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Compile Data Set for Download or QSAR

Found 5645 hits of ic50 for UniProtKB: P21802   
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 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 |r|
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))		BDBM50587623
PNG
(CHEMBL5173892)
Show SMILES COc1cc(CCc2cc(n[nH]2)-c2nc3ccc(cc3[nH]2)N2C[C@H](C)O[C@H](C)C2)cc(OC)c1 |r|
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n/an/a 0.110n/an/an/an/an/an/a


TBA



Citation and Details

Article DOI: 10.1016/j.ejmech.2020.112990
BindingDB Entry DOI: 10.7270/Q2WD44HQ
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)


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


(Homo sapiens (Human))		BDBM301217
PNG
(3-(2,6-Difluoro-3,5-dimethoxyphenyl)-1-methyl-1,3,...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc4[nH]ccc4c3N(C)C2=O)c1F
Show InChI InChI=1S/C18H16F2N4O3/c1-23-15-9(7-22-17-10(15)4-5-21-17)8-24(18(23)25)16-13(19)11(26-2)6-12(27-3)14(16)20/h4-7H,8H2,1-3H3,(H,21,22)
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n/an/a 0.150n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of human FGFR2 using biotinylated-EQEDEPEGDYFEWLE peptide as substrate incubated for 1 hr in presence of ATP by FRET assay

Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00713
BindingDB Entry DOI: 10.7270/Q2S1867R
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 |r|
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))		BDBM50588768
PNG
(CHEMBL5175256)
Show SMILES [2H]C([2H])([2H])NC(=O)c1cncc(c1)-c1cnn2cc(-c3ccn(n3)C(C)C)c(N[C@H]3CCOC3)nc12 |r|
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n/an/a 0.200n/an/an/an/an/an/a


TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.2c01366
BindingDB Entry DOI: 10.7270/Q2PG1WPR
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM50576988
PNG
(CHEMBL4862576)
Show SMILES COc1cc(OC)cc(c1)N(CCNC(C)C)c1ccc2ncc(-c3cnn(C)c3)c(=O)n2c1
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n/an/a 0.200n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of human N-terminal GST fusion tagged FGFR2 cytoplasmic domain (399 to 821 end residues) expressed in baculovirus infected Sf21 insect cel...

Citation and Details

Article DOI: 10.1016/j.ejmech.2021.113499
BindingDB Entry DOI: 10.7270/Q2HH6PWN
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM50588744
PNG
(CHEMBL5189383)
Show SMILES COc1cc(OC)cc(c1)N(CCNC(C)C)c1ccc2nc(cnc2c1)-c1cnn(C)c1
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TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.2c01366
BindingDB Entry DOI: 10.7270/Q2PG1WPR
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM50587622
PNG
(CHEMBL5171314)
Show SMILES COc1cc(CCc2cc(n[nH]2)-c2nc3cc(F)c(cc3[nH]2)N2CCOCC2)cc(OC)c1
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n/an/a 0.270n/an/an/an/an/an/a


TBA



Citation and Details

Article DOI: 10.1016/j.ejmech.2020.112990
BindingDB Entry DOI: 10.7270/Q2WD44HQ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM50587621
PNG
(CHEMBL5179660)
Show SMILES COc1cc(CCc2cc(n[nH]2)-c2nc3cc(F)c(cc3[nH]2)N2C[C@H](C)O[C@H](C)C2)cc(OC)c1 |r|
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n/an/a 0.290n/an/an/an/an/an/a


TBA



Citation and Details

Article DOI: 10.1016/j.ejmech.2020.112990
BindingDB Entry DOI: 10.7270/Q2WD44HQ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM301220
PNG
(3-(2-Chloro-6-fluoro-3,5-dimethoxyphenyl)-1-methyl...)
Show SMILES COc1cc(OC)c(Cl)c(N2Cc3cnc4[nH]ccc4c3N(C)C2=O)c1F
Show InChI InChI=1S/C18H16ClFN4O3/c1-23-15-9(7-22-17-10(15)4-5-21-17)8-24(18(23)25)16-13(19)11(26-2)6-12(27-3)14(16)20/h4-7H,8H2,1-3H3,(H,21,22)
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n/an/a 0.300n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of human FGFR2 using biotinylated-EQEDEPEGDYFEWLE peptide as substrate incubated for 1 hr in presence of ATP by FRET assay

Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00713
BindingDB Entry DOI: 10.7270/Q2S1867R
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM161438
PNG
(US10124003, Ex. Compound 51 | US10835536, Ex. Comp...)
Show SMILES COc1cc(OC)cc(c1)C#CC1=CN(C2CN(C2)C(=O)C=C)C2N=CN=C(N)C12 |c:26,t:13,28|
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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US Patent
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 | US10835536, Ex. Comp...)
Show SMILES COC(=O)[C@@H]1C[C@@H](CN1C(=O)C=C)n1cc(C#Cc2cc(OC)cc(OC)c2)c2c(N)ncnc12 |r|
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))		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))		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 | US10835536, Ex. Comp...)
Show SMILES COc1cc(OC)cc(c1)C#CC1=CN(C2CN(C2)C(=O)C=C)C2N=CN=C(N)C12 |c:26,t:13,28|
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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US Patent
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)


BindingDB Entry DOI: 10.7270/Q2B27XBQ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM161453
PNG
(US10124003, Ex. Compound 66 | US10835536, Ex. Comp...)
Show SMILES COC(=O)[C@@H]1C[C@@H](CN1C(=O)C=C)n1cc(C#Cc2cc(OC)cc(OC)c2)c2c(N)ncnc12 |r|
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)


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))		BDBM161438
PNG
(US10124003, Ex. Compound 51 | US10835536, Ex. Comp...)
Show SMILES COc1cc(OC)cc(c1)C#CC1=CN(C2CN(C2)C(=O)C=C)C2N=CN=C(N)C12 |c:26,t:13,28|
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 US10835536 (2020)


BindingDB Entry DOI: 10.7270/Q23N26F5
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM161453
PNG
(US10124003, Ex. Compound 66 | US10835536, Ex. Comp...)
Show SMILES COC(=O)[C@@H]1C[C@@H](CN1C(=O)C=C)n1cc(C#Cc2cc(OC)cc(OC)c2)c2c(N)ncnc12 |r|
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 US10835536 (2020)


BindingDB Entry DOI: 10.7270/Q23N26F5
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM161396
PNG
(US10124003, Ex. Compound 9 | US10835536, Ex. Comp ...)
Show SMILES COc1cc(OC)cc(c1)C#Cc1nn(C2CN(C2)C(=O)C=C)c2ncnc(N)c12
Show InChI InChI=1S/C21H20N6O3/c1-4-18(28)26-10-14(11-26)27-21-19(20(22)23-12-24-21)17(25-27)6-5-13-7-15(29-2)9-16(8-13)30-3/h4,7-9,12,14H,1,10-11H2,2-3H3,(H2,22,23,24)
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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 US10894048 (2021)


BindingDB Entry DOI: 10.7270/Q2319ZZF
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM478146
PNG
(US10894048, Ex Comp 66)
Show SMILES COC(=O)[C@@H]1C[C@@H](CN1C(=O)C=C)n1nc(C#Cc2cc(OC)cc(OC)c2)c2c(N)ncnc12 |r|
Show InChI InChI=1S/C24H24N6O5/c1-5-20(31)29-12-15(10-19(29)24(32)35-4)30-23-21(22(25)26-13-27-23)18(28-30)7-6-14-8-16(33-2)11-17(9-14)34-3/h5,8-9,11,13,15,19H,1,10,12H2,2-4H3,(H2,25,26,27)/t15-,19-/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 US10894048 (2021)


BindingDB Entry DOI: 10.7270/Q2319ZZF
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM301310
PNG
(3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(mo...)
Show SMILES CCN1C(=O)N(Cc2cnc3[nH]c(CN4CCOCC4)cc3c12)c1c(F)c(OC)cc(OC)c1F
Show InChI InChI=1S/C24H27F2N5O4/c1-4-30-21-14(11-27-23-16(21)9-15(28-23)13-29-5-7-35-8-6-29)12-31(24(30)32)22-19(25)17(33-2)10-18(34-3)20(22)26/h9-11H,4-8,12-13H2,1-3H3,(H,27,28)
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n/an/a 0.400n/an/an/an/an/an/a


TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.2c01366
BindingDB Entry DOI: 10.7270/Q2PG1WPR
More data for this
Ligand-Target Pair		3D
3D Structure (crystal)
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM161426
PNG
(US10124003, Ex. Compound 39 | US10894048, Ex Comp ...)
Show SMILES COc1cc(OC)cc(c1)C#Cc1cn([C@H]2CCN(C2)C(=O)C=C)c2ncnc(N)c12 |r|
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 US10894048 (2021)


BindingDB Entry DOI: 10.7270/Q2319ZZF
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM161426
PNG
(US10124003, Ex. Compound 39 | US10894048, Ex Comp ...)
Show SMILES COc1cc(OC)cc(c1)C#Cc1cn([C@H]2CCN(C2)C(=O)C=C)c2ncnc(N)c12 |r|
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))		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))		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=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))		BDBM161419
PNG
(US10124003, Ex. Compound 32 | US10835536, Ex. Comp...)
Show SMILES COc1cc(OC)cc(c1)C#Cc1nn([C@H]2C[C@@H](C#C)N(C2)C(=O)C=C)c2ncnc(N)c12 |r|
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)


BindingDB Entry DOI: 10.7270/Q2B27XBQ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM161426
PNG
(US10124003, Ex. Compound 39 | US10894048, Ex Comp ...)
Show SMILES COc1cc(OC)cc(c1)C#Cc1cn([C@H]2CCN(C2)C(=O)C=C)c2ncnc(N)c12 |r|
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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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)


BindingDB Entry DOI: 10.7270/Q2B27XBQ
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 0.400n/an/an/an/an/an/a



Shanghai University

Curated by ChEMBL


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

J Med Chem 62: 7473-7488 (2019)


Article DOI: 10.1021/acs.jmedchem.9b00510
BindingDB Entry DOI: 10.7270/Q2KP85D8
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 0.400n/an/an/an/an/an/a



Shanghai Institute of Materia Medica

Curated by ChEMBL


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

ACS Med Chem Lett 7: 629-34 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00066
BindingDB Entry DOI: 10.7270/Q2P272M2
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 0.400n/an/an/an/an/an/a



Shanghai Institute of Materia Medica

Curated by ChEMBL


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

ACS Med Chem Lett 7: 629-34 (2016)


Article DOI: 10.1021/acsmedchemlett.6b00066
BindingDB Entry DOI: 10.7270/Q2P272M2
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM161419
PNG
(US10124003, Ex. Compound 32 | US10835536, Ex. Comp...)
Show SMILES COc1cc(OC)cc(c1)C#Cc1nn([C@H]2C[C@@H](C#C)N(C2)C(=O)C=C)c2ncnc(N)c12 |r|
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 US10835536 (2020)


BindingDB Entry DOI: 10.7270/Q23N26F5
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM472833
PNG
(US10835536, Ex. Comp 39)
Show SMILES COc1cc(OC)cc(c1)C#CC1=CN([C@H]2CCN(C2)C(=O)C=C)C2N=CN=C(N)C12 |r,c:27,t:13,29|
Show InChI InChI=1S/C23H25N5O3/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/h4,9-12,14,17,21,23H,1,7-8,13H2,2-3H3,(H2,24,25,26)/t17-,21?,23?/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 US10835536 (2020)


BindingDB Entry DOI: 10.7270/Q23N26F5
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM161419
PNG
(US10124003, Ex. Compound 32 | US10835536, Ex. Comp...)
Show SMILES COc1cc(OC)cc(c1)C#Cc1nn([C@H]2C[C@@H](C#C)N(C2)C(=O)C=C)c2ncnc(N)c12 |r|
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 US10894048 (2021)


BindingDB Entry DOI: 10.7270/Q2319ZZF
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM161419
PNG
(US10124003, Ex. Compound 32 | US10835536, Ex. Comp...)
Show SMILES COc1cc(OC)cc(c1)C#Cc1nn([C@H]2C[C@@H](C#C)N(C2)C(=O)C=C)c2ncnc(N)c12 |r|
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))		BDBM50587619
PNG
(CHEMBL5205436)
Show SMILES COc1cc(OC)c(Cl)c(CCc2cc(n[nH]2)-c2nc3ccc(cc3[nH]2)N2CCN(C)CC2)c1Cl
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n/an/a 0.430n/an/an/an/an/an/a


TBA



Citation and Details

Article DOI: 10.1016/j.ejmech.2020.112990
BindingDB Entry DOI: 10.7270/Q2WD44HQ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM50587620
PNG
(CHEMBL5189958)
Show SMILES COc1cc(CCc2cc(n[nH]2)-c2nc3cc(F)c(cc3[nH]2)N2CCN(C)CC2)cc(OC)c1
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n/an/a 0.437n/an/an/an/an/an/a


TBA



Citation and Details

Article DOI: 10.1016/j.ejmech.2020.112990
BindingDB Entry DOI: 10.7270/Q2WD44HQ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(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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n/an/a 0.470n/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 2


(Homo sapiens (Human))		BDBM301310
PNG
(3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(mo...)
Show SMILES CCN1C(=O)N(Cc2cnc3[nH]c(CN4CCOCC4)cc3c12)c1c(F)c(OC)cc(OC)c1F
Show InChI InChI=1S/C24H27F2N5O4/c1-4-30-21-14(11-27-23-16(21)9-15(28-23)13-29-5-7-35-8-6-29)12-31(24(30)32)22-19(25)17(33-2)10-18(34-3)20(22)26/h9-11H,4-8,12-13H2,1-3H3,(H,27,28)
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n/an/a 0.5n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of FGFR2 (unknown origin)

Citation and Details

Article DOI: 10.1016/j.ejmech.2021.113499
BindingDB Entry DOI: 10.7270/Q2HH6PWN
More data for this
Ligand-Target Pair		3D
3D Structure (crystal)
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)


Article DOI: 10.1016/j.ejmech.2018.05.005
BindingDB Entry DOI: 10.7270/Q2736TM3
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM50596830
PNG
(CHEMBL5179166)
Show SMILES CCN1CCN(CC1)c1ccc(Nc2ncnc(n2)-c2cccnc2Nc2c(Cl)c(OC)cc(OC)c2Cl)cc1
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TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c01776
BindingDB Entry DOI: 10.7270/Q2765KCQ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM50525939
PNG
(Balversa | Erdafitinib | Jnj-42756493)
Show SMILES COc1cc(OC)cc(c1)N(CCNC(C)C)c1ccc2ncc(nc2c1)-c1cnn(C)c1
Show InChI InChI=1S/C25H30N6O2/c1-17(2)26-8-9-31(20-10-21(32-4)13-22(11-20)33-5)19-6-7-23-24(12-19)29-25(15-27-23)18-14-28-30(3)16-18/h6-7,10-17,26H,8-9H2,1-5H3
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TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c01776
BindingDB Entry DOI: 10.7270/Q2765KCQ
More data for this
Ligand-Target Pair		3D
3D Structure (crystal)
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM301310
PNG
(3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(mo...)
Show SMILES CCN1C(=O)N(Cc2cnc3[nH]c(CN4CCOCC4)cc3c12)c1c(F)c(OC)cc(OC)c1F
Show InChI InChI=1S/C24H27F2N5O4/c1-4-30-21-14(11-27-23-16(21)9-15(28-23)13-29-5-7-35-8-6-29)12-31(24(30)32)22-19(25)17(33-2)10-18(34-3)20(22)26/h9-11H,4-8,12-13H2,1-3H3,(H,27,28)
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TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c01776
BindingDB Entry DOI: 10.7270/Q2765KCQ
More data for this
Ligand-Target Pair		3D
3D Structure (crystal)
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM50596831
PNG
(CHEMBL5177100)
Show SMILES COc1cc(OC)c(Cl)c(Nc2ncccc2-c2ncnc(Nc3ccc(cc3)N3C[C@H](C)N[C@H](C)C3)n2)c1Cl |r|
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TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c01776
BindingDB Entry DOI: 10.7270/Q2765KCQ
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(Homo sapiens (Human))		BDBM50596832
PNG
(CHEMBL5198569)
Show SMILES CCN1CCN(CC1)c1cccc(Nc2ncnc(n2)-c2cccnc2Nc2c(Cl)c(OC)cc(OC)c2Cl)c1
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n/an/a<0.5n/an/an/an/an/an/a


TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c01776
BindingDB Entry DOI: 10.7270/Q2765KCQ
More data for this
Ligand-Target Pair
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