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Compile Data Set for Download or QSAR

Found 231 hits with Last Name = 'phan' and Initial = 't'   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Fibroblast growth factor receptor 2


(Homo sapiens (Human))
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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1.30n/an/an/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Irreversible inhibition of human FGFR2 preincubated with enzyme followed by peptide substrate addition by caliper capillary electrophoresis method


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
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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1.60n/an/an/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Irreversible inhibition of human FGFR1 using 5-FAM-KKKKEEIYFFF-NH2 as substrate preincubated with enzyme followed by peptide substrate addition by ca...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(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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2.20n/an/an/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Irreversible inhibition of human FGFR3 preincubated with enzyme followed by peptide substrate addition by caliper capillary electrophoresis method


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 4


(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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73n/an/an/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Irreversible inhibition of human FGFR4 preincubated with enzyme followed by peptide substrate addition by caliper capillary electrophoresis method


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238808
PNG
(CHEMBL4102642)
Show SMILES CCN1CCN(CCNc2ncc3cc(-c4cc(OC)cc(OC)c4Cl)c(=O)n(CCc4ccc(NC(=O)C=C)cc4)c3n2)CC1
Show InChI InChI=1S/C34H40ClN7O4/c1-5-30(43)38-25-9-7-23(8-10-25)11-13-42-32-24(19-28(33(42)44)27-20-26(45-3)21-29(46-4)31(27)35)22-37-34(39-32)36-12-14-41-17-15-40(6-2)16-18-41/h5,7-10,19-22H,1,6,11-18H2,2-4H3,(H,38,43)(H,36,37,39)
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n/an/a 0.200n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
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/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
In vitro antagonist activity against rat prostatic androgen receptor (AR)


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Protein kinase B (Akt1 E49C, C296S, C310S and C344S )


(Homo sapiens (Human))
BDBM25013
PNG
(4-[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S...)
Show SMILES CCn1c(nc2c(ncc(OC[C@H]3CCCNC3)c12)C#CC(C)(C)O)-c1nonc1N
Show InChI InChI=1/C21H27N7O3/c1-4-28-18-15(30-12-13-6-5-9-23-10-13)11-24-14(7-8-21(2,3)29)16(18)25-20(28)17-19(22)27-31-26-17/h11,13,23,29H,4-6,9-10,12H2,1-3H3,(H2,22,27)/t13-/s2
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n/an/a 0.400n/an/an/an/an/an/a



Technische Universitšt Dortmund



Assay Description
IC50 determinations for activated Akt1 were measured with the KinEASE assay (Cisbio) according to the manufacturer’s instructions. The kinases A...


ACS Chem Biol 10: 279-88 (2015)


Article DOI: 10.1021/cb500355c
BindingDB Entry DOI: 10.7270/Q218358G
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Discoidin domain-containing receptor 2


(Homo sapiens (Human))
BDBM13216
PNG
(BMS-354825 | CHEMBL1421 | DASATINIB | N-(2-Chloro-...)
Show SMILES Cc1nc(Nc2ncc(s2)C(=O)Nc2c(C)cccc2Cl)cc(n1)N1CCN(CCO)CC1
Show InChI InChI=1S/C22H26ClN7O2S/c1-14-4-3-5-16(23)20(14)28-21(32)17-13-24-22(33-17)27-18-12-19(26-15(2)25-18)30-8-6-29(7-9-30)10-11-31/h3-5,12-13,31H,6-11H2,1-2H3,(H,28,32)(H,24,25,26,27)
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n/an/a 0.400n/an/an/an/an/an/a



Technical University of Dortmund

Curated by ChEMBL


Assay Description
Inhibition of wild type DDR2 (unknown origin) preincubated for 30 mins before substrate addition by FRET assay


J Med Chem 57: 4252-62 (2014)


Article DOI: 10.1021/jm500167q
BindingDB Entry DOI: 10.7270/Q2Z039P4
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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n/an/a 0.600n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of human FGFR1 using 5-FAM-KKKKEEIYFFF-NH2 as substrate preincubated for 15 mins followed by peptide substrate addition measured after 3 h...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238813
PNG
(CHEMBL4083740)
Show SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCCCNC(=O)C=C)c2n1
Show InChI InChI=1S/C23H25Cl2N5O4/c1-5-17(31)27-8-6-7-9-30-21-13(12-28-23(26-2)29-21)10-14(22(30)32)18-19(24)15(33-3)11-16(34-4)20(18)25/h5,10-12H,1,6-9H2,2-4H3,(H,27,31)(H,26,28,29)
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n/an/a 0.700n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
In vitro antagonist activity against rat prostatic androgen receptor (AR)


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
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=1/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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n/an/a 0.700n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238823
PNG
(CHEMBL4086567)
Show SMILES COc1cc(OC)c(Cl)c(c1)-c1cc2cnc(NCCN3CCN(C)CC3)nc2n(CCc2ccc(NC(=O)C=C)cc2)c1=O
Show InChI InChI=1S/C33H38ClN7O4/c1-5-29(42)37-24-8-6-22(7-9-24)10-12-41-31-23(21-36-33(38-31)35-11-13-40-16-14-39(2)15-17-40)18-27(32(41)43)26-19-25(44-3)20-28(45-4)30(26)34/h5-9,18-21H,1,10-17H2,2-4H3,(H,37,42)(H,35,36,38)
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n/an/a 0.800n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of human FGFR1 using 5-FAM-KKKKEEIYFFF-NH2 as substrate preincubated for 15 mins followed by peptide substrate addition measured after 3 h...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238811
PNG
(CHEMBL4073347)
Show SMILES COc1cc(OC)c(Cl)c(c1)-c1cc2cnc(NC(CO)CO)nc2n(CCc2ccc(NC(=O)C=C)cc2)c1=O
Show InChI InChI=1S/C29H30ClN5O6/c1-4-25(38)32-19-7-5-17(6-8-19)9-10-35-27-18(14-31-29(34-27)33-20(15-36)16-37)11-23(28(35)39)22-12-21(40-2)13-24(41-3)26(22)30/h4-8,11-14,20,36-37H,1,9-10,15-16H2,2-3H3,(H,32,38)(H,31,33,34)
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n/an/a 0.800n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM287067
PNG
(8-(2-((1-acryloylazetidin-3-yl)(methyl)amino)ethyl...)
Show SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCN(C)C3CN(C3)C(=O)C=C)c2n1
Show InChI InChI=1S/C25H28Cl2N6O4/c1-6-19(34)32-12-15(13-32)31(3)7-8-33-23-14(11-29-25(28-2)30-23)9-16(24(33)35)20-21(26)17(36-4)10-18(37-5)22(20)27/h6,9-11,15H,1,7-8,12-13H2,2-5H3,(H,28,29,30)
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n/an/a 1n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238810
PNG
(CHEMBL4092456)
Show SMILES COc1cc(OC)c(Cl)c(c1)-c1cc2cnc(NCCO)nc2n(CCc2ccc(NC(=O)C=C)cc2)c1=O
Show InChI InChI=1S/C28H28ClN5O5/c1-4-24(36)32-19-7-5-17(6-8-19)9-11-34-26-18(16-31-28(33-26)30-10-12-35)13-22(27(34)37)21-14-20(38-2)15-23(39-3)25(21)29/h4-8,13-16,35H,1,9-12H2,2-3H3,(H,32,36)(H,30,31,33)
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n/an/a 1n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238809
PNG
(CHEMBL4084708)
Show SMILES COc1cc(OC)c(Cl)c(c1)-c1cc2cnc(NCCN3CCN(CC3)C(C)=O)nc2n(CCc2ccc(NC(=O)C=C)cc2)c1=O
Show InChI InChI=1S/C34H38ClN7O5/c1-5-30(44)38-25-8-6-23(7-9-25)10-12-42-32-24(18-28(33(42)45)27-19-26(46-3)20-29(47-4)31(27)35)21-37-34(39-32)36-11-13-40-14-16-41(17-15-40)22(2)43/h5-9,18-21H,1,10-17H2,2-4H3,(H,38,44)(H,36,37,39)
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n/an/a 1.10n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of human FGFR1 using 5-FAM-KKKKEEIYFFF-NH2 as substrate preincubated for 15 mins followed by peptide substrate addition measured after 3 h...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
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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n/an/a 1.10n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
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 1.20n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238804
PNG
(CHEMBL4099578)
Show SMILES CNc1ncc2cc(-c3cc(OC)cc(OC)c3Cl)c(=O)n(CCc3ccc(NC(=O)C=C)cc3)c2n1
Show InChI InChI=1S/C27H26ClN5O4/c1-5-23(34)31-18-8-6-16(7-9-18)10-11-33-25-17(15-30-27(29-2)32-25)12-21(26(33)35)20-13-19(36-3)14-22(37-4)24(20)28/h5-9,12-15H,1,10-11H2,2-4H3,(H,31,34)(H,29,30,32)
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n/an/a 1.30n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238806
PNG
(CHEMBL4083151)
Show SMILES CNc1ncc2cc(-c3cc(OC)cc(OC)c3Cl)c(=O)n(CCc3ccc(NC(=O)C=C)cn3)c2n1
Show InChI InChI=1S/C26H25ClN6O4/c1-5-22(34)31-17-7-6-16(29-14-17)8-9-33-24-15(13-30-26(28-2)32-24)10-20(25(33)35)19-11-18(36-3)12-21(37-4)23(19)27/h5-7,10-14H,1,8-9H2,2-4H3,(H,31,34)(H,28,30,32)
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n/an/a 1.30n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of human FGFR1 using 5-FAM-KKKKEEIYFFF-NH2 as substrate preincubated for 15 mins followed by peptide substrate addition measured after 3 h...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238805
PNG
(CHEMBL4061286)
Show SMILES CNc1ncc2cc(-c3cc(OC)cc(OC)c3Cl)c(=O)n(CCc3ccc(NC(=O)C=C)nc3)c2n1
Show InChI InChI=1S/C26H25ClN6O4/c1-5-22(34)31-21-7-6-15(13-29-21)8-9-33-24-16(14-30-26(28-2)32-24)10-19(25(33)35)18-11-17(36-3)12-20(37-4)23(18)27/h5-7,10-14H,1,8-9H2,2-4H3,(H,28,30,32)(H,29,31,34)
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n/an/a 1.30n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
In vitro antagonist activity against rat prostatic androgen receptor (AR)


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM287067
PNG
(8-(2-((1-acryloylazetidin-3-yl)(methyl)amino)ethyl...)
Show SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCN(C)C3CN(C3)C(=O)C=C)c2n1
Show InChI InChI=1S/C25H28Cl2N6O4/c1-6-19(34)32-12-15(13-32)31(3)7-8-33-23-14(11-29-25(28-2)30-23)9-16(24(33)35)20-21(26)17(36-4)10-18(37-5)22(20)27/h6,9-11,15H,1,7-8,12-13H2,2-5H3,(H,28,29,30)
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n/an/a 1.30n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 2


(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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n/an/a 1.30n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of human FGFR2 preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238818
PNG
(CHEMBL4064081)
Show SMILES COc1cc(OC)c(Cl)c(c1)-c1cc2cnc(NCCN3CCOCC3)nc2n(CCc2ccc(NC(=O)C=C)cc2)c1=O
Show InChI InChI=1S/C32H35ClN6O5/c1-4-28(40)36-23-7-5-21(6-8-23)9-11-39-30-22(20-35-32(37-30)34-10-12-38-13-15-44-16-14-38)17-26(31(39)41)25-18-24(42-2)19-27(43-3)29(25)33/h4-8,17-20H,1,9-16H2,2-3H3,(H,36,40)(H,34,35,37)
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n/an/a 1.40n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of human FGFR1 using 5-FAM-KKKKEEIYFFF-NH2 as substrate preincubated for 15 mins followed by peptide substrate addition measured after 3 h...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238824
PNG
(CHEMBL4064756)
Show SMILES COc1cc(OC)c(Cl)c(c1)-c1cc2cnc(NCCCN3CCOCC3)nc2n(CCc2ccc(NC(=O)C=C)cc2)c1=O
Show InChI InChI=1S/C33H37ClN6O5/c1-4-29(41)37-24-8-6-22(7-9-24)10-13-40-31-23(21-36-33(38-31)35-11-5-12-39-14-16-45-17-15-39)18-27(32(40)42)26-19-25(43-2)20-28(44-3)30(26)34/h4,6-9,18-21H,1,5,10-17H2,2-3H3,(H,37,41)(H,35,36,38)
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n/an/a 1.5n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of human FGFR1 using 5-FAM-KKKKEEIYFFF-NH2 as substrate preincubated for 15 mins followed by peptide substrate addition measured after 3 h...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM287559
PNG
(8-(2-((1-acryloylpiperidin-4-yl)(methyl)amino)ethy...)
Show SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCN(C)C3CCN(CC3)C(=O)C=C)c2n1
Show InChI InChI=1S/C27H32Cl2N6O4/c1-6-21(36)34-9-7-17(8-10-34)33(3)11-12-35-25-16(15-31-27(30-2)32-25)13-18(26(35)37)22-23(28)19(38-4)14-20(39-5)24(22)29/h6,13-15,17H,1,7-12H2,2-5H3,(H,30,31,32)
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n/an/a 1.5n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238803
PNG
(CHEMBL4066763)
Show SMILES CNc1ncc2cc(-c3cc(OC)cc(OC)c3Cl)c(=O)n(CCc3cccc(NC(=O)C=C)n3)c2n1
Show InChI InChI=1S/C26H25ClN6O4/c1-5-22(34)31-21-8-6-7-16(30-21)9-10-33-24-15(14-29-26(28-2)32-24)11-19(25(33)35)18-12-17(36-3)13-20(37-4)23(18)27/h5-8,11-14H,1,9-10H2,2-4H3,(H,28,29,32)(H,30,31,34)
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n/an/a 1.60n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238805
PNG
(CHEMBL4061286)
Show SMILES CNc1ncc2cc(-c3cc(OC)cc(OC)c3Cl)c(=O)n(CCc3ccc(NC(=O)C=C)nc3)c2n1
Show InChI InChI=1S/C26H25ClN6O4/c1-5-22(34)31-21-7-6-15(13-29-21)8-9-33-24-16(14-30-26(28-2)32-24)10-19(25(33)35)18-11-17(36-3)12-20(37-4)23(18)27/h5-7,10-14H,1,8-9H2,2-4H3,(H,28,30,32)(H,29,31,34)
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n/an/a 1.60n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238803
PNG
(CHEMBL4066763)
Show SMILES CNc1ncc2cc(-c3cc(OC)cc(OC)c3Cl)c(=O)n(CCc3cccc(NC(=O)C=C)n3)c2n1
Show InChI InChI=1S/C26H25ClN6O4/c1-5-22(34)31-21-8-6-7-16(30-21)9-10-33-24-15(14-29-26(28-2)32-24)11-19(25(33)35)18-12-17(36-3)13-20(37-4)23(18)27/h5-8,11-14H,1,9-10H2,2-4H3,(H,28,29,32)(H,30,31,34)
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n/an/a 1.70n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM286523
PNG
(8-(2-((1-acryloylpyrrolidin-3-yl)oxy)ethyl)-6-(2,6...)
Show SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCOC3CCN(C3)C(=O)C=C)c2n1
Show InChI InChI=1/C25H27Cl2N5O5/c1-5-19(33)31-7-6-15(13-31)37-9-8-32-23-14(12-29-25(28-2)30-23)10-16(24(32)34)20-21(26)17(35-3)11-18(36-4)22(20)27/h5,10-12,15H,1,6-9,13H2,2-4H3,(H,28,29,30)
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n/an/a 1.80n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238821
PNG
(CHEMBL4088057)
Show SMILES CNc1ncc2cc(-c3cc(OC)cc(OC)c3Cl)c(=O)n(CCc3ccnc(NC(=O)C=C)c3)c2n1
Show InChI InChI=1S/C26H25ClN6O4/c1-5-22(34)31-21-10-15(6-8-29-21)7-9-33-24-16(14-30-26(28-2)32-24)11-19(25(33)35)18-12-17(36-3)13-20(37-4)23(18)27/h5-6,8,10-14H,1,7,9H2,2-4H3,(H,28,30,32)(H,29,31,34)
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n/an/a 1.90n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of human FGFR1 using 5-FAM-KKKKEEIYFFF-NH2 as substrate preincubated for 15 mins followed by peptide substrate addition measured after 3 h...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Discoidin domain-containing receptor 2


(Homo sapiens (Human))
BDBM50437147
PNG
(CHEMBL2403875)
Show SMILES CC(C)(C)c1cc(NC(=O)Nc2cccc(Nc3ncnc4ccccc34)c2)n(n1)-c1cccc(N)c1
Show InChI InChI=1S/C28H28N8O/c1-28(2,3)24-16-25(36(35-24)21-11-6-8-18(29)14-21)34-27(37)33-20-10-7-9-19(15-20)32-26-22-12-4-5-13-23(22)30-17-31-26/h4-17H,29H2,1-3H3,(H,30,31,32)(H2,33,34,37)
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n/an/a 2n/an/an/an/an/an/a



Technical University of Dortmund

Curated by ChEMBL


Assay Description
Inhibition of wild type DDR2 (unknown origin) preincubated for 30 mins before substrate addition by FRET assay


J Med Chem 57: 4252-62 (2014)


Article DOI: 10.1021/jm500167q
BindingDB Entry DOI: 10.7270/Q2Z039P4
More data for this
Ligand-Target Pair
Discoidin domain-containing receptor 2


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



Technical University of Dortmund

Curated by ChEMBL


Assay Description
Inhibition of wild type DDR2 (unknown origin) preincubated for 30 mins before substrate addition by FRET assay


J Med Chem 57: 4252-62 (2014)


Article DOI: 10.1021/jm500167q
BindingDB Entry DOI: 10.7270/Q2Z039P4
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238816
PNG
(CHEMBL4084079)
Show SMILES CNc1ncc2cc(-c3cc(OC)cc(OC)c3Cl)c(=O)n(CCc3cnc(NC(=O)C=C)cn3)c2n1
Show InChI InChI=1S/C25H24ClN7O4/c1-5-21(34)31-20-13-28-15(12-29-20)6-7-33-23-14(11-30-25(27-2)32-23)8-18(24(33)35)17-9-16(36-3)10-19(37-4)22(17)26/h5,8-13H,1,6-7H2,2-4H3,(H,27,30,32)(H,29,31,34)
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n/an/a 2.10n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
In vitro antagonist activity against rat prostatic androgen receptor (AR)


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238821
PNG
(CHEMBL4088057)
Show SMILES CNc1ncc2cc(-c3cc(OC)cc(OC)c3Cl)c(=O)n(CCc3ccnc(NC(=O)C=C)c3)c2n1
Show InChI InChI=1S/C26H25ClN6O4/c1-5-22(34)31-21-10-15(6-8-29-21)7-9-33-24-16(14-30-26(28-2)32-24)11-19(25(33)35)18-12-17(36-3)13-20(37-4)23(18)27/h5-6,8,10-14H,1,7,9H2,2-4H3,(H,28,30,32)(H,29,31,34)
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n/an/a 2.20n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM286388
PNG
(8-(2-(4-acryloylpiperazin-1-yl)ethyl)-6-(2,6-dichl...)
Show SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCN3CCN(CC3)C(=O)C=C)c2n1
Show InChI InChI=1S/C25H28Cl2N6O4/c1-5-19(34)32-9-6-31(7-10-32)8-11-33-23-15(14-29-25(28-2)30-23)12-16(24(33)35)20-21(26)17(36-3)13-18(37-4)22(20)27/h5,12-14H,1,6-11H2,2-4H3,(H,28,29,30)
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n/an/a 2.30n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of human FGFR1 using 5-FAM-KKKKEEIYFFF-NH2 as substrate preincubated for 15 mins followed by peptide substrate addition measured after 3 h...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238810
PNG
(CHEMBL4092456)
Show SMILES COc1cc(OC)c(Cl)c(c1)-c1cc2cnc(NCCO)nc2n(CCc2ccc(NC(=O)C=C)cc2)c1=O
Show InChI InChI=1S/C28H28ClN5O5/c1-4-24(36)32-19-7-5-17(6-8-19)9-11-34-26-18(16-31-28(33-26)30-10-12-35)13-22(27(34)37)21-14-20(38-2)15-23(39-3)25(21)29/h4-8,13-16,35H,1,9-12H2,2-3H3,(H,32,36)(H,30,31,33)
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n/an/a 2.40n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238802
PNG
(CHEMBL4095783)
Show SMILES CNc1ncc2cc(-c3cc(OC)cc(OC)c3Cl)c(=O)n(CCc3cccc(NC(=O)C=C)c3)c2n1
Show InChI InChI=1S/C27H26ClN5O4/c1-5-23(34)31-18-8-6-7-16(11-18)9-10-33-25-17(15-30-27(29-2)32-25)12-21(26(33)35)20-13-19(36-3)14-22(37-4)24(20)28/h5-8,11-15H,1,9-10H2,2-4H3,(H,31,34)(H,29,30,32)
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n/an/a 2.80n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Discoidin domain-containing receptor 2


(Homo sapiens (Human))
BDBM50437152
PNG
(CHEMBL2403816)
Show SMILES CC(C)(C)c1cc(NC(=O)Nc2ccc(Nc3ncnc4ccccc34)cc2)n(n1)-c1cccc(N)c1
Show InChI InChI=1S/C28H28N8O/c1-28(2,3)24-16-25(36(35-24)21-8-6-7-18(29)15-21)34-27(37)33-20-13-11-19(12-14-20)32-26-22-9-4-5-10-23(22)30-17-31-26/h4-17H,29H2,1-3H3,(H,30,31,32)(H2,33,34,37)
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n/an/a 3n/an/an/an/an/an/a



Technical University of Dortmund

Curated by ChEMBL


Assay Description
Inhibition of wild type DDR2 (unknown origin) preincubated for 30 mins before substrate addition by FRET assay


J Med Chem 57: 4252-62 (2014)


Article DOI: 10.1021/jm500167q
BindingDB Entry DOI: 10.7270/Q2Z039P4
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238804
PNG
(CHEMBL4099578)
Show SMILES CNc1ncc2cc(-c3cc(OC)cc(OC)c3Cl)c(=O)n(CCc3ccc(NC(=O)C=C)cc3)c2n1
Show InChI InChI=1S/C27H26ClN5O4/c1-5-23(34)31-18-8-6-16(7-9-18)10-11-33-25-17(15-30-27(29-2)32-25)12-21(26(33)35)20-13-19(36-3)14-22(37-4)24(20)28/h5-9,12-15H,1,10-11H2,2-4H3,(H,31,34)(H,29,30,32)
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n/an/a 3.40n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238812
PNG
(CHEMBL4100201)
Show SMILES COc1cc(OC)c(Cl)c(c1)-c1cc2cnc(NCC(O)CO)nc2n(CCc2ccc(NC(=O)C=C)cc2)c1=O
Show InChI InChI=1/C29H30ClN5O6/c1-4-25(38)33-19-7-5-17(6-8-19)9-10-35-27-18(14-31-29(34-27)32-15-20(37)16-36)11-23(28(35)39)22-12-21(40-2)13-24(41-3)26(22)30/h4-8,11-14,20,36-37H,1,9-10,15-16H2,2-3H3,(H,33,38)(H,31,32,34)
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n/an/a 3.90n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(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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n/an/a 4.10n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of human FGFR3 preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM287559
PNG
(8-(2-((1-acryloylpiperidin-4-yl)(methyl)amino)ethy...)
Show SMILES CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCN(C)C3CCN(CC3)C(=O)C=C)c2n1
Show InChI InChI=1S/C27H32Cl2N6O4/c1-6-21(36)34-9-7-17(8-10-34)33(3)11-12-35-25-16(15-31-27(30-2)32-25)13-18(26(35)37)22-23(28)19(38-4)14-20(39-5)24(22)29/h6,13-15,17H,1,7-12H2,2-5H3,(H,30,31,32)
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n/an/a 4.10n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238820
PNG
(CHEMBL4072676)
Show SMILES CNc1ncc2cc(-c3cc(OC)cc(OC)c3Cl)c(=O)n(CCc3ccc(cc3)N(C)C(=O)C=C)c2n1
Show InChI InChI=1S/C28H28ClN5O4/c1-6-24(35)33(3)19-9-7-17(8-10-19)11-12-34-26-18(16-31-28(30-2)32-26)13-22(27(34)36)21-14-20(37-4)15-23(38-5)25(21)29/h6-10,13-16H,1,11-12H2,2-5H3,(H,30,31,32)
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n/an/a 4.70n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
In vitro antagonist activity against rat prostatic androgen receptor (AR)


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238807
PNG
(CHEMBL4102058)
Show SMILES COc1cc(OC)c(Cl)c(c1)-c1cc2cnc(NC3CCN(C)CC3)nc2n(CCc2ccc(NC(=O)C=C)cc2)c1=O
Show InChI InChI=1S/C32H35ClN6O4/c1-5-28(40)35-22-8-6-20(7-9-22)10-15-39-30-21(19-34-32(37-30)36-23-11-13-38(2)14-12-23)16-26(31(39)41)25-17-24(42-3)18-27(43-4)29(25)33/h5-9,16-19,23H,1,10-15H2,2-4H3,(H,35,40)(H,34,36,37)
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n/an/a 4.70n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238814
PNG
(CHEMBL4085605)
Show SMILES CNc1ncc2cc(-c3cc(OC)cc(OC)c3Cl)c(=O)n(Cc3cccc(NC(=O)C=C)c3)c2n1
Show InChI InChI=1S/C26H24ClN5O4/c1-5-22(33)30-17-8-6-7-15(9-17)14-32-24-16(13-29-26(28-2)31-24)10-20(25(32)34)19-11-18(35-3)12-21(36-4)23(19)27/h5-13H,1,14H2,2-4H3,(H,30,33)(H,28,29,31)
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n/an/a 5.30n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
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=1/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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n/an/a 5.60n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 1


(Homo sapiens (Human))
BDBM50238802
PNG
(CHEMBL4095783)
Show SMILES CNc1ncc2cc(-c3cc(OC)cc(OC)c3Cl)c(=O)n(CCc3cccc(NC(=O)C=C)c3)c2n1
Show InChI InChI=1S/C27H26ClN5O4/c1-5-23(34)31-18-8-6-7-16(11-18)9-10-33-25-17(15-30-27(29-2)32-25)12-21(26(33)35)20-13-19(36-3)14-22(37-4)24(20)28/h5-8,11-15H,1,9-10H2,2-4H3,(H,31,34)(H,29,30,32)
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n/an/a 6n/an/an/an/an/an/a



Principia Biopharma, Inc.

Curated by ChEMBL


Assay Description
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 m...


J Med Chem 60: 6516-6527 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00360
BindingDB Entry DOI: 10.7270/Q2C53P3H
More data for this
Ligand-Target Pair
Protein kinase B (Akt1 E49C, C296S, C310S and C344S )


(Homo sapiens (Human))
BDBM50313650
PNG
(8-(4-(1-aminocyclobutyl)phenyl)-9-phenyl-[1,2,4]tr...)
Show SMILES NC1(CCC1)c1ccc(cc1)-c1nc2ccn3c(n[nH]c3=O)c2cc1-c1ccccc1
Show InChI InChI=1S/C25H21N5O/c26-25(12-4-13-25)18-9-7-17(8-10-18)22-19(16-5-2-1-3-6-16)15-20-21(27-22)11-14-30-23(20)28-29-24(30)31/h1-3,5-11,14-15H,4,12-13,26H2,(H,29,31)
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n/an/a 6n/an/an/an/an/an/a



Technische Universitšt Dortmund



Assay Description
IC50 determinations for activated Akt1 were measured with the KinEASE assay (Cisbio) according to the manufacturer’s instructions. The kinases A...


ACS Chem Biol 10: 279-88 (2015)


Article DOI: 10.1021/cb500355c
BindingDB Entry DOI: 10.7270/Q218358G
More data for this
Ligand-Target Pair
Discoidin domain-containing receptor 2


(Homo sapiens (Human))
BDBM16673
PNG
(4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamo...)
Show SMILES CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(c3)C(F)(F)F)cc2)ccn1
Show InChI InChI=1S/C21H16ClF3N4O3/c1-26-19(30)18-11-15(8-9-27-18)32-14-5-2-12(3-6-14)28-20(31)29-13-4-7-17(22)16(10-13)21(23,24)25/h2-11H,1H3,(H,26,30)(H2,28,29,31)
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n/an/a 7n/an/an/an/an/an/a



Technical University of Dortmund

Curated by ChEMBL


Assay Description
Inhibition of wild type DDR2 (unknown origin) preincubated for 30 mins before substrate addition by FRET assay


J Med Chem 57: 4252-62 (2014)


Article DOI: 10.1021/jm500167q
BindingDB Entry DOI: 10.7270/Q2Z039P4
More data for this
Ligand-Target Pair
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