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Compile Data Set for Download or QSAR

Found 2831 hits of ic50 for UniProtKB: P11362   
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 1


(Homo sapiens (human))
BDBM286987
PNG
(8-(3-(4-acryloylpiperazin-1-yl)propyl)-2-((cyclopr...)
Show SMILES COc1cc(OC)c(Cl)c(c1Cl)-c1cc2cnc(NCC3CC3)nc2n(CCCN2CCN(CC2)C(=O)C=C)c1=O
Show InChI InChI=1S/C29H34Cl2N6O4/c1-4-23(38)36-12-10-35(11-13-36)8-5-9-37-27-19(17-33-29(34-27)32-16-18-6-7-18)14-20(28(37)39)24-25(30)21(40-2)15-22(41-3)26(24)31/h4,14-15,17-18H,1,5-13,16H2,2-3H3,(H,32,33,34)
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n/an/a 0.100n/an/an/an/an/a25



Principia Biopharma, Inc.

US Patent


Assay Description
A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin...


US Patent US9567334 (2017)

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


(Homo sapiens (human))
BDBM302362
PNG
(6-[(2-Aminoethoxy)methyl]-5-(7-methoxy-5-methyl-1-...)
Show SMILES COc1cc(C)cc2cc(sc12)-c1c(COCCN)cn2ncnc(N)c12
Show InChI InChI=1S/C19H21N5O2S/c1-11-5-12-7-15(27-18(12)14(6-11)25-2)16-13(9-26-4-3-20)8-24-17(16)19(21)22-10-23-24/h5-8,10H,3-4,9,20H2,1-2H3,(H2,21,22,23)
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n/an/a 0.200n/an/an/an/an/an/a



BAYER INTELLECTUAL PROPERTY GMBH

US Patent


Assay Description
Usually, test compounds were tested on the same microtiter plate at 11 different concentrations in the range of 20 μM to 0.1 nM (e.g. 20 μM...


US Patent US9598416 (2017)

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


(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<0.200n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in human KG1 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 1


(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 FGFR1 in human KG1 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 1


(Homo sapiens (human))
BDBM50189870
PNG
(CHEMBL3827818)
Show SMILES CC(Oc1ccc2[nH]nc(-c3nc4cc(ccc4[nH]3)N3CCOCC3)c2c1)c1c(Cl)cncc1Cl
Show InChI InChI=1S/C25H22Cl2N6O2/c1-14(23-18(26)12-28-13-19(23)27)35-16-3-5-20-17(11-16)24(32-31-20)25-29-21-4-2-15(10-22(21)30-25)33-6-8-34-9-7-33/h2-5,10-14H,6-9H2,1H3,(H,29,30)(H,31,32)
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n/an/a 0.200n/an/an/an/an/an/a



East China University of Science& Technology

Curated by ChEMBL


Assay Description
Inhibition of recombinant human FGFR1 using poly (Glu, Tyr) 4:1 as substrate after 60 mins by ELISA


J Med Chem 59: 6690-708 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00056
BindingDB Entry DOI: 10.7270/Q2474CT3
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (human))
BDBM302404
PNG
(US9598416, Example 50)
Show SMILES COc1cc(C)cc2cc(sc12)-c1c(CN2CCN(C)CC2)cn2ncnc(N)c12
Show InChI InChI=1S/C22H26N6OS/c1-14-8-15-10-18(30-21(15)17(9-14)29-3)19-16(11-27-6-4-26(2)5-7-27)12-28-20(19)22(23)24-13-25-28/h8-10,12-13H,4-7,11H2,1-3H3,(H2,23,24,25)
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n/an/a 0.300n/an/an/an/an/an/a



BAYER INTELLECTUAL PROPERTY GMBH

US Patent


Assay Description
Usually, test compounds were tested on the same microtiter plate at 11 different concentrations in the range of 20 μM to 0.1 nM (e.g. 20 μM...


US Patent US9598416 (2017)

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


(Homo sapiens (human))
BDBM286978
PNG
(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2-chloro...)
Show SMILES COc1cc(OC)c(Cl)c(c1)-c1cc2cnc(NCC(C)(C)O)nc2n(CCCN2CCN(CC2)C(=O)C=C)c1=O
Show InChI InChI=1S/C29H37ClN6O5/c1-6-24(37)35-12-10-34(11-13-35)8-7-9-36-26-19(17-31-28(33-26)32-18-29(2,3)39)14-22(27(36)38)21-15-20(40-4)16-23(41-5)25(21)30/h6,14-17,39H,1,7-13,18H2,2-5H3,(H,31,32,33)
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n/an/a 0.300n/an/an/an/an/a25



Principia Biopharma, Inc.

US Patent


Assay Description
A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin...


US Patent US9567334 (2017)

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


(Homo sapiens (human))
BDBM50189872
PNG
(CHEMBL3827492)
Show SMILES CC(Oc1ccc2[nH]nc(-c3nc4cc(NCCN(C)C)ccc4[nH]3)c2c1)c1c(Cl)cncc1Cl
Show InChI InChI=1S/C25H25Cl2N7O/c1-14(23-18(26)12-28-13-19(23)27)35-16-5-7-20-17(11-16)24(33-32-20)25-30-21-6-4-15(10-22(21)31-25)29-8-9-34(2)3/h4-7,10-14,29H,8-9H2,1-3H3,(H,30,31)(H,32,33)
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n/an/a 0.300n/an/an/an/an/an/a



East China University of Science& Technology

Curated by ChEMBL


Assay Description
Inhibition of recombinant human FGFR1 using poly (Glu, Tyr) 4:1 as substrate after 60 mins by ELISA


J Med Chem 59: 6690-708 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00056
BindingDB Entry DOI: 10.7270/Q2474CT3
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (human))
BDBM50189781
PNG
(CHEMBL3828009)
Show SMILES C[C@@H](Oc1ccc2[nH]nc(\C=C\c3cnn(CCO)c3)c2c1)c1c(Cl)cncc1Cl
Show InChI InChI=1S/C21H19Cl2N5O2/c1-13(21-17(22)10-24-11-18(21)23)30-15-3-5-20-16(8-15)19(26-27-20)4-2-14-9-25-28(12-14)6-7-29/h2-5,8-13,29H,6-7H2,1H3,(H,26,27)/b4-2+/t13-/m1/s1
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n/an/a 0.300n/an/an/an/an/an/a



East China University of Science& Technology

Curated by ChEMBL


Assay Description
Inhibition of recombinant human FGFR1 using poly (Glu, Tyr) 4:1 as substrate after 60 mins by ELISA


J Med Chem 59: 6690-708 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00056
BindingDB Entry DOI: 10.7270/Q2474CT3
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (human))
BDBM130859
PNG
(US8829199, 114)
Show SMILES CC1CCC(C)N1Cc1ccc2[nH]c(cc2c1)C(=O)c1cnn(c1N)-c1ccc2nc(C)nc2c1
Show InChI InChI=1S/C27H29N7O/c1-15-4-5-16(2)33(15)14-18-6-8-22-19(10-18)11-25(32-22)26(35)21-13-29-34(27(21)28)20-7-9-23-24(12-20)31-17(3)30-23/h6-13,15-16,32H,4-5,14,28H2,1-3H3,(H,30,31)
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n/an/a 0.320n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha; F. Hoffmann-La Roche AG

US Patent


Assay Description
The FGFR1-inhibiting activity was measured based on the activity to inhibit phosphorylation of the biotinylated peptide EGPWLEEEEEAYGWMDF by the huma...


US Patent US8829199 (2014)


BindingDB Entry DOI: 10.7270/Q26T0KB8
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (human))
BDBM286391
PNG
(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Show SMILES COc1cc(OC)c(Cl)c(c1Cl)-c1cc2cnc(NC(C)C)nc2n(CCCN2CCN(CC2)C(=O)C=C)c1=O
Show InChI InChI=1S/C28H34Cl2N6O4/c1-6-22(37)35-12-10-34(11-13-35)8-7-9-36-26-18(16-31-28(33-26)32-17(2)3)14-19(27(36)38)23-24(29)20(39-4)15-21(40-5)25(23)30/h6,14-17H,1,7-13H2,2-5H3,(H,31,32,33)
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n/an/a 0.400n/an/an/an/an/a25



Principia Biopharma, Inc.

US Patent


Assay Description
A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin...


US Patent US9567334 (2017)

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


(Homo sapiens (human))
BDBM50189785
PNG
(CHEMBL3828439)
Show SMILES CC(Oc1ccc2[nH]nc(-c3nc4cc(ccc4[nH]3)N(C)C(=O)CN(C)C)c2c1)c1c(Cl)cncc1Cl
Show InChI InChI=1S/C26H25Cl2N7O2/c1-14(24-18(27)11-29-12-19(24)28)37-16-6-8-20-17(10-16)25(33-32-20)26-30-21-7-5-15(9-22(21)31-26)35(4)23(36)13-34(2)3/h5-12,14H,13H2,1-4H3,(H,30,31)(H,32,33)
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n/an/a 0.400n/an/an/an/an/an/a



East China University of Science& Technology

Curated by ChEMBL


Assay Description
Inhibition of recombinant human FGFR1 using poly (Glu, Tyr) 4:1 as substrate after 60 mins by ELISA


J Med Chem 59: 6690-708 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00056
BindingDB Entry DOI: 10.7270/Q2474CT3
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(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 0.400n/an/an/an/an/a25



Principia Biopharma, Inc.

US Patent


Assay Description
A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin...


US Patent US9567334 (2017)

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


(Homo sapiens (human))
BDBM194837
PNG
(US9206184, 18 | US9206184, 19)
Show SMILES CCOCc1c(CN2CCNCC2)n2ncnc(N)c2c1-c1cc2cc(C)cc(OC)c2s1
Show InChI InChI=1S/C24H30N6O2S/c1-4-32-13-17-18(12-29-7-5-26-6-8-29)30-22(24(25)27-14-28-30)21(17)20-11-16-9-15(2)10-19(31-3)23(16)33-20/h9-11,14,26H,4-8,12-13H2,1-3H3,(H2,25,27,28)
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n/an/a 0.5n/an/an/an/a7.022



BAYER INTELLECTUAL PROPERTY GmbH

US Patent


Assay Description
For the assay, 50 nl of each stock solution of the test compound in DMSO was pipetted into a black, low-volume 384-well microtiter plate (Greiner Bio...


US Patent US9206184 (2015)


BindingDB Entry DOI: 10.7270/Q2SN07SH
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(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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Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in human H1581 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 1


(Homo sapiens (human))
BDBM194880
PNG
(US9206184, 61)
Show SMILES COc1cc(C)cc2cc(sc12)-c1c(-c2cnco2)c(CN2CCNCC2)n2ncnc(N)c12
Show InChI InChI=1S/C24H25N7O2S/c1-14-7-15-9-19(34-23(15)17(8-14)32-2)21-20(18-10-27-13-33-18)16(11-30-5-3-26-4-6-30)31-22(21)24(25)28-12-29-31/h7-10,12-13,26H,3-6,11H2,1-2H3,(H2,25,28,29)
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n/an/a 0.5n/an/an/an/a7.022



BAYER INTELLECTUAL PROPERTY GmbH

US Patent


Assay Description
For the assay, 50 nl of each stock solution of the test compound in DMSO was pipetted into a black, low-volume 384-well microtiter plate (Greiner Bio...


US Patent US9206184 (2015)


BindingDB Entry DOI: 10.7270/Q2SN07SH
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (human))
BDBM50189873
PNG
(CHEMBL3827725)
Show SMILES COCCNc1ccc2[nH]c(nc2c1)-c1n[nH]c2ccc(OC(C)c3c(Cl)cncc3Cl)cc12
Show InChI InChI=1S/C24H22Cl2N6O2/c1-13(22-17(25)11-27-12-18(22)26)34-15-4-6-19-16(10-15)23(32-31-19)24-29-20-5-3-14(9-21(20)30-24)28-7-8-33-2/h3-6,9-13,28H,7-8H2,1-2H3,(H,29,30)(H,31,32)
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n/an/a 0.600n/an/an/an/an/an/a



East China University of Science& Technology

Curated by ChEMBL


Assay Description
Inhibition of recombinant human FGFR1 using poly (Glu, Tyr) 4:1 as substrate after 60 mins by ELISA


J Med Chem 59: 6690-708 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00056
BindingDB Entry DOI: 10.7270/Q2474CT3
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(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



East China University of Science& Technology

Curated by ChEMBL


Assay Description
Inhibition of recombinant human FGFR1 using poly (Glu, Tyr) 4:1 as substrate after 60 mins by ELISA


J Med Chem 59: 6690-708 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00056
BindingDB Entry DOI: 10.7270/Q2474CT3
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (human))
BDBM302379
PNG
(5-(7-Methoxy-5-methyl-1-benzothiophen-2-yl)-6-(pip...)
Show SMILES COc1cc(C)cc2cc(sc12)-c1c(CN2CCNCC2)cn2ncnc(N)c12
Show InChI InChI=1S/C21H24N6OS/c1-13-7-14-9-17(29-20(14)16(8-13)28-2)18-15(10-26-5-3-23-4-6-26)11-27-19(18)21(22)24-12-25-27/h7-9,11-12,23H,3-6,10H2,1-2H3,(H2,22,24,25)
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n/an/a 0.600n/an/an/an/an/an/a



BAYER INTELLECTUAL PROPERTY GMBH

US Patent


Assay Description
Usually, test compounds were tested on the same microtiter plate at 11 different concentrations in the range of 20 μM to 0.1 nM (e.g. 20 μM...


US Patent US9598416 (2017)

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


(Homo sapiens (human))
BDBM302385
PNG
(4-{[4-Amino-5-(5-chloro-7-methoxy-1-benzothiophen-...)
Show SMILES COc1cc(Cl)cc2cc(sc12)-c1c(CN2CCNC(=O)C2)cn2ncnc(N)c12
Show InChI InChI=1S/C20H19ClN6O2S/c1-29-14-6-13(21)4-11-5-15(30-19(11)14)17-12(7-26-3-2-23-16(28)9-26)8-27-18(17)20(22)24-10-25-27/h4-6,8,10H,2-3,7,9H2,1H3,(H,23,28)(H2,22,24,25)
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n/an/a 0.600n/an/an/an/an/an/a



BAYER INTELLECTUAL PROPERTY GMBH

US Patent


Assay Description
Usually, test compounds were tested on the same microtiter plate at 11 different concentrations in the range of 20 μM to 0.1 nM (e.g. 20 μM...


US Patent US9598416 (2017)

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


(Homo sapiens (human))
BDBM287005
PNG
(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Show SMILES COc1cc(OC)c(Cl)c(c1Cl)-c1cc2cnc(NCCO)nc2n(CCCN2CCN(CC2)C(=O)C=C)c1=O
Show InChI InChI=1S/C27H32Cl2N6O5/c1-4-21(37)34-11-9-33(10-12-34)7-5-8-35-25-17(16-31-27(32-25)30-6-13-36)14-18(26(35)38)22-23(28)19(39-2)15-20(40-3)24(22)29/h4,14-16,36H,1,5-13H2,2-3H3,(H,30,31,32)
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Principia Biopharma, Inc.

US Patent


Assay Description
A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin...


US Patent US9567334 (2017)

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


(Homo sapiens (human))
BDBM286984
PNG
(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Show SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCCN3CCN(CC3)C(=O)C=C)c2n1
Show InChI InChI=1S/C26H30Cl2N6O4/c1-5-20(35)33-11-9-32(10-12-33)7-6-8-34-24-16(15-30-26(29-2)31-24)13-17(25(34)36)21-22(27)18(37-3)14-19(38-4)23(21)28/h5,13-15H,1,6-12H2,2-4H3,(H,29,30,31)
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Principia Biopharma, Inc.

US Patent


Assay Description
A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin...


US Patent US9567334 (2017)

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


(Homo sapiens (human))
BDBM130860
PNG
(US8829199, 115)
Show SMILES Cc1nc2ccc(cc2n1)-n1ncc(C(=O)c2cc3cc(CN4CCCC(F)C4)ccc3[nH]2)c1N
Show InChI InChI=1S/C26H26FN7O/c1-15-30-22-7-5-19(11-23(22)31-15)34-26(28)20(12-29-34)25(35)24-10-17-9-16(4-6-21(17)32-24)13-33-8-2-3-18(27)14-33/h4-7,9-12,18,32H,2-3,8,13-14,28H2,1H3,(H,30,31)
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n/an/a 0.670n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha; F. Hoffmann-La Roche AG

US Patent


Assay Description
The FGFR1-inhibiting activity was measured based on the activity to inhibit phosphorylation of the biotinylated peptide EGPWLEEEEEAYGWMDF by the huma...


US Patent US8829199 (2014)


BindingDB Entry DOI: 10.7270/Q26T0KB8
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (human))
BDBM50322535
PNG
(3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N...)
Show SMILES CN1CCN(Cc2ccc(NC(=O)c3ccc(C)c(c3)C#Cc3cnc4cccnn34)cc2C(F)(F)F)CC1
Show InChI InChI=1S/C29H27F3N6O/c1-20-5-6-22(16-21(20)8-10-25-18-33-27-4-3-11-34-38(25)27)28(39)35-24-9-7-23(26(17-24)29(30,31)32)19-37-14-12-36(2)13-15-37/h3-7,9,11,16-18H,12-15,19H2,1-2H3,(H,35,39)
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n/an/a 0.700n/an/an/an/an/an/a



Fudan University

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 (unknown origin)


Bioorg Med Chem Lett 24: 5639-43 (2014)


Article DOI: 10.1016/j.bmcl.2014.10.078
BindingDB Entry DOI: 10.7270/Q2765GZ3
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Fibroblast growth factor receptor 1


(Homo sapiens (human))
BDBM194844
PNG
(US9206184, 25)
Show SMILES COc1cc(C)cc2cc(sc12)-c1c(COCC2CC2)c(CN2CCNCC2)n2ncnc(N)c12
Show InChI InChI=1S/C26H32N6O2S/c1-16-9-18-11-22(35-25(18)21(10-16)33-2)23-19(14-34-13-17-3-4-17)20(12-31-7-5-28-6-8-31)32-24(23)26(27)29-15-30-32/h9-11,15,17,28H,3-8,12-14H2,1-2H3,(H2,27,29,30)
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n/an/a 0.700n/an/an/an/a7.022



BAYER INTELLECTUAL PROPERTY GmbH

US Patent


Assay Description
For the assay, 50 nl of each stock solution of the test compound in DMSO was pipetted into a black, low-volume 384-well microtiter plate (Greiner Bio...


US Patent US9206184 (2015)


BindingDB Entry DOI: 10.7270/Q2SN07SH
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (human))
BDBM194837
PNG
(US9206184, 18 | US9206184, 19)
Show SMILES CCOCc1c(CN2CCNCC2)n2ncnc(N)c2c1-c1cc2cc(C)cc(OC)c2s1
Show InChI InChI=1S/C24H30N6O2S/c1-4-32-13-17-18(12-29-7-5-26-6-8-29)30-22(24(25)27-14-28-30)21(17)20-11-16-9-15(2)10-19(31-3)23(16)33-20/h9-11,14,26H,4-8,12-13H2,1-3H3,(H2,25,27,28)
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BAYER INTELLECTUAL PROPERTY GmbH

US Patent


Assay Description
For the assay, 50 nl of each stock solution of the test compound in DMSO was pipetted into a black, low-volume 384-well microtiter plate (Greiner Bio...


US Patent US9206184 (2015)


BindingDB Entry DOI: 10.7270/Q2SN07SH
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (human))
BDBM302419
PNG
(US9598416, Example 65)
Show SMILES COc1cc(C)cc2cc(sc12)-c1c(CN2CC[C@H](C2)N(C)C)cn2ncnc(N)c12
Show InChI InChI=1S/C23H28N6OS/c1-14-7-15-9-19(31-22(15)18(8-14)30-4)20-16(10-28-6-5-17(12-28)27(2)3)11-29-21(20)23(24)25-13-26-29/h7-9,11,13,17H,5-6,10,12H2,1-4H3,(H2,24,25,26)/t17-/m1/s1
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n/an/a 0.700n/an/an/an/an/an/a



BAYER INTELLECTUAL PROPERTY GMBH

US Patent


Assay Description
Usually, test compounds were tested on the same microtiter plate at 11 different concentrations in the range of 20 μM to 0.1 nM (e.g. 20 μM...


US Patent US9598416 (2017)

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


(Homo sapiens (human))
BDBM302363
PNG
(N-{[4-Amino-5-(7-methoxy-5-methyl-1-benzothiophen-...)
Show SMILES COc1cc(C)cc2cc(sc12)-c1c(CNC(C)=O)cn2ncnc(N)c12
Show InChI InChI=1S/C19H19N5O2S/c1-10-4-12-6-15(27-18(12)14(5-10)26-3)16-13(7-21-11(2)25)8-24-17(16)19(20)22-9-23-24/h4-6,8-9H,7H2,1-3H3,(H,21,25)(H2,20,22,23)
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n/an/a 0.700n/an/an/an/an/an/a



BAYER INTELLECTUAL PROPERTY GMBH

US Patent


Assay Description
Usually, test compounds were tested on the same microtiter plate at 11 different concentrations in the range of 20 μM to 0.1 nM (e.g. 20 μM...


US Patent US9598416 (2017)

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


(Homo sapiens (human))
BDBM287015
PNG
((R)-8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-...)
Show SMILES COc1cc(OC)c(Cl)c(c1Cl)-c1cc2cnc(N[C@@H]3CCOC3)nc2n(CCCN2CCN(CC2)C(=O)C=C)c1=O
Show InChI InChI=1S/C29H34Cl2N6O5/c1-4-23(38)36-11-9-35(10-12-36)7-5-8-37-27-18(16-32-29(34-27)33-19-6-13-42-17-19)14-20(28(37)39)24-25(30)21(40-2)15-22(41-3)26(24)31/h4,14-16,19H,1,5-13,17H2,2-3H3,(H,32,33,34)/t19-/m1/s1
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n/an/a 0.700n/an/an/an/an/a25



Principia Biopharma, Inc.

US Patent


Assay Description
A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin...


US Patent US9567334 (2017)

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


(Homo sapiens (human))
BDBM287006
PNG
(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Show SMILES COc1cc(OC)c(Cl)c(c1Cl)-c1cc2cnc(NCC3CCOCC3)nc2n(CCCN2CCN(CC2)C(=O)C=C)c1=O
Show InChI InChI=1S/C31H38Cl2N6O5/c1-4-25(40)38-12-10-37(11-13-38)8-5-9-39-29-21(19-35-31(36-29)34-18-20-6-14-44-15-7-20)16-22(30(39)41)26-27(32)23(42-2)17-24(43-3)28(26)33/h4,16-17,19-20H,1,5-15,18H2,2-3H3,(H,34,35,36)
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Principia Biopharma, Inc.

US Patent


Assay Description
A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin...


US Patent US9567334 (2017)

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


(Homo sapiens (human))
BDBM286381
PNG
(8-(2-((1-acryloylpiperidin-3-yl)oxy)ethyl)-6-(2,6-...)
Show SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCOC3CCCN(C3)C(=O)C=C)c2n1
Show InChI InChI=1S/C26H29Cl2N5O5/c1-5-20(34)32-8-6-7-16(14-32)38-10-9-33-24-15(13-30-26(29-2)31-24)11-17(25(33)35)21-22(27)18(36-3)12-19(37-4)23(21)28/h5,11-13,16H,1,6-10,14H2,2-4H3,(H,29,30,31)
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Principia Biopharma, Inc.

US Patent


Assay Description
A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin...


US Patent US9567334 (2017)

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


(Homo sapiens (human))
BDBM287508
PNG
(8-(2-((1-acryloylazetidin-3-yl)(methyl)amino)ethyl...)
Show SMILES CCNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCN(C)C3CN(C3)C(=O)C=C)c2n1
Show InChI InChI=1S/C26H30Cl2N6O4/c1-6-20(35)33-13-16(14-33)32(3)8-9-34-24-15(12-30-26(31-24)29-7-2)10-17(25(34)36)21-22(27)18(37-4)11-19(38-5)23(21)28/h6,10-12,16H,1,7-9,13-14H2,2-5H3,(H,29,30,31)
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Principia Biopharma, Inc.

US Patent


Assay Description
A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin...


US Patent US9567334 (2017)

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


(Homo sapiens (human))
BDBM287058
PNG
((R)-8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-...)
Show SMILES COC[C@@H](C)Nc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCCN3CCN(CC3)C(=O)C=C)c2n1
Show InChI InChI=1S/C29H36Cl2N6O5/c1-6-23(38)36-12-10-35(11-13-36)8-7-9-37-27-19(16-32-29(34-27)33-18(2)17-40-3)14-20(28(37)39)24-25(30)21(41-4)15-22(42-5)26(24)31/h6,14-16,18H,1,7-13,17H2,2-5H3,(H,32,33,34)/t18-/m1/s1
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Principia Biopharma, Inc.

US Patent


Assay Description
A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin...


US Patent US9567334 (2017)

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


(Homo sapiens (human))
BDBM50189868
PNG
(CHEMBL3828465)
Show SMILES CC(Oc1ccc2[nH]nc(-c3nc4cc(ccc4[nH]3)N3CCC(CC3)N3CCCCC3)c2c1)c1c(Cl)cncc1Cl
Show InChI InChI=1S/C31H33Cl2N7O/c1-19(29-24(32)17-34-18-25(29)33)41-22-6-8-26-23(16-22)30(38-37-26)31-35-27-7-5-21(15-28(27)36-31)40-13-9-20(10-14-40)39-11-3-2-4-12-39/h5-8,15-20H,2-4,9-14H2,1H3,(H,35,36)(H,37,38)
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n/an/a 0.800n/an/an/an/an/an/a



East China University of Science& Technology

Curated by ChEMBL


Assay Description
Inhibition of recombinant human FGFR1 using poly (Glu, Tyr) 4:1 as substrate after 60 mins by ELISA


J Med Chem 59: 6690-708 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00056
BindingDB Entry DOI: 10.7270/Q2474CT3
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (human))
BDBM286995
PNG
(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Show SMILES COc1cc(OC)c(Cl)c(c1Cl)-c1cc2cnc(Nc3ccccc3)nc2n(CCCN2CCN(CC2)C(=O)C=C)c1=O
Show InChI InChI=1S/C31H32Cl2N6O4/c1-4-25(40)38-15-13-37(14-16-38)11-8-12-39-29-20(19-34-31(36-29)35-21-9-6-5-7-10-21)17-22(30(39)41)26-27(32)23(42-2)18-24(43-3)28(26)33/h4-7,9-10,17-19H,1,8,11-16H2,2-3H3,(H,34,35,36)
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Principia Biopharma, Inc.

US Patent


Assay Description
A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin...


US Patent US9567334 (2017)

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


(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 0.800n/an/an/an/an/an/a



Chinese Academy of Sciences (CAS)

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR1 (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 1


(Homo sapiens (human))
BDBM130811
PNG
(US8829199, 40)
Show SMILES Cc1nc2ccc(cc2n1)-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 0.810n/an/an/an/an/an/a



Chugai Seiyaku Kabushiki Kaisha; F. Hoffmann-La Roche AG

US Patent


Assay Description
The FGFR1-inhibiting activity was measured based on the activity to inhibit phosphorylation of the biotinylated peptide EGPWLEEEEEAYGWMDF by the huma...


US Patent US8829199 (2014)


BindingDB Entry DOI: 10.7270/Q26T0KB8
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (human))
BDBM194845
PNG
(US9206184, 26)
Show SMILES COc1cc(C)cc2cc(sc12)-c1c(COC2CCC2)c(CN2CCNCC2)n2ncnc(N)c12
Show InChI InChI=1S/C26H32N6O2S/c1-16-10-17-12-22(35-25(17)21(11-16)33-2)23-19(14-34-18-4-3-5-18)20(13-31-8-6-28-7-9-31)32-24(23)26(27)29-15-30-32/h10-12,15,18,28H,3-9,13-14H2,1-2H3,(H2,27,29,30)
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n/an/a 0.900n/an/an/an/a7.022



BAYER INTELLECTUAL PROPERTY GmbH

US Patent


Assay Description
For the assay, 50 nl of each stock solution of the test compound in DMSO was pipetted into a black, low-volume 384-well microtiter plate (Greiner Bio...


US Patent US9206184 (2015)


BindingDB Entry DOI: 10.7270/Q2SN07SH
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (human))
BDBM302421
PNG
(US9598416, Example 67)
Show SMILES COc1cc(C)cc2cc(sc12)-c1c(CN2CCCC(C2)N(C)C)cn2ncnc(N)c12
Show InChI InChI=1S/C24H30N6OS/c1-15-8-16-10-20(32-23(16)19(9-15)31-4)21-17(12-30-22(21)24(25)26-14-27-30)11-29-7-5-6-18(13-29)28(2)3/h8-10,12,14,18H,5-7,11,13H2,1-4H3,(H2,25,26,27)
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BAYER INTELLECTUAL PROPERTY GMBH

US Patent


Assay Description
Usually, test compounds were tested on the same microtiter plate at 11 different concentrations in the range of 20 μM to 0.1 nM (e.g. 20 μM...


US Patent US9598416 (2017)

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


(Homo sapiens (human))
BDBM194841
PNG
(US9206184, 22)
Show SMILES COc1cc(C)cc2cc(sc12)-c1c(COCCO)c(CN2CCNCC2)n2ncnc(N)c12
Show InChI InChI=1S/C24H30N6O3S/c1-15-9-16-11-20(34-23(16)19(10-15)32-2)21-17(13-33-8-7-31)18(12-29-5-3-26-4-6-29)30-22(21)24(25)27-14-28-30/h9-11,14,26,31H,3-8,12-13H2,1-2H3,(H2,25,27,28)
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BAYER INTELLECTUAL PROPERTY GmbH

US Patent


Assay Description
For the assay, 50 nl of each stock solution of the test compound in DMSO was pipetted into a black, low-volume 384-well microtiter plate (Greiner Bio...


US Patent US9206184 (2015)


BindingDB Entry DOI: 10.7270/Q2SN07SH
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (human))
BDBM287048
PNG
(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Show SMILES COc1cc(OC)c(Cl)c(c1Cl)-c1cc2cnc(N[C@H]3CC[C@H](O)CC3)nc2n(CCCN2CCN(CC2)C(=O)C=C)c1=O
Show InChI InChI=1S/C31H38Cl2N6O5/c1-4-25(41)38-14-12-37(13-15-38)10-5-11-39-29-19(18-34-31(36-29)35-20-6-8-21(40)9-7-20)16-22(30(39)42)26-27(32)23(43-2)17-24(44-3)28(26)33/h4,16-18,20-21,40H,1,5-15H2,2-3H3,(H,34,35,36)/t20-,21-
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n/an/a 0.900n/an/an/an/an/a25



Principia Biopharma, Inc.

US Patent


Assay Description
A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin...


US Patent US9567334 (2017)

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


(Homo sapiens (human))
BDBM302381
PNG
((3S)-3-({[4-Amino-5-(7-methoxy-5-methyl-1-benzothi...)
Show SMILES COc1cc(C)cc2cc(sc12)-c1c(CN[C@H]2CCNC2=O)cn2ncnc(N)c12
Show InChI InChI=1S/C21H22N6O2S/c1-11-5-12-7-16(30-19(12)15(6-11)29-2)17-13(8-24-14-3-4-23-21(14)28)9-27-18(17)20(22)25-10-26-27/h5-7,9-10,14,24H,3-4,8H2,1-2H3,(H,23,28)(H2,22,25,26)/t14-/m0/s1
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n/an/a 0.900n/an/an/an/an/an/a



BAYER INTELLECTUAL PROPERTY GMBH

US Patent


Assay Description
Usually, test compounds were tested on the same microtiter plate at 11 different concentrations in the range of 20 μM to 0.1 nM (e.g. 20 μM...


US Patent US9598416 (2017)

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


(Homo sapiens (human))
BDBM287529
PNG
(8-(2-((1-acryloylazetidin-3-yl)amino)ethyl)-6-(2,6...)
Show SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCNC3CN(C3)C(=O)C=C)c2n1
Show InChI InChI=1S/C24H26Cl2N6O4/c1-5-18(33)31-11-14(12-31)28-6-7-32-22-13(10-29-24(27-2)30-22)8-15(23(32)34)19-20(25)16(35-3)9-17(36-4)21(19)26/h5,8-10,14,28H,1,6-7,11-12H2,2-4H3,(H,27,29,30)
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n/an/a 0.900n/an/an/an/an/a25



Principia Biopharma, Inc.

US Patent


Assay Description
A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin...


US Patent US9567334 (2017)

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


(Homo sapiens (human))
BDBM50355393
PNG
(CHEMBL1834657 | US9434697, BGJ398)
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 0.900n/an/an/an/an/an/a



Novartis Institute for BioMedical Research

Curated by ChEMBL


Assay Description
Inhibition of recombinant FGFR1


J Med Chem 54: 7066-83 (2011)


Article DOI: 10.1021/jm2006222
BindingDB Entry DOI: 10.7270/Q22N52N1
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Fibroblast growth factor receptor 1


(Homo sapiens (human))
BDBM194836
PNG
(US9206184, 17)
Show SMILES COCc1c(CN2CCNCC2)n2ncnc(N)c2c1-c1cc2cc(C)cc(OC)c2s1
Show InChI InChI=1S/C23H28N6O2S/c1-14-8-15-10-19(32-22(15)18(9-14)31-3)20-16(12-30-2)17(11-28-6-4-25-5-7-28)29-21(20)23(24)26-13-27-29/h8-10,13,25H,4-7,11-12H2,1-3H3,(H2,24,26,27)
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BAYER INTELLECTUAL PROPERTY GmbH

US Patent


Assay Description
For the assay, 50 nl of each stock solution of the test compound in DMSO was pipetted into a black, low-volume 384-well microtiter plate (Greiner Bio...


US Patent US9206184 (2015)


BindingDB Entry DOI: 10.7270/Q2SN07SH
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (human))
BDBM286999
PNG
(8-((1-((4-acryloylpiperazin-1-yl)methyl)cyclopropy...)
Show SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CC3(CN4CCN(CC4)C(=O)C=C)CC3)c2n1
Show InChI InChI=1S/C28H32Cl2N6O4/c1-5-21(37)35-10-8-34(9-11-35)15-28(6-7-28)16-36-25-17(14-32-27(31-2)33-25)12-18(26(36)38)22-23(29)19(39-3)13-20(40-4)24(22)30/h5,12-14H,1,6-11,15-16H2,2-4H3,(H,31,32,33)
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Principia Biopharma, Inc.

US Patent


Assay Description
A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin...


US Patent US9567334 (2017)

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


(Homo sapiens (human))
BDBM286998
PNG
(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Show SMILES CCNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCCN3CCN(CC3)C(=O)C=C)c2n1
Show InChI InChI=1S/C27H32Cl2N6O4/c1-5-21(36)34-12-10-33(11-13-34)8-7-9-35-25-17(16-31-27(32-25)30-6-2)14-18(26(35)37)22-23(28)19(38-3)15-20(39-4)24(22)29/h5,14-16H,1,6-13H2,2-4H3,(H,30,31,32)
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Principia Biopharma, Inc.

US Patent


Assay Description
A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin...


US Patent US9567334 (2017)

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


(Homo sapiens (human))
BDBM286992
PNG
(8-(2-((1-acryloylpiperidin-4-yl)oxy)ethyl)-6-(2,6-...)
Show SMILES CCNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCOC3CCN(CC3)C(=O)C=C)c2n1
Show InChI InChI=1S/C27H31Cl2N5O5/c1-5-21(35)33-9-7-17(8-10-33)39-12-11-34-25-16(15-31-27(32-25)30-6-2)13-18(26(34)36)22-23(28)19(37-3)14-20(38-4)24(22)29/h5,13-15,17H,1,6-12H2,2-4H3,(H,30,31,32)
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Principia Biopharma, Inc.

US Patent


Assay Description
A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin...


US Patent US9567334 (2017)

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


(Homo sapiens (human))
BDBM287044
PNG
(8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dich...)
Show SMILES COc1cc(OC)c(Cl)c(c1Cl)-c1cc2cnc(NCCOC(C)C)nc2n(CCCN2CCN(CC2)C(=O)C=C)c1=O
Show InChI InChI=1S/C30H38Cl2N6O5/c1-6-24(39)37-13-11-36(12-14-37)9-7-10-38-28-20(18-34-30(35-28)33-8-15-43-19(2)3)16-21(29(38)40)25-26(31)22(41-4)17-23(42-5)27(25)32/h6,16-19H,1,7-15H2,2-5H3,(H,33,34,35)
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Principia Biopharma, Inc.

US Patent


Assay Description
A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of FGFR family (FGFR1, FGFR2, FGFR3, FGFR4) kin...


US Patent US9567334 (2017)

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


(Homo sapiens (human))
BDBM50189787
PNG
(CHEMBL3827178)
Show SMILES C[C@@H](Oc1ccc2[nH]nc(-c3nc4cc(ccc4[nH]3)N3CCN(C)CC3)c2c1)c1c(Cl)cncc1Cl
Show InChI InChI=1S/C26H25Cl2N7O/c1-15(24-19(27)13-29-14-20(24)28)36-17-4-6-21-18(12-17)25(33-32-21)26-30-22-5-3-16(11-23(22)31-26)35-9-7-34(2)8-10-35/h3-6,11-15H,7-10H2,1-2H3,(H,30,31)(H,32,33)/t15-/m1/s1
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East China University of Science& Technology

Curated by ChEMBL


Assay Description
Inhibition of recombinant human FGFR1 using poly (Glu, Tyr) 4:1 as substrate after 60 mins by ELISA


J Med Chem 59: 6690-708 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00056
BindingDB Entry DOI: 10.7270/Q2474CT3
More data for this
Ligand-Target Pair
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