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Patent code US10584114

Compile Data Set for Download or QSAR
Found 82 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))
BDBM21
PNG
(6-[(4R,5S,6S,7R)-4,7-dibenzyl-3-(5-carboxypentyl)-...)
Show SMILES COc1cc2c(Nc3ccc(Br)cc3F)ncnc2cc1OCC1CCN(C)CC1
Show InChI InChI=1S/C22H24BrFN4O2/c1-28-7-5-14(6-8-28)12-30-21-11-19-16(10-20(21)29-2)22(26-13-25-19)27-18-4-3-15(23)9-17(18)24/h3-4,9-11,13-14H,5-8,12H2,1-2H3,(H,25,26,27)
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US Patent
n/an/a 4n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In order to assess the activity of chemical compounds against the relevant kinase of interest, the Caliper LifeSciences electrophoretic mobility shif...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
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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n/an/a 7.90n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In order to assess the activity of chemical compounds against the relevant kinase of interest, the Caliper LifeSciences electrophoretic mobility shif...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
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 11n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In order to assess the activity of chemical compounds against the relevant kinase of interest, the Caliper LifeSciences electrophoretic mobility shif...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
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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n/an/a 12n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In order to assess the activity of chemical compounds against the relevant kinase of interest, the Caliper LifeSciences electrophoretic mobility shif...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
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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n/an/a 45n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In order to assess the activity of chemical compounds against the relevant kinase of interest, the Caliper LifeSciences electrophoretic mobility shif...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
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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n/an/a 53n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In order to assess the activity of chemical compounds against the relevant kinase of interest, the Caliper LifeSciences electrophoretic mobility shif...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
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 order to assess the activity of chemical compounds against the relevant kinase of interest, the Caliper LifeSciences electrophoretic mobility shif...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM434989
PNG
(US10584114, Compound 101)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)[C@H]2CC[C@@H](CC2)C(=O)NCc2ccc(nc2)-n2cccn2)n[nH]1
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n/an/a<500n/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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435001
PNG
(US10584114, Compound 114)
Show SMILES Cc1cc(Nc2cc(C)cc(n2)[C@]2(O)CC[C@@H](C(=O)NCc3ccc(nc3)-n3cccn3)C(C)(C)C2)n[nH]1
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n/an/a<500n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435011
PNG
(US10584114, Compound 131)
Show SMILES CO[C@@]1(CC[C@@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@@H](C)c1cnc(cn1)-n1cc(F)cn1
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US Patent
n/an/a<500n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435013
PNG
(US10584114, Compound 136)
Show SMILES CCO[C@@]1(CC[C@@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@@H](C)c1ccc(nc1)-n1cc(F)cn1
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n/an/a<500n/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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435013
PNG
(US10584114, Compound 136)
Show SMILES CCO[C@@]1(CC[C@@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@@H](C)c1ccc(nc1)-n1cc(F)cn1
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n/an/a<500n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM434998
PNG
(US10584114, Compound 111)
Show SMILES C[C@H](NC(=O)[C@H]1CC[C@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
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n/an/a<500n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435021
PNG
(US10584114, Compound 148)
Show SMILES C[C@H](NC(=O)[C@@]1(C)CC[C@@](O)(CO1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
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n/an/a<500n/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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435023
PNG
(US10584114, Compound 150)
Show SMILES CO[C@@]1(CC[C@@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)NCc1cnc(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 wild type RET (ProQinase 1090-0000-1) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435000
PNG
(US10584114, Compound 113)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)[C@H]2CC[C@@H](CC2)C(=O)NCc2ccc(nc2)-n2cc(Cl)cn2)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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435001
PNG
(US10584114, Compound 114)
Show SMILES Cc1cc(Nc2cc(C)cc(n2)[C@]2(O)CC[C@@H](C(=O)NCc3ccc(nc3)-n3cccn3)C(C)(C)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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435004
PNG
(US10584114, Compound 120)
Show SMILES C[C@H](NC(=O)[C@H]1CC[C@@](O)(CC1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-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 wild type RET (ProQinase 1090-0000-1) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435005
PNG
(US10584114, Compound 121)
Show SMILES C[C@H](NC(=O)[C@H]1CC[C@@](F)(CC1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
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n/an/a<500n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435010
PNG
(US10584114, Compound 130)
Show SMILES CO[C@@]1(CC[C@@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@@H](C)c1ccc(nc1)-n1cc(F)cn1
PDB

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n/an/a<500n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435017
PNG
(US10584114, Compound 142)
Show SMILES CO[C@]1(CC[C@](F)(CC1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@@H](C)c1ccc(nc1)-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 wild type RET (ProQinase 1090-0000-1) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435019
PNG
(US10584114, Compound 146)
Show SMILES C[C@H](NC(=O)[C@@H]1CC[C@](O)(CO1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
PDB

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n/an/a<500n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM434991
PNG
(US10584114, Compound 103)
Show SMILES C[C@H](NC(=O)[C@H]1CC[C@@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cccn1
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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM434991
PNG
(US10584114, Compound 103)
Show SMILES C[C@H](NC(=O)[C@H]1CC[C@@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cccn1
PDB

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US Patent
n/an/a<500n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435000
PNG
(US10584114, Compound 113)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)[C@H]2CC[C@@H](CC2)C(=O)NCc2ccc(nc2)-n2cc(Cl)cn2)n[nH]1
PDB
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n/an/a<500n/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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435015
PNG
(US10584114, Compound 138)
Show SMILES CO[C@@]1(CC[C@](O)(CC1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@@H](C)c1ccc(nc1)-n1cc(F)cn1
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n/an/a<500n/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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435018
PNG
(US10584114, Compound 144)
Show SMILES C[C@H](NC(=O)C1CCC(=CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435024
PNG
(US10584114, Compound 151)
Show SMILES CO[C@@]1(CC[C@@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@H](C)c1ccc(nc1)-n1cc(F)cn1
PDB

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n/an/a<500n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM434999
PNG
(US10584114, Compound 112)
Show SMILES C[C@H](NC(=O)[C@H]1CC[C@@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-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 wild type RET (ProQinase 1090-0000-1) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435005
PNG
(US10584114, Compound 121)
Show SMILES C[C@H](NC(=O)[C@H]1CC[C@@](F)(CC1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-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 wild type RET (ProQinase 1090-0000-1) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435008
PNG
(US10584114, Compound 128)
Show SMILES C[C@H](NC(=O)[C@H]1CC[C@@](O)(C[C@H]1C)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-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 wild type RET (ProQinase 1090-0000-1) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435018
PNG
(US10584114, Compound 144)
Show SMILES C[C@H](NC(=O)C1CCC(=CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
PDB

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n/an/a<500n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435024
PNG
(US10584114, Compound 151)
Show SMILES CO[C@@]1(CC[C@@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@H](C)c1ccc(nc1)-n1cc(F)cn1
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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM434996
PNG
(US10584114, Compound 109)
Show SMILES C[C@H](NC(=O)[C@H]1CC[C@@H](CC1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
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 mutant RET (ProQinase 1096-0000-1) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435010
PNG
(US10584114, Compound 130)
Show SMILES CO[C@@]1(CC[C@@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@@H](C)c1ccc(nc1)-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 wild type RET (ProQinase 1090-0000-1) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435021
PNG
(US10584114, Compound 148)
Show SMILES C[C@H](NC(=O)[C@@]1(C)CC[C@@](O)(CO1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
PDB

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n/an/a<500n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435023
PNG
(US10584114, Compound 150)
Show SMILES CO[C@@]1(CC[C@@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)NCc1cnc(cn1)-n1cc(F)cn1
PDB

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n/an/a<500n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM434989
PNG
(US10584114, Compound 101)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)[C@H]2CC[C@@H](CC2)C(=O)NCc2ccc(nc2)-n2cccn2)n[nH]1
PDB

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n/an/a<500n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM434995
PNG
(US10584114, Compound 107)
Show SMILES C[C@@H]1C[C@](O)(CC[C@@H]1C(=O)NCc1ccc(nc1)-n1cccn1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1
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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM434995
PNG
(US10584114, Compound 107)
Show SMILES C[C@@H]1C[C@](O)(CC[C@@H]1C(=O)NCc1ccc(nc1)-n1cccn1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1
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 mutant RET (ProQinase 1096-0000-1) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM434996
PNG
(US10584114, Compound 109)
Show SMILES C[C@H](NC(=O)[C@H]1CC[C@@H](CC1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM434999
PNG
(US10584114, Compound 112)
Show SMILES C[C@H](NC(=O)[C@H]1CC[C@@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
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 mutant RET (ProQinase 1096-0000-1) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435004
PNG
(US10584114, Compound 120)
Show SMILES C[C@H](NC(=O)[C@H]1CC[C@@](O)(CC1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
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 mutant RET (ProQinase 1096-0000-1) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435011
PNG
(US10584114, Compound 131)
Show SMILES CO[C@@]1(CC[C@@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@@H](C)c1cnc(cn1)-n1cc(F)cn1
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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435017
PNG
(US10584114, Compound 142)
Show SMILES CO[C@]1(CC[C@](F)(CC1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@@H](C)c1ccc(nc1)-n1cc(F)cn1
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 mutant RET (ProQinase 1096-0000-1) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM434994
PNG
(US10584114, Compound 106)
Show SMILES Cc1cc(C)n(n1)-c1ccc(CNC(=O)[C@H]2CC[C@@H](CC2)c2nc(C)cc(Nc3cc(C)[nH]n3)n2)cn1
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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435008
PNG
(US10584114, Compound 128)
Show SMILES C[C@H](NC(=O)[C@H]1CC[C@@](O)(C[C@H]1C)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
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 mutant RET (ProQinase 1096-0000-1) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435015
PNG
(US10584114, Compound 138)
Show SMILES CO[C@@]1(CC[C@](O)(CC1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@@H](C)c1ccc(nc1)-n1cc(F)cn1
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 mutant RET (ProQinase 1096-0000-1) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435019
PNG
(US10584114, Compound 146)
Show SMILES C[C@H](NC(=O)[C@@H]1CC[C@](O)(CO1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM434997
PNG
(US10584114, Compound 110)
Show SMILES C[C@H](NC(=O)[C@H]1CC[C@H](CC1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
PDB

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n/an/a 1.25E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435016
PNG
(US10584114, Compound 141)
Show SMILES CO[C@@]1(CC[C@](F)(CC1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@@H](C)c1ccc(nc1)-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 wild type RET (ProQinase 1090-0000-1) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435020
PNG
(US10584114, Compound 147)
Show SMILES C[C@H](NC(=O)[C@]1(C)CC[C@](O)(CO1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
PDB

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n/an/a 1.25E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435002
PNG
(US10584114, Compound 116)
Show SMILES C[C@H](NC(=O)[C@@H]1CC[C@H](C[C@@H]1C)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
PDB

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n/an/a 1.25E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435012
PNG
(US10584114, Compound 135)
Show SMILES C[C@H](NC(=O)[C@@H]1CC[C@](O)(CC1(C)C)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
PDB
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n/an/a 1.25E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM434998
PNG
(US10584114, Compound 111)
Show SMILES C[C@H](NC(=O)[C@H]1CC[C@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
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n/an/a 1.25E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435022
PNG
(US10584114, Compound 149)
Show SMILES CO[C@@]1(CC[C@@H](CC1)c1cc(C)nc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@@H](C)c1ccc(nc1)-n1cc(F)cn1
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n/an/a 1.25E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM434993
PNG
(US10584114, Compound 105)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)[C@H]2CC[C@@H](CC2)C(=O)NCc2ccc(nc2)-n2cc(F)cn2)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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435016
PNG
(US10584114, Compound 141)
Show SMILES CO[C@@]1(CC[C@](F)(CC1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@@H](C)c1ccc(nc1)-n1cc(F)cn1
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n/an/a 1.25E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM434993
PNG
(US10584114, Compound 105)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)[C@H]2CC[C@@H](CC2)C(=O)NCc2ccc(nc2)-n2cc(F)cn2)n[nH]1
PDB

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n/an/a 1.25E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435020
PNG
(US10584114, Compound 147)
Show SMILES C[C@H](NC(=O)[C@]1(C)CC[C@](O)(CO1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM434997
PNG
(US10584114, Compound 110)
Show SMILES C[C@H](NC(=O)[C@H]1CC[C@H](CC1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
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n/an/a 1.25E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435006
PNG
(US10584114, Compound 122)
Show SMILES C[C@H](NC(=O)[C@H]1CC[C@](F)(CC1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
PDB

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n/an/a 1.25E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435006
PNG
(US10584114, Compound 122)
Show SMILES C[C@H](NC(=O)[C@H]1CC[C@](F)(CC1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435022
PNG
(US10584114, Compound 149)
Show SMILES CO[C@@]1(CC[C@@H](CC1)c1cc(C)nc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@@H](C)c1ccc(nc1)-n1cc(F)cn1
PDB

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n/an/a 1.25E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435012
PNG
(US10584114, Compound 135)
Show SMILES C[C@H](NC(=O)[C@@H]1CC[C@](O)(CC1(C)C)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
PDB

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n/an/a 1.25E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435007
PNG
(US10584114, Compound 124)
Show SMILES C[C@H](NC(=O)[C@@H]1CC[C@H](CC1(C)C)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
PDB

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n/an/a 1.25E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM434994
PNG
(US10584114, Compound 106)
Show SMILES Cc1cc(C)n(n1)-c1ccc(CNC(=O)[C@H]2CC[C@@H](CC2)c2nc(C)cc(Nc3cc(C)[nH]n3)n2)cn1
PDB

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n/an/a 1.25E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM21
PNG
(6-[(4R,5S,6S,7R)-4,7-dibenzyl-3-(5-carboxypentyl)-...)
Show SMILES COc1cc2c(Nc3ccc(Br)cc3F)ncnc2cc1OCC1CCN(C)CC1
Show InChI InChI=1S/C22H24BrFN4O2/c1-28-7-5-14(6-8-28)12-30-21-11-19-16(10-20(21)29-2)22(26-13-25-19)27-18-4-3-15(23)9-17(18)24/h3-4,9-11,13-14H,5-8,12H2,1-2H3,(H,25,26,27)
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n/an/a 3.60E+3n/an/an/an/an/an/a



BLUEPRINT MEDICINES CORPORATION

US Patent


Assay Description
In order to assess the activity of chemical compounds against the relevant kinase of interest, the Caliper LifeSciences electrophoretic mobility shif...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM434990
PNG
(US10584114, Compound 102)
Show SMILES C[C@H](NC(=O)[C@H]1CC[C@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cccn1
PDB
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n/an/a 6.00E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435014
PNG
(US10584114, Compound 137)
Show SMILES CO[C@]1(CC[C@](O)(CC1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@@H](C)c1ccc(nc1)-n1cc(F)cn1
PDB
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n/an/a 6.00E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435009
PNG
(US10584114, Compound 129)
Show SMILES CO[C@]1(CC[C@@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@@H](C)c1ccc(nc1)-n1cc(F)cn1
PDB
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n/an/a 6.00E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435003
PNG
(US10584114, Compound 119)
Show SMILES C[C@H](NC(=O)[C@H]1CC[C@](O)(CC1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
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n/an/a 6.00E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435007
PNG
(US10584114, Compound 124)
Show SMILES C[C@H](NC(=O)[C@@H]1CC[C@H](CC1(C)C)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-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 wild type RET (ProQinase 1090-0000-1) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435014
PNG
(US10584114, Compound 137)
Show SMILES CO[C@]1(CC[C@](O)(CC1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@@H](C)c1ccc(nc1)-n1cc(F)cn1
PDB

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n/an/a 6.00E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM434988
PNG
(US10584114, Compound 100)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)[C@@H]2CC[C@@H](CC2)C(=O)NCc2ccc(nc2)-n2cccn2)n[nH]1
PDB

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n/an/a 6.00E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM434992
PNG
(US10584114, Compound 104)
Show SMILES C[C@H]1C[C@@H](CC[C@H]1C(=O)NCc1ccc(nc1)-n1cccn1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1
PDB
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n/an/a 6.00E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM434988
PNG
(US10584114, Compound 100)
Show SMILES Cc1cc(Nc2cc(C)nc(n2)[C@@H]2CC[C@@H](CC2)C(=O)NCc2ccc(nc2)-n2cccn2)n[nH]1
PDB
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n/an/a 6.00E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret


(Homo sapiens (Human))
BDBM435002
PNG
(US10584114, Compound 116)
Show SMILES C[C@H](NC(=O)[C@@H]1CC[C@H](C[C@@H]1C)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
PDB
MMDB

Reactome pathway
KEGG

UniProtKB/SwissProt
UniProtKB/TrEMBL

B.MOAD
DrugBank
antibodypedia
GoogleScholar
UniChem
US Patent
n/an/a 6.00E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HE...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435003
PNG
(US10584114, Compound 119)
Show SMILES C[C@H](NC(=O)[C@H]1CC[C@](O)(CC1)c1cc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cc(F)cn1
PDB

GoogleScholar
UniChem
US Patent
n/an/a 6.00E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM434992
PNG
(US10584114, Compound 104)
Show SMILES C[C@H]1C[C@@H](CC[C@H]1C(=O)NCc1ccc(nc1)-n1cccn1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1
PDB

GoogleScholar
UniChem
US Patent
n/an/a 6.00E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM434990
PNG
(US10584114, Compound 102)
Show SMILES C[C@H](NC(=O)[C@H]1CC[C@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)c1ccc(nc1)-n1cccn1
PDB

GoogleScholar
UniChem
US Patent
n/an/a 6.00E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
RET kinase mutant (V804L)


(Homo sapiens (Human))
BDBM435009
PNG
(US10584114, Compound 129)
Show SMILES CO[C@]1(CC[C@@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@@H](C)c1ccc(nc1)-n1cc(F)cn1
PDB

GoogleScholar
UniChem
US Patent
n/an/a 6.00E+3n/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) was incubated in a total of 12.5 μL of buffer (100 mM HEPES...


US Patent US10584114 (2020)


BindingDB Entry DOI: 10.7270/Q27083V8
More data for this
Ligand-Target Pair
* indicates data uncertainty>20%