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Patent code US10689705

Compile Data Set for Download or QSAR

Found 212 hits of Enzyme Inhibition Constant Data   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM448228
PNG
(US10689705, Compound 5)
Show SMILES CC1CCC(C)N1Cc1ccc2[nH]c(cc2c1)C(=O)c1cnn(c1N)-c1ccc2nc(C)[nH]c2c1
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US Patent
n/an/a 0.320n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR1 inhibitory activities of compounds were measured based on their activity to inhibit phosphorylation of the biotinylated peptide (EGPWLEEEEE...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM448227
PNG
(US10689705, Compound 4)
Show SMILES Cc1nc2ccc(cc2[nH]1)-n1ncc(C(=O)c2cc3cc(CN4CCCC(F)C4)ccc3[nH]2)c1N
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n/an/a 0.670n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR1 inhibitory activities of compounds were measured based on their activity to inhibit phosphorylation of the biotinylated peptide (EGPWLEEEEE...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM448229
PNG
(US10689705, Compound 6)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3ccc(OCC4(C)COC4)cc3[nH]2)c1N
Show InChI InChI=1S/C25H24N6O3/c1-14-28-19-6-4-16(8-21(19)29-14)31-24(26)18(10-27-31)23(32)22-7-15-3-5-17(9-20(15)30-22)34-13-25(2)11-33-12-25/h3-10,30H,11-13,26H2,1-2H3,(H,28,29)
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n/an/a 0.810n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR1 inhibitory activities of compounds were measured based on their activity to inhibit phosphorylation of the biotinylated peptide (EGPWLEEEEE...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50197685
PNG
(CHEMBL3681278 | US10689705, Compound 1)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3ccc(CN4CCOCC4)cc3[nH]2)c1N
Show InChI InChI=1S/C25H25N7O2/c1-15-28-20-5-4-18(12-22(20)29-15)32-25(26)19(13-27-32)24(33)23-11-17-3-2-16(10-21(17)30-23)14-31-6-8-34-9-7-31/h2-5,10-13,30H,6-9,14,26H2,1H3,(H,28,29)
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n/an/a 1.40n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR1 inhibitory activities of compounds were measured based on their activity to inhibit phosphorylation of the biotinylated peptide (EGPWLEEEEE...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM448247
PNG
(US10689705, Compound 24)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3ccc(cc3[nH]2)-c2cnn(C)c2)c1N
Show InChI InChI=1S/C24H20N8O/c1-13-28-19-6-5-17(9-21(19)29-13)32-24(25)18(11-27-32)23(33)22-8-15-4-3-14(7-20(15)30-22)16-10-26-31(2)12-16/h3-12,30H,25H2,1-2H3,(H,28,29)
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n/an/a 2.30n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR1 inhibitory activities of compounds were measured based on their activity to inhibit phosphorylation of the biotinylated peptide (EGPWLEEEEE...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM448268
PNG
(US10689705, Compound 45)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3ccc(OCCN4CCOCC4)cc3[nH]2)c1N
Show InChI InChI=1S/C26H27N7O3/c1-16-29-21-5-3-18(13-23(21)30-16)33-26(27)20(15-28-33)25(34)24-12-17-2-4-19(14-22(17)31-24)36-11-8-32-6-9-35-10-7-32/h2-5,12-15,31H,6-11,27H2,1H3,(H,29,30)
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n/an/a 2.70n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR1 inhibitory activities of compounds were measured based on their activity to inhibit phosphorylation of the biotinylated peptide (EGPWLEEEEE...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM448226
PNG
(US10689705, Compound 3)
Show SMILES C[C@H]1COCCN1Cc1ccc2cc([nH]c2c1)C(=O)c1cnn(c1N)-c1ccc2[nH]c(C)nc2c1
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n/an/a 2.70n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR1 inhibitory activities of compounds were measured based on their activity to inhibit phosphorylation of the biotinylated peptide (EGPWLEEEEE...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM130903
PNG
(US10689705, Compound 7 | US8829199, 196)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3ccc(CN4CCC(F)(F)CC4)cc3[nH]2)c1N
Show InChI InChI=1S/C26H25F2N7O/c1-15-31-20-5-4-18(12-22(20)32-15)35-25(29)19(13-30-35)24(36)23-11-17-3-2-16(10-21(17)33-23)14-34-8-6-26(27,28)7-9-34/h2-5,10-13,33H,6-9,14,29H2,1H3,(H,31,32)
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n/an/a 2.90n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR1 inhibitory activities of compounds were measured based on their activity to inhibit phosphorylation of the biotinylated peptide (EGPWLEEEEE...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM448290
PNG
(US10689705, Compound 67)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3ccc(OC4CCOCC4)cc3[nH]2)c1N
Show InChI InChI=1S/C25H24N6O3/c1-14-28-20-5-3-16(11-22(20)29-14)31-25(26)19(13-27-31)24(32)23-10-15-2-4-18(12-21(15)30-23)34-17-6-8-33-9-7-17/h2-5,10-13,17,30H,6-9,26H2,1H3,(H,28,29)
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n/an/a 3n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR1 inhibitory activities of compounds were measured based on their activity to inhibit phosphorylation of the biotinylated peptide (EGPWLEEEEE...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM448283
PNG
(US10689705, Compound 60)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3cc(ccc3[nH]2)C(=O)N2CCCC(F)(F)C2)c1N
Show InChI InChI=1S/C26H23F2N7O2/c1-14-31-20-6-4-17(11-21(20)32-14)35-24(29)18(12-30-35)23(36)22-10-16-9-15(3-5-19(16)33-22)25(37)34-8-2-7-26(27,28)13-34/h3-6,9-12,33H,2,7-8,13,29H2,1H3,(H,31,32)
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n/an/a 3.10n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR3 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM448268
PNG
(US10689705, Compound 45)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3ccc(OCCN4CCOCC4)cc3[nH]2)c1N
Show InChI InChI=1S/C26H27N7O3/c1-16-29-21-5-3-18(13-23(21)30-16)33-26(27)20(15-28-33)25(34)24-12-17-2-4-19(14-22(17)31-24)36-11-8-32-6-9-35-10-7-32/h2-5,12-15,31H,6-11,27H2,1H3,(H,29,30)
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n/an/a 3.20n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM50197685
PNG
(CHEMBL3681278 | US10689705, Compound 1)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3ccc(CN4CCOCC4)cc3[nH]2)c1N
Show InChI InChI=1S/C25H25N7O2/c1-15-28-20-5-4-18(12-22(20)29-15)32-25(26)19(13-27-32)24(33)23-11-17-3-2-16(10-21(17)30-23)14-31-6-8-34-9-7-31/h2-5,10-13,30H,6-9,14,26H2,1H3,(H,28,29)
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n/an/a 3.40n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM50197685
PNG
(CHEMBL3681278 | US10689705, Compound 1)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3ccc(CN4CCOCC4)cc3[nH]2)c1N
Show InChI InChI=1S/C25H25N7O2/c1-15-28-20-5-4-18(12-22(20)29-15)32-25(26)19(13-27-32)24(33)23-11-17-3-2-16(10-21(17)30-23)14-31-6-8-34-9-7-31/h2-5,10-13,30H,6-9,14,26H2,1H3,(H,28,29)
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n/an/a 3.5n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR3 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM448229
PNG
(US10689705, Compound 6)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3ccc(OCC4(C)COC4)cc3[nH]2)c1N
Show InChI InChI=1S/C25H24N6O3/c1-14-28-19-6-4-16(8-21(19)29-14)31-24(26)18(10-27-31)23(32)22-7-15-3-5-17(9-20(15)30-22)34-13-25(2)11-33-12-25/h3-10,30H,11-13,26H2,1-2H3,(H,28,29)
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n/an/a 3.70n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR3 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM448281
PNG
(US10689705, Compound 58)
Show SMILES COc1cc2[nH]c(cc2cc1Cl)C(=O)c1cnn(c1N)-c1ccc2[nH]c(C)nc2c1
Show InChI InChI=1S/C21H17ClN6O2/c1-10-25-15-4-3-12(7-17(15)26-10)28-21(23)13(9-24-28)20(29)18-6-11-5-14(22)19(30-2)8-16(11)27-18/h3-9,27H,23H2,1-2H3,(H,25,26)
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n/an/a 4n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM448290
PNG
(US10689705, Compound 67)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3ccc(OC4CCOCC4)cc3[nH]2)c1N
Show InChI InChI=1S/C25H24N6O3/c1-14-28-20-5-3-16(11-22(20)29-14)31-25(26)19(13-27-31)24(32)23-10-15-2-4-18(12-21(15)30-23)34-17-6-8-33-9-7-17/h2-5,10-13,17,30H,6-9,26H2,1H3,(H,28,29)
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n/an/a 4.30n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM448226
PNG
(US10689705, Compound 3)
Show SMILES C[C@H]1COCCN1Cc1ccc2cc([nH]c2c1)C(=O)c1cnn(c1N)-c1ccc2[nH]c(C)nc2c1
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n/an/a 4.30n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50197683
PNG
(CHEMBL3907479 | US10689705, Compound 49)
Show SMILES Cc1nc2ccc(cc2[nH]1)-n1ncc(C(=O)c2cc3ccccc3[nH]2)c1N
Show InChI InChI=1S/C20H16N6O/c1-11-23-16-7-6-13(9-17(16)24-11)26-20(21)14(10-22-26)19(27)18-8-12-4-2-3-5-15(12)25-18/h2-10,25H,21H2,1H3,(H,23,24)
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n/an/a 5n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR1 inhibitory activities of compounds were measured based on their activity to inhibit phosphorylation of the biotinylated peptide (EGPWLEEEEE...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM448268
PNG
(US10689705, Compound 45)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3ccc(OCCN4CCOCC4)cc3[nH]2)c1N
Show InChI InChI=1S/C26H27N7O3/c1-16-29-21-5-3-18(13-23(21)30-16)33-26(27)20(15-28-33)25(34)24-12-17-2-4-19(14-22(17)31-24)36-11-8-32-6-9-35-10-7-32/h2-5,12-15,31H,6-11,27H2,1H3,(H,29,30)
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n/an/a 5.40n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR3 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM448226
PNG
(US10689705, Compound 3)
Show SMILES C[C@H]1COCCN1Cc1ccc2cc([nH]c2c1)C(=O)c1cnn(c1N)-c1ccc2[nH]c(C)nc2c1
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n/an/a 5.40n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR3 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM448283
PNG
(US10689705, Compound 60)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3cc(ccc3[nH]2)C(=O)N2CCCC(F)(F)C2)c1N
Show InChI InChI=1S/C26H23F2N7O2/c1-14-31-20-6-4-17(11-21(20)32-14)35-24(29)18(12-30-35)23(36)22-10-16-9-15(3-5-19(16)33-22)25(37)34-8-2-7-26(27,28)13-34/h3-6,9-12,33H,2,7-8,13,29H2,1H3,(H,31,32)
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n/an/a 5.40n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM448249
PNG
(US10689705, Compound 26)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3ccc(cc3[nH]2)-c2ccc(F)cn2)c1N
Show InChI InChI=1S/C25H18FN7O/c1-13-30-20-7-5-17(10-22(20)31-13)33-25(27)18(12-29-33)24(34)23-9-15-3-2-14(8-21(15)32-23)19-6-4-16(26)11-28-19/h2-12,32H,27H2,1H3,(H,30,31)
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n/an/a 5.5n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM448281
PNG
(US10689705, Compound 58)
Show SMILES COc1cc2[nH]c(cc2cc1Cl)C(=O)c1cnn(c1N)-c1ccc2[nH]c(C)nc2c1
Show InChI InChI=1S/C21H17ClN6O2/c1-10-25-15-4-3-12(7-17(15)26-10)28-21(23)13(9-24-28)20(29)18-6-11-5-14(22)19(30-2)8-16(11)27-18/h3-9,27H,23H2,1-2H3,(H,25,26)
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n/an/a 5.5n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR1 inhibitory activities of compounds were measured based on their activity to inhibit phosphorylation of the biotinylated peptide (EGPWLEEEEE...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM448233
PNG
(US10689705, Compound 10)
Show SMILES Cc1nc2ccc(cc2[nH]1)-n1ncc(C(=O)c2cc3ccc(cc3[nH]2)C#N)c1N
Show InChI InChI=1S/C21H15N7O/c1-11-25-16-5-4-14(8-18(16)26-11)28-21(23)15(10-24-28)20(29)19-7-13-3-2-12(9-22)6-17(13)27-19/h2-8,10,27H,23H2,1H3,(H,25,26)
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n/an/a 6.20n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM448290
PNG
(US10689705, Compound 67)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3ccc(OC4CCOCC4)cc3[nH]2)c1N
Show InChI InChI=1S/C25H24N6O3/c1-14-28-20-5-3-16(11-22(20)29-14)31-25(26)19(13-27-31)24(32)23-10-15-2-4-18(12-21(15)30-23)34-17-6-8-33-9-7-17/h2-5,10-13,17,30H,6-9,26H2,1H3,(H,28,29)
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n/an/a 6.70n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR3 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM448225
PNG
(US10689705, Compound 2)
Show SMILES CN1CCC(CC1)c1ccc2cc([nH]c2c1)C(=O)c1cnn(c1N)-c1ccc2nc(C)[nH]c2c1
Show InChI InChI=1S/C26H27N7O/c1-15-29-21-6-5-19(13-23(21)30-15)33-26(27)20(14-28-33)25(34)24-12-18-4-3-17(11-22(18)31-24)16-7-9-32(2)10-8-16/h3-6,11-14,16,31H,7-10,27H2,1-2H3,(H,29,30)
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n/an/a 6.90n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR1 inhibitory activities of compounds were measured based on their activity to inhibit phosphorylation of the biotinylated peptide (EGPWLEEEEE...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM448237
PNG
(US10689705, Compound 14)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3cc4OCCOc4cc3[nH]2)c1N
Show InChI InChI=1S/C22H18N6O3/c1-11-25-15-3-2-13(8-17(15)26-11)28-22(23)14(10-24-28)21(29)18-6-12-7-19-20(9-16(12)27-18)31-5-4-30-19/h2-3,6-10,27H,4-5,23H2,1H3,(H,25,26)
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n/an/a 7.60n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM448270
PNG
(US10689705, Compound 47)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3cc(CN4CCN(CC4)S(C)(=O)=O)ccc3[nH]2)c1N
Show InChI InChI=1S/C26H28N8O3S/c1-16-29-22-6-4-19(13-23(22)30-16)34-26(27)20(14-28-34)25(35)24-12-18-11-17(3-5-21(18)31-24)15-32-7-9-33(10-8-32)38(2,36)37/h3-6,11-14,31H,7-10,15,27H2,1-2H3,(H,29,30)
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n/an/a 7.90n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR1 inhibitory activities of compounds were measured based on their activity to inhibit phosphorylation of the biotinylated peptide (EGPWLEEEEE...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM448262
PNG
(US10689705, Compound 39)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3cc(OCC4CC4)ccc3[nH]2)c1N
Show InChI InChI=1S/C24H22N6O2/c1-13-27-20-6-4-16(10-21(20)28-13)30-24(25)18(11-26-30)23(31)22-9-15-8-17(5-7-19(15)29-22)32-12-14-2-3-14/h4-11,14,29H,2-3,12,25H2,1H3,(H,27,28)
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n/an/a 8.30n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM448225
PNG
(US10689705, Compound 2)
Show SMILES CN1CCC(CC1)c1ccc2cc([nH]c2c1)C(=O)c1cnn(c1N)-c1ccc2nc(C)[nH]c2c1
Show InChI InChI=1S/C26H27N7O/c1-15-29-21-6-5-19(13-23(21)30-15)33-26(27)20(14-28-33)25(34)24-12-18-4-3-17(11-22(18)31-24)16-7-9-32(2)10-8-16/h3-6,11-14,16,31H,7-10,27H2,1-2H3,(H,29,30)
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n/an/a 8.40n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM448227
PNG
(US10689705, Compound 4)
Show SMILES Cc1nc2ccc(cc2[nH]1)-n1ncc(C(=O)c2cc3cc(CN4CCCC(F)C4)ccc3[nH]2)c1N
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n/an/a 8.5n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM448293
PNG
(US10689705, Compound 70)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3cc(F)c(Br)cc3[nH]2)c1N
Show InChI InChI=1S/C20H14BrFN6O/c1-9-25-15-3-2-11(6-17(15)26-9)28-20(23)12(8-24-28)19(29)18-5-10-4-14(22)13(21)7-16(10)27-18/h2-8,27H,23H2,1H3,(H,25,26)
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n/an/a 8.5n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM448245
PNG
(US10689705, Compound 22)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3ccc(I)cc3[nH]2)c1N
Show InChI InChI=1S/C20H15IN6O/c1-10-24-15-5-4-13(8-17(15)25-10)27-20(22)14(9-23-27)19(28)18-6-11-2-3-12(21)7-16(11)26-18/h2-9,26H,22H2,1H3,(H,24,25)
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n/an/a 8.60n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM50197712
PNG
(CHEMBL3676329 | US10689705, Compound 44)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3ccc(Br)cc3[nH]2)c1N
Show InChI InChI=1S/C20H15BrN6O/c1-10-24-15-5-4-13(8-17(15)25-10)27-20(22)14(9-23-27)19(28)18-6-11-2-3-12(21)7-16(11)26-18/h2-9,26H,22H2,1H3,(H,24,25)
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n/an/a 8.90n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM448233
PNG
(US10689705, Compound 10)
Show SMILES Cc1nc2ccc(cc2[nH]1)-n1ncc(C(=O)c2cc3ccc(cc3[nH]2)C#N)c1N
Show InChI InChI=1S/C21H15N7O/c1-11-25-16-5-4-14(8-18(16)26-11)28-21(23)15(10-24-28)20(29)19-7-13-3-2-12(9-22)6-17(13)27-19/h2-8,10,27H,23H2,1H3,(H,25,26)
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n/an/a 9n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR1 inhibitory activities of compounds were measured based on their activity to inhibit phosphorylation of the biotinylated peptide (EGPWLEEEEE...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM130903
PNG
(US10689705, Compound 7 | US8829199, 196)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3ccc(CN4CCC(F)(F)CC4)cc3[nH]2)c1N
Show InChI InChI=1S/C26H25F2N7O/c1-15-31-20-5-4-18(12-22(20)32-15)35-25(29)19(13-30-35)24(36)23-11-17-3-2-16(10-21(17)33-23)14-34-8-6-26(27,28)7-9-34/h2-5,10-13,33H,6-9,14,29H2,1H3,(H,31,32)
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n/an/a 9.40n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM448231
PNG
(US10689705, Compound 8)
Show SMILES COCCN(CCOC)Cc1ccc2cc([nH]c2c1)C(=O)c1cnn(c1N)-c1ccc2[nH]c(C)nc2c1
Show InChI InChI=1S/C27H31N7O3/c1-17-30-22-7-6-20(14-24(22)31-17)34-27(28)21(15-29-34)26(35)25-13-19-5-4-18(12-23(19)32-25)16-33(8-10-36-2)9-11-37-3/h4-7,12-15,32H,8-11,16,28H2,1-3H3,(H,30,31)
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n/an/a 9.60n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR1 inhibitory activities of compounds were measured based on their activity to inhibit phosphorylation of the biotinylated peptide (EGPWLEEEEE...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM448232
PNG
(US10689705, Compound 9)
Show SMILES CN1CCN(CCOc2ccc3cc([nH]c3c2)C(=O)c2cnn(c2N)-c2ccc3[nH]c(C)nc3c2)CC1
Show InChI InChI=1S/C27H30N8O2/c1-17-30-22-6-4-19(14-24(22)31-17)35-27(28)21(16-29-35)26(36)25-13-18-3-5-20(15-23(18)32-25)37-12-11-34-9-7-33(2)8-10-34/h3-6,13-16,32H,7-12,28H2,1-2H3,(H,30,31)
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n/an/a 10n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR1 inhibitory activities of compounds were measured based on their activity to inhibit phosphorylation of the biotinylated peptide (EGPWLEEEEE...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM448236
PNG
(US10689705, Compound 13)
Show SMILES Cc1nc2ccc(cc2[nH]1)-n1ncc(C(=O)c2cc3ccc(cc3[nH]2)-c2cccs2)c1N
Show InChI InChI=1S/C24H18N6OS/c1-13-27-18-7-6-16(11-20(18)28-13)30-24(25)17(12-26-30)23(31)21-9-14-4-5-15(10-19(14)29-21)22-3-2-8-32-22/h2-12,29H,25H2,1H3,(H,27,28)
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n/an/a 10n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM448240
PNG
(US10689705, Compound 17)
Show SMILES Cc1nc2ccc(cc2[nH]1)-n1ncc(C(=O)c2cc3cc(ccc3[nH]2)C2CCN(CC2)C2CCCC2)c1N
Show InChI InChI=1S/C30H33N7O/c1-18-33-26-9-7-23(16-27(26)34-18)37-30(31)24(17-32-37)29(38)28-15-21-14-20(6-8-25(21)35-28)19-10-12-36(13-11-19)22-4-2-3-5-22/h6-9,14-17,19,22,35H,2-5,10-13,31H2,1H3,(H,33,34)
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n/an/a 11n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR1 inhibitory activities of compounds were measured based on their activity to inhibit phosphorylation of the biotinylated peptide (EGPWLEEEEE...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM448234
PNG
(US10689705, Compound 11)
Show SMILES CC(C)N1CCC(CC1)c1ccc2[nH]c(cc2c1)C(=O)c1cnn(c1N)-c1ccc2nc(C)[nH]c2c1
Show InChI InChI=1S/C28H31N7O/c1-16(2)34-10-8-18(9-11-34)19-4-6-23-20(12-19)13-26(33-23)27(36)22-15-30-35(28(22)29)21-5-7-24-25(14-21)32-17(3)31-24/h4-7,12-16,18,33H,8-11,29H2,1-3H3,(H,31,32)
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n/an/a 11n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR1 inhibitory activities of compounds were measured based on their activity to inhibit phosphorylation of the biotinylated peptide (EGPWLEEEEE...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM448270
PNG
(US10689705, Compound 47)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3cc(CN4CCN(CC4)S(C)(=O)=O)ccc3[nH]2)c1N
Show InChI InChI=1S/C26H28N8O3S/c1-16-29-22-6-4-19(13-23(22)30-16)34-26(27)20(14-28-34)25(35)24-12-18-11-17(3-5-21(18)31-24)15-32-7-9-33(10-8-32)38(2,36)37/h3-6,11-14,31H,7-10,15,27H2,1-2H3,(H,29,30)
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US Patent
n/an/a 11n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))
BDBM448228
PNG
(US10689705, Compound 5)
Show SMILES CC1CCC(C)N1Cc1ccc2[nH]c(cc2c1)C(=O)c1cnn(c1N)-c1ccc2nc(C)[nH]c2c1
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US Patent
n/an/a 12n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR3 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM448248
PNG
(US10689705, Compound 25)
Show SMILES COCCOc1ccc2[nH]c(cc2c1)C(=O)c1cnn(c1N)-c1ccc2[nH]c(C)nc2c1
Show InChI InChI=1S/C23H22N6O3/c1-13-26-19-5-3-15(11-20(19)27-13)29-23(24)17(12-25-29)22(30)21-10-14-9-16(32-8-7-31-2)4-6-18(14)28-21/h3-6,9-12,28H,7-8,24H2,1-2H3,(H,26,27)
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US Patent
n/an/a 12n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM448240
PNG
(US10689705, Compound 17)
Show SMILES Cc1nc2ccc(cc2[nH]1)-n1ncc(C(=O)c2cc3cc(ccc3[nH]2)C2CCN(CC2)C2CCCC2)c1N
Show InChI InChI=1S/C30H33N7O/c1-18-33-26-9-7-23(16-27(26)34-18)37-30(31)24(17-32-37)29(38)28-15-21-14-20(6-8-25(21)35-28)19-10-12-36(13-11-19)22-4-2-3-5-22/h6-9,14-17,19,22,35H,2-5,10-13,31H2,1H3,(H,33,34)
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US Patent
n/an/a 12n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM448228
PNG
(US10689705, Compound 5)
Show SMILES CC1CCC(C)N1Cc1ccc2[nH]c(cc2c1)C(=O)c1cnn(c1N)-c1ccc2nc(C)[nH]c2c1
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US Patent
n/an/a 12n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM448229
PNG
(US10689705, Compound 6)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3ccc(OCC4(C)COC4)cc3[nH]2)c1N
Show InChI InChI=1S/C25H24N6O3/c1-14-28-19-6-4-16(8-21(19)29-14)31-24(26)18(10-27-31)23(32)22-7-15-3-5-17(9-20(15)30-22)34-13-25(2)11-33-12-25/h3-10,30H,11-13,26H2,1-2H3,(H,28,29)
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US Patent
n/an/a 12n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM448261
PNG
(US10689705, Compound 38)
Show SMILES CCCCOc1ccc2[nH]c(cc2c1)C(=O)c1cnn(c1N)-c1ccc2[nH]c(C)nc2c1
Show InChI InChI=1S/C24H24N6O2/c1-3-4-9-32-17-6-8-19-15(10-17)11-22(29-19)23(31)18-13-26-30(24(18)25)16-5-7-20-21(12-16)28-14(2)27-20/h5-8,10-13,29H,3-4,9,25H2,1-2H3,(H,27,28)
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US Patent
n/an/a 12n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

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


(Homo sapiens (Human))
BDBM448276
PNG
(US10689705, Compound 53)
Show SMILES Cc1nc2cc(ccc2[nH]1)-n1ncc(C(=O)c2cc3cc4OC(F)(F)Oc4cc3[nH]2)c1N
Show InChI InChI=1S/C21H14F2N6O3/c1-9-26-13-3-2-11(6-15(13)27-9)29-20(24)12(8-25-29)19(30)16-4-10-5-17-18(7-14(10)28-16)32-21(22,23)31-17/h2-8,28H,24H2,1H3,(H,26,27)
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US Patent
n/an/a 14n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR2 inhibitory activities of compounds listed in Tables 1-1 to 1-5 were measured based on their activity to inhibit phosphorylation of the biot...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM448250
PNG
(US10689705, Compound 27)
Show SMILES Cc1nc2ccc(cc2[nH]1)-n1ncc(C(=O)c2cc3ccc(CO)cc3[nH]2)c1N
Show InChI InChI=1S/C21H18N6O2/c1-11-24-16-5-4-14(8-18(16)25-11)27-21(22)15(9-23-27)20(29)19-7-13-3-2-12(10-28)6-17(13)26-19/h2-9,26,28H,10,22H2,1H3,(H,24,25)
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US Patent
n/an/a 15n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha

US Patent


Assay Description
The FGFR1 inhibitory activities of compounds were measured based on their activity to inhibit phosphorylation of the biotinylated peptide (EGPWLEEEEE...


US Patent US10689705 (2020)

More data for this
Ligand-Target Pair
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* indicates data uncertainty>20%