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Compile Data Set for Download or QSAR

Found 2162 hits of ic50 data for polymerid = 856   
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))
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=1/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))
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))
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)


Article DOI: 10.1074/jbc.M512374200
BindingDB Entry DOI: 10.7270/Q2SB47VT
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=1/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=1/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))
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=1/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-/s2
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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=1/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)


Article DOI: 10.1016/j.bmcl.2005.01.023
BindingDB Entry DOI: 10.7270/Q2B27XBQ
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=1/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))
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=1/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-/s2
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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)


Article DOI: 10.1016/j.bmcl.2005.01.023
BindingDB Entry DOI: 10.7270/Q2B27XBQ
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
BindingDB Entry DOI: 10.7270/Q2FX7CQK
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))
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=1/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-/s2
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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)


Article DOI: 10.1016/j.bmcl.2005.01.023
BindingDB Entry DOI: 10.7270/Q2B27XBQ
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=1/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+/s2
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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)


Article DOI: 10.1016/j.bmcl.2005.01.023
BindingDB Entry DOI: 10.7270/Q2B27XBQ
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=1/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+/s2
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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))
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))
BDBM50166736
PNG
(CHEMBL3797594)
Show SMILES COc1cc(CCc2cc(Nc3ncnc4cc(ccc34)N3CCC(C3)N(C)C)n[nH]2)cc(OC)c1
Show InChI InChI=1/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))
BDBM50166610
PNG
(CHEMBL3800526)
Show SMILES COc1cc(CCc2cc(Nc3ncnc4cc(ccc34)N3CCN4CCCCC4C3)n[nH]2)cc(OC)c1
Show InChI InChI=1/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))
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=1/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-/s2
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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))
BDBM287008
PNG
(8-(2-((1-acryloylazetidin-3-yl)oxy)ethyl)-6-(2,6-d...)
Show SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCOC3CN(C3)C(=O)C=C)c2n1
Show InChI InChI=1S/C24H25Cl2N5O5/c1-5-18(32)30-11-14(12-30)36-7-6-31-22-13(10-28-24(27-2)29-22)8-15(23(31)33)19-20(25)16(34-3)9-17(35-4)21(19)26/h5,8-10,14H,1,6-7,11-12H2,2-4H3,(H,27,28,29)
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n/an/a 0.5n/an/an/an/an/an/a



Principia Biopharma Inc

US Patent


Assay Description
The cell-based effects of FGFR inhibitors were determined by measuring inhibition of FGFR-dependent cell line growth. The cell lines SNU-16 was used ...


US Patent US10294223 (2019)

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


(Homo sapiens (Human))
BDBM50468395
PNG
(CHEMBL4294625)
Show SMILES CNC(=O)n1ccc2cc(Oc3ccnc(NC(=O)c4ccc(cc4)C4CCN(CCO)CC4)c3)c(OCCO)cc12
Show InChI InChI=1S/C31H35N5O6/c1-32-31(40)36-13-9-24-18-28(27(20-26(24)36)41-17-16-38)42-25-6-10-33-29(19-25)34-30(39)23-4-2-21(3-5-23)22-7-11-35(12-8-22)14-15-37/h2-6,9-10,13,18-20,22,37-38H,7-8,11-12,14-17H2,1H3,(H,32,40)(H,33,34,39)
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n/an/a 0.5n/an/an/an/an/an/a



Chinese Academy of Sciences

Curated by ChEMBL


Assay Description
Inhibition of human N-terminal GST-tagged FGFR2 (399 to 821 residues) cytoplasmic domain expressed in baculovirus expression system after 60 mins by ...


Eur J Med Chem 154: 9-28 (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))
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))
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))
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))
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))
BDBM50065454
PNG
(CHEBI:63453 | CHEMBL3348846)
Show SMILES COc1cc(CCc2cc(NC(=O)c3ccc(cc3)N3C[C@H](C)N[C@H](C)C3)n[nH]2)cc(OC)c1
Show InChI InChI=1S/C26H33N5O3/c1-17-15-31(16-18(2)27-17)22-9-6-20(7-10-22)26(32)28-25-13-21(29-30-25)8-5-19-11-23(33-3)14-24(12-19)34-4/h6-7,9-14,17-18,27H,5,8,15-16H2,1-4H3,(H2,28,29,30,32)/t17-,18+
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n/an/a 0.600n/an/an/an/an/an/a



Fudan University

Curated by ChEMBL


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


Bioorg Med Chem Lett 27: 3782-3786 (2017)

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


(Homo sapiens (Human))
BDBM350052
PNG
(US10208024, Example 51)
Show SMILES COCCN1CCC(CC1)n1cc(cn1)-c1cnc(N)c(n1)-c1cc(C)c(=O)n(n1)-c1cc(OC)cc(OC)c1
Show InChI InChI=1S/C28H34N8O4/c1-18-11-24(33-36(28(18)37)21-12-22(39-3)14-23(13-21)40-4)26-27(29)30-16-25(32-26)19-15-31-35(17-19)20-5-7-34(8-6-20)9-10-38-2/h11-17,20H,5-10H2,1-4H3,(H2,29,30)
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n/an/a 0.600n/an/an/an/an/an/a



Array BioPharma Inc

US Patent


Assay Description
FGFR1, 2 and 3 kinase activity was measured by the Invitrogen LanthaScreen™ Assay technology which directly measures the amount of substrate phosphor...


US Patent US10208024 (2019)


Article DOI: 10.1016/j.bmcl.2004.06.019
BindingDB Entry DOI: 10.7270/Q2CJ8GNW
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)


Article DOI: 10.1016/j.bmcl.2005.01.023
BindingDB Entry DOI: 10.7270/Q2B27XBQ
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)


Article DOI: 10.1074/jbc.M512374200
BindingDB Entry DOI: 10.7270/Q2SB47VT
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))
BDBM357253
PNG
((5-Amino-1-(2-cyclopropyl-1H-benzo[d]imidazol-5-yl...)
Show SMILES CCn1cc(cn1)-c1ccc2cc([nH]c2c1)C(=O)c1cnn(c1N)-c1ccc2[nH]c(nc2c1)C1CC1
Show InChI InChI=1S/C27H24N8O/c1-2-34-14-18(12-29-34)16-5-6-17-10-24(31-22(17)9-16)25(36)20-13-30-35(26(20)28)19-7-8-21-23(11-19)33-27(32-21)15-3-4-15/h5-15,31H,2-4,28H2,1H3,(H,32,33)
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n/an/a 0.700n/an/an/an/an/an/a



Zhejiang Hisun Pharmaceutical Co., Ltd

US Patent


Assay Description
The following assay was used to determine the inhibition rate of the preferred compounds of the present invention to the kinase activity of the recom...


US Patent US10214515 (2019)


Article DOI: 10.1021/jm070284z
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/C26H31N7O2/c1-32-8-10-33(11-9-32)20-6-7-23-24(15-20)27-17-28-26(23)29-25-14-19(30-31-25)5-4-18-12-21(34-2)16-22(13-18)35-3/h6-7,12-17H,4-5,8-11H2,1-3H3,(H2,27,28,29,30,31)
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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))
BDBM287520
PNG
(8-(2-((1-acryloylazetidin-3-yl)(methyl)amino)ethyl...)
Show SMILES COc1cc(OC)c(Cl)c(c1Cl)-c1cc2cnc(N)nc2n(CCN(C)C2CN(C2)C(=O)C=C)c1=O
Show InChI InChI=1S/C24H26Cl2N6O4/c1-5-18(33)31-11-14(12-31)30(2)6-7-32-22-13(10-28-24(27)29-22)8-15(23(32)34)19-20(25)16(35-3)9-17(36-4)21(19)26/h5,8-10,14H,1,6-7,11-12H2,2-4H3,(H2,27,28,29)
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US Patent
n/an/a 0.700n/an/an/an/an/an/a



Principia Biopharma Inc

US Patent


Assay Description
The cell-based effects of FGFR inhibitors were determined by measuring inhibition of FGFR-dependent cell line growth. The cell lines SNU-16 was used ...


US Patent US10294223 (2019)

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))
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)


Article DOI: 10.1074/jbc.M512374200
BindingDB Entry DOI: 10.7270/Q2SB47VT
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM350042
PNG
(US10208024, Example 41)
Show SMILES COc1cc(OC)c(F)c(c1)-n1nc(ccc1=O)-c1nc(cnc1N)-c1cnn(c1)C1CCNCC1
Show InChI InChI=1S/C24H25FN8O3/c1-35-16-9-19(22(25)20(10-16)36-2)33-21(34)4-3-17(31-33)23-24(26)28-12-18(30-23)14-11-29-32(13-14)15-5-7-27-8-6-15/h3-4,9-13,15,27H,5-8H2,1-2H3,(H2,26,28)
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US Patent
n/an/a 0.800n/an/an/an/an/an/a



Array BioPharma Inc

US Patent


Assay Description
FGFR1, 2 and 3 kinase activity was measured by the Invitrogen LanthaScreen™ Assay technology which directly measures the amount of substrate phosphor...


US Patent US10208024 (2019)


Article DOI: 10.1016/j.bmcl.2004.06.019
BindingDB Entry DOI: 10.7270/Q2CJ8GNW
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=1/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))
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))
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))
BDBM50260185
PNG
(CHEMBL4096041)
Show SMILES COc1cc(OC)c(Cl)c(N2Cc3cnc(Nc4ccccc4)nc3N(C3CCN(CC3)C(=O)\C=C\CN(C)C)C2=O)c1Cl
Show InChI InChI=1S/C31H35Cl2N7O4/c1-37(2)14-8-11-25(41)38-15-12-22(13-16-38)40-29-20(18-34-30(36-29)35-21-9-6-5-7-10-21)19-39(31(40)42)28-26(32)23(43-3)17-24(44-4)27(28)33/h5-11,17-18,22H,12-16,19H2,1-4H3,(H,34,35,36)/b11-8+
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n/an/a 0.840n/an/an/an/an/an/a



Guangzhou Institutes of Biomedicine and Health

Curated by ChEMBL


Assay Description
Inhibition of human recombinant cytoplasmic His-tagged FGFR2 (403 to 822 residues) expressed in baculovirus using Tyr-4 peptide after 1 hr by FRET-ba...


Eur J Med Chem 135: 531-543 (2017)

More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
BDBM350051
PNG
(US10208024, Example 50)
Show SMILES COc1cc(OC)cc(c1)-n1nc(cc(C)c1=O)-c1nc(cnc1N)-c1cnn(c1)C1CCNCC1
Show InChI InChI=1S/C25H28N8O3/c1-15-8-21(31-33(25(15)34)18-9-19(35-2)11-20(10-18)36-3)23-24(26)28-13-22(30-23)16-12-29-32(14-16)17-4-6-27-7-5-17/h8-14,17,27H,4-7H2,1-3H3,(H2,26,28)
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US Patent
n/an/a 0.900n/an/an/an/an/an/a



Array BioPharma Inc

US Patent


Assay Description
FGFR1, 2 and 3 kinase activity was measured by the Invitrogen LanthaScreen™ Assay technology which directly measures the amount of substrate phosphor...


US Patent US10208024 (2019)


Article DOI: 10.1016/j.bmcl.2004.06.019
BindingDB Entry DOI: 10.7270/Q2CJ8GNW
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))
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))
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/C29H35N7O4/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,(H,30,31)(H,32,33)
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US Patent
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)


Article DOI: 10.1021/jm030603w
BindingDB Entry DOI: 10.7270/Q27946S6
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
BindingDB Entry DOI: 10.7270/Q2445PQT
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
BindingDB Entry DOI: 10.7270/Q2445PQT
More data for this
Ligand-Target Pair
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