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Compile Data Set for Download or QSAR

Found 53 hits with Last Name = 'lovegrove' and Initial = 'v'   
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
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151347
PNG
(2-(3-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-n...)
Show SMILES Cc1cccc(n1)-c1n[nH]cc1-c1ccc2ncccc2n1
Show InChI InChI=1S/C17H13N5/c1-11-4-2-5-16(20-11)17-12(10-19-22-17)13-7-8-14-15(21-13)6-3-9-18-14/h2-10H,1H3,(H,19,22)
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n/an/a 4n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of recombinant Activin A receptor type II-like kinase (ALK5) expressed in baculovirus/Sf9 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151362
PNG
(4-(6-Methyl-pyridin-2-yl)-5-[1,5]naphthyridin-2-yl...)
Show SMILES Cc1cccc(n1)-c1nc(N)sc1-c1ccc2ncccc2n1
Show InChI InChI=1S/C17H13N5S/c1-10-4-2-5-13(20-10)15-16(23-17(18)22-15)14-8-7-11-12(21-14)6-3-9-19-11/h2-9H,1H3,(H2,18,22)
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n/an/a 6n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of recombinant Activin A receptor type II-like kinase (ALK5) expressed in baculovirus/Sf9 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151353
PNG
(4-(4-Fluoro-phenyl)-5-[1,5]naphthyridin-2-yl-thiaz...)
Show SMILES Nc1nc(c(s1)-c1ccc2ncccc2n1)-c1ccc(F)cc1
Show InChI InChI=1S/C17H11FN4S/c18-11-5-3-10(4-6-11)15-16(23-17(19)22-15)14-8-7-12-13(21-14)2-1-9-20-12/h1-9H,(H2,19,22)
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GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of recombinant Activin A receptor type II-like kinase (ALK5) expressed in baculovirus/Sf9 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151363
PNG
(4-(3-Chloro-phenyl)-5-[1,5]naphthyridin-2-yl-thiaz...)
Show SMILES Nc1nc(c(s1)-c1ccc2ncccc2n1)-c1cccc(Cl)c1
Show InChI InChI=1S/C17H11ClN4S/c18-11-4-1-3-10(9-11)15-16(23-17(19)22-15)14-7-6-12-13(21-14)5-2-8-20-12/h1-9H,(H2,19,22)
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GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of recombinant Activin A receptor type II-like kinase (ALK5) expressed in baculovirus/Sf9 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151357
PNG
(2-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyri...)
Show SMILES c1[nH]nc(c1-c1ccc2ncccc2n1)-c1ccccn1
Show InChI InChI=1S/C16H11N5/c1-2-8-18-15(4-1)16-11(10-19-21-16)12-6-7-13-14(20-12)5-3-9-17-13/h1-10H,(H,19,21)
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n/an/a 10n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of recombinant Activin A receptor type II-like kinase (ALK5) expressed in baculovirus/Sf9 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151362
PNG
(4-(6-Methyl-pyridin-2-yl)-5-[1,5]naphthyridin-2-yl...)
Show SMILES Cc1cccc(n1)-c1nc(N)sc1-c1ccc2ncccc2n1
Show InChI InChI=1S/C17H13N5S/c1-10-4-2-5-13(20-10)15-16(23-17(18)22-15)14-8-7-11-12(21-14)6-3-9-19-11/h2-9H,1H3,(H2,18,22)
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GlaxoSmithKline

Curated by ChEMBL


Assay Description
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151363
PNG
(4-(3-Chloro-phenyl)-5-[1,5]naphthyridin-2-yl-thiaz...)
Show SMILES Nc1nc(c(s1)-c1ccc2ncccc2n1)-c1cccc(Cl)c1
Show InChI InChI=1S/C17H11ClN4S/c18-11-4-1-3-10(9-11)15-16(23-17(19)22-15)14-7-6-12-13(21-14)5-2-8-20-12/h1-9H,(H2,19,22)
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GlaxoSmithKline

Curated by ChEMBL


Assay Description
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151347
PNG
(2-(3-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-n...)
Show SMILES Cc1cccc(n1)-c1n[nH]cc1-c1ccc2ncccc2n1
Show InChI InChI=1S/C17H13N5/c1-11-4-2-5-16(20-11)17-12(10-19-22-17)13-7-8-14-15(21-13)6-3-9-18-14/h2-10H,1H3,(H,19,22)
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GlaxoSmithKline

Curated by ChEMBL


Assay Description
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151363
PNG
(4-(3-Chloro-phenyl)-5-[1,5]naphthyridin-2-yl-thiaz...)
Show SMILES Nc1nc(c(s1)-c1ccc2ncccc2n1)-c1cccc(Cl)c1
Show InChI InChI=1S/C17H11ClN4S/c18-11-4-1-3-10(9-11)15-16(23-17(19)22-15)14-7-6-12-13(21-14)5-2-8-20-12/h1-9H,(H2,19,22)
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n/an/a 20n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Binding affinity to Activin A receptor type II-like kinase (ALK5) in fluorescence polarization binding assay; Range is (0.020-0.026)


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151346
PNG
(5-(1,5-naphthyridin-2-yl)-4-(pyridin-2-yl)thiazol-...)
Show SMILES Nc1nc(c(s1)-c1ccc2ncccc2n1)-c1ccccn1
Show InChI InChI=1S/C16H11N5S/c17-16-21-14(12-4-1-2-8-19-12)15(22-16)13-7-6-10-11(20-13)5-3-9-18-10/h1-9H,(H2,17,21)
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GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of recombinant Activin A receptor type II-like kinase (ALK5) expressed in baculovirus/Sf9 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151347
PNG
(2-(3-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-n...)
Show SMILES Cc1cccc(n1)-c1n[nH]cc1-c1ccc2ncccc2n1
Show InChI InChI=1S/C17H13N5/c1-11-4-2-5-16(20-11)17-12(10-19-22-17)13-7-8-14-15(21-13)6-3-9-18-14/h2-10H,1H3,(H,19,22)
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GlaxoSmithKline

Curated by ChEMBL


Assay Description
Binding affinity to Activin A receptor type II-like kinase (ALK5) in fluorescence polarization binding assay; Range is (0.020-0.026)


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151362
PNG
(4-(6-Methyl-pyridin-2-yl)-5-[1,5]naphthyridin-2-yl...)
Show SMILES Cc1cccc(n1)-c1nc(N)sc1-c1ccc2ncccc2n1
Show InChI InChI=1S/C17H13N5S/c1-10-4-2-5-13(20-10)15-16(23-17(18)22-15)14-8-7-11-12(21-14)6-3-9-19-11/h2-9H,1H3,(H2,18,22)
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GlaxoSmithKline

Curated by ChEMBL


Assay Description
Binding affinity to Activin A receptor type II-like kinase (ALK5) in fluorescence polarization binding assay; Range is (0.019-0.032)


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151353
PNG
(4-(4-Fluoro-phenyl)-5-[1,5]naphthyridin-2-yl-thiaz...)
Show SMILES Nc1nc(c(s1)-c1ccc2ncccc2n1)-c1ccc(F)cc1
Show InChI InChI=1S/C17H11FN4S/c18-11-5-3-10(4-6-11)15-16(23-17(19)22-15)14-8-7-12-13(21-14)2-1-9-20-12/h1-9H,(H2,19,22)
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n/an/a 30n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151354
PNG
(5-(8-Methyl-[1,5]naphthyridin-2-yl)-4-pyridin-2-yl...)
Show SMILES Cc1ccnc2ccc(nc12)-c1sc(N)nc1-c1ccccn1
Show InChI InChI=1S/C17H13N5S/c1-10-7-9-20-12-5-6-13(21-14(10)12)16-15(22-17(18)23-16)11-4-2-3-8-19-11/h2-9H,1H3,(H2,18,22)
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GlaxoSmithKline

Curated by ChEMBL


Assay Description
Binding affinity to Activin A receptor type II-like kinase (ALK5) in fluorescence polarization binding assay; Range is (0.021-0.042)


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151357
PNG
(2-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyri...)
Show SMILES c1[nH]nc(c1-c1ccc2ncccc2n1)-c1ccccn1
Show InChI InChI=1S/C16H11N5/c1-2-8-18-15(4-1)16-11(10-19-21-16)12-6-7-13-14(20-12)5-3-9-17-13/h1-10H,(H,19,21)
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GlaxoSmithKline

Curated by ChEMBL


Assay Description
Binding affinity to Activin A receptor type II-like kinase (ALK5) in fluorescence polarization binding assay; Range is (0.029-0.032)


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151346
PNG
(5-(1,5-naphthyridin-2-yl)-4-(pyridin-2-yl)thiazol-...)
Show SMILES Nc1nc(c(s1)-c1ccc2ncccc2n1)-c1ccccn1
Show InChI InChI=1S/C16H11N5S/c17-16-21-14(12-4-1-2-8-19-12)15(22-16)13-7-6-10-11(20-13)5-3-9-18-10/h1-9H,(H2,17,21)
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GlaxoSmithKline

Curated by ChEMBL


Assay Description
Binding affinity to Activin A receptor type II-like kinase (ALK5) in fluorescence polarization binding assay; Range is (0.038-0.042)


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151353
PNG
(4-(4-Fluoro-phenyl)-5-[1,5]naphthyridin-2-yl-thiaz...)
Show SMILES Nc1nc(c(s1)-c1ccc2ncccc2n1)-c1ccc(F)cc1
Show InChI InChI=1S/C17H11FN4S/c18-11-5-3-10(4-6-11)15-16(23-17(19)22-15)14-8-7-12-13(21-14)2-1-9-20-12/h1-9H,(H2,19,22)
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GlaxoSmithKline

Curated by ChEMBL


Assay Description
Binding affinity to Activin A receptor type II-like kinase (ALK5) in fluorescence polarization binding assay; Range is (0.040-0.044)


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151357
PNG
(2-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyri...)
Show SMILES c1[nH]nc(c1-c1ccc2ncccc2n1)-c1ccccn1
Show InChI InChI=1S/C16H11N5/c1-2-8-18-15(4-1)16-11(10-19-21-16)12-6-7-13-14(20-12)5-3-9-17-13/h1-10H,(H,19,21)
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GlaxoSmithKline

Curated by ChEMBL


Assay Description
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151346
PNG
(5-(1,5-naphthyridin-2-yl)-4-(pyridin-2-yl)thiazol-...)
Show SMILES Nc1nc(c(s1)-c1ccc2ncccc2n1)-c1ccccn1
Show InChI InChI=1S/C16H11N5S/c17-16-21-14(12-4-1-2-8-19-12)15(22-16)13-7-6-10-11(20-13)5-3-9-18-10/h1-9H,(H2,17,21)
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n/an/a 120n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151354
PNG
(5-(8-Methyl-[1,5]naphthyridin-2-yl)-4-pyridin-2-yl...)
Show SMILES Cc1ccnc2ccc(nc12)-c1sc(N)nc1-c1ccccn1
Show InChI InChI=1S/C17H13N5S/c1-10-7-9-20-12-5-6-13(21-14(10)12)16-15(22-17(18)23-16)11-4-2-3-8-19-11/h2-9H,1H3,(H2,18,22)
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GlaxoSmithKline

Curated by ChEMBL


Assay Description
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151352
PNG
(5-(6-Methyl-[1,5]naphthyridin-4-yl)-4-pyridin-2-yl...)
Show SMILES Cc1ccc2nccc(-c3sc(N)nc3-c3ccccn3)c2n1
Show InChI InChI=1S/C17H13N5S/c1-10-5-6-13-14(21-10)11(7-9-20-13)16-15(22-17(18)23-16)12-4-2-3-8-19-12/h2-9H,1H3,(H2,18,22)
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n/an/a 260n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151352
PNG
(5-(6-Methyl-[1,5]naphthyridin-4-yl)-4-pyridin-2-yl...)
Show SMILES Cc1ccc2nccc(-c3sc(N)nc3-c3ccccn3)c2n1
Show InChI InChI=1S/C17H13N5S/c1-10-5-6-13-14(21-10)11(7-9-20-13)16-15(22-17(18)23-16)12-4-2-3-8-19-12/h2-9H,1H3,(H2,18,22)
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n/an/a 380n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Binding affinity to Activin A receptor type II-like kinase (ALK5) in fluorescence polarization binding assay; Range is (0.180-0.790)


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151348
PNG
(4-(pyridin-2-yl)-5-(quinolin-4-yl)thiazol-2-amine ...)
Show SMILES Nc1nc(c(s1)-c1ccnc2ccccc12)-c1ccccn1
Show InChI InChI=1S/C17H12N4S/c18-17-21-15(14-7-3-4-9-19-14)16(22-17)12-8-10-20-13-6-2-1-5-11(12)13/h1-10H,(H2,18,21)
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n/an/a 420n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151348
PNG
(4-(pyridin-2-yl)-5-(quinolin-4-yl)thiazol-2-amine ...)
Show SMILES Nc1nc(c(s1)-c1ccnc2ccccc12)-c1ccccn1
Show InChI InChI=1S/C17H12N4S/c18-17-21-15(14-7-3-4-9-19-14)16(22-17)12-8-10-20-13-6-2-1-5-11(12)13/h1-10H,(H2,18,21)
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n/an/a 720n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Binding affinity to Activin A receptor type II-like kinase (ALK5) in fluorescence polarization binding assay; Range is (0.095-5.521)


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151350
PNG
(4-(4-Chloro-pyridin-2-yl)-5-quinolin-4-yl-thiazol-...)
Show SMILES Nc1nc(c(s1)-c1ccnc2ccccc12)-c1cc(Cl)ccn1
Show InChI InChI=1S/C17H11ClN4S/c18-10-5-7-21-14(9-10)15-16(23-17(19)22-15)12-6-8-20-13-4-2-1-3-11(12)13/h1-9H,(H2,19,22)
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n/an/a 1.02E+3n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Binding affinity to Activin A receptor type II-like kinase (ALK5) in fluorescence polarization binding assay; Range is (0.289-3.621)


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151351
PNG
(5''-Quinolin-4-yl-[2,4'']bithiazolyl-2''-ylamine |...)
Show SMILES Nc1nc(-c2nccs2)c(s1)-c1ccnc2ccccc12
Show InChI InChI=1S/C15H10N4S2/c16-15-19-12(14-18-7-8-20-14)13(21-15)10-5-6-17-11-4-2-1-3-9(10)11/h1-8H,(H2,16,19)
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n/an/a 1.17E+3n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Binding affinity to Activin A receptor type II-like kinase (ALK5) in fluorescence polarization binding assay; Range is (0.783-1.764)


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151356
PNG
(4-(2-Fluoro-phenyl)-5-quinolin-4-yl-thiazol-2-ylam...)
Show SMILES Nc1nc(c(s1)-c1ccnc2ccccc12)-c1ccccc1F
Show InChI InChI=1S/C18H12FN3S/c19-14-7-3-1-6-13(14)16-17(23-18(20)22-16)12-9-10-21-15-8-4-2-5-11(12)15/h1-10H,(H2,20,22)
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n/an/a 1.25E+3n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Binding affinity to Activin A receptor type II-like kinase (ALK5) in fluorescence polarization binding assay; Range is (0.356-4.455)


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151349
PNG
(4-(5-Chloro-pyridin-2-yl)-5-quinolin-4-yl-thiazol-...)
Show SMILES Nc1nc(c(s1)-c1ccnc2ccccc12)-c1ccc(Cl)cn1
Show InChI InChI=1S/C17H11ClN4S/c18-10-5-6-14(21-9-10)15-16(23-17(19)22-15)12-7-8-20-13-4-2-1-3-11(12)13/h1-9H,(H2,19,22)
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n/an/a 1.77E+3n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Binding affinity to Activin A receptor type II-like kinase (ALK5) in fluorescence polarization binding assay; Range is (0.864-3.661)


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151358
PNG
(4-Pyridin-2-yl-5-quinolin-2-yl-thiazol-2-ylamine |...)
Show SMILES Nc1nc(c(s1)-c1ccc2ccccc2n1)-c1ccccn1
Show InChI InChI=1S/C17H12N4S/c18-17-21-15(13-7-3-4-10-19-13)16(22-17)14-9-8-11-5-1-2-6-12(11)20-14/h1-10H,(H2,18,21)
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n/an/a 3.54E+3n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Binding affinity to Activin A receptor type II-like kinase (ALK5) in fluorescence polarization binding assay; Range is (1.375-9.154)


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151364
PNG
(4-(pyridin-3-yl)-5-(quinolin-4-yl)thiazol-2-amine ...)
Show SMILES Nc1nc(c(s1)-c1ccnc2ccccc12)-c1cccnc1
Show InChI InChI=1S/C17H12N4S/c18-17-21-15(11-4-3-8-19-10-11)16(22-17)13-7-9-20-14-6-2-1-5-12(13)14/h1-10H,(H2,18,21)
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n/an/a 3.98E+3n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Binding affinity to Activin A receptor type II-like kinase (ALK5) in fluorescence polarization binding assay; Range is (2.423-6.540)


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151351
PNG
(5''-Quinolin-4-yl-[2,4'']bithiazolyl-2''-ylamine |...)
Show SMILES Nc1nc(-c2nccs2)c(s1)-c1ccnc2ccccc12
Show InChI InChI=1S/C15H10N4S2/c16-15-19-12(14-18-7-8-20-14)13(21-15)10-5-6-17-11-4-2-1-3-9(10)11/h1-8H,(H2,16,19)
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n/an/a 6.58E+3n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151356
PNG
(4-(2-Fluoro-phenyl)-5-quinolin-4-yl-thiazol-2-ylam...)
Show SMILES Nc1nc(c(s1)-c1ccnc2ccccc12)-c1ccccc1F
Show InChI InChI=1S/C18H12FN3S/c19-14-7-3-1-6-13(14)16-17(23-18(20)22-16)12-9-10-21-15-8-4-2-5-11(12)15/h1-10H,(H2,20,22)
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n/an/a 6.67E+3n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151355
PNG
(5-[1,8]Naphthyridin-4-yl-4-pyridin-2-yl-thiazol-2-...)
Show SMILES Nc1nc(c(s1)-c1ccnc2ncccc12)-c1ccccn1
Show InChI InChI=1S/C16H11N5S/c17-16-21-13(12-5-1-2-7-18-12)14(22-16)10-6-9-20-15-11(10)4-3-8-19-15/h1-9H,(H2,17,21)
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n/an/a 7.94E+3n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Binding affinity to Activin A receptor type II-like kinase (ALK5) in fluorescence polarization binding assay; Range is (3.221-19.588)


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151365
PNG
(5-(6-Ethoxy-[1,5]naphthyridin-2-yl)-4-pyridin-2-yl...)
Show SMILES CCOc1ccc2nc(ccc2n1)-c1sc(N)nc1-c1ccccn1
Show InChI InChI=1S/C18H15N5OS/c1-2-24-15-9-8-11-12(22-15)6-7-14(21-11)17-16(23-18(19)25-17)13-5-3-4-10-20-13/h3-10H,2H2,1H3,(H2,19,23)
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n/an/a>1.00E+4n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151364
PNG
(4-(pyridin-3-yl)-5-(quinolin-4-yl)thiazol-2-amine ...)
Show SMILES Nc1nc(c(s1)-c1ccnc2ccccc12)-c1cccnc1
Show InChI InChI=1S/C17H12N4S/c18-17-21-15(11-4-3-8-19-10-11)16(22-17)13-7-9-20-14-6-2-1-5-12(13)14/h1-10H,(H2,18,21)
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n/an/a>1.00E+4n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151350
PNG
(4-(4-Chloro-pyridin-2-yl)-5-quinolin-4-yl-thiazol-...)
Show SMILES Nc1nc(c(s1)-c1ccnc2ccccc12)-c1cc(Cl)ccn1
Show InChI InChI=1S/C17H11ClN4S/c18-10-5-7-21-14(9-10)15-16(23-17(19)22-15)12-6-8-20-13-4-2-1-3-11(12)13/h1-9H,(H2,19,22)
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n/an/a>1.00E+4n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151349
PNG
(4-(5-Chloro-pyridin-2-yl)-5-quinolin-4-yl-thiazol-...)
Show SMILES Nc1nc(c(s1)-c1ccnc2ccccc12)-c1ccc(Cl)cn1
Show InChI InChI=1S/C17H11ClN4S/c18-10-5-6-14(21-9-10)15-16(23-17(19)22-15)12-7-8-20-13-4-2-1-3-11(12)13/h1-9H,(H2,19,22)
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n/an/a>1.00E+4n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151358
PNG
(4-Pyridin-2-yl-5-quinolin-2-yl-thiazol-2-ylamine |...)
Show SMILES Nc1nc(c(s1)-c1ccc2ccccc2n1)-c1ccccn1
Show InChI InChI=1S/C17H12N4S/c18-17-21-15(13-7-3-4-10-19-13)16(22-17)14-9-8-11-5-1-2-6-12(11)20-14/h1-10H,(H2,18,21)
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n/an/a>1.00E+4n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151361
PNG
(5-(naphthalen-1-yl)-4-(pyridin-2-yl)thiazol-2-amin...)
Show SMILES Nc1nc(c(s1)-c1cccc2ccccc12)-c1ccccn1
Show InChI InChI=1S/C18H13N3S/c19-18-21-16(15-10-3-4-11-20-15)17(22-18)14-9-5-7-12-6-1-2-8-13(12)14/h1-11H,(H2,19,21)
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n/an/a>1.00E+4n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151359
PNG
(4-(5-Methyl-pyridin-2-yl)-5-quinolin-4-yl-thiazol-...)
Show SMILES Cc1ccc(nc1)-c1nc(N)sc1-c1ccnc2ccccc12
Show InChI InChI=1S/C18H14N4S/c1-11-6-7-15(21-10-11)16-17(23-18(19)22-16)13-8-9-20-14-5-3-2-4-12(13)14/h2-10H,1H3,(H2,19,22)
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n/an/a>1.00E+4n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Binding affinity for Activin A receptor type II-like kinase (ALK5) in fluorescence polarization binding assay


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151360
PNG
(4-(2-Methoxy-phenyl)-5-quinolin-4-yl-thiazol-2-yla...)
Show SMILES COc1ccccc1-c1nc(N)sc1-c1ccnc2ccccc12
Show InChI InChI=1S/C19H15N3OS/c1-23-16-9-5-3-7-14(16)17-18(24-19(20)22-17)13-10-11-21-15-8-4-2-6-12(13)15/h2-11H,1H3,(H2,20,22)
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n/an/a>1.00E+4n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151360
PNG
(4-(2-Methoxy-phenyl)-5-quinolin-4-yl-thiazol-2-yla...)
Show SMILES COc1ccccc1-c1nc(N)sc1-c1ccnc2ccccc12
Show InChI InChI=1S/C19H15N3OS/c1-23-16-9-5-3-7-14(16)17-18(24-19(20)22-17)13-10-11-21-15-8-4-2-6-12(13)15/h2-11H,1H3,(H2,20,22)
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n/an/a>1.00E+4n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Binding affinity for Activin A receptor type II-like kinase (ALK5) in fluorescence polarization binding assay


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151359
PNG
(4-(5-Methyl-pyridin-2-yl)-5-quinolin-4-yl-thiazol-...)
Show SMILES Cc1ccc(nc1)-c1nc(N)sc1-c1ccnc2ccccc12
Show InChI InChI=1S/C18H14N4S/c1-11-6-7-15(21-10-11)16-17(23-18(19)22-16)13-8-9-20-14-5-3-2-4-12(13)14/h2-10H,1H3,(H2,19,22)
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n/an/a>1.00E+4n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151365
PNG
(5-(6-Ethoxy-[1,5]naphthyridin-2-yl)-4-pyridin-2-yl...)
Show SMILES CCOc1ccc2nc(ccc2n1)-c1sc(N)nc1-c1ccccn1
Show InChI InChI=1S/C18H15N5OS/c1-2-24-15-9-8-11-12(22-15)6-7-14(21-11)17-16(23-18(19)25-17)13-5-3-4-10-20-13/h3-10H,2H2,1H3,(H2,19,23)
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n/an/a>1.00E+4n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Binding affinity for Activin A receptor type II-like kinase (ALK5) in fluorescence polarization binding assay


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151355
PNG
(5-[1,8]Naphthyridin-4-yl-4-pyridin-2-yl-thiazol-2-...)
Show SMILES Nc1nc(c(s1)-c1ccnc2ncccc12)-c1ccccn1
Show InChI InChI=1S/C16H11N5S/c17-16-21-13(12-5-1-2-7-18-12)14(22-16)10-6-9-20-15-11(10)4-3-8-19-15/h1-9H,(H2,17,21)
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n/an/a>1.00E+4n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
TGF-beta receptor type-1


(Homo sapiens (Human))
BDBM50151361
PNG
(5-(naphthalen-1-yl)-4-(pyridin-2-yl)thiazol-2-amin...)
Show SMILES Nc1nc(c(s1)-c1cccc2ccccc12)-c1ccccn1
Show InChI InChI=1S/C18H13N3S/c19-18-21-16(15-10-3-4-11-20-15)17(22-18)14-9-5-7-12-6-1-2-8-13(12)14/h1-11H,(H2,19,21)
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n/an/a 1.10E+4n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Binding affinity to Activin A receptor type II-like kinase (ALK5) in fluorescence polarization binding assay; Range is (5.326-22.574)


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
Ribosomal protein S6 kinase alpha-5


(Homo sapiens (Human))
BDBM50151347
PNG
(2-(3-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-n...)
Show SMILES Cc1cccc(n1)-c1n[nH]cc1-c1ccc2ncccc2n1
Show InChI InChI=1S/C17H13N5/c1-11-4-2-5-16(20-11)17-12(10-19-22-17)13-7-8-14-15(21-13)6-3-9-18-14/h2-10H,1H3,(H,19,22)
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n/an/a>1.60E+4n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of MSK-1 kinase binding in fluorescence polarization assay


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
Serine/threonine-protein kinase B-raf


(Homo sapiens (Human))
BDBM50151347
PNG
(2-(3-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-n...)
Show SMILES Cc1cccc(n1)-c1n[nH]cc1-c1ccc2ncccc2n1
Show InChI InChI=1S/C17H13N5/c1-11-4-2-5-16(20-11)17-12(10-19-22-17)13-7-8-14-15(21-13)6-3-9-18-14/h2-10H,1H3,(H,19,22)
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n/an/a>1.60E+4n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of Protein kinase Raf-B binding in fluorescence polarization assay


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase LCK


(Mus musculus)
BDBM50151347
PNG
(2-(3-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-n...)
Show SMILES Cc1cccc(n1)-c1n[nH]cc1-c1ccc2ncccc2n1
Show InChI InChI=1S/C17H13N5/c1-11-4-2-5-16(20-11)17-12(10-19-22-17)13-7-8-14-15(21-13)6-3-9-18-14/h2-10H,1H3,(H,19,22)
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n/an/a>1.60E+4n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of p56 Lck tyrosine kinase binding in HTRF assay


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
Tyrosine-protein kinase ITK/TSK


(Homo sapiens (Human))
BDBM50151347
PNG
(2-(3-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-n...)
Show SMILES Cc1cccc(n1)-c1n[nH]cc1-c1ccc2ncccc2n1
Show InChI InChI=1S/C17H13N5/c1-11-4-2-5-16(20-11)17-12(10-19-22-17)13-7-8-14-15(21-13)6-3-9-18-14/h2-10H,1H3,(H,19,22)
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n/an/a>1.60E+4n/an/an/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Inhibition of IL-2-inducible T-cell kinase binding in HTRF assay


J Med Chem 47: 4494-506 (2004)


Article DOI: 10.1021/jm0400247
BindingDB Entry DOI: 10.7270/Q2VQ325T
More data for this
Ligand-Target Pair
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