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Compile Data Set for Download or QSAR

Found 110 hits of ic50 for UniProtKB: P07949   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kcal/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296812
PNG
(6-ethoxy-4-(5-(6-(3- fluoro-4- methoxybenzyl)-3,6-...)
Show SMILES CCOc1cc(-c2cnc(cn2)N2CC3CC(C2)N3Cc2ccc(OC)c(F)c2)c2c(cnn2c1)C#N
Show InChI InChI=1S/C27H26FN7O2/c1-3-37-21-8-22(27-18(9-29)10-32-35(27)16-21)24-11-31-26(12-30-24)33-14-19-7-20(15-33)34(19)13-17-4-5-25(36-2)23(28)6-17/h4-6,8,10-12,16,19-20H,3,7,13-15H2,1-2H3
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US Patent
n/an/a 39n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296735
PNG
(US10112942, Example 470 | US10137124, Example 470 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OCCn3ccnc3)cn3ncc(C#N)c23)cn1
Show InChI InChI=1S/C30H29N9O2/c1-40-29-5-2-21(13-34-29)16-38-24-10-25(38)18-37(17-24)28-4-3-22(14-33-28)27-11-26(41-9-8-36-7-6-32-20-36)19-39-30(27)23(12-31)15-35-39/h2-7,11,13-15,19-20,24-25H,8-10,16-18H2,1H3
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UniProtKB/SwissProt

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UniChem
US Patent
n/an/a 41n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296716
PNG
(US10112942, Example 451 | US10137124, Example 451 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OCC3(F)CNC3)cn3ncc(C#N)c23)cn1
Show InChI InChI=1S/C29H29FN8O2/c1-39-27-5-2-19(9-34-27)12-37-22-6-23(37)14-36(13-22)26-4-3-20(10-33-26)25-7-24(40-18-29(30)16-32-17-29)15-38-28(25)21(8-31)11-35-38/h2-5,7,9-11,15,22-23,32H,6,12-14,16-18H2,1H3
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n/an/a 52.4n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296381
PNG
(US10112942, Example 115 | US10137124, Example 115 ...)
Show SMILES CC(C)OC(=O)N1CC2(C1)CCN(CC2)c1ccc(cn1)-c1cc(OCCO)cn2ncc(C#N)c12
Show InChI InChI=1S/C26H30N6O4/c1-18(2)36-25(34)31-16-26(17-31)5-7-30(8-6-26)23-4-3-19(13-28-23)22-11-21(35-10-9-33)15-32-24(22)20(12-27)14-29-32/h3-4,11,13-15,18,33H,5-10,16-17H2,1-2H3
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US Patent
n/an/a 54.3n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM430529
PNG
(US10555944, Example 261 | US10953005, Example 261)
Show SMILES CCOc1cc(-c2ccc(nc2)N2CC3CC(C2)N3C(=O)[C@H](N(C)C)c2cccc(Cl)c2)c2c(cnn2c1)C#N |r|
Show InChI InChI=1S/C30H30ClN7O2/c1-4-40-25-12-26(28-21(13-32)15-34-37(28)18-25)20-8-9-27(33-14-20)36-16-23-11-24(17-36)38(23)30(39)29(35(2)3)19-6-5-7-22(31)10-19/h5-10,12,14-15,18,23-24,29H,4,11,16-17H2,1-3H3/t23?,24?,29-/m1/s1
PDB

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n/an/a 58.7n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296809
PNG
(US10112942, Example 544 | US10137124, Example 544 ...)
Show SMILES CCOc1cc(-c2cnc(cn2)N2CC3CC(C2)N3Cc2cnc(OC)c(F)c2)c2c(cnn2c1)C#N
Show InChI InChI=1S/C26H25FN8O2/c1-3-37-20-6-21(25-17(7-28)9-32-35(25)15-20)23-10-30-24(11-29-23)33-13-18-5-19(14-33)34(18)12-16-4-22(27)26(36-2)31-8-16/h4,6,8-11,15,18-19H,3,5,12-14H2,1-2H3
PDB

UniProtKB/SwissProt

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PC sid
UniChem
US Patent
n/an/a 65n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296709
PNG
(US10112942, Example 444 | US10137124, Example 444 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OCCC3CCN(C)CC3)cn3ncc(C#N)c23)cn1
Show InChI InChI=1S/C33H38N8O2/c1-38-10-7-23(8-11-38)9-12-43-29-14-30(33-26(15-34)18-37-41(33)22-29)25-4-5-31(35-17-25)39-20-27-13-28(21-39)40(27)19-24-3-6-32(42-2)36-16-24/h3-6,14,16-18,22-23,27-28H,7-13,19-21H2,1-2H3
PDB

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US Patent
n/an/a 68.5n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296772
PNG
(US10112942, Example 507 | US10137124, Example 507 ...)
Show SMILES CCOc1cc(-c2ccc(nc2)N2C[C@@H]3C[C@H]2CN3c2ccc(OC)nc2)c2c(cnn2c1)C#N |r|
Show InChI InChI=1S/C26H25N7O2/c1-3-35-22-9-23(26-18(10-27)12-30-33(26)16-22)17-4-6-24(28-11-17)32-15-20-8-21(32)14-31(20)19-5-7-25(34-2)29-13-19/h4-7,9,11-13,16,20-21H,3,8,14-15H2,1-2H3/t20-,21-/m0/s1
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n/an/a 79n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296521
PNG
(US10112942, Example 255 | US10137124, Example 255 ...)
Show SMILES CCOc1cc(-c2ccc(nc2)N2CCN(CC2)C(=O)C(N)c2ccc(F)cc2)c2c(cnn2c1)C#N
Show InChI InChI=1S/C27H26FN7O2/c1-2-37-22-13-23(26-20(14-29)16-32-35(26)17-22)19-5-8-24(31-15-19)33-9-11-34(12-10-33)27(36)25(30)18-3-6-21(28)7-4-18/h3-8,13,15-17,25H,2,9-12,30H2,1H3
PDB

UniProtKB/SwissProt

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US Patent
n/an/a 80.1n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296727
PNG
(US10112942, Example 462 | US10137124, Example 462 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OCCC3CN(C)C3)cn3ncc(C#N)c23)cn1
Show InChI InChI=1S/C31H34N8O2/c1-36-15-22(16-36)7-8-41-27-10-28(31-24(11-32)14-35-39(31)20-27)23-4-5-29(33-13-23)37-18-25-9-26(19-37)38(25)17-21-3-6-30(40-2)34-12-21/h3-6,10,12-14,20,22,25-26H,7-9,15-19H2,1-2H3
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US Patent
n/an/a 84.8n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296376
PNG
(US10112942, Example 110 | US10137124, Example 110 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OCCO)cn3ncc(C#N)c23)cn1
Show InChI InChI=1S/C27H27N7O3/c1-36-26-5-2-18(11-30-26)14-33-21-8-22(33)16-32(15-21)25-4-3-19(12-29-25)24-9-23(37-7-6-35)17-34-27(24)20(10-28)13-31-34/h2-5,9,11-13,17,21-22,35H,6-8,14-16H2,1H3
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n/an/a 90n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296707
PNG
(US10112942, Example 442 | US10137124, Example 442 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OCC3CCN(C)CC3)cn3ncc(C#N)c23)cn1
Show InChI InChI=1S/C32H36N8O2/c1-37-9-7-22(8-10-37)21-42-28-12-29(32-25(13-33)16-36-40(32)20-28)24-4-5-30(34-15-24)38-18-26-11-27(19-38)39(26)17-23-3-6-31(41-2)35-14-23/h3-6,12,14-16,20,22,26-27H,7-11,17-19,21H2,1-2H3
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n/an/a 101n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296817
PNG
(US10112942, Example 552 | US10137124, Example 552 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2cnc(cn2)-c2cc(OC[C@H]3CNCCO3)cn3ncc(C#N)c23)cn1 |r|
Show InChI InChI=1S/C29H31N9O3/c1-39-28-3-2-19(9-34-28)14-37-21-6-22(37)16-36(15-21)27-13-32-26(12-33-27)25-7-23(41-18-24-11-31-4-5-40-24)17-38-29(25)20(8-30)10-35-38/h2-3,7,9-10,12-13,17,21-22,24,31H,4-6,11,14-16,18H2,1H3/t21?,22?,24-/m1/s1
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PC sid
UniChem
US Patent
n/an/a 101n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296808
PNG
(US10112942, Example 543 | US10112942, Example 546 ...)
Show SMILES CCOc1cc(-c2cnc(cn2)N2CC3CC(C2)N3Cc2ccc(OC)nc2)c2c(cnn2c1)C#N
Show InChI InChI=1S/C26H26N8O2/c1-3-36-21-7-22(26-18(8-27)10-31-34(26)16-21)23-11-29-24(12-28-23)32-14-19-6-20(15-32)33(19)13-17-4-5-25(35-2)30-9-17/h4-5,7,9-12,16,19-20H,3,6,13-15H2,1-2H3
PDB

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US Patent
n/an/a 102n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296520
PNG
(US10112942, Example 254 | US10137124, Example 254 ...)
Show SMILES CCOc1cc(-c2ccc(nc2)N2CCN(CC2)C(=O)[C@H](N)c2cccc(Cl)c2)c2c(cnn2c1)C#N |r|
Show InChI InChI=1S/C27H26ClN7O2/c1-2-37-22-13-23(26-20(14-29)16-32-35(26)17-22)19-6-7-24(31-15-19)33-8-10-34(11-9-33)27(36)25(30)18-4-3-5-21(28)12-18/h3-7,12-13,15-17,25H,2,8-11,30H2,1H3/t25-/m1/s1
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n/an/a 104n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296703
PNG
(US10112942, Example 438 | US10137124, Example 438 ...)
Show SMILES COc1ncc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OCCN3CCOCC3)cn3ncc(C#N)c23)cc1Cl
Show InChI InChI=1S/C31H33ClN8O3/c1-41-31-28(32)10-21(14-35-31)17-39-24-11-25(39)19-38(18-24)29-3-2-22(15-34-29)27-12-26(20-40-30(27)23(13-33)16-36-40)43-9-6-37-4-7-42-8-5-37/h2-3,10,12,14-16,20,24-25H,4-9,11,17-19H2,1H3
PDB

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US Patent
n/an/a 105n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296715
PNG
(US10112942, Example 450 | US10137124, Example 450 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OCC3CN(C3)C(C)=O)cn3ncc(C#N)c23)cn1
Show InChI InChI=1S/C31H32N8O3/c1-20(40)36-13-22(14-36)19-42-27-8-28(31-24(9-32)12-35-39(31)18-27)23-4-5-29(33-11-23)37-16-25-7-26(17-37)38(25)15-21-3-6-30(41-2)34-10-21/h3-6,8,10-12,18,22,25-26H,7,13-17,19H2,1-2H3
PDB

UniProtKB/SwissProt

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PC sid
UniChem
US Patent
n/an/a 113n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296711
PNG
(US10112942, Example 446 | US10137124, Example 446 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OCCN3CCCC3)cn3ncc(C#N)c23)cn1
Show InChI InChI=1S/C31H34N8O2/c1-40-30-7-4-22(15-34-30)18-38-25-12-26(38)20-37(19-25)29-6-5-23(16-33-29)28-13-27(41-11-10-36-8-2-3-9-36)21-39-31(28)24(14-32)17-35-39/h4-7,13,15-17,21,25-26H,2-3,8-12,18-20H2,1H3
PDB

UniProtKB/SwissProt

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PC sid
UniChem
US Patent
n/an/a 120n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296724
PNG
(US10112942, Example 459 | US10137124, Example 459 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OC3C[C@H](O)C3)cn3ncc(C#N)c23)cn1 |r,wU:26.29,(12.54,-2.37,;11.21,-1.6,;9.87,-2.37,;8.54,-1.6,;7.21,-2.37,;7.21,-3.91,;5.87,-4.68,;4.54,-3.91,;3.21,-4.68,;3.21,-3.14,;4.54,-2.37,;3.21,-1.6,;1.87,-2.37,;1.87,-3.91,;.54,-1.6,;-.8,-2.37,;-2.13,-1.6,;-2.13,-.06,;-.8,.71,;.54,-.06,;-3.46,.71,;-4.8,-.06,;-6.13,.71,;-7.46,-.06,;-8.95,.33,;-9.72,1.67,;-11.05,.9,;-12.54,1.3,;-10.28,-.44,;-6.13,2.25,;-4.8,3.02,;-4.48,4.52,;-2.94,4.68,;-2.32,3.28,;-.83,2.88,;.66,2.48,;-3.46,2.25,;8.54,-4.68,;9.87,-3.91,)|
Show InChI InChI=1S/C29H29N7O3/c1-38-28-5-2-18(11-32-28)14-35-21-6-22(35)16-34(15-21)27-4-3-19(12-31-27)26-9-25(39-24-7-23(37)8-24)17-36-29(26)20(10-30)13-33-36/h2-5,9,11-13,17,21-24,37H,6-8,14-16H2,1H3/t21?,22?,23-,24?
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296704
PNG
(US10112942, Example 439 | US10137124, Example 439 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OCCN3CCOCC3)cn3ncc(C#N)c23)cn1
Show InChI InChI=1S/C31H34N8O3/c1-40-30-5-2-22(15-34-30)18-38-25-12-26(38)20-37(19-25)29-4-3-23(16-33-29)28-13-27(21-39-31(28)24(14-32)17-35-39)42-11-8-36-6-9-41-10-7-36/h2-5,13,15-17,21,25-26H,6-12,18-20H2,1H3
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296773
PNG
(US10112942, Example 508 | US10137124, Example 508 ...)
Show SMILES CCOc1cc(-c2ccc(nc2)N2CCC3(CN3S(=O)(=O)c3ccc(C)cc3)CC2)c2c(cnn2c1)C#N
Show InChI InChI=1S/C28H28N6O3S/c1-3-37-23-14-25(27-22(15-29)17-31-33(27)18-23)21-6-9-26(30-16-21)32-12-10-28(11-13-32)19-34(28)38(35,36)24-7-4-20(2)5-8-24/h4-9,14,16-18H,3,10-13,19H2,1-2H3
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296774
PNG
(US10112942, Example 509 | US10137124, Example 509 ...)
Show SMILES CCOc1cc(-c2ccc(nc2)N2CCC3(CN3S(=O)(=O)c3ccccc3)CC2)c2c(cnn2c1)C#N
Show InChI InChI=1S/C27H26N6O3S/c1-2-36-22-14-24(26-21(15-28)17-30-32(26)18-22)20-8-9-25(29-16-20)31-12-10-27(11-13-31)19-33(27)37(34,35)23-6-4-3-5-7-23/h3-9,14,16-18H,2,10-13,19H2,1H3
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296821
PNG
(US10112942, Example 556 | US10137124, Example 556 ...)
Show SMILES COc1cc(-c2cnc(cn2)N2CC3CC(C2)N3Cc2ccc(OC)nc2)c2c(Cl)cnn2c1
Show InChI InChI=1S/C24H24ClN7O2/c1-33-18-6-19(24-20(25)8-29-32(24)14-18)21-9-27-22(10-26-21)30-12-16-5-17(13-30)31(16)11-15-3-4-23(34-2)28-7-15/h3-4,6-10,14,16-17H,5,11-13H2,1-2H3
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296818
PNG
(US10112942, Example 553 | US10137124, Example 553 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2cnc(cn2)-c2cc(OCC3(F)CNC3)cn3ncc(C#N)c23)cn1
Show InChI InChI=1S/C28H28FN9O2/c1-39-26-3-2-18(7-34-26)11-37-20-4-21(37)13-36(12-20)25-10-32-24(9-33-25)23-5-22(40-17-28(29)15-31-16-28)14-38-27(23)19(6-30)8-35-38/h2-3,5,7-10,14,20-21,31H,4,11-13,15-17H2,1H3
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296748
PNG
(US10112942, Example 483 | US10137124, Example 483 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OC[C@H](O)CN(C)C)cn3ncc(C#N)c23)cn1 |r|
Show InChI InChI=1S/C30H34N8O3/c1-35(2)17-25(39)19-41-26-9-27(30-22(10-31)13-34-38(30)18-26)21-5-6-28(32-12-21)36-15-23-8-24(16-36)37(23)14-20-4-7-29(40-3)33-11-20/h4-7,9,11-13,18,23-25,39H,8,14-17,19H2,1-3H3/t23?,24?,25-/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296736
PNG
(US10112942, Example 471 | US10137124, Example 471 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OCc3cccnc3)cn3ncc(C#N)c23)cn1
Show InChI InChI=1S/C31H28N8O2/c1-40-30-7-4-21(13-35-30)16-38-25-9-26(38)18-37(17-25)29-6-5-23(14-34-29)28-10-27(41-20-22-3-2-8-33-12-22)19-39-31(28)24(11-32)15-36-39/h2-8,10,12-15,19,25-26H,9,16-18,20H2,1H3
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296241
PNG
(US10112942, Example 48 | US10137124, Example 48 | ...)
Show SMILES CCOc1cc(-c2ccc(nc2)N2CC3CC(C2)N3Cc2ccc(OC)nc2)c2c(cnn2c1)C#N
Show InChI InChI=1S/C27H27N7O2/c1-3-36-23-9-24(27-20(10-28)13-31-34(27)17-23)19-5-6-25(29-12-19)32-15-21-8-22(16-32)33(21)14-18-4-7-26(35-2)30-11-18/h4-7,9,11-13,17,21-22H,3,8,14-16H2,1-2H3
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296775
PNG
(6-ethoxy-4-(6-(1-((4- fluorophenyl) sulfonyl)-1,6-...)
Show SMILES CCOc1cc(-c2ccc(nc2)N2CCC3(CN3S(=O)(=O)c3ccc(F)cc3)CC2)c2c(cnn2c1)C#N
Show InChI InChI=1S/C27H25FN6O3S/c1-2-37-22-13-24(26-20(14-29)16-31-33(26)17-22)19-3-8-25(30-15-19)32-11-9-27(10-12-32)18-34(27)38(35,36)23-6-4-21(28)5-7-23/h3-8,13,15-17H,2,9-12,18H2,1H3
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296195
PNG
(US10112942, Example 2 | US10137124, Example 2 | US...)
Show SMILES COc1cc(-c2ccc(nc2)N2CCN(Cc3ccccc3)CC2)c2c(cnn2c1)C#N
Show InChI InChI=1S/C25H24N6O/c1-32-22-13-23(25-21(14-26)16-28-31(25)18-22)20-7-8-24(27-15-20)30-11-9-29(10-12-30)17-19-5-3-2-4-6-19/h2-8,13,15-16,18H,9-12,17H2,1H3
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296743
PNG
(US10112942, Example 478 | US10137124, Example 478 ...)
Show SMILES COc1ncc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OC[C@H](C)O)cn3ncc(C#N)c23)cc1F |r|
Show InChI InChI=1S/C28H28FN7O3/c1-17(37)16-39-23-7-24(27-20(8-30)11-33-36(27)15-23)19-3-4-26(31-10-19)34-13-21-6-22(14-34)35(21)12-18-5-25(29)28(38-2)32-9-18/h3-5,7,9-11,15,17,21-22,37H,6,12-14,16H2,1-2H3/t17-,21?,22?/m0/s1
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296725
PNG
(US10112942, Example 460 | US10137124, Example 460 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OC[C@@H]3C[C@H](O)C3)cn3ncc(C#N)c23)cn1 |r,wU:25.27,27.30,(12.95,-2.37,;11.61,-1.6,;10.28,-2.37,;8.94,-1.6,;7.61,-2.37,;7.61,-3.91,;6.28,-4.68,;4.94,-3.91,;3.61,-4.68,;3.61,-3.14,;4.94,-2.37,;3.61,-1.6,;2.28,-2.37,;2.28,-3.91,;.94,-1.6,;-.39,-2.37,;-1.72,-1.6,;-1.72,-.06,;-.39,.71,;.94,-.06,;-3.06,.71,;-4.39,-.06,;-5.72,.71,;-7.06,-.06,;-8.39,.71,;-9.73,-.06,;-11.21,.34,;-11.61,-1.15,;-12.95,-1.92,;-10.12,-1.55,;-5.72,2.25,;-4.39,3.02,;-4.07,4.52,;-2.54,4.68,;-1.91,3.28,;-.43,2.88,;1.06,2.48,;-3.06,2.25,;8.94,-4.68,;10.28,-3.91,)|
Show InChI InChI=1S/C30H31N7O3/c1-39-29-5-2-19(11-33-29)14-36-23-8-24(36)16-35(15-23)28-4-3-21(12-32-28)27-9-26(40-18-20-6-25(38)7-20)17-37-30(27)22(10-31)13-34-37/h2-5,9,11-13,17,20,23-25,38H,6-8,14-16,18H2,1H3/t20-,23?,24?,25+
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296712
PNG
(US10112942, Example 447 | US10137124, Example 447 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OCCN3CCCC3=O)cn3ncc(C#N)c23)cn1
Show InChI InChI=1S/C31H32N8O3/c1-41-29-7-4-21(14-34-29)17-38-24-11-25(38)19-37(18-24)28-6-5-22(15-33-28)27-12-26(20-39-31(27)23(13-32)16-35-39)42-10-9-36-8-2-3-30(36)40/h4-7,12,14-16,20,24-25H,2-3,8-11,17-19H2,1H3
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296807
PNG
(US10112942, Example 542 | US10137124, Example 542 ...)
Show SMILES CCOc1cc(-c2cnc(cn2)N2CCN(CC2)C(=O)[C@H](O)c2cccc(Cl)c2)c2c(cnn2c1)C#N |r|
Show InChI InChI=1S/C26H24ClN7O3/c1-2-37-20-11-21(24-18(12-28)13-31-34(24)16-20)22-14-30-23(15-29-22)32-6-8-33(9-7-32)26(36)25(35)17-4-3-5-19(27)10-17/h3-5,10-11,13-16,25,35H,2,6-9H2,1H3/t25-/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296744
PNG
(US10112942, Example 479 | US10137124, Example 479 ...)
Show SMILES COc1ncc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OC[C@H](C)O)cn3ncc(C#N)c23)cc1Cl |r|
Show InChI InChI=1S/C28H28ClN7O3/c1-17(37)16-39-23-7-24(27-20(8-30)11-33-36(27)15-23)19-3-4-26(31-10-19)34-13-21-6-22(14-34)35(21)12-18-5-25(29)28(38-2)32-9-18/h3-5,7,9-11,15,17,21-22,37H,6,12-14,16H2,1-2H3/t17-,21?,22?/m0/s1
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296698
PNG
(US10112942, Example 433 | US10137124, Example 433 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OC[C@@H]3CNCCO3)cn3ncc(C#N)c23)cn1 |r|
Show InChI InChI=1S/C30H32N8O3/c1-39-29-5-2-20(11-34-29)15-37-23-8-24(37)17-36(16-23)28-4-3-21(12-33-28)27-9-25(41-19-26-14-32-6-7-40-26)18-38-30(27)22(10-31)13-35-38/h2-5,9,11-13,18,23-24,26,32H,6-8,14-17,19H2,1H3/t23?,24?,26-/m0/s1
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296740
PNG
(US10112942, Example 475 | US10137124, Example 475 ...)
Show SMILES COc1ncc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OC[C@@H](C)O)cn3ncc(C#N)c23)cc1F |r|
Show InChI InChI=1S/C28H28FN7O3/c1-17(37)16-39-23-7-24(27-20(8-30)11-33-36(27)15-23)19-3-4-26(31-10-19)34-13-21-6-22(14-34)35(21)12-18-5-25(29)28(38-2)32-9-18/h3-5,7,9-11,15,17,21-22,37H,6,12-14,16H2,1-2H3/t17-,21?,22?/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296214
PNG
(US10112942, Example 21 | US10137124, Example 21 | ...)
Show SMILES CN1CCN(CCOc2cc(-c3ccc(nc3)N3CCN(Cc4ccccc4)CC3)c3c(cnn3c2)C#N)CC1
Show InChI InChI=1S/C31H36N8O/c1-35-9-11-36(12-10-35)17-18-40-28-19-29(31-27(20-32)22-34-39(31)24-28)26-7-8-30(33-21-26)38-15-13-37(14-16-38)23-25-5-3-2-4-6-25/h2-8,19,21-22,24H,9-18,23H2,1H3
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296702
PNG
(US10112942, Example 437 | US10137124, Example 437 ...)
Show SMILES COc1ncc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OCCN3CCOCC3)cn3ncc(C#N)c23)cc1C
Show InChI InChI=1S/C32H36N8O3/c1-22-11-23(15-35-32(22)41-2)18-39-26-12-27(39)20-38(19-26)30-4-3-24(16-34-30)29-13-28(21-40-31(29)25(14-33)17-36-40)43-10-7-37-5-8-42-9-6-37/h3-4,11,13,15-17,21,26-27H,5-10,12,18-20H2,1-2H3
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296717
PNG
(US10112942, Example 452 | US10137124, Example 452 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OCC3(F)CN(C)C3)cn3ncc(C#N)c23)cn1
Show InChI InChI=1S/C30H31FN8O2/c1-36-17-30(31,18-36)19-41-25-8-26(29-22(9-32)12-35-39(29)16-25)21-4-5-27(33-11-21)37-14-23-7-24(15-37)38(23)13-20-3-6-28(40-2)34-10-20/h3-6,8,10-12,16,23-24H,7,13-15,17-19H2,1-2H3
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM303768
PNG
(6-ethoxy-4-(5-(6-((6- ethylpyridin-3- yl)methyl)-3...)
Show SMILES CCOc1cc(-c2cnc(cn2)N2CC3CC(C2)N3Cc2ccc(CC)nc2)c2c(cnn2c1)C#N
Show InChI InChI=1S/C27H28N8O/c1-3-20-6-5-18(10-29-20)14-34-21-7-22(34)16-33(15-21)26-13-30-25(12-31-26)24-8-23(36-4-2)17-35-27(24)19(9-28)11-32-35/h5-6,8,10-13,17,21-22H,3-4,7,14-16H2,1-2H3
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296824
PNG
(6-ethoxy-4-(5-(6-((6- methoxy-5- methylpyridin-3- ...)
Show SMILES CCOc1cc(-c2cnc(cn2)N2CC3CC(C2)N3Cc2cnc(OC)c(C)c2)c2c(cnn2c1)C#N
Show InChI InChI=1S/C27H28N8O2/c1-4-37-22-7-23(26-19(8-28)10-32-35(26)16-22)24-11-30-25(12-29-24)33-14-20-6-21(15-33)34(20)13-18-5-17(2)27(36-3)31-9-18/h5,7,9-12,16,20-21H,4,6,13-15H2,1-3H3
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296816
PNG
(US10112942, Example 551 | US10137124, Example 551 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2cnc(cn2)-c2cc(OC[C@@H]3CNCCO3)cn3ncc(C#N)c23)cn1 |r|
Show InChI InChI=1S/C29H31N9O3/c1-39-28-3-2-19(9-34-28)14-37-21-6-22(37)16-36(15-21)27-13-32-26(12-33-27)25-7-23(41-18-24-11-31-4-5-40-24)17-38-29(25)20(8-30)10-35-38/h2-3,7,9-10,12-13,17,21-22,24,31H,4-6,11,14-16,18H2,1H3/t21?,22?,24-/m0/s1
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296701
PNG
(US10112942, Example 436 | US10137124, Example 436 ...)
Show SMILES COc1ccc(cn1)C(=O)N1C2CC1CN(C2)c1ccc(cn1)-c1cc(OCCN2CCOCC2)cn2ncc(C#N)c12
Show InChI InChI=1S/C31H32N8O4/c1-41-29-5-3-22(16-34-29)31(40)39-24-12-25(39)19-37(18-24)28-4-2-21(15-33-28)27-13-26(20-38-30(27)23(14-32)17-35-38)43-11-8-36-6-9-42-10-7-36/h2-5,13,15-17,20,24-25H,6-12,18-19H2,1H3
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296813
PNG
(6-ethoxy-4-(5-(6-((5- methoxypyridin-2- yl)methyl)...)
Show SMILES CCOc1cc(-c2cnc(cn2)N2CC3CC(C2)N3Cc2ccc(OC)cn2)c2c(cnn2c1)C#N
Show InChI InChI=1S/C26H26N8O2/c1-3-36-22-7-23(26-17(8-27)9-31-34(26)16-22)24-11-30-25(12-29-24)32-14-19-6-20(15-32)33(19)13-18-4-5-21(35-2)10-28-18/h4-5,7,9-12,16,19-20H,3,6,13-15H2,1-2H3
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296777
PNG
(6-ethoxy-4-(6-(1-((4- methoxyphenyl) sulfonyl)-1,6...)
Show SMILES CCOc1cc(-c2ccc(nc2)N2CCC3(CN3S(=O)(=O)c3ccc(OC)cc3)CC2)c2c(cnn2c1)C#N
Show InChI InChI=1S/C28H28N6O4S/c1-3-38-23-14-25(27-21(15-29)17-31-33(27)18-23)20-4-9-26(30-16-20)32-12-10-28(11-13-32)19-34(28)39(35,36)24-7-5-22(37-2)6-8-24/h4-9,14,16-18H,3,10-13,19H2,1-2H3
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296402
PNG
(US10112942, Example 136 | US10137124, Example 136 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OC[C@H](C)O)cn3ncc(C#N)c23)cn1 |r|
Show InChI InChI=1S/C28H29N7O3/c1-18(36)17-38-24-8-25(28-21(9-29)12-32-35(28)16-24)20-4-5-26(30-11-20)33-14-22-7-23(15-33)34(22)13-19-3-6-27(37-2)31-10-19/h3-6,8,10-12,16,18,22-23,36H,7,13-15,17H2,1-2H3/t18-,22?,23?/m0/s1
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296714
PNG
(US10112942, Example 449 | US10137124, Example 449 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OCC3CN(C)C3)cn3ncc(C#N)c23)cn1
Show InChI InChI=1S/C30H32N8O2/c1-35-13-21(14-35)19-40-26-8-27(30-23(9-31)12-34-38(30)18-26)22-4-5-28(32-11-22)36-16-24-7-25(17-36)37(24)15-20-3-6-29(39-2)33-10-20/h3-6,8,10-12,18,21,24-25H,7,13-17,19H2,1-2H3
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296815
PNG
(US10112942, Example 550 | US10137124, Example 550 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2cnc(cn2)-c2cc(OCCN3CCOCC3)cn3ncc(C#N)c23)cn1
Show InChI InChI=1S/C30H33N9O3/c1-40-29-3-2-21(13-34-29)17-38-23-10-24(38)19-37(18-23)28-16-32-27(15-33-28)26-11-25(20-39-30(26)22(12-31)14-35-39)42-9-6-36-4-7-41-8-5-36/h2-3,11,13-16,20,23-24H,4-10,17-19H2,1H3
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM296788
PNG
(US10112942, Example 523 | US10137124, Example 523 ...)
Show SMILES CCOc1cc(-c2ccc(nc2)N2CC[C@@]3(C2)CCCNC3)c2c(cnn2c1)C#N |r|
Show InChI InChI=1S/C23H26N6O/c1-2-30-19-10-20(22-18(11-24)13-27-29(22)14-19)17-4-5-21(26-12-17)28-9-7-23(16-28)6-3-8-25-15-23/h4-5,10,12-14,25H,2-3,6-9,15-16H2,1H3/t23-/m0/s1
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]


(Homo sapiens (Human))
BDBM303406
PNG
(US10137124, Example 183 | US10172851, Example 183 ...)
Show SMILES COc1ccc(CN2C3CC2CN(C3)c2ccc(cc2)-c2cc(OCC(C)(C)O)cn3ncc(C#N)c23)cn1
Show InChI InChI=1S/C30H32N6O3/c1-30(2,37)19-39-26-11-27(29-22(12-31)14-33-36(29)18-26)21-5-7-23(8-6-21)34-16-24-10-25(17-34)35(24)15-20-4-9-28(38-3)32-13-20/h4-9,11,13-14,18,24-25,37H,10,15-17,19H2,1-3H3
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Eli Lilly and Company

US Patent


Assay Description
The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...


US Patent US10555944 (2020)


BindingDB Entry DOI: 10.7270/Q279473N
More data for this
Ligand-Target Pair
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