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Patent code US10202365

Compile Data Set for Download or QSAR
Found 79 hits of Enzyme Inhibition Constant Data   
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


(Homo sapiens (Human))
BDBM84747
PNG
((B) ZD6474 | US10155768, Vandetanib | US10183928, ...)
Show SMILES CN1CCC(COc2cc3ncnc(Cc4ccc(Br)cc4F)c3cc2C)CC1
Show InChI InChI=1S/C23H25BrFN3O/c1-15-9-19-21(10-17-3-4-18(24)11-20(17)25)26-14-27-22(19)12-23(15)29-13-16-5-7-28(2)8-6-16/h3-4,9,11-12,14,16H,5-8,10,13H2,1-2H3
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US Patent
n/an/a 1.20n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM50363397
PNG
(CHEMBL1946170 | REGORAFENIB | US10183928, Regorafe...)
Show SMILES CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(c3)C(F)(F)F)c(F)c2)ccn1
Show InChI InChI=1S/C21H15ClF4N4O3/c1-27-19(31)18-10-13(6-7-28-18)33-12-3-5-17(16(23)9-12)30-20(32)29-11-2-4-15(22)14(8-11)21(24,25)26/h2-10H,1H3,(H,27,31)(H2,29,30,32)
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US Patent
n/an/a 5.10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM16673
PNG
(4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamo...)
Show SMILES CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(c3)C(F)(F)F)cc2)ccn1
Show InChI InChI=1S/C21H16ClF3N4O3/c1-26-19(30)18-11-15(8-9-27-18)32-14-5-2-12(3-6-14)28-20(31)29-13-4-7-17(22)16(10-13)21(23,24)25/h2-11H,1H3,(H,26,30)(H2,28,29,31)
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US Patent
n/an/a 7.90n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345847
PNG
(US10202365, Compound 24)
Show SMILES Cc1cc(C)n(n1)-c1ccc(CNC(=O)c2ccc(cn2)-c2nc(C)cc(Nc3cc(C)[nH]n3)n2)cn1
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US Patent
n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345851
PNG
(US10202365, Compound 28)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(nc2)-n2cc(CCO)cn2)n[nH]1
PDB

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US Patent
n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345847
PNG
(US10202365, Compound 24)
Show SMILES Cc1cc(C)n(n1)-c1ccc(CNC(=O)c2ccc(cn2)-c2nc(C)cc(Nc3cc(C)[nH]n3)n2)cn1
PDB

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US Patent
n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345841
PNG
(US10202365, Compound 18)
Show SMILES Cc1cnn(c1)-c1ccc(CNC(=O)c2ccc(cn2)-c2nc(C)cc(Nc3cc(C)[nH]n3)n2)cn1
PDB

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US Patent
n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345856
PNG
(US10202365, Compound 33)
Show SMILES C[C@@H](NC(=O)c1ccc(cn1)-c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
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US Patent
n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345852
PNG
(US10202365, Compound 29)
Show SMILES C[C@H](NC(=O)c1ncc(cc1C)-c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
PDB

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UniChem
US Patent
n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345848
PNG
(US10202365, Compound 25)
Show SMILES C[C@H](NC(=O)c1ccc(cn1)-c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
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n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345841
PNG
(US10202365, Compound 18)
Show SMILES Cc1cnn(c1)-c1ccc(CNC(=O)c2ccc(cn2)-c2nc(C)cc(Nc3cc(C)[nH]n3)n2)cn1
PDB
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US Patent
n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345853
PNG
(US10202365, Compound 30)
Show SMILES C[C@H](NC(=O)c1ncc(cc1F)-c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
PDB
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US Patent
n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345849
PNG
(US10202365, Compound 26)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(nc2)-n2ccc(n2)C2CC2)n[nH]1
PDB

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US Patent
n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345848
PNG
(US10202365, Compound 25)
Show SMILES C[C@H](NC(=O)c1ccc(cn1)-c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
PDB

GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345834
PNG
(US10202365, Compound 11)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(Cl)cc2)n[nH]1
PDB

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UniChem
US Patent
n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345852
PNG
(US10202365, Compound 29)
Show SMILES C[C@H](NC(=O)c1ncc(cc1C)-c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
PDB
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US Patent
n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345846
PNG
(US10202365, Compound 23)
Show SMILES C[C@H](NC(=O)c1ncc(cc1C)-c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cccn1
PDB
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n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345844
PNG
(US10202365, Compound 21)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2cnc(cn2)-n2cc(F)cn2)n[nH]1
PDB
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US Patent
n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345853
PNG
(US10202365, Compound 30)
Show SMILES C[C@H](NC(=O)c1ncc(cc1F)-c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
PDB

GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345844
PNG
(US10202365, Compound 21)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2cnc(cn2)-n2cc(F)cn2)n[nH]1
PDB

GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345842
PNG
(US10202365, Compound 19)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2cnc(C(=O)NCc3ccc(nc3)-n3cccn3)c(C)c2)n[nH]1
PDB
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n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345858
PNG
(US10202365, Compound 35)
Show SMILES C[C@H](NC(=O)c1ccc(cn1)-c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1cnc(cn1)-n1cc(F)cn1
PDB
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US Patent
n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345857
PNG
(US10202365, Compound 34)
Show SMILES CC[C@@H](NC(=O)c1ccc(cn1)-c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
PDB
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n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345842
PNG
(US10202365, Compound 19)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2cnc(C(=O)NCc3ccc(nc3)-n3cccn3)c(C)c2)n[nH]1
PDB

GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345849
PNG
(US10202365, Compound 26)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(nc2)-n2ccc(n2)C2CC2)n[nH]1
PDB
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n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345846
PNG
(US10202365, Compound 23)
Show SMILES C[C@H](NC(=O)c1ncc(cc1C)-c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cccn1
PDB

GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a<10n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM50363397
PNG
(CHEMBL1946170 | REGORAFENIB | US10183928, Regorafe...)
Show SMILES CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(c3)C(F)(F)F)c(F)c2)ccn1
Show InChI InChI=1S/C21H15ClF4N4O3/c1-27-19(31)18-10-13(6-7-28-18)33-12-3-5-17(16(23)9-12)30-20(32)29-11-2-4-15(22)14(8-11)21(24,25)26/h2-10H,1H3,(H,27,31)(H2,29,30,32)
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US Patent
n/an/a 29.8n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804M)


(Homo sapiens (Human))
BDBM16673
PNG
(4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamo...)
Show SMILES CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(c3)C(F)(F)F)cc2)ccn1
Show InChI InChI=1S/C21H16ClF3N4O3/c1-26-19(30)18-11-15(8-9-27-18)32-14-5-2-12(3-6-14)28-20(31)29-13-4-7-17(22)16(10-13)21(23,24)25/h2-11H,1H3,(H,26,30)(H2,28,29,31)
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n/an/a 32.4n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM50021574
PNG
(BMS-907351 | CABOZANTINIB | CHEBI:72317 | Cabomety...)
Show SMILES COc1cc2nccc(Oc3ccc(NC(=O)C4(CC4)C(=O)Nc4ccc(F)cc4)cc3)c2cc1OC
Show InChI InChI=1S/C28H24FN3O5/c1-35-24-15-21-22(16-25(24)36-2)30-14-11-23(21)37-20-9-7-19(8-10-20)32-27(34)28(12-13-28)26(33)31-18-5-3-17(29)4-6-18/h3-11,14-16H,12-13H2,1-2H3,(H,31,33)(H,32,34)
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n/an/a 46n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804M)


(Homo sapiens (Human))
BDBM50363397
PNG
(CHEMBL1946170 | REGORAFENIB | US10183928, Regorafe...)
Show SMILES CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(c3)C(F)(F)F)c(F)c2)ccn1
Show InChI InChI=1S/C21H15ClF4N4O3/c1-27-19(31)18-10-13(6-7-28-18)33-12-3-5-17(16(23)9-12)30-20(32)29-11-2-4-15(22)14(8-11)21(24,25)26/h2-10H,1H3,(H,27,31)(H2,29,30,32)
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n/an/a 46.7n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345834
PNG
(US10202365, Compound 11)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(Cl)cc2)n[nH]1
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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345850
PNG
(US10202365, Compound 27)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(nc2)-n2cc(cn2)C2CC2)n[nH]1
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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345825
PNG
(US10202365, Compound 2)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccccc2)n[nH]1
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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345833
PNG
(US10202365, Compound 10)
Show SMILES COc1ccc(CNC(=O)c2ccc(cn2)-c2nc(C)cc(Nc3cc(C)[nH]n3)n2)cc1
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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345835
PNG
(US10202365, Compound 12)
Show SMILES CCOc1ccc(CNC(=O)c2ccc(cn2)-c2nc(C)cc(Nc3cc(C)[nH]n3)n2)cc1
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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345837
PNG
(US10202365, Compound 14)
Show SMILES CC(C)Oc1ccc(CNC(=O)c2ccc(cn2)-c2nc(C)cc(Nc3cc(C)[nH]n3)n2)cc1
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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345855
PNG
(US10202365, Compound 32)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(nc2)-n2cc(C(F)F)c(C)n2)n[nH]1
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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345835
PNG
(US10202365, Compound 12)
Show SMILES CCOc1ccc(CNC(=O)c2ccc(cn2)-c2nc(C)cc(Nc3cc(C)[nH]n3)n2)cc1
PDB

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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345851
PNG
(US10202365, Compound 28)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(nc2)-n2cc(CCO)cn2)n[nH]1
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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345825
PNG
(US10202365, Compound 2)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccccc2)n[nH]1
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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345838
PNG
(US10202365, Compound 15)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(OC(F)F)cc2)n[nH]1
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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345845
PNG
(US10202365, Compound 22)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(nc2)-n2cc(cn2)C#N)n[nH]1
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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345836
PNG
(US10202365, Compound 13)
Show SMILES CCOc1ccc(CNC(=O)c2ncc(cc2C)-c2nc(C)cc(Nc3cc(C)[nH]n3)n2)cc1
PDB
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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345832
PNG
(US10202365, Compound 9)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(F)cc2)n[nH]1
PDB

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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345831
PNG
(US10202365, Compound 8)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2cccc(F)c2)n[nH]1
PDB

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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345824
PNG
(US10202365, Compound 1)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccoc2)n[nH]1
PDB

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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345830
PNG
(US10202365, Compound 7)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(C)cn2)n[nH]1
PDB

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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345830
PNG
(US10202365, Compound 7)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(C)cn2)n[nH]1
PDB
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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345855
PNG
(US10202365, Compound 32)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(nc2)-n2cc(C(F)F)c(C)n2)n[nH]1
PDB

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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345854
PNG
(US10202365, Compound 31)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(nc2)-n2cc(cn2)C(F)F)n[nH]1
PDB
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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345845
PNG
(US10202365, Compound 22)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(nc2)-n2cc(cn2)C#N)n[nH]1
PDB

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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345827
PNG
(US10202365, Compound 4)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)N2Cc3ccccc3C2)n[nH]1
PDB
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BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345838
PNG
(US10202365, Compound 15)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(OC(F)F)cc2)n[nH]1
PDB

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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345828
PNG
(US10202365, Compound 5)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(C)cc2)n[nH]1
PDB
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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345829
PNG
(US10202365, Compound 6)
Show SMILES C[C@@H](NC(=O)c1ccc(cn1)-c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccccc1
PDB

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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345828
PNG
(US10202365, Compound 5)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(C)cc2)n[nH]1
PDB

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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345837
PNG
(US10202365, Compound 14)
Show SMILES CC(C)Oc1ccc(CNC(=O)c2ccc(cn2)-c2nc(C)cc(Nc3cc(C)[nH]n3)n2)cc1
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BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345824
PNG
(US10202365, Compound 1)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccoc2)n[nH]1
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BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345827
PNG
(US10202365, Compound 4)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)N2Cc3ccccc3C2)n[nH]1
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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345833
PNG
(US10202365, Compound 10)
Show SMILES COc1ccc(CNC(=O)c2ccc(cn2)-c2nc(C)cc(Nc3cc(C)[nH]n3)n2)cc1
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BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345854
PNG
(US10202365, Compound 31)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(nc2)-n2cc(cn2)C(F)F)n[nH]1
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n/an/a 55n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345832
PNG
(US10202365, Compound 9)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(F)cc2)n[nH]1
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BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM16673
PNG
(4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamo...)
Show SMILES CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(c3)C(F)(F)F)cc2)ccn1
Show InChI InChI=1S/C21H16ClF3N4O3/c1-26-19(30)18-11-15(8-9-27-18)32-14-5-2-12(3-6-14)28-20(31)29-13-4-7-17(22)16(10-13)21(23,24)25/h2-11H,1H3,(H,26,30)(H2,28,29,31)
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n/an/a 95.2n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345829
PNG
(US10202365, Compound 6)
Show SMILES C[C@@H](NC(=O)c1ccc(cn1)-c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccccc1
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BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345840
PNG
(US10202365, Compound 17)
Show SMILES CCOc1ccc(cc1)[C@H](C)NC(=O)c1ncc(cc1C)-c1nc(C)cc(Nc2cc(C)[nH]n2)n1
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BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345843
PNG
(US10202365, Compound 20)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(OC(F)(F)F)cc2)n[nH]1
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BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345839
PNG
(US10202365, Compound 16)
Show SMILES CCOc1ccc(cc1)[C@@H](C)NC(=O)c1ncc(cc1C)-c1nc(C)cc(Nc2cc(C)[nH]n2)n1
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BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345826
PNG
(US10202365, Compound 3)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2cncs2)n[nH]1
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n/an/a>100n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345831
PNG
(US10202365, Compound 8)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2cccc(F)c2)n[nH]1
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BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345856
PNG
(US10202365, Compound 33)
Show SMILES C[C@@H](NC(=O)c1ccc(cn1)-c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
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n/an/a>100n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345850
PNG
(US10202365, Compound 27)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(nc2)-n2cc(cn2)C2CC2)n[nH]1
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n/an/a>100n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345826
PNG
(US10202365, Compound 3)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2cncs2)n[nH]1
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BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM345843
PNG
(US10202365, Compound 20)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)-c2ccc(nc2)C(=O)NCc2ccc(OC(F)(F)F)cc2)n[nH]1
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BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of wild type RET (ProQinase 1090-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEP...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345857
PNG
(US10202365, Compound 34)
Show SMILES CC[C@@H](NC(=O)c1ccc(cn1)-c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
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n/an/a>100n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM345858
PNG
(US10202365, Compound 35)
Show SMILES C[C@H](NC(=O)c1ccc(cn1)-c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1cnc(cn1)-n1cc(F)cn1
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BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM50021574
PNG
(BMS-907351 | CABOZANTINIB | CHEBI:72317 | Cabomety...)
Show SMILES COc1cc2nccc(Oc3ccc(NC(=O)C4(CC4)C(=O)Nc4ccc(F)cc4)cc3)c2cc1OC
Show InChI InChI=1S/C28H24FN3O5/c1-35-24-15-21-22(16-25(24)36-2)30-14-11-23(21)37-20-9-7-19(8-10-20)32-27(34)28(12-13-28)26(33)31-18-5-3-17(29)4-6-18/h3-11,14-16H,12-13H2,1-2H3,(H,31,33)(H,32,34)
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BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804M)


(Homo sapiens (Human))
BDBM50021574
PNG
(BMS-907351 | CABOZANTINIB | CHEBI:72317 | Cabomety...)
Show SMILES COc1cc2nccc(Oc3ccc(NC(=O)C4(CC4)C(=O)Nc4ccc(F)cc4)cc3)c2cc1OC
Show InChI InChI=1S/C28H24FN3O5/c1-35-24-15-21-22(16-25(24)36-2)30-14-11-23(21)37-20-9-7-19(8-10-20)32-27(34)28(12-13-28)26(33)31-18-5-3-17(29)4-6-18/h3-11,14-16H,12-13H2,1-2H3,(H,31,33)(H,32,34)
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BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804M)


(Homo sapiens (Human))
BDBM84747
PNG
((B) ZD6474 | US10155768, Vandetanib | US10183928, ...)
Show SMILES CN1CCC(COc2cc3ncnc(Cc4ccc(Br)cc4F)c3cc2C)CC1
Show InChI InChI=1S/C23H25BrFN3O/c1-15-9-19-21(10-17-3-4-18(24)11-20(17)25)26-14-27-22(19)12-23(15)29-13-16-5-7-28(2)8-6-16/h3-4,9,11-12,14,16H,5-8,10,13H2,1-2H3
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BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM84747
PNG
((B) ZD6474 | US10155768, Vandetanib | US10183928, ...)
Show SMILES CN1CCC(COc2cc3ncnc(Cc4ccc(Br)cc4F)c3cc2C)CC1
Show InChI InChI=1S/C23H25BrFN3O/c1-15-9-19-21(10-17-3-4-18(24)11-20(17)25)26-14-27-22(19)12-23(15)29-13-16-5-7-28(2)8-6-16/h3-4,9,11-12,14,16H,5-8,10,13H2,1-2H3
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BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In each well of a 384-well plate, 7.5 nM-10 nM of mutant RET (ProQinase 1096-0000-1) is incubated in a total of 12.5 μL of buffer (100 mM HEPES ...


US Patent US10202365 (2019)

More data for this
Ligand-Target Pair
* indicates data uncertainty>20%