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
When setting conditions for the measurement of the inhibitory effect of the compounds on FGFR2 kinase activity, FL-Peptide 22 (Caliper Life Sciences,...


US Patent US10124003 (2018)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50234570
PNG
(CHEMBL4091628)
Show SMILES CN1CCN(Cc2ccc(NC(=O)c3ccc(Cl)c(c3)C#Cc3cncc(c3)N3CCOCC3)cc2C(F)(F)F)CC1
Show InChI InChI=1S/C31H31ClF3N5O2/c1-38-8-10-39(11-9-38)21-25-4-6-26(18-28(25)31(33,34)35)37-30(41)24-5-7-29(32)23(17-24)3-2-22-16-27(20-36-19-22)40-12-14-42-15-13-40/h4-7,16-20H,8-15,21H2,1H3,(H,37,41)
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n/an/a 0.300n/an/an/an/an/an/a



Chinese Academy of Sciences

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA


Eur J Med Chem 126: 122-132 (2017)


Article DOI: 10.1016/j.ejmech.2016.10.003
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166738
PNG
(CHEMBL3797845)
Show SMILES COc1cc(CCc2cc(Nc3ncnc4cc(ccc34)N3CCC(CC3)N(C)C)n[nH]2)cc(OC)c1
Show InChI InChI=1S/C28H35N7O2/c1-34(2)21-9-11-35(12-10-21)22-7-8-25-26(16-22)29-18-30-28(25)31-27-15-20(32-33-27)6-5-19-13-23(36-3)17-24(14-19)37-4/h7-8,13-18,21H,5-6,9-12H2,1-4H3,(H2,29,30,31,32,33)
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n/an/a 0.300n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM161453
PNG
(US10124003, Ex. Compound 66 | US9108973, 66)
Show SMILES COC(=O)[C@@H]1C[C@@H](CN1C(=O)C=C)n1cc(C#Cc2cc(OC)cc(OC)c2)c2c(N)ncnc12
Show InChI InChI=1S/C25H25N5O5/c1-5-21(31)30-13-17(10-20(30)25(32)35-4)29-12-16(22-23(26)27-14-28-24(22)29)7-6-15-8-18(33-2)11-19(9-15)34-3/h5,8-9,11-12,14,17,20H,1,10,13H2,2-4H3,(H2,26,27,28)/t17-,20-/m0/s1
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n/an/a<0.300n/an/an/an/a7.525



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
When setting conditions for the measurement of the inhibitory effect of the compounds on FGFR2 kinase activity, FL-Peptide 22 (Caliper Life Sciences,...


US Patent US9108973 (2015)


BindingDB Entry DOI: 10.7270/Q2XW4HJV
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM161438
PNG
(US10124003, Ex. Compound 51 | US9108973, 51)
Show SMILES COc1cc(OC)cc(c1)C#CC1=CN(C2CN(C2)C(=O)C=C)C2N=CN=C(N)C12
Show InChI InChI=1S/C22H23N5O3/c1-4-19(28)26-11-16(12-26)27-10-15(20-21(23)24-13-25-22(20)27)6-5-14-7-17(29-2)9-18(8-14)30-3/h4,7-10,13,16,20,22H,1,11-12H2,2-3H3,(H2,23,24,25)
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n/an/a<0.300n/an/an/an/a7.525



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
When setting conditions for the measurement of the inhibitory effect of the compounds on FGFR2 kinase activity, FL-Peptide 22 (Caliper Life Sciences,...


US Patent US9108973 (2015)


BindingDB Entry DOI: 10.7270/Q2XW4HJV
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166608
PNG
(CHEMBL3797507)
Show SMILES CCN1CCN(CC1)c1ccc2c(Nc3cc(CCc4c(Cl)c(OC)cc(OC)c4Cl)[nH]n3)ncnc2c1
Show InChI InChI=1S/C27H31Cl2N7O2/c1-4-35-9-11-36(12-10-35)18-6-8-19-21(14-18)30-16-31-27(19)32-24-13-17(33-34-24)5-7-20-25(28)22(37-2)15-23(38-3)26(20)29/h6,8,13-16H,4-5,7,9-12H2,1-3H3,(H2,30,31,32,33,34)
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n/an/a 0.300n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM161438
PNG
(US10124003, Ex. Compound 51 | US9108973, 51)
Show SMILES COc1cc(OC)cc(c1)C#CC1=CN(C2CN(C2)C(=O)C=C)C2N=CN=C(N)C12
Show InChI InChI=1S/C22H23N5O3/c1-4-19(28)26-11-16(12-26)27-10-15(20-21(23)24-13-25-22(20)27)6-5-14-7-17(29-2)9-18(8-14)30-3/h4,7-10,13,16,20,22H,1,11-12H2,2-3H3,(H2,23,24,25)
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n/an/a<0.300n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
When setting conditions for the measurement of the inhibitory effect of the compounds on FGFR2 kinase activity, FL-Peptide 22 (Caliper Life Sciences,...


US Patent US10124003 (2018)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166610
PNG
(CHEMBL3800526)
Show SMILES COc1cc(CCc2cc(Nc3ncnc4cc(ccc34)N3CCN4CCCCC4C3)n[nH]2)cc(OC)c1
Show InChI InChI=1S/C29H35N7O2/c1-37-24-13-20(14-25(17-24)38-2)6-7-21-15-28(34-33-21)32-29-26-9-8-22(16-27(26)30-19-31-29)36-12-11-35-10-4-3-5-23(35)18-36/h8-9,13-17,19,23H,3-7,10-12,18H2,1-2H3,(H2,30,31,32,33,34)
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n/an/a<0.400n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of FGFR2 in human KATO III cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM161419
PNG
(US10124003, Ex. Compound 32 | US9108973, 32)
Show SMILES COc1cc(OC)cc(c1)C#Cc1nn([C@H]2C[C@@H](C#C)N(C2)C(=O)C=C)c2ncnc(N)c12
Show InChI InChI=1S/C24H22N6O3/c1-5-16-11-17(13-29(16)21(31)6-2)30-24-22(23(25)26-14-27-24)20(28-30)8-7-15-9-18(32-3)12-19(10-15)33-4/h1,6,9-10,12,14,16-17H,2,11,13H2,3-4H3,(H2,25,26,27)/t16-,17+/m1/s1
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n/an/a 0.400n/an/an/an/a7.525



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
When setting conditions for the measurement of the inhibitory effect of the compounds on FGFR2 kinase activity, FL-Peptide 22 (Caliper Life Sciences,...


US Patent US9108973 (2015)


BindingDB Entry DOI: 10.7270/Q2XW4HJV
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM161426
PNG
(US10124003, Ex. Compound 39 | US9108973, 39 | US91...)
Show SMILES COc1cc(OC)cc(c1)C#Cc1cn([C@H]2CCN(C2)C(=O)C=C)c2ncnc(N)c12
Show InChI InChI=1S/C23H23N5O3/c1-4-20(29)27-8-7-17(13-27)28-12-16(21-22(24)25-14-26-23(21)28)6-5-15-9-18(30-2)11-19(10-15)31-3/h4,9-12,14,17H,1,7-8,13H2,2-3H3,(H2,24,25,26)/t17-/m0/s1
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n/an/a 0.400n/an/an/an/a7.525



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
When setting conditions for the measurement of the inhibitory effect of the compounds on FGFR2 kinase activity, FL-Peptide 22 (Caliper Life Sciences,...


US Patent US9108973 (2015)


BindingDB Entry DOI: 10.7270/Q2XW4HJV
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM161419
PNG
(US10124003, Ex. Compound 32 | US9108973, 32)
Show SMILES COc1cc(OC)cc(c1)C#Cc1nn([C@H]2C[C@@H](C#C)N(C2)C(=O)C=C)c2ncnc(N)c12
Show InChI InChI=1S/C24H22N6O3/c1-5-16-11-17(13-29(16)21(31)6-2)30-24-22(23(25)26-14-27-24)20(28-30)8-7-15-9-18(32-3)12-19(10-15)33-4/h1,6,9-10,12,14,16-17H,2,11,13H2,3-4H3,(H2,25,26,27)/t16-,17+/m1/s1
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n/an/a 0.400n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
When setting conditions for the measurement of the inhibitory effect of the compounds on FGFR2 kinase activity, FL-Peptide 22 (Caliper Life Sciences,...


US Patent US10124003 (2018)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166736
PNG
(CHEMBL3797594)
Show SMILES COc1cc(CCc2cc(Nc3ncnc4cc(ccc34)N3CCC(C3)N(C)C)n[nH]2)cc(OC)c1
Show InChI InChI=1S/C27H33N7O2/c1-33(2)21-9-10-34(16-21)20-7-8-24-25(14-20)28-17-29-27(24)30-26-13-19(31-32-26)6-5-18-11-22(35-3)15-23(12-18)36-4/h7-8,11-15,17,21H,5-6,9-10,16H2,1-4H3,(H2,28,29,30,31,32)
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n/an/a 0.400n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166655
PNG
(CHEMBL3798342)
Show SMILES COc1cc(CCc2cc(Nc3ncnc4cc(ccc34)N3CCOCC3)n[nH]2)cc(OC)c1
Show InChI InChI=1S/C25H28N6O3/c1-32-20-11-17(12-21(15-20)33-2)3-4-18-13-24(30-29-18)28-25-22-6-5-19(14-23(22)26-16-27-25)31-7-9-34-10-8-31/h5-6,11-16H,3-4,7-10H2,1-2H3,(H2,26,27,28,29,30)
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n/an/a 0.400n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM161426
PNG
(US10124003, Ex. Compound 39 | US9108973, 39 | US91...)
Show SMILES COc1cc(OC)cc(c1)C#Cc1cn([C@H]2CCN(C2)C(=O)C=C)c2ncnc(N)c12
Show InChI InChI=1S/C23H23N5O3/c1-4-20(29)27-8-7-17(13-27)28-12-16(21-22(24)25-14-26-23(21)28)6-5-15-9-18(30-2)11-19(10-15)31-3/h4,9-12,14,17H,1,7-8,13H2,2-3H3,(H2,24,25,26)/t17-/m0/s1
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n/an/a 0.400n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
When setting conditions for the measurement of the inhibitory effect of the compounds on FGFR2 kinase activity, FL-Peptide 22 (Caliper Life Sciences,...


US Patent US10124003 (2018)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166609
PNG
(CHEMBL3797416)
Show SMILES CCN1CCN(CC1)c1ccc2c(Nc3cc(CCc4cc(OC)cc(OC)c4)[nH]n3)nc(CC)nc2c1
Show InChI InChI=1S/C29H37N7O2/c1-5-27-30-26-18-22(36-13-11-35(6-2)12-14-36)9-10-25(26)29(31-27)32-28-17-21(33-34-28)8-7-20-15-23(37-3)19-24(16-20)38-4/h9-10,15-19H,5-8,11-14H2,1-4H3,(H2,30,31,32,33,34)
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n/an/a 0.5n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166749
PNG
(CHEMBL3799403)
Show SMILES COc1cc(CCc2cc(Nc3ncnc4cc(ccc34)N3CCN(CC3)C(C)C)n[nH]2)cc(OC)c1
Show InChI InChI=1S/C28H35N7O2/c1-19(2)34-9-11-35(12-10-34)22-7-8-25-26(16-22)29-18-30-28(25)31-27-15-21(32-33-27)6-5-20-13-23(36-3)17-24(14-20)37-4/h7-8,13-19H,5-6,9-12H2,1-4H3,(H2,29,30,31,32,33)
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n/an/a 0.600n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM161440
PNG
(US10124003, Ex. Compound 53 | US9108973, 53)
Show SMILES COc1cc(OC)cc(c1)C#Cc1cn(C2CN(C2)C(=O)\C=C\CN2CCCC2)c2ncnc(N)c12
Show InChI InChI=1S/C27H30N6O3/c1-35-22-12-19(13-23(14-22)36-2)7-8-20-15-33(27-25(20)26(28)29-18-30-27)21-16-32(17-21)24(34)6-5-11-31-9-3-4-10-31/h5-6,12-15,18,21H,3-4,9-11,16-17H2,1-2H3,(H2,28,29,30)/b6-5+
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n/an/a 0.600n/an/an/an/a7.525



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
When setting conditions for the measurement of the inhibitory effect of the compounds on FGFR2 kinase activity, FL-Peptide 22 (Caliper Life Sciences,...


US Patent US9108973 (2015)


BindingDB Entry DOI: 10.7270/Q2XW4HJV
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166748
PNG
(CHEMBL3799426)
Show SMILES COc1cc(CCc2cc(Nc3ncnc4cc(ccc34)N3CCN(CC3)C3CCC3)n[nH]2)cc(OC)c1
Show InChI InChI=1S/C29H35N7O2/c1-37-24-14-20(15-25(18-24)38-2)6-7-21-16-28(34-33-21)32-29-26-9-8-23(17-27(26)30-19-31-29)36-12-10-35(11-13-36)22-4-3-5-22/h8-9,14-19,22H,3-7,10-13H2,1-2H3,(H2,30,31,32,33,34)
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n/an/a 0.600n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166643
PNG
(CHEMBL3799093)
Show SMILES CCN1CCN(CC1)c1ccc2c(Nc3cc(CCc4cc(OC)cc(OC)c4)[nH]n3)nc(Cl)nc2c1
Show InChI InChI=1S/C27H32ClN7O2/c1-4-34-9-11-35(12-10-34)20-7-8-23-24(16-20)29-27(28)31-26(23)30-25-15-19(32-33-25)6-5-18-13-21(36-2)17-22(14-18)37-3/h7-8,13-17H,4-6,9-12H2,1-3H3,(H2,29,30,31,32,33)
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n/an/a 0.600n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166839
PNG
(CHEMBL3799611)
Show SMILES CCN1CCN(CC1)c1ccc2c(Nc3cc(CCc4cc(OC)cc(OC)c4)[nH]n3)nc(C)nc2c1
Show InChI InChI=1S/C28H35N7O2/c1-5-34-10-12-35(13-11-34)22-8-9-25-26(17-22)29-19(2)30-28(25)31-27-16-21(32-33-27)7-6-20-14-23(36-3)18-24(15-20)37-4/h8-9,14-18H,5-7,10-13H2,1-4H3,(H2,29,30,31,32,33)
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n/an/a 0.600n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM161440
PNG
(US10124003, Ex. Compound 53 | US9108973, 53)
Show SMILES COc1cc(OC)cc(c1)C#Cc1cn(C2CN(C2)C(=O)\C=C\CN2CCCC2)c2ncnc(N)c12
Show InChI InChI=1S/C27H30N6O3/c1-35-22-12-19(13-23(14-22)36-2)7-8-20-15-33(27-25(20)26(28)29-18-30-27)21-16-32(17-21)24(34)6-5-11-31-9-3-4-10-31/h5-6,12-15,18,21H,3-4,9-11,16-17H2,1-2H3,(H2,28,29,30)/b6-5+
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n/an/a 0.600n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
When setting conditions for the measurement of the inhibitory effect of the compounds on FGFR2 kinase activity, FL-Peptide 22 (Caliper Life Sciences,...


US Patent US10124003 (2018)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(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 0.603n/an/an/an/an/an/a



ASTEX THERAPEUTICS LTD

US Patent


Assay Description
In a final reaction volume of 30 μL, FGFR2 (h) (150 ng/ml) was incubated with 50 mM HEPES pH 7.5, 6 mM MnCl2, 1 mM DTT, 0.1 mM Na3VO4, 0.01% Tri...


US Patent US9757364 (2017)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166747
PNG
(CHEMBL3798940)
Show SMILES COCCN1CCN(CC1)c1ccc2c(Nc3cc(CCc4cc(OC)cc(OC)c4)[nH]n3)ncnc2c1
Show InChI InChI=1S/C28H35N7O3/c1-36-13-12-34-8-10-35(11-9-34)22-6-7-25-26(17-22)29-19-30-28(25)31-27-16-21(32-33-27)5-4-20-14-23(37-2)18-24(15-20)38-3/h6-7,14-19H,4-5,8-13H2,1-3H3,(H2,29,30,31,32,33)
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n/an/a 0.700n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166823
PNG
(CHEMBL3799885)
Show SMILES CCCc1nc(Nc2cc(CCc3cc(OC)cc(OC)c3)[nH]n2)c2ccc(cc2n1)N1CCN(CC)CC1
Show InChI InChI=1S/C30H39N7O2/c1-5-7-28-31-27-19-23(37-14-12-36(6-2)13-15-37)10-11-26(27)30(32-28)33-29-18-22(34-35-29)9-8-21-16-24(38-3)20-25(17-21)39-4/h10-11,16-20H,5-9,12-15H2,1-4H3,(H2,31,32,33,34,35)
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n/an/a 0.700n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166740
PNG
(CHEMBL3797998)
Show SMILES COc1cc(CCc2cc(Nc3ncnc4cc(ccc34)N3CCCN(C)CC3)n[nH]2)cc(OC)c1
Show InChI InChI=1S/C27H33N7O2/c1-33-9-4-10-34(12-11-33)21-7-8-24-25(16-21)28-18-29-27(24)30-26-15-20(31-32-26)6-5-19-13-22(35-2)17-23(14-19)36-3/h7-8,13-18H,4-6,9-12H2,1-3H3,(H2,28,29,30,31,32)
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n/an/a 0.700n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166772
PNG
(CHEMBL3799354)
Show SMILES COc1cc(CCc2cc(Nc3ncnc4cc(ccc34)N3CCN(C)CC3)n[nH]2)cc(OC)c1
Show InChI InChI=1S/C14H19NO4/c1-19-10-4-2-9(3-5-10)8-15-11-6-7-12(16)14(18)13(11)17/h2-7,11-18H,8H2,1H3
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n/an/a 0.700n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 in human SNU16 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM339822
PNG
(US9757364, Compound 15)
Show SMILES COc1cc(OC)cc(c1)N(CCO)c1ccc2ncc(-c3cnn(C)c3)c(Cl)c2n1
Show InChI InChI=1S/C22H22ClN5O3/c1-27-13-14(11-25-27)18-12-24-19-4-5-20(26-22(19)21(18)23)28(6-7-29)15-8-16(30-2)10-17(9-15)31-3/h4-5,8-13,29H,6-7H2,1-3H3
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US Patent
n/an/a 0.759n/an/an/an/an/an/a



ASTEX THERAPEUTICS LTD

US Patent


Assay Description
In a final reaction volume of 30 μL, FGFR2 (h) (150 ng/ml) was incubated with 50 mM HEPES pH 7.5, 6 mM MnCl2, 1 mM DTT, 0.1 mM Na3VO4, 0.01% Tri...


US Patent US9757364 (2017)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166610
PNG
(CHEMBL3800526)
Show SMILES COc1cc(CCc2cc(Nc3ncnc4cc(ccc34)N3CCN4CCCCC4C3)n[nH]2)cc(OC)c1
Show InChI InChI=1S/C29H35N7O2/c1-37-24-13-20(14-25(17-24)38-2)6-7-21-15-28(34-33-21)32-29-26-9-8-22(16-27(26)30-19-31-29)36-12-11-35-10-4-3-5-23(35)18-36/h8-9,13-17,19,23H,3-7,10-12,18H2,1-2H3,(H2,30,31,32,33,34)
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n/an/a 0.800n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 in human SNU16 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166840
PNG
(CHEMBL3798997)
Show SMILES CCN1CCN(CC1)c1ccc2c(Nc3cc(CCc4cc(OC)cc(OC)c4)[nH]n3)ncnc2c1
Show InChI InChI=1S/C27H33N7O2/c1-4-33-9-11-34(12-10-33)21-7-8-24-25(16-21)28-18-29-27(24)30-26-15-20(31-32-26)6-5-19-13-22(35-2)17-23(14-19)36-3/h7-8,13-18H,4-6,9-12H2,1-3H3,(H2,28,29,30,31,32)
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n/an/a 0.800n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166656
PNG
(CHEMBL3800072)
Show SMILES COc1cc(CCc2cc(Nc3ncnc4cc(ccc34)C3CCN(C)CC3)n[nH]2)cc(OC)c1
Show InChI InChI=1S/C27H32N6O2/c1-33-10-8-19(9-11-33)20-5-7-24-25(14-20)28-17-29-27(24)30-26-15-21(31-32-26)6-4-18-12-22(34-2)16-23(13-18)35-3/h5,7,12-17,19H,4,6,8-11H2,1-3H3,(H2,28,29,30,31,32)
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n/an/a 0.800n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166612
PNG
(CHEMBL3798532)
Show SMILES COCCOc1ccc2c(Nc3cc(CCc4cc(OC)cc(OC)c4)[nH]n3)ncnc2c1
Show InChI InChI=1S/C24H27N5O4/c1-30-8-9-33-18-6-7-21-22(14-18)25-15-26-24(21)27-23-12-17(28-29-23)5-4-16-10-19(31-2)13-20(11-16)32-3/h6-7,10-15H,4-5,8-9H2,1-3H3,(H2,25,26,27,28,29)
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n/an/a 0.900n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166746
PNG
(CHEMBL3798911)
Show SMILES COc1cc(CCc2cc(Nc3ncnc4cc(ccc34)N3CCNC(C)(C)C3)n[nH]2)cc(OC)c1
Show InChI InChI=1S/C27H33N7O2/c1-27(2)16-34(10-9-30-27)20-7-8-23-24(14-20)28-17-29-26(23)31-25-13-19(32-33-25)6-5-18-11-21(35-3)15-22(12-18)36-4/h7-8,11-15,17,30H,5-6,9-10,16H2,1-4H3,(H2,28,29,31,32,33)
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n/an/a 0.900n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM342461
PNG
(US9776988, Example 21)
Show SMILES COc1cc(CCc2cc(n[nH]2)-c2nc3ccc(cc3[nH]2)N2CCN(CC2)C(=O)N2CCOCC2)cc(OC)c1
Show InChI InChI=1S/C29H33N7O4/c1-38-23-15-20(16-24(19-23)39-2)3-4-21-17-27(33-32-21)28-30-25-6-5-22(18-26(25)31-28)34-7-9-35(10-8-34)29(37)36-11-13-40-14-12-36/h5-6,15-19H,3-4,7-14H2,1-2H3/b28-27+
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n/an/a 0.950n/an/an/an/an/an/a



Celon Pharma S.A.

US Patent


Assay Description
The compounds were dissolved in 100% DMSO, and obtained solutions were serially diluted in reaction buffer (50 mM Tris pH 7.5, 10 mM MgCl2, 0.25 mM E...


US Patent US9776988 (2017)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50355393
PNG
(CHEMBL1834657 | US9434697, BGJ398 | US9730931, BGJ...)
Show SMILES CCN1CCN(CC1)c1ccc(Nc2cc(ncn2)N(C)C(=O)Nc2c(Cl)c(OC)cc(OC)c2Cl)cc1
Show InChI InChI=1S/C26H31Cl2N7O3/c1-5-34-10-12-35(13-11-34)18-8-6-17(7-9-18)31-21-15-22(30-16-29-21)33(2)26(36)32-25-23(27)19(37-3)14-20(38-4)24(25)28/h6-9,14-16H,5,10-13H2,1-4H3,(H,32,36)(H,29,30,31)
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n/an/a 1n/an/an/an/an/an/a



The First Affiliated Hospital of Zhengzhou University

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 (unknown origin) using peptidic substrates in presence of ATP by Kinase-Glo luminescent kinase assay


Eur J Med Chem 126: 476-490 (2017)


Article DOI: 10.1016/j.ejmech.2016.11.052
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50232830
PNG
(CHEMBL4092990)
Show SMILES COc1cc(OC)c(Cl)c(NC(=O)N(Cc2ccc(NC(=O)C=C)cc2)c2cc(Nc3ccc(cc3)N3CCN(C)CC3)ncn2)c1Cl
Show InChI InChI=1S/C34H36Cl2N8O4/c1-5-30(45)40-24-8-6-22(7-9-24)20-44(34(46)41-33-31(35)26(47-3)18-27(48-4)32(33)36)29-19-28(37-21-38-29)39-23-10-12-25(13-11-23)43-16-14-42(2)15-17-43/h5-13,18-19,21H,1,14-17,20H2,2-4H3,(H,40,45)(H,41,46)(H,37,38,39)
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n/an/a<1n/an/an/an/an/an/a



The First Affiliated Hospital of Zhengzhou University

Curated by ChEMBL


Assay Description
Inhibition of FGFR2 (unknown origin)


Eur J Med Chem 126: 476-490 (2017)


Article DOI: 10.1016/j.ejmech.2016.11.052
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM161439
PNG
(US10124003, Ex. Compound 52 | US9108973, 52 | US91...)
Show SMILES COc1cc(OC)cc(c1)C#Cc1cn(C2CN(C2)C(=O)\C=C\CN(C)C)c2ncnc(N)c12
Show InChI InChI=1S/C25H28N6O3/c1-29(2)9-5-6-22(32)30-14-19(15-30)31-13-18(23-24(26)27-16-28-25(23)31)8-7-17-10-20(33-3)12-21(11-17)34-4/h5-6,10-13,16,19H,9,14-15H2,1-4H3,(H2,26,27,28)/b6-5+
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US Patent
n/an/a 1n/an/an/an/a7.525



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
When setting conditions for the measurement of the inhibitory effect of the compounds on FGFR2 kinase activity, FL-Peptide 22 (Caliper Life Sciences,...


US Patent US9108973 (2015)


BindingDB Entry DOI: 10.7270/Q2XW4HJV
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM161450
PNG
(US10124003, Ex. Compound 63 | US9108973, 63)
Show SMILES COc1cc(OC)cc(c1)C#Cc1cn(C2CN(C2)C(=O)\C=C\CN2CC[C@@H](O)C2)c2ncnc(N)c12
Show InChI InChI=1S/C27H30N6O4/c1-36-22-10-18(11-23(12-22)37-2)5-6-19-13-33(27-25(19)26(28)29-17-30-27)20-14-32(15-20)24(35)4-3-8-31-9-7-21(34)16-31/h3-4,10-13,17,20-21,34H,7-9,14-16H2,1-2H3,(H2,28,29,30)/b4-3+/t21-/m1/s1
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n/an/a 1n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
When setting conditions for the measurement of the inhibitory effect of the compounds on FGFR2 kinase activity, FL-Peptide 22 (Caliper Life Sciences,...


US Patent US10124003 (2018)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM161450
PNG
(US10124003, Ex. Compound 63 | US9108973, 63)
Show SMILES COc1cc(OC)cc(c1)C#Cc1cn(C2CN(C2)C(=O)\C=C\CN2CC[C@@H](O)C2)c2ncnc(N)c12
Show InChI InChI=1S/C27H30N6O4/c1-36-22-10-18(11-23(12-22)37-2)5-6-19-13-33(27-25(19)26(28)29-17-30-27)20-14-32(15-20)24(35)4-3-8-31-9-7-21(34)16-31/h3-4,10-13,17,20-21,34H,7-9,14-16H2,1-2H3,(H2,28,29,30)/b4-3+/t21-/m1/s1
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n/an/a 1n/an/an/an/a7.525



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
When setting conditions for the measurement of the inhibitory effect of the compounds on FGFR2 kinase activity, FL-Peptide 22 (Caliper Life Sciences,...


US Patent US9108973 (2015)


BindingDB Entry DOI: 10.7270/Q2XW4HJV
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM161439
PNG
(US10124003, Ex. Compound 52 | US9108973, 52 | US91...)
Show SMILES COc1cc(OC)cc(c1)C#Cc1cn(C2CN(C2)C(=O)\C=C\CN(C)C)c2ncnc(N)c12
Show InChI InChI=1S/C25H28N6O3/c1-29(2)9-5-6-22(32)30-14-19(15-30)31-13-18(23-24(26)27-16-28-25(23)31)8-7-17-10-20(33-3)12-21(11-17)34-4/h5-6,10-13,16,19H,9,14-15H2,1-4H3,(H2,26,27,28)/b6-5+
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n/an/a 1n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
When setting conditions for the measurement of the inhibitory effect of the compounds on FGFR2 kinase activity, FL-Peptide 22 (Caliper Life Sciences,...


US Patent US10124003 (2018)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM50166772
PNG
(CHEMBL3799354)
Show SMILES COc1cc(CCc2cc(Nc3ncnc4cc(ccc34)N3CCN(C)CC3)n[nH]2)cc(OC)c1
Show InChI InChI=1S/C14H19NO4/c1-19-10-4-2-9(3-5-10)8-15-11-6-7-12(16)14(18)13(11)17/h2-7,11-18H,8H2,1H3
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n/an/a 1n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA


Bioorg Med Chem Lett 26: 2594-9 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.028
BindingDB Entry DOI: 10.7270/Q20C4XNM
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM342487
PNG
(US9776988, Example 3)
Show SMILES COc1cc(CCc2cc(n[nH]2)-c2nc3ccc(cc3[nH]2)C(=O)NC2CCOCC2)cc(OC)c1
Show InChI InChI=1S/C26H27N5O4/c1-33-20-11-16(12-21(15-20)34-2)3-5-19-14-24(31-30-19)25-28-22-6-4-17(13-23(22)29-25)26(32)27-18-7-9-35-10-8-18/h4,6,11-15,18H,3,5,7-10H2,1-2H3,(H,27,32)/b25-24+
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n/an/a 1.07n/an/an/an/an/an/a



Celon Pharma S.A.

US Patent


Assay Description
The compounds were dissolved in 100% DMSO, and obtained solutions were serially diluted in reaction buffer (50 mM Tris pH 7.5, 10 mM MgCl2, 0.25 mM E...


US Patent US9776988 (2017)

More data for this
Ligand-Target Pair
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