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Found 813 hits Enz. Inhib. hit(s) with Target = 'Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]'   
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
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311699
PNG
(Ex. Cpd. 151 | US10807986, Example 151 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CCN3CCSCC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C26H30N6O2S/c1-26(9-10-26)32-20(4-3-11-31-12-14-35-15-13-31)21(22-23(27)28-17-29-24(22)32)25(33)30-19-7-5-18(6-8-19)16-34-2/h5-8,17H,9-16H2,1-2H3,(H,30,33)(H2,27,28,29)
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US Patent
n/an/a 0.300n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311643
PNG
(Ex. Cpd. 95 | US10807986, Example 95 | US11046696,...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CC)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C22H23N5O2/c1-4-5-16-17(21(28)26-15-8-6-14(7-9-15)12-29-3)18-19(23)24-13-25-20(18)27(16)22(2)10-11-22/h6-9,13H,10-12H2,1-3H3,(H,26,28)(H2,23,24,25)
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n/an/a 0.300n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311622
PNG
(Ex. Cpd. 59 | US10807986, Example 59 | US11046696,...)
Show SMILES CSCc1ccc(NC(=O)c2c(Br)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C19H20BrN5OS/c1-19(7-8-19)25-15(20)13(14-16(21)22-10-23-17(14)25)18(26)24-12-5-3-11(4-6-12)9-27-2/h3-6,10H,7-9H2,1-2H3,(H,24,26)(H2,21,22,23)
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n/an/a 0.300n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311651
PNG
(Ex. Cpd. 103 | US10807986, Example 103 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CCC3(O)CCC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C26H29N5O3/c1-25(13-14-25)31-19(5-3-10-26(33)11-4-12-26)20(21-22(27)28-16-29-23(21)31)24(32)30-18-8-6-17(7-9-18)15-34-2/h6-9,16,33H,4,10-15H2,1-2H3,(H,30,32)(H2,27,28,29)
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n/an/a 0.300n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311699
PNG
(Ex. Cpd. 151 | US10807986, Example 151 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CCN3CCSCC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C26H30N6O2S/c1-26(9-10-26)32-20(4-3-11-31-12-14-35-15-13-31)21(22-23(27)28-17-29-24(22)32)25(33)30-19-7-5-18(6-8-19)16-34-2/h5-8,17H,9-16H2,1-2H3,(H,30,33)(H2,27,28,29)
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TBA

Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET kinase activity, the website of AnaSpec states that...


Citation and Details

BindingDB Entry DOI: 10.7270/Q2280BR0
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311639
PNG
(Ex. Cpd. 91 | US10807986, Example 91 | US11046696,...)
Show SMILES COCc1ccc(NC(=O)c2c(C#Cc3cnc4cccnn34)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C27H24N8O2/c1-27(11-12-27)34-20(10-9-19-14-29-21-4-3-13-32-35(19)21)22(23-24(28)30-16-31-25(23)34)26(36)33-18-7-5-17(6-8-18)15-37-2/h3-8,13-14,16H,11-12,15H2,1-2H3,(H,33,36)(H2,28,30,31)
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US Patent
n/an/a 0.300n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311634
PNG
(Ex. Cpd. 86 | US10807986, Example 86 | US11046696,...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CCC(C)(C)O)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C25H29N5O3/c1-24(2,32)11-5-6-18-19(23(31)29-17-9-7-16(8-10-17)14-33-4)20-21(26)27-15-28-22(20)30(18)25(3)12-13-25/h7-10,15,32H,11-14H2,1-4H3,(H,29,31)(H2,26,27,28)
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n/an/a 0.300n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311622
PNG
(Ex. Cpd. 59 | US10807986, Example 59 | US11046696,...)
Show SMILES CSCc1ccc(NC(=O)c2c(Br)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C19H20BrN5OS/c1-19(7-8-19)25-15(20)13(14-16(21)22-10-23-17(14)25)18(26)24-12-5-3-11(4-6-12)9-27-2/h3-6,10H,7-9H2,1-2H3,(H,24,26)(H2,21,22,23)
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US Patent
n/an/a 0.300n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311639
PNG
(Ex. Cpd. 91 | US10807986, Example 91 | US11046696,...)
Show SMILES COCc1ccc(NC(=O)c2c(C#Cc3cnc4cccnn34)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C27H24N8O2/c1-27(11-12-27)34-20(10-9-19-14-29-21-4-3-13-32-35(19)21)22(23-24(28)30-16-31-25(23)34)26(36)33-18-7-5-17(6-8-18)15-37-2/h3-8,13-14,16H,11-12,15H2,1-2H3,(H,33,36)(H2,28,30,31)
PDB

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US Patent
n/an/a 0.300n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311705
PNG
(Ex. Cpd. 157 | US10807986, Example 157 | US1104669...)
Show SMILES CCC(O)CC#Cc1c(C(=O)Nc2ccc(COC)cc2)c2c(N)ncnc2n1C1(C)CC1
Show InChI InChI=1S/C25H29N5O3/c1-4-18(31)6-5-7-19-20(24(32)29-17-10-8-16(9-11-17)14-33-3)21-22(26)27-15-28-23(21)30(19)25(2)12-13-25/h8-11,15,18,31H,4,6,12-14H2,1-3H3,(H,29,32)(H2,26,27,28)
PDB

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n/an/a 0.300n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311717
PNG
(Ex. Cpd. 169 | US10807986, Example 169 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CCn3cccc3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C26H26N6O2/c1-26(11-12-26)32-20(6-5-15-31-13-3-4-14-31)21(22-23(27)28-17-29-24(22)32)25(33)30-19-9-7-18(8-10-19)16-34-2/h3-4,7-10,13-14,17H,11-12,15-16H2,1-2H3,(H,30,33)(H2,27,28,29)
PDB

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n/an/a 0.300n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311705
PNG
(Ex. Cpd. 157 | US10807986, Example 157 | US1104669...)
Show SMILES CCC(O)CC#Cc1c(C(=O)Nc2ccc(COC)cc2)c2c(N)ncnc2n1C1(C)CC1
Show InChI InChI=1S/C25H29N5O3/c1-4-18(31)6-5-7-19-20(24(32)29-17-10-8-16(9-11-17)14-33-3)21-22(26)27-15-28-23(21)30(19)25(2)12-13-25/h8-11,15,18,31H,4,6,12-14H2,1-3H3,(H,29,32)(H2,26,27,28)
PDB

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US Patent
n/an/a 0.300n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311643
PNG
(Ex. Cpd. 95 | US10807986, Example 95 | US11046696,...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CC)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C22H23N5O2/c1-4-5-16-17(21(28)26-15-8-6-14(7-9-15)12-29-3)18-19(23)24-13-25-20(18)27(16)22(2)10-11-22/h6-9,13H,10-12H2,1-3H3,(H,26,28)(H2,23,24,25)
PDB

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n/an/a 0.300n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311651
PNG
(Ex. Cpd. 103 | US10807986, Example 103 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CCC3(O)CCC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C26H29N5O3/c1-25(13-14-25)31-19(5-3-10-26(33)11-4-12-26)20(21-22(27)28-16-29-23(21)31)24(32)30-18-8-6-17(7-9-18)15-34-2/h6-9,16,33H,4,10-15H2,1-2H3,(H,30,32)(H2,27,28,29)
PDB

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US Patent
n/an/a 0.300n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311699
PNG
(Ex. Cpd. 151 | US10807986, Example 151 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CCN3CCSCC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C26H30N6O2S/c1-26(9-10-26)32-20(4-3-11-31-12-14-35-15-13-31)21(22-23(27)28-17-29-24(22)32)25(33)30-19-7-5-18(6-8-19)16-34-2/h5-8,17H,9-16H2,1-2H3,(H,30,33)(H2,27,28,29)
PDB

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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311700
PNG
(Ex. Cpd. 152 | US10807986, Example 152 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CCC3CCOCC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C27H31N5O3/c1-27(12-13-27)32-21(5-3-4-18-10-14-35-15-11-18)22(23-24(28)29-17-30-25(23)32)26(33)31-20-8-6-19(7-9-20)16-34-2/h6-9,17-18H,4,10-16H2,1-2H3,(H,31,33)(H2,28,29,30)
PDB

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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311717
PNG
(Ex. Cpd. 169 | US10807986, Example 169 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CCn3cccc3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C26H26N6O2/c1-26(11-12-26)32-20(6-5-15-31-13-3-4-14-31)21(22-23(27)28-17-29-24(22)32)25(33)30-19-9-7-18(8-10-19)16-34-2/h3-4,7-10,13-14,17H,11-12,15-16H2,1-2H3,(H,30,33)(H2,27,28,29)
PDB

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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311700
PNG
(Ex. Cpd. 152 | US10807986, Example 152 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CCC3CCOCC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C27H31N5O3/c1-27(12-13-27)32-21(5-3-4-18-10-14-35-15-11-18)22(23-24(28)29-17-30-25(23)32)26(33)31-20-8-6-19(7-9-20)16-34-2/h6-9,17-18H,4,10-16H2,1-2H3,(H,31,33)(H2,28,29,30)
PDB

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US Patent
n/an/a 0.300n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311634
PNG
(Ex. Cpd. 86 | US10807986, Example 86 | US11046696,...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CCC(C)(C)O)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C25H29N5O3/c1-24(2,32)11-5-6-18-19(23(31)29-17-9-7-16(8-10-17)14-33-4)20-21(26)27-15-28-22(20)30(18)25(3)12-13-25/h7-10,15,32H,11-14H2,1-4H3,(H,29,31)(H2,26,27,28)
PDB

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n/an/a 0.300n/an/an/an/an/an/a



Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311723
PNG
(Ex. Cpd. 175 | US10807986, Example 175 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#Cc3cncc(F)c3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C26H23FN6O2/c1-26(9-10-26)33-20(8-5-17-11-18(27)13-29-12-17)21(22-23(28)30-15-31-24(22)33)25(34)32-19-6-3-16(4-7-19)14-35-2/h3-4,6-7,11-13,15H,9-10,14H2,1-2H3,(H,32,34)(H2,28,30,31)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311652
PNG
(Ex. Cpd. 104 | US10807986, Example 104 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CC(O)C3CC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C25H27N5O3/c1-25(11-12-25)30-18(9-10-19(31)16-5-6-16)20(21-22(26)27-14-28-23(21)30)24(32)29-17-7-3-15(4-8-17)13-33-2/h3-4,7-8,14,16,19,31H,5-6,11-13H2,1-2H3,(H,29,32)(H2,26,27,28)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311636
PNG
(Ex. Cpd. 88 | US10807986, Example 88 | US11046696,...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CCN3CCCC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C26H30N6O2/c1-26(11-12-26)32-20(6-5-15-31-13-3-4-14-31)21(22-23(27)28-17-29-24(22)32)25(33)30-19-9-7-18(8-10-19)16-34-2/h7-10,17H,3-4,11-16H2,1-2H3,(H,30,33)(H2,27,28,29)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311652
PNG
(Ex. Cpd. 104 | US10807986, Example 104 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CC(O)C3CC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C25H27N5O3/c1-25(11-12-25)30-18(9-10-19(31)16-5-6-16)20(21-22(26)27-14-28-23(21)30)24(32)29-17-7-3-15(4-8-17)13-33-2/h3-4,7-8,14,16,19,31H,5-6,11-13H2,1-2H3,(H,29,32)(H2,26,27,28)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311653
PNG
(Ex. Cpd. 105 | US10807986, Example 105 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CCN3CCCCC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C27H32N6O2/c1-27(12-13-27)33-21(7-6-16-32-14-4-3-5-15-32)22(23-24(28)29-18-30-25(23)33)26(34)31-20-10-8-19(9-11-20)17-35-2/h8-11,18H,3-5,12-17H2,1-2H3,(H,31,34)(H2,28,29,30)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311653
PNG
(Ex. Cpd. 105 | US10807986, Example 105 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CCN3CCCCC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C27H32N6O2/c1-27(12-13-27)33-21(7-6-16-32-14-4-3-5-15-32)22(23-24(28)29-18-30-25(23)33)26(34)31-20-10-8-19(9-11-20)17-35-2/h8-11,18H,3-5,12-17H2,1-2H3,(H,31,34)(H2,28,29,30)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311723
PNG
(Ex. Cpd. 175 | US10807986, Example 175 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#Cc3cncc(F)c3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C26H23FN6O2/c1-26(9-10-26)33-20(8-5-17-11-18(27)13-29-12-17)21(22-23(28)30-15-31-24(22)33)25(34)32-19-6-3-16(4-7-19)14-35-2/h3-4,6-7,11-13,15H,9-10,14H2,1-2H3,(H,32,34)(H2,28,30,31)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311636
PNG
(Ex. Cpd. 88 | US10807986, Example 88 | US11046696,...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CCN3CCCC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C26H30N6O2/c1-26(11-12-26)32-20(6-5-15-31-13-3-4-14-31)21(22-23(27)28-17-29-24(22)32)25(33)30-19-9-7-18(8-10-19)16-34-2/h7-10,17H,3-4,11-16H2,1-2H3,(H,30,33)(H2,27,28,29)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311704
PNG
(Ex. Cpd. 156 | US10807986, Example 156 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CCC3NC(=O)NC3=O)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C25H25N7O4/c1-25(10-11-25)32-17(5-3-4-16-22(33)31-24(35)30-16)18(19-20(26)27-13-28-21(19)32)23(34)29-15-8-6-14(7-9-15)12-36-2/h6-9,13,16H,4,10-12H2,1-2H3,(H,29,34)(H2,26,27,28)(H2,30,31,33,35)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311679
PNG
(Ex. Cpd. 131 | US10807986, Example 131 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CC3(O)CCCC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C26H29N5O3/c1-25(13-14-25)31-19(9-12-26(33)10-3-4-11-26)20(21-22(27)28-16-29-23(21)31)24(32)30-18-7-5-17(6-8-18)15-34-2/h5-8,16,33H,3-4,10-11,13-15H2,1-2H3,(H,30,32)(H2,27,28,29)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311660
PNG
(Ex. Cpd. 112 | US10807986, Example 112)
Show SMILES COCc1ccc(NC(=O)c2c(C#CC3CCC(=O)CC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C27H29N5O3/c1-27(13-14-27)32-21(12-7-17-5-10-20(33)11-6-17)22(23-24(28)29-16-30-25(23)32)26(34)31-19-8-3-18(4-9-19)15-35-2/h3-4,8-9,16-17H,5-6,10-11,13-15H2,1-2H3,(H,31,34)(H2,28,29,30)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311703
PNG
(Ex. Cpd. 155 | US10807986, Example 155 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#Cc3ccc(N)nc3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C26H25N7O2/c1-26(11-12-26)33-19(9-5-16-6-10-20(27)29-13-16)21(22-23(28)30-15-31-24(22)33)25(34)32-18-7-3-17(4-8-18)14-35-2/h3-4,6-8,10,13,15H,11-12,14H2,1-2H3,(H2,27,29)(H,32,34)(H2,28,30,31)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311707
PNG
(Ex. Cpd. 159 | US10807986, Example 159 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#Cc3cnc4ccoc4c3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C28H24N6O3/c1-28(10-11-28)34-21(8-5-18-13-22-20(30-14-18)9-12-37-22)23(24-25(29)31-16-32-26(24)34)27(35)33-19-6-3-17(4-7-19)15-36-2/h3-4,6-7,9,12-14,16H,10-11,15H2,1-2H3,(H,33,35)(H2,29,31,32)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311707
PNG
(Ex. Cpd. 159 | US10807986, Example 159 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#Cc3cnc4ccoc4c3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C28H24N6O3/c1-28(10-11-28)34-21(8-5-18-13-22-20(30-14-18)9-12-37-22)23(24-25(29)31-16-32-26(24)34)27(35)33-19-6-3-17(4-7-19)15-36-2/h3-4,6-7,9,12-14,16H,10-11,15H2,1-2H3,(H,33,35)(H2,29,31,32)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311704
PNG
(Ex. Cpd. 156 | US10807986, Example 156 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CCC3NC(=O)NC3=O)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C25H25N7O4/c1-25(10-11-25)32-17(5-3-4-16-22(33)31-24(35)30-16)18(19-20(26)27-13-28-21(19)32)23(34)29-15-8-6-14(7-9-15)12-36-2/h6-9,13,16H,4,10-12H2,1-2H3,(H,29,34)(H2,26,27,28)(H2,30,31,33,35)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311703
PNG
(Ex. Cpd. 155 | US10807986, Example 155 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#Cc3ccc(N)nc3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C26H25N7O2/c1-26(11-12-26)33-19(9-5-16-6-10-20(27)29-13-16)21(22-23(28)30-15-31-24(22)33)25(34)32-18-7-3-17(4-8-18)14-35-2/h3-4,6-8,10,13,15H,11-12,14H2,1-2H3,(H2,27,29)(H,32,34)(H2,28,30,31)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311679
PNG
(Ex. Cpd. 131 | US10807986, Example 131 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CC3(O)CCCC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C26H29N5O3/c1-25(13-14-25)31-19(9-12-26(33)10-3-4-11-26)20(21-22(27)28-16-29-23(21)31)24(32)30-18-7-5-17(6-8-18)15-34-2/h5-8,16,33H,3-4,10-11,13-15H2,1-2H3,(H,30,32)(H2,27,28,29)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311660
PNG
(Ex. Cpd. 112 | US10807986, Example 112)
Show SMILES COCc1ccc(NC(=O)c2c(C#CC3CCC(=O)CC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C27H29N5O3/c1-27(13-14-27)32-21(12-7-17-5-10-20(33)11-6-17)22(23-24(28)29-16-30-25(23)32)26(34)31-19-8-3-18(4-9-19)15-35-2/h3-4,8-9,16-17H,5-6,10-11,13-15H2,1-2H3,(H,31,34)(H2,28,29,30)
PDB

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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311673
PNG
(Ex. Cpd. 125 | US10807986, Example 125 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CCC3(O)COC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C25H27N5O4/c1-24(10-11-24)30-18(4-3-9-25(32)13-34-14-25)19(20-21(26)27-15-28-22(20)30)23(31)29-17-7-5-16(6-8-17)12-33-2/h5-8,15,32H,9-14H2,1-2H3,(H,29,31)(H2,26,27,28)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311741
PNG
(Ex. Cpd. 193 | US10807986, Example 193 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#Cc3cncs3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C24H22N6O2S/c1-24(9-10-24)30-18(8-7-17-11-26-14-33-17)19(20-21(25)27-13-28-22(20)30)23(31)29-16-5-3-15(4-6-16)12-32-2/h3-6,11,13-14H,9-10,12H2,1-2H3,(H,29,31)(H2,25,27,28)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311637
PNG
(Ex. Cpd. 89)
Show SMILES COCc1ccc(NC(=O)c2c(OCC3CCCO3)n(c3ncncc23)C2(C)CC2)cc1
Show InChI InChI=1S/C24H28N4O4/c1-24(9-10-24)28-21-19(12-25-15-26-21)20(23(28)32-14-18-4-3-11-31-18)22(29)27-17-7-5-16(6-8-17)13-30-2/h5-8,12,15,18H,3-4,9-11,13-14H2,1-2H3,(H,27,29)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311635
PNG
(Ex. Cpd. 87 | US10807986, Example 87 | US11046696,...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CC3CCOCC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C26H29N5O3/c1-26(11-12-26)31-20(8-5-17-9-13-34-14-10-17)21(22-23(27)28-16-29-24(22)31)25(32)30-19-6-3-18(4-7-19)15-33-2/h3-4,6-7,16-17H,9-15H2,1-2H3,(H,30,32)(H2,27,28,29)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM469423
PNG
(US10807986, Example 89 | US11046696, Compound 89)
Show SMILES COCc1ccc(NC(=O)c2c(OC[C@H]3CCCO3)n(c3ncnc(N)c23)C2(C)CC2)cc1 |r|
Show InChI InChI=1S/C24H29N5O4/c1-24(9-10-24)29-21-18(20(25)26-14-27-21)19(23(29)33-13-17-4-3-11-32-17)22(30)28-16-7-5-15(6-8-16)12-31-2/h5-8,14,17H,3-4,9-13H2,1-2H3,(H,28,30)(H2,25,26,27)/t17-/m1/s1
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311708
PNG
(Ex. Cpd. 160 | US10807986, Example 160 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#Cc3cn[nH]c3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C24H23N7O2/c1-24(9-10-24)31-18(8-5-16-11-28-29-12-16)19(20-21(25)26-14-27-22(20)31)23(32)30-17-6-3-15(4-7-17)13-33-2/h3-4,6-7,11-12,14H,9-10,13H2,1-2H3,(H,28,29)(H,30,32)(H2,25,26,27)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311691
PNG
(Ex. Cpd. 143 | US10807986, Example 143 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CCC3(O)CCOCC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C27H31N5O4/c1-26(10-11-26)32-20(4-3-9-27(34)12-14-36-15-13-27)21(22-23(28)29-17-30-24(22)32)25(33)31-19-7-5-18(6-8-19)16-35-2/h5-8,17,34H,9-16H2,1-2H3,(H,31,33)(H2,28,29,30)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311741
PNG
(Ex. Cpd. 193 | US10807986, Example 193 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#Cc3cncs3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C24H22N6O2S/c1-24(9-10-24)30-18(8-7-17-11-26-14-33-17)19(20-21(25)27-13-28-22(20)30)23(31)29-16-5-3-15(4-6-16)12-32-2/h3-6,11,13-14H,9-10,12H2,1-2H3,(H,29,31)(H2,25,27,28)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311708
PNG
(Ex. Cpd. 160 | US10807986, Example 160 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#Cc3cn[nH]c3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C24H23N7O2/c1-24(9-10-24)31-18(8-5-16-11-28-29-12-16)19(20-21(25)26-14-27-22(20)31)23(32)30-17-6-3-15(4-7-17)13-33-2/h3-4,6-7,11-12,14H,9-10,13H2,1-2H3,(H,28,29)(H,30,32)(H2,25,26,27)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311700
PNG
(Ex. Cpd. 152 | US10807986, Example 152 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CCC3CCOCC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C27H31N5O3/c1-27(12-13-27)32-21(5-3-4-18-10-14-35-15-11-18)22(23-24(28)29-17-30-25(23)32)26(33)31-20-8-6-19(7-9-20)16-34-2/h6-9,17-18H,4,10-16H2,1-2H3,(H,31,33)(H2,28,29,30)
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TBA

Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET kinase activity, the website of AnaSpec states that...


Citation and Details

BindingDB Entry DOI: 10.7270/Q2280BR0
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311635
PNG
(Ex. Cpd. 87 | US10807986, Example 87 | US11046696,...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CC3CCOCC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C26H29N5O3/c1-26(11-12-26)31-20(8-5-17-9-13-34-14-10-17)21(22-23(27)28-16-29-24(22)31)25(32)30-19-6-3-18(4-7-19)15-33-2/h3-4,6-7,16-17H,9-15H2,1-2H3,(H,30,32)(H2,27,28,29)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L) (i.e., RET with V804L mutation) kinase acti...


US Patent US10155768 (2018)


BindingDB Entry DOI: 10.7270/Q2X350J3
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311691
PNG
(Ex. Cpd. 143 | US10807986, Example 143 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CCC3(O)CCOCC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C27H31N5O4/c1-26(10-11-26)32-20(4-3-9-27(34)12-14-36-15-13-27)21(22-23(28)29-17-30-24(22)32)25(33)31-19-7-5-18(6-8-19)16-35-2/h5-8,17,34H,9-16H2,1-2H3,(H,31,33)(H2,28,29,30)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [V804L]


(Homo sapiens (Human))
BDBM311673
PNG
(Ex. Cpd. 125 | US10807986, Example 125 | US1104669...)
Show SMILES COCc1ccc(NC(=O)c2c(C#CCC3(O)COC3)n(c3ncnc(N)c23)C2(C)CC2)cc1
Show InChI InChI=1S/C25H27N5O4/c1-24(10-11-24)30-18(4-3-9-25(32)13-34-14-25)19(20-21(26)27-15-28-22(20)30)23(31)29-17-7-5-16(6-8-17)12-33-2/h5-8,15,32H,9-14H2,1-2H3,(H,29,31)(H2,26,27,28)
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Taiho Pharmaceutical Co., Ltd.

US Patent


Assay Description
Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mut...


US Patent US10807986 (2020)


BindingDB Entry DOI: 10.7270/Q29G5QWG
More data for this
Ligand-Target Pair
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