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Compile Data Set for Download or QSAR

Found 4326 hits of ic50 for UniProtKB: P22607   
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 3


(Homo sapiens (Human))		BDBM161438
PNG
(US10124003, Ex. Compound 51 | US10835536, Ex. Comp...)
Show SMILES COc1cc(OC)cc(c1)C#CC1=CN(C2CN(C2)C(=O)C=C)C2N=CN=C(N)C12 |c:26,t:13,28|
Show InChI InChI=1S/C22H23N5O3/c1-4-19(28)26-11-16(12-26)27-10-15(20-21(23)24-13-25-22(20)27)6-5-14-7-17(29-2)9-18(8-14)30-3/h4,7-10,13,16,20,22H,1,11-12H2,2-3H3,(H2,23,24,25)
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n/an/a 0.100n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Purified recombinant human FGFR3 protein was purchased from Carna Biosciences, Inc. When setting conditions for the measurement of the inhibitory ef...

US Patent US9108973 (2015)


BindingDB Entry DOI: 10.7270/Q2XW4HJV
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM161396
PNG
(US10124003, Ex. Compound 9 | US10835536, Ex. Comp ...)
Show SMILES COc1cc(OC)cc(c1)C#Cc1nn(C2CN(C2)C(=O)C=C)c2ncnc(N)c12
Show InChI InChI=1S/C21H20N6O3/c1-4-18(28)26-10-14(11-26)27-21-19(20(22)23-12-24-21)17(25-27)6-5-13-7-15(29-2)9-16(8-13)30-3/h4,7-9,12,14H,1,10-11H2,2-3H3,(H2,22,23,24)
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n/an/a 0.100n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
The inhibitory effect of the compounds on FGFR3 kinase activity was measured according to the method of Test Example 3. Purified recombinant human FG...

US Patent US10894048 (2021)


BindingDB Entry DOI: 10.7270/Q2319ZZF
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(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 0.100n/an/an/an/an/an/a



BAYER INTELLECTUAL PROPERTY GMBH

US Patent




US Patent US9598416 (2017)


BindingDB Entry DOI: 10.7270/Q2Q2428R
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM161392
PNG
(US10124003, Ex. Compound 5 | US10835536, Ex. Comp ...)
Show SMILES COc1cc(OC)cc(c1)C#Cc1nn([C@H]2CCN(C2)C(=O)C#C)c2ncnc(N)c12 |r|
Show InChI InChI=1S/C22H20N6O3/c1-4-19(29)27-8-7-15(12-27)28-22-20(21(23)24-13-25-22)18(26-28)6-5-14-9-16(30-2)11-17(10-14)31-3/h1,9-11,13,15H,7-8,12H2,2-3H3,(H2,23,24,25)/t15-/m0/s1
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
The inhibitory effect of the compounds on FGFR3 kinase activity was measured according to the method of Test Example 3. Purified recombinant human FG...

US Patent US10894048 (2021)


BindingDB Entry DOI: 10.7270/Q2319ZZF
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(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




US Patent US9598416 (2017)


BindingDB Entry DOI: 10.7270/Q2Q2428R
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(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 FGFR3 in human RT112 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 3


(Homo sapiens (Human))		BDBM194899
PNG
(US9206184, 80)
Show SMILES COc1cc(C)cc2cc(sc12)-c1c(CN2CCNC(=O)C2)c(Cl)n2ncnc(N)c12
Show InChI InChI=1S/C21H21ClN6O2S/c1-11-5-12-7-15(31-19(12)14(6-11)30-2)17-13(8-27-4-3-24-16(29)9-27)20(22)28-18(17)21(23)25-10-26-28/h5-7,10H,3-4,8-9H2,1-2H3,(H,24,29)(H2,23,25,26)
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n/an/a 0.200n/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 3


(Homo sapiens (Human))		BDBM161392
PNG
(US10124003, Ex. Compound 5 | US10835536, Ex. Comp ...)
Show SMILES COc1cc(OC)cc(c1)C#Cc1nn([C@H]2CCN(C2)C(=O)C#C)c2ncnc(N)c12 |r|
Show InChI InChI=1S/C22H20N6O3/c1-4-19(29)27-8-7-15(12-27)28-22-20(21(23)24-13-25-22)18(26-28)6-5-14-9-16(30-2)11-17(10-14)31-3/h1,9-11,13,15H,7-8,12H2,2-3H3,(H2,23,24,25)/t15-/m0/s1
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Purified recombinant human FGFR3 protein was purchased from Carna Biosciences, Inc. When setting conditions for the measurement of the inhibitory ef...

US Patent US9108973 (2015)


BindingDB Entry DOI: 10.7270/Q2XW4HJV
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM50588768
PNG
(CHEMBL5175256)
Show SMILES [2H]C([2H])([2H])NC(=O)c1cncc(c1)-c1cnn2cc(-c3ccn(n3)C(C)C)c(N[C@H]3CCOC3)nc12 |r|
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TBA



Citation and Details

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


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



BAYER INTELLECTUAL PROPERTY GMBH

US Patent




US Patent US9598416 (2017)


BindingDB Entry DOI: 10.7270/Q2Q2428R
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM50525936
PNG
(CHEMBL4577380)
Show SMILES C[C@H](Nc1c(-c2nc3cnc(cc3[nH]2)N2CCOCC2)c(=O)[nH]c2cn(C)nc12)c1ncccn1 |r|
Show InChI InChI=1S/C23H24N10O2/c1-13(21-24-4-3-5-25-21)27-20-18(23(34)30-16-12-32(2)31-19(16)20)22-28-14-10-17(26-11-15(14)29-22)33-6-8-35-9-7-33/h3-5,10-13,27H,6-9H2,1-2H3,(H,28,29)(H,30,34)/t13-/m0/s1
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n/an/a 0.212n/an/an/an/an/an/a



Therachem Research Medilab, LLC.

Curated by ChEMBL


Assay Description
Inhibition of human FGFR3 V555M mutant using FL-peptide substrate measured after 45 mins in presence of ATP by mobility shift assay

ACS Med Chem Lett 10: 1374-1375 (2019)


Article DOI: 10.1021/acsmedchemlett.9b00427
BindingDB Entry DOI: 10.7270/Q2WQ077Z
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM50525933
PNG
(CHEMBL4568760)
Show SMILES CC[C@H](Nc1c(-c2nc3cc(C)c(cc3[nH]2)N2CCOCC2)c(=O)[nH]c2cn(C)nc12)c1ncccn1 |r|
Show InChI InChI=1S/C26H29N9O2/c1-4-16(24-27-6-5-7-28-24)29-23-21(26(36)32-19-14-34(3)33-22(19)23)25-30-17-12-15(2)20(13-18(17)31-25)35-8-10-37-11-9-35/h5-7,12-14,16,29H,4,8-11H2,1-3H3,(H,30,31)(H,32,36)/t16-/m0/s1
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n/an/a 0.265n/an/an/an/an/an/a



Therachem Research Medilab, LLC.

Curated by ChEMBL


Assay Description
Inhibition of human FGFR3 V555M mutant using FL-peptide substrate measured after 45 mins in presence of ATP by mobility shift assay

ACS Med Chem Lett 10: 1374-1375 (2019)


Article DOI: 10.1021/acsmedchemlett.9b00427
BindingDB Entry DOI: 10.7270/Q2WQ077Z
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM301217
PNG
(3-(2,6-Difluoro-3,5-dimethoxyphenyl)-1-methyl-1,3,...)
Show SMILES COc1cc(OC)c(F)c(N2Cc3cnc4[nH]ccc4c3N(C)C2=O)c1F
Show InChI InChI=1S/C18H16F2N4O3/c1-23-15-9(7-22-17-10(15)4-5-21-17)8-24(18(23)25)16-13(19)11(26-2)6-12(27-3)14(16)20/h4-7H,8H2,1-3H3,(H,21,22)
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n/an/a 0.270n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of human FGFR3 using biotinylated-EQEDEPEGDYFEWLE peptide as substrate incubated for 1 hr in presence of ATP by FRET assay

Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00713
BindingDB Entry DOI: 10.7270/Q2S1867R
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM50525937
PNG
(CHEMBL4461304)
Show SMILES CC(C)[C@H](Nc1c(-c2nc3ccc(cc3[nH]2)N2CCN(C)CC2)c(=O)[nH]c2cn(C)nc12)c1ccccn1 |r|
Show InChI InChI=1S/C28H33N9O/c1-17(2)24(20-7-5-6-10-29-20)33-26-23(28(38)32-22-16-36(4)34-25(22)26)27-30-19-9-8-18(15-21(19)31-27)37-13-11-35(3)12-14-37/h5-10,15-17,24,33H,11-14H2,1-4H3,(H,30,31)(H,32,38)/t24-/m0/s1
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n/an/a 0.288n/an/an/an/an/an/a



Therachem Research Medilab, LLC.

Curated by ChEMBL


Assay Description
Inhibition of human FGFR3 V555M mutant using FL-peptide substrate measured after 45 mins in presence of ATP by mobility shift assay

ACS Med Chem Lett 10: 1374-1375 (2019)


Article DOI: 10.1021/acsmedchemlett.9b00427
BindingDB Entry DOI: 10.7270/Q2WQ077Z
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM161396
PNG
(US10124003, Ex. Compound 9 | US10835536, Ex. Comp ...)
Show SMILES COc1cc(OC)cc(c1)C#Cc1nn(C2CN(C2)C(=O)C=C)c2ncnc(N)c12
Show InChI InChI=1S/C21H20N6O3/c1-4-18(28)26-10-14(11-26)27-21-19(20(22)23-12-24-21)17(25-27)6-5-13-7-15(29-2)9-16(8-13)30-3/h4,7-9,12,14H,1,10-11H2,2-3H3,(H2,22,23,24)
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n/an/a 0.300n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
The inhibitory effect of the compounds on FGFR3 kinase activity was measured according to the method of Test Example 3. Purified recombinant human FG...

US Patent US10894048 (2021)


BindingDB Entry DOI: 10.7270/Q2319ZZF
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM161396
PNG
(US10124003, Ex. Compound 9 | US10835536, Ex. Comp ...)
Show SMILES COc1cc(OC)cc(c1)C#Cc1nn(C2CN(C2)C(=O)C=C)c2ncnc(N)c12
Show InChI InChI=1S/C21H20N6O3/c1-4-18(28)26-10-14(11-26)27-21-19(20(22)23-12-24-21)17(25-27)6-5-13-7-15(29-2)9-16(8-13)30-3/h4,7-9,12,14H,1,10-11H2,2-3H3,(H2,22,23,24)
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n/an/a 0.300n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Purified recombinant human FGFR3 protein was purchased from Carna Biosciences, Inc. When setting conditions for the measurement of the inhibitory ef...

US Patent US9108973 (2015)


BindingDB Entry DOI: 10.7270/Q2XW4HJV
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(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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BAYER INTELLECTUAL PROPERTY GMBH

US Patent




US Patent US9598416 (2017)


BindingDB Entry DOI: 10.7270/Q2Q2428R
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM50525935
PNG
(CHEMBL4443370)
Show SMILES C[C@H](Nc1c(-c2nc3ccc(cc3[nH]2)N2C[C@H](C)O[C@H](C)C2)c(=O)[nH]c2cn(C)nc12)c1ncccn1 |r|
Show InChI InChI=1S/C26H29N9O2/c1-14-11-35(12-15(2)37-14)17-6-7-18-19(10-17)31-25(30-18)21-23(29-16(3)24-27-8-5-9-28-24)22-20(32-26(21)36)13-34(4)33-22/h5-10,13-16,29H,11-12H2,1-4H3,(H,30,31)(H,32,36)/t14-,15+,16-/m0/s1
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n/an/a 0.373n/an/an/an/an/an/a



Therachem Research Medilab, LLC.

Curated by ChEMBL


Assay Description
Inhibition of human FGFR3 wild-type using FL-peptide substrate measured after 50 mins in presence of ATP by mobility shift assay

ACS Med Chem Lett 10: 1374-1375 (2019)


Article DOI: 10.1021/acsmedchemlett.9b00427
BindingDB Entry DOI: 10.7270/Q2WQ077Z
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(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 0.400n/an/an/an/an/an/a



BAYER INTELLECTUAL PROPERTY GMBH

US Patent




US Patent US9598416 (2017)


BindingDB Entry DOI: 10.7270/Q2Q2428R
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM302365
PNG
(4-{[4-Amino-5-(7-methoxy-5-methyl-1-benzothiophen-...)
Show SMILES COc1cc(C)cc2cc(sc12)-c1c(CN2CCNC(=O)C2)cn2ncnc(N)c12
Show InChI InChI=1S/C21H22N6O2S/c1-12-5-13-7-16(30-20(13)15(6-12)29-2)18-14(8-26-4-3-23-17(28)10-26)9-27-19(18)21(22)24-11-25-27/h5-7,9,11H,3-4,8,10H2,1-2H3,(H,23,28)(H2,22,24,25)
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n/an/a 0.400n/an/an/an/an/an/a



BAYER INTELLECTUAL PROPERTY GMBH

US Patent




US Patent US9598416 (2017)


BindingDB Entry DOI: 10.7270/Q2Q2428R
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM592070
PNG
(US11566028, Example 63 | US11566028, Example 9)
Show SMILES CNC(=O)c1cncc(c1)-c1cnn2cc(-c3cnn(c3)C(C)C)c(O[C@H]3CCOC3)nc12 |r|
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n/an/a 0.400n/an/an/an/an/an/a


TBA



Citation and Details

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


(Homo sapiens (Human))		BDBM50525935
PNG
(CHEMBL4443370)
Show SMILES C[C@H](Nc1c(-c2nc3ccc(cc3[nH]2)N2C[C@H](C)O[C@H](C)C2)c(=O)[nH]c2cn(C)nc12)c1ncccn1 |r|
Show InChI InChI=1S/C26H29N9O2/c1-14-11-35(12-15(2)37-14)17-6-7-18-19(10-17)31-25(30-18)21-23(29-16(3)24-27-8-5-9-28-24)22-20(32-26(21)36)13-34(4)33-22/h5-10,13-16,29H,11-12H2,1-4H3,(H,30,31)(H,32,36)/t14-,15+,16-/m0/s1
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n/an/a 0.408n/an/an/an/an/an/a



Therachem Research Medilab, LLC.

Curated by ChEMBL


Assay Description
Inhibition of human FGFR3 V555M mutant using FL-peptide substrate measured after 45 mins in presence of ATP by mobility shift assay

ACS Med Chem Lett 10: 1374-1375 (2019)


Article DOI: 10.1021/acsmedchemlett.9b00427
BindingDB Entry DOI: 10.7270/Q2WQ077Z
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM50525934
PNG
(CHEMBL4529789)
Show SMILES C[C@H](Nc1c(-c2nc3c(F)cc(cc3[nH]2)N2CCOCC2)c(=O)[nH]c2cn(C)nc12)c1ncccn1 |r|
Show InChI InChI=1S/C24H24FN9O2/c1-13(22-26-4-3-5-27-22)28-21-18(24(35)30-17-12-33(2)32-20(17)21)23-29-16-11-14(10-15(25)19(16)31-23)34-6-8-36-9-7-34/h3-5,10-13,28H,6-9H2,1-2H3,(H,29,31)(H,30,35)/t13-/m0/s1
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n/an/a 0.410n/an/an/an/an/an/a



Therachem Research Medilab, LLC.

Curated by ChEMBL


Assay Description
Inhibition of human FGFR3 V555M mutant using FL-peptide substrate measured after 45 mins in presence of ATP by mobility shift assay

ACS Med Chem Lett 10: 1374-1375 (2019)


Article DOI: 10.1021/acsmedchemlett.9b00427
BindingDB Entry DOI: 10.7270/Q2WQ077Z
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM50525936
PNG
(CHEMBL4577380)
Show SMILES C[C@H](Nc1c(-c2nc3cnc(cc3[nH]2)N2CCOCC2)c(=O)[nH]c2cn(C)nc12)c1ncccn1 |r|
Show InChI InChI=1S/C23H24N10O2/c1-13(21-24-4-3-5-25-21)27-20-18(23(34)30-16-12-32(2)31-19(16)20)22-28-14-10-17(26-11-15(14)29-22)33-6-8-35-9-7-33/h3-5,10-13,27H,6-9H2,1-2H3,(H,28,29)(H,30,34)/t13-/m0/s1
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n/an/a 0.411n/an/an/an/an/an/a



Therachem Research Medilab, LLC.

Curated by ChEMBL


Assay Description
Inhibition of human FGFR3 wild-type using FL-peptide substrate measured after 50 mins in presence of ATP by mobility shift assay

ACS Med Chem Lett 10: 1374-1375 (2019)


Article DOI: 10.1021/acsmedchemlett.9b00427
BindingDB Entry DOI: 10.7270/Q2WQ077Z
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM50525939
PNG
(Balversa | Erdafitinib | Jnj-42756493)
Show SMILES COc1cc(OC)cc(c1)N(CCNC(C)C)c1ccc2ncc(nc2c1)-c1cnn(C)c1
Show InChI InChI=1S/C25H30N6O2/c1-17(2)26-8-9-31(20-10-21(32-4)13-22(11-20)33-5)19-6-7-23-24(12-19)29-25(15-27-23)18-14-28-30(3)16-18/h6-7,10-17,26H,8-9H2,1-5H3
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n/an/a 0.420n/an/an/an/an/an/a


TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.2c01413
BindingDB Entry DOI: 10.7270/Q25D8WX6
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM128502
PNG
(US8796244, 81)
Show SMILES CC(C)(CO)Nc1ccc(nn1)-c1ccn2c(cnc2c1)-c1cccc(NC(=O)NCC(F)(F)F)c1
Show InChI InChI=1S/C24H24F3N7O2/c1-23(2,14-35)31-20-7-6-18(32-33-20)15-8-9-34-19(12-28-21(34)11-15)16-4-3-5-17(10-16)30-22(36)29-13-24(25,26)27/h3-12,35H,13-14H2,1-2H3,(H,31,33)(H2,29,30,36)
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n/an/a 0.447n/an/an/an/a8.025



Astex Therapeutics Ltd

US Patent


Assay Description
Enzymes (from Upstate) were prepared at 2× final concentration in 1× kinase assay buffer (Table 1). Enzymes were then incubated with test compounds, ...

US Patent US8796244 (2014)


BindingDB Entry DOI: 10.7270/Q20C4TFP
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM128624
PNG
(US8796244, 213)
Show SMILES FC(F)(F)CNC(=O)Nc1cccc(c1)-c1cnc2cc(ccn12)-c1nccc(n1)-n1ccnc1
Show InChI InChI=1S/C23H17F3N8O/c24-23(25,26)13-30-22(35)31-17-3-1-2-15(10-17)18-12-29-20-11-16(5-8-34(18)20)21-28-6-4-19(32-21)33-9-7-27-14-33/h1-12,14H,13H2,(H2,30,31,35)
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n/an/a 0.460n/an/an/an/a8.025



Astex Therapeutics Ltd

US Patent


Assay Description
Enzymes (from Upstate) were prepared at 2× final concentration in 1× kinase assay buffer (Table 1). Enzymes were then incubated with test compounds, ...

US Patent US8796244 (2014)


BindingDB Entry DOI: 10.7270/Q20C4TFP
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM50602226
PNG
(CHEMBL5177696)
Show SMILES COc1cc(OC)cc(c1)N(CCNC(C)C)c1ccc2ncc(nc2c1)-c1cnn(CCCCCCC(=O)NO)c1
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TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.2c01413
BindingDB Entry DOI: 10.7270/Q25D8WX6
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM50593531
PNG
(ASP-5878 | ASP5878 | Asp 5878 | Asp-5878 | Asp5878)
Show SMILES COc1cc(OC)c(F)c(COc2cnc(Nc3cnn(CCO)c3)nc2)c1F
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n/an/a 0.470n/an/an/an/an/an/a


TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c01977
BindingDB Entry DOI: 10.7270/Q2R49VVS
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM50525934
PNG
(CHEMBL4529789)
Show SMILES C[C@H](Nc1c(-c2nc3c(F)cc(cc3[nH]2)N2CCOCC2)c(=O)[nH]c2cn(C)nc12)c1ncccn1 |r|
Show InChI InChI=1S/C24H24FN9O2/c1-13(22-26-4-3-5-27-22)28-21-18(24(35)30-17-12-33(2)32-20(17)21)23-29-16-11-14(10-15(25)19(16)31-23)34-6-8-36-9-7-34/h3-5,10-13,28H,6-9H2,1-2H3,(H,29,31)(H,30,35)/t13-/m0/s1
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n/an/a 0.480n/an/an/an/an/an/a



Therachem Research Medilab, LLC.

Curated by ChEMBL


Assay Description
Inhibition of human FGFR3 wild-type using FL-peptide substrate measured after 50 mins in presence of ATP by mobility shift assay

ACS Med Chem Lett 10: 1374-1375 (2019)


Article DOI: 10.1021/acsmedchemlett.9b00427
BindingDB Entry DOI: 10.7270/Q2WQ077Z
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM128551
PNG
(US8796244, 133)
Show SMILES OC1CCCN(C1)c1ccc(nn1)-c1ccn2c(cnc2c1)-c1cccc(NC(=O)NCC(F)(F)F)c1
Show InChI InChI=1S/C25H24F3N7O2/c26-25(27,28)15-30-24(37)31-18-4-1-3-17(11-18)21-13-29-23-12-16(8-10-35(21)23)20-6-7-22(33-32-20)34-9-2-5-19(36)14-34/h1,3-4,6-8,10-13,19,36H,2,5,9,14-15H2,(H2,30,31,37)
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n/an/a 0.484n/an/an/an/a8.025



Astex Therapeutics Ltd

US Patent


Assay Description
Enzymes (from Upstate) were prepared at 2× final concentration in 1× kinase assay buffer (Table 1). Enzymes were then incubated with test compounds, ...

US Patent US8796244 (2014)


BindingDB Entry DOI: 10.7270/Q20C4TFP
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM139913
PNG
(US8895745, 375)
Show SMILES Cn1cnc(c1)-c1ccn2c(cnc2c1)-c1cccc(NC(=O)NCC(F)(F)F)c1
Show InChI InChI=1S/C20H17F3N6O/c1-28-10-16(26-12-28)13-5-6-29-17(9-24-18(29)8-13)14-3-2-4-15(7-14)27-19(30)25-11-20(21,22)23/h2-10,12H,11H2,1H3,(H2,25,27,30)
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n/an/a 0.490n/an/an/an/a7.5n/a



Astex Therapeutics Limited

US Patent


Assay Description
Enzymes (from Upstate) were prepared at 2x final concentration in 1x kinase assay buffer (as described below). Enzymes were then incubated with test ...

US Patent US8895745 (2014)


BindingDB Entry DOI: 10.7270/Q2833QQC
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM301220
PNG
(3-(2-Chloro-6-fluoro-3,5-dimethoxyphenyl)-1-methyl...)
Show SMILES COc1cc(OC)c(Cl)c(N2Cc3cnc4[nH]ccc4c3N(C)C2=O)c1F
Show InChI InChI=1S/C18H16ClFN4O3/c1-23-15-9(7-22-17-10(15)4-5-21-17)8-24(18(23)25)16-13(19)11(26-2)6-12(27-3)14(16)20/h4-7H,8H2,1-3H3,(H,21,22)
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n/an/a 0.490n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of human FGFR3 using biotinylated-EQEDEPEGDYFEWLE peptide as substrate incubated for 1 hr in presence of ATP by FRET assay

Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00713
BindingDB Entry DOI: 10.7270/Q2S1867R
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(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 |r|
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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BAYER INTELLECTUAL PROPERTY GMBH

US Patent




US Patent US9598416 (2017)


BindingDB Entry DOI: 10.7270/Q2Q2428R
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM194900
PNG
(US9206184, 81 | US9206184, 82)
Show SMILES COc1cc(C)cc2cc(sc12)-c1c(CNCC(C)(C)O)c(Cl)n2ncnc(N)c12
Show InChI InChI=1S/C21H24ClN5O2S/c1-11-5-12-7-15(30-18(12)14(6-11)29-4)16-13(8-24-9-21(2,3)28)19(22)27-17(16)20(23)25-10-26-27/h5-7,10,24,28H,8-9H2,1-4H3,(H2,23,25,26)
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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 3


(Homo sapiens (Human))		BDBM302420
PNG
(US9598416, Example 66)
Show SMILES COc1cc(C)cc2cc(sc12)-c1c(CN2CC[C@@H](C2)N(C)C)cn2ncnc(N)c12 |r|
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-/m0/s1
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BAYER INTELLECTUAL PROPERTY GMBH

US Patent




US Patent US9598416 (2017)


BindingDB Entry DOI: 10.7270/Q2Q2428R
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


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



Chinese Academy of Sciences

Curated by ChEMBL


Assay Description
Inhibition of human N-terminal GST-tagged FGFR3 (436 to 806 residues) cytoplasmic domain expressed in baculovirus expression system after 60 mins by ...

Eur J Med Chem 154: 9-28 (2018)


Article DOI: 10.1016/j.ejmech.2018.05.005
BindingDB Entry DOI: 10.7270/Q2736TM3
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM161389
PNG
(US10124003, Ref. Ex. Compound 3 | US10835536, Ex. ...)
Show SMILES COc1cc(OC)cc(c1)C#Cc1nn([C@H]2CCN(C2)C(=O)C=C)c2ncnc(N)c12 |r|
Show InChI InChI=1S/C22H22N6O3/c1-4-19(29)27-8-7-15(12-27)28-22-20(21(23)24-13-25-22)18(26-28)6-5-14-9-16(30-2)11-17(10-14)31-3/h4,9-11,13,15H,1,7-8,12H2,2-3H3,(H2,23,24,25)/t15-/m0/s1
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n/an/a 0.5n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
The inhibitory effect of the compounds on FGFR3 kinase activity was measured according to the method of Test Example 3. Purified recombinant human FG...

US Patent US10894048 (2021)


BindingDB Entry DOI: 10.7270/Q2319ZZF
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM161434
PNG
(US10894048, Ex Comp 47 | US9108973, 47)
Show SMILES COc1cc(OC)cc(c1)C#Cc1cn([C@H]2CCN(C2)C(=O)C#CC(C)(C)O)c2ncnc(N)c12 |r|
Show InChI InChI=1S/C26H27N5O4/c1-26(2,33)9-7-22(32)30-10-8-19(15-30)31-14-18(23-24(27)28-16-29-25(23)31)6-5-17-11-20(34-3)13-21(12-17)35-4/h11-14,16,19,33H,8,10,15H2,1-4H3,(H2,27,28,29)/t19-/m0/s1
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n/an/a 0.5n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
The inhibitory effect of the compounds on FGFR3 kinase activity was measured according to the method of Test Example 3. Purified recombinant human FG...

US Patent US10894048 (2021)


BindingDB Entry DOI: 10.7270/Q2319ZZF
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM50596833
PNG
(CHEMBL5193966)
Show SMILES COc1cc(OC)c(Cl)c(Nc2ncccc2-c2ncnc(Nc3cnn(c3)C3CCN(CC3)C(C)C)n2)c1Cl
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TBA



Citation and Details

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


(Homo sapiens (Human))		BDBM50355393
PNG
(BGJ398 | CHEMBL1834657 | US9434697, BGJ398 | US973...)
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<0.5n/an/an/an/an/an/a


TBA



Citation and Details

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


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



Citation and Details

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


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



Citation and Details

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


(Homo sapiens (Human))		BDBM50596832
PNG
(CHEMBL5198569)
Show SMILES CCN1CCN(CC1)c1cccc(Nc2ncnc(n2)-c2cccnc2Nc2c(Cl)c(OC)cc(OC)c2Cl)c1
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TBA



Citation and Details

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


(Homo sapiens (Human))		BDBM50596833
PNG
(CHEMBL5193966)
Show SMILES COc1cc(OC)c(Cl)c(Nc2ncccc2-c2ncnc(Nc3cnn(c3)C3CCN(CC3)C(C)C)n2)c1Cl
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TBA



Citation and Details

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


(Homo sapiens (Human))		BDBM50596834
PNG
(CHEMBL5181852)
Show SMILES COc1cc(OC)c(Cl)c(Nc2ncccc2-c2ncnc(Nc3cnn(c3)C3CCNCC3)n2)c1Cl
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Citation and Details

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


(Homo sapiens (Human))		BDBM592070
PNG
(US11566028, Example 63 | US11566028, Example 9)
Show SMILES CNC(=O)c1cncc(c1)-c1cnn2cc(-c3cnn(c3)C(C)C)c(O[C@H]3CCOC3)nc12 |r|
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Citation and Details

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


(Homo sapiens (Human))		BDBM128659
PNG
(US8796244, 250)
Show SMILES FC(F)(F)CNC(=O)Nc1cccc(c1)-c1cnc2cc(ccn12)-c1nnc(NC2CC2)s1
Show InChI InChI=1S/C21H18F3N7OS/c22-21(23,24)11-26-19(32)27-15-3-1-2-12(8-15)16-10-25-17-9-13(6-7-31(16)17)18-29-30-20(33-18)28-14-4-5-14/h1-3,6-10,14H,4-5,11H2,(H,28,30)(H2,26,27,32)
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n/an/a 0.5n/an/an/an/a8.025



Astex Therapeutics Ltd

US Patent


Assay Description
Enzymes (from Upstate) were prepared at 2× final concentration in 1× kinase assay buffer (Table 1). Enzymes were then incubated with test compounds, ...

US Patent US8796244 (2014)


BindingDB Entry DOI: 10.7270/Q20C4TFP
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM161389
PNG
(US10124003, Ref. Ex. Compound 3 | US10835536, Ex. ...)
Show SMILES COc1cc(OC)cc(c1)C#Cc1nn([C@H]2CCN(C2)C(=O)C=C)c2ncnc(N)c12 |r|
Show InChI InChI=1S/C22H22N6O3/c1-4-19(29)27-8-7-15(12-27)28-22-20(21(23)24-13-25-22)18(26-28)6-5-14-9-16(30-2)11-17(10-14)31-3/h4,9-11,13,15H,1,7-8,12H2,2-3H3,(H2,23,24,25)/t15-/m0/s1
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Purified recombinant human FGFR3 protein was purchased from Carna Biosciences, Inc. When setting conditions for the measurement of the inhibitory ef...

US Patent US9108973 (2015)


BindingDB Entry DOI: 10.7270/Q2XW4HJV
More data for this
Ligand-Target Pair
Fibroblast growth factor receptor 3


(Homo sapiens (Human))		BDBM161434
PNG
(US10894048, Ex Comp 47 | US9108973, 47)
Show SMILES COc1cc(OC)cc(c1)C#Cc1cn([C@H]2CCN(C2)C(=O)C#CC(C)(C)O)c2ncnc(N)c12 |r|
Show InChI InChI=1S/C26H27N5O4/c1-26(2,33)9-7-22(32)30-10-8-19(15-30)31-14-18(23-24(27)28-16-29-25(23)31)6-5-17-11-20(34-3)13-21(12-17)35-4/h11-14,16,19,33H,8,10,15H2,1-4H3,(H2,27,28,29)/t19-/m0/s1
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n/an/a 0.5n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Purified recombinant human FGFR3 protein was purchased from Carna Biosciences, Inc. When setting conditions for the measurement of the inhibitory ef...

US Patent US9108973 (2015)


BindingDB Entry DOI: 10.7270/Q2XW4HJV
More data for this
Ligand-Target Pair
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