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Patent code US11066414

Compile Data Set for Download or QSAR

Found 981 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
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505527
PNG
(6-(((S)-(1-(($#8226; R,5S,6s)-3- azabicyclo[3.1 0]...)
Show SMILES CC[C@@H](Nc1c(cnc2c(Cl)cc(N[C@H](C3=CN(NN3)C3[C@H]4CNC[C@@H]34)c3cccnc3)cc12)C#N)c1ccccc1
Show InChI InChI=1S/C32H32ClN9/c1-2-27(19-7-4-3-5-8-19)39-29-21(13-34)15-37-31-23(29)11-22(12-26(31)33)38-30(20-9-6-10-35-14-20)28-18-42(41-40-28)32-24-16-36-17-25(24)32/h3-12,14-15,18,24-25,27,30,32,36,38,40-41H,2,16-17H2,1H3,(H,37,39)/t24-,25+,27-,30+,32?/m1/s1
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n/an/a 1n/an/an/an/an/an/a



Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505589
PNG
(6-(((SHHl-(tert-butyl)piperidin-4-yl)- 1H-1,2,3-tr...)
Show SMILES C[C@@H](Nc1c(cnc2c(Cl)cc(N[C@H](C3=CN(NN3)C3CCN(CC3)C(C)(C)C)c3csc4CN(CCc34)C3COC3)cc12)C#N)c1ccccc1
Show InChI InChI=1S/C40H48ClN9OS/c1-25(26-8-6-5-7-9-26)44-37-27(18-42)19-43-38-32(37)16-28(17-34(38)41)45-39(33-24-52-36-21-48(13-12-31(33)36)30-22-51-23-30)35-20-50(47-46-35)29-10-14-49(15-11-29)40(2,3)4/h5-9,16-17,19-20,24-25,29-30,39,45-47H,10-15,21-23H2,1-4H3,(H,43,44)/t25-,39+/m1/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505779
PNG
(6-(((S)-(1-cyclopropyl-1H-1,2,3-triazol-4- yl)(iso...)
Show SMILES CC[C@@H](Nc1c(cnc2c(Cl)cc(N[C@H](C3=CN(NN3)C3CC3)c3cccc4CNCc34)cc12)C#N)c1ccccc1
Show InChI InChI=1S/C33H33ClN8/c1-2-29(20-7-4-3-5-8-20)39-31-22(15-35)17-37-32-26(31)13-23(14-28(32)34)38-33(30-19-42(41-40-30)24-11-12-24)25-10-6-9-21-16-36-18-27(21)25/h3-10,13-14,17,19,24,29,33,36,38,40-41H,2,11-12,16,18H2,1H3,(H,37,39)/t29-,33+/m1/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505784
PNG
((S)-6-(((1-cyclopropyl-1H-1,2,3-triazol- 4-yl)(6-(...)
Show SMILES CC(C)(C)CNc1c(cnc2c(cc(N[C@H](C3=CN(NN3)C3CC3)c3csc4CN(CCc34)C3COC3)cc12)C#N)C#N
Show InChI InChI=1S/C32H37N9OS/c1-32(2,3)18-36-30-20(11-34)12-35-29-19(10-33)8-21(9-25(29)30)37-31(27-13-41(39-38-27)22-4-5-22)26-17-43-28-14-40(7-6-24(26)28)23-15-42-16-23/h8-9,12-13,17,22-23,31,37-39H,4-7,14-16,18H2,1-3H3,(H,35,36)/t31-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM506026
PNG
(6-(((SMM[1,1'-bi(cyclopropan)]- 1-yl)-1H-1,2,3- tr...)
Show SMILES Cc1nc(F)ccc1[C@H](Nc1cc(C#N)c2ncc(C#N)c(NC3CCOCC3(C)C)c2c1)C1=CN(NN1)C1(CC1)C1CC1
Show InChI InChI=1S/C33H36FN9O/c1-19-24(6-7-28(34)38-19)31(26-17-43(42-41-26)33(9-10-33)22-4-5-22)39-23-12-20(14-35)29-25(13-23)30(21(15-36)16-37-29)40-27-8-11-44-18-32(27,2)3/h6-7,12-13,16-17,22,27,31,39,41-42H,4-5,8-11,18H2,1-3H3,(H,37,40)/t27?,31-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505404
PNG
((S)-6-((benzo[d]thiazol-7-yl(1-(1- cyanocyclopropy...)
Show SMILES CC(C)(C)CNc1c(cnc2c(cc(N[C@H](C3=CN(NN3)C3(CC3)C#N)c3cccc4ncsc34)cc12)C#N)C#N
Show InChI InChI=1S/C30H28N10S/c1-29(2,3)16-35-26-19(12-32)13-34-25-18(11-31)9-20(10-22(25)26)37-27(21-5-4-6-23-28(21)41-17-36-23)24-14-40(39-38-24)30(15-33)7-8-30/h4-6,9-10,13-14,17,27,37-39H,7-8,16H2,1-3H3,(H,34,35)/t27-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505700
PNG
((S)-8-chloro-4-((3-chloro-4- fluorophenyl)amino)-6...)
Show SMILES CCN1CCC(CC1)N1NNC(=C1)[C@@H](Nc1cc(Cl)c2ncc(C#N)c(Nc3ccc(F)c(Cl)c3)c2c1)c1cccnc1
Show InChI InChI=1S/C31H30Cl2FN9/c1-2-42-10-7-23(8-11-42)43-18-28(40-41-43)30(19-4-3-9-36-16-19)39-22-12-24-29(38-21-5-6-27(34)25(32)13-21)20(15-35)17-37-31(24)26(33)14-22/h3-6,9,12-14,16-18,23,30,39-41H,2,7-8,10-11H2,1H3,(H,37,38)/t30-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505759
PNG
((S)-1-(4-(benzo[d]thiazol-7-yl((8- bromo-3-cyano-4...)
Show SMILES CC(C)(C)CNc1c(cnc2c(Br)cc(N[C@H](C3=CN(NN3)C3(CC3)C(N)=O)c3cccc4ncsc34)cc12)C#N
Show InChI InChI=1S/C29H30BrN9OS/c1-28(2,3)14-34-23-16(11-31)12-33-24-19(23)9-17(10-20(24)30)36-25(18-5-4-6-21-26(18)41-15-35-21)22-13-39(38-37-22)29(7-8-29)27(32)40/h4-6,9-10,12-13,15,25,36-38H,7-8,14H2,1-3H3,(H2,32,40)(H,33,34)/t25-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505794
PNG
((S)-8-chloro-6-(((1-cyclopropyl-1H-1,2,3- triazol-...)
Show SMILES CC(C)(C)CNc1c(cnc2c(Cl)cc(N[C@H](C3=CN(NN3)C3CC3)c3cccc4cnccc34)cc12)C#N
Show InChI InChI=1S/C30H31ClN8/c1-30(2,3)17-35-27-19(13-32)15-34-28-24(27)11-20(12-25(28)31)36-29(26-16-39(38-37-26)21-7-8-21)23-6-4-5-18-14-33-10-9-22(18)23/h4-6,9-12,14-16,21,29,36-38H,7-8,17H2,1-3H3,(H,34,35)/t29-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505973
PNG
(6-(((S)-(6-fluoro-2-methylpyridin-3-yl)(1- ((1R,2S...)
Show SMILES Cc1nc(F)ccc1[C@H](Nc1cc(C#N)c2ncc(C#N)c(NCC(C)(C)C)c2c1)C1=CN(NN1)[C@@H]1C[C@@H]1F
Show InChI InChI=1S/C28H29F2N9/c1-15-19(5-6-24(30)35-15)27(22-13-39(38-37-22)23-9-21(23)29)36-18-7-16(10-31)25-20(8-18)26(17(11-32)12-33-25)34-14-28(2,3)4/h5-8,12-13,21,23,27,36-38H,9,14H2,1-4H3,(H,33,34)/t21-,23+,27-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505974
PNG
(6-(((S)-(6-fluoro-2- methylpyridin-3-yl)(1-((S)- 1...)
Show SMILES C[C@@H](CF)N1NNC(=C1)[C@@H](Nc1cc(C#N)c2ncc(C#N)c(NCC(C)(C)C)c2c1)c1ccc(F)nc1C
Show InChI InChI=1S/C28H31F2N9/c1-16(10-29)39-14-23(37-38-39)27(21-6-7-24(30)35-17(21)2)36-20-8-18(11-31)25-22(9-20)26(19(12-32)13-33-25)34-15-28(3,4)5/h6-9,13-14,16,27,36-38H,10,15H2,1-5H3,(H,33,34)/t16-,27-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM506166
PNG
((S)-6-(((1-(bicyclo[1.1.1]pentan- 1-yl)-1H-1,2,3- ...)
Show SMILES CC(C)(CNc1c(cnc2c(cc(N[C@H](C3=CN(NN3)C34CC(C3)C4)c3ccc(F)c4ncccc34)cc12)C#N)C#N)C(F)(F)F
Show InChI InChI=1S/C33H29F4N9/c1-31(2,33(35,36)37)17-42-28-20(14-39)15-41-27-19(13-38)8-21(9-24(27)28)43-30(23-5-6-25(34)29-22(23)4-3-7-40-29)26-16-46(45-44-26)32-10-18(11-32)12-32/h3-9,15-16,18,30,43-45H,10-12,17H2,1-2H3,(H,41,42)/t18?,30-,32?/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505417
PNG
((S)-8-chloro-6-(((1-cyclopropyl-1H- 1,2,3-triazol-...)
Show SMILES CC(C)(C)CNc1c(cnc2c(Cl)cc(NC(C3=CN(NN3)C3CC3)c3csc4CN(CCc34)C3COC3)cc12)C#N
Show InChI InChI=1S/C31H37ClN8OS/c1-31(2,3)17-35-28-18(10-33)11-34-29-23(28)8-19(9-25(29)32)36-30(26-12-40(38-37-26)20-4-5-20)24-16-42-27-13-39(7-6-22(24)27)21-14-41-15-21/h8-9,11-12,16,20-21,30,36-38H,4-7,13-15,17H2,1-3H3,(H,34,35)
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505782
PNG
(8-chloro-4-(((R)-3-cyano-1-phenyl- propyl)amino)-6...)
Show SMILES Cc1nc(F)ccc1[C@H](Nc1cc(Cl)c2ncc(C#N)c(N[C@H](CCC#N)c3ccccc3)c2c1)C1=CN(NN1)C1CC1
Show InChI InChI=1S/C32H29ClFN9/c1-19-24(11-12-29(34)38-19)32(28-18-43(42-41-28)23-9-10-23)39-22-14-25-30(21(16-36)17-37-31(25)26(33)15-22)40-27(8-5-13-35)20-6-3-2-4-7-20/h2-4,6-7,11-12,14-15,17-18,23,27,32,39,41-42H,5,8-10H2,1H3,(H,37,40)/t27-,32+/m1/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505829
PNG
((S)-1-(4-(((8-chloro-3-cyano-4- (neopentylamino)qu...)
Show SMILES Cc1nc(F)ccc1[C@H](Nc1cc(Cl)c2ncc(C#N)c(NCC(C)(C)C)c2c1)C1=CN(NN1)C1(CCC1)C(N)=O
Show InChI InChI=1S/C29H33ClFN9O/c1-16-19(6-7-23(31)36-16)26(22-14-40(39-38-22)29(27(33)41)8-5-9-29)37-18-10-20-24(35-15-28(2,3)4)17(12-32)13-34-25(20)21(30)11-18/h6-7,10-11,13-14,26,37-39H,5,8-9,15H2,1-4H3,(H2,33,41)(H,34,35)/t26-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505841
PNG
((S)-1-(4-(((3,8-dicyano- 4-(neopentylamino)- quino...)
Show SMILES Cc1nc(F)ccc1[C@H](Nc1cc(C#N)c2ncc(C#N)c(NCC(C)(C)C)c2c1)C1=CN(NN1)C1(CC1)C(N)=O
Show InChI InChI=1S/C29H31FN10O/c1-16-20(5-6-23(30)36-16)26(22-14-40(39-38-22)29(7-8-29)27(33)41)37-19-9-17(11-31)24-21(10-19)25(18(12-32)13-34-24)35-15-28(2,3)4/h5-6,9-10,13-14,26,37-39H,7-8,15H2,1-4H3,(H2,33,41)(H,34,35)/t26-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505928
PNG
((S)-6-(((1-(1-cyanocyclopropyl)-1H- 1,2,3-triazol-...)
Show SMILES CC(C)(C)CNc1c(cnc2c(cc(N[C@H](C3=CN(NN3)C3(CC3)C#N)c3cccc4ncccc34)cc12)C#N)C#N
Show InChI InChI=1S/C32H30N10/c1-31(2,3)19-38-29-21(15-34)16-37-28-20(14-33)12-22(13-25(28)29)39-30(24-6-4-8-26-23(24)7-5-11-36-26)27-17-42(41-40-27)32(18-35)9-10-32/h4-8,11-13,16-17,30,39-41H,9-10,19H2,1-3H3,(H,37,38)/t30-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM506203
PNG
((S)-6-(((2-methyl-1-oxo-1,2- dihydroisoquinolin-5-...)
Show SMILES Cn1ccc2c(cccc2c1=O)[C@H](Nc1cc(C#N)c2ncc(C#N)c(NCC(C)(C)C)c2c1)C1=CN(NN1)C1(C)COC1
Show InChI InChI=1S/C33H35N9O2/c1-32(2,3)17-37-29-21(14-35)15-36-28-20(13-34)11-22(12-26(28)29)38-30(27-16-42(40-39-27)33(4)18-44-19-33)24-7-6-8-25-23(24)9-10-41(5)31(25)43/h6-12,15-16,30,38-40H,17-19H2,1-5H3,(H,36,37)/t30-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM506229
PNG
((S)-6-(((2-methyl-1-oxo-1,2- dihydroisoquinolin- 5...)
Show SMILES Cn1ccc2c(cccc2c1=O)[C@H](Nc1cc(C#N)c2ncc(C#N)c(NCC(C)(C)C)c2c1)C1=CN(NN1)C1(C)CC1
Show InChI InChI=1S/C33H35N9O/c1-32(2,3)19-37-29-21(16-35)17-36-28-20(15-34)13-22(14-26(28)29)38-30(27-18-42(40-39-27)33(4)10-11-33)24-7-6-8-25-23(24)9-12-41(5)31(25)43/h6-9,12-14,17-18,30,38-40H,10-11,19H2,1-5H3,(H,36,37)/t30-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM506233
PNG
((S)-6-(((1-(bicyclo[1.1.1]pentan- 1-yl)-1H-1,2,3- ...)
Show SMILES Cn1ccc2c(cccc2c1=O)[C@H](Nc1cc(C#N)c2ncc(C#N)c(NCC(C)(C)C(F)(F)F)c2c1)C1=CN(NN1)C12CC(C1)C2
Show InChI InChI=1S/C34H32F3N9O/c1-32(2,34(35,36)37)18-41-29-21(15-39)16-40-28-20(14-38)9-22(10-26(28)29)42-30(27-17-46(44-43-27)33-11-19(12-33)13-33)24-5-4-6-25-23(24)7-8-45(3)31(25)47/h4-10,16-17,19,30,42-44H,11-13,18H2,1-3H3,(H,40,41)/t19?,30-,33?/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM506234
PNG
((S)-6-(((2-methyl-1-oxo-1,2- dihydroisoquinolin-5-...)
Show SMILES Cn1ccc2c(cccc2c1=O)[C@H](Nc1cc(C#N)c2ncc(C#N)c(NCC(C)(C)C(F)(F)F)c2c1)C1=CN(NN1)C1(C)CC1
Show InChI InChI=1S/C33H32F3N9O/c1-31(2,33(34,35)36)18-40-28-20(15-38)16-39-27-19(14-37)12-21(13-25(27)28)41-29(26-17-45(43-42-26)32(3)9-10-32)23-6-5-7-24-22(23)8-11-44(4)30(24)46/h5-8,11-13,16-17,29,41-43H,9-10,18H2,1-4H3,(H,39,40)/t29-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505409
PNG
(8-chloro-4-(((R)-3-cyano-1-phenyl- propyl)amino)-6...)
Show SMILES Cc1nc(F)ccc1[C@](O)(Nc1cc(Cl)c2ncc(C#N)c(N[C@H](CCC#N)c3ccccc3)c2c1)C1=CN(NN1)C1CC1
Show InChI InChI=1S/C32H29ClFN9O/c1-19-25(11-12-29(34)38-19)32(44,28-18-43(42-41-28)23-9-10-23)40-22-14-24-30(21(16-36)17-37-31(24)26(33)15-22)39-27(8-5-13-35)20-6-3-2-4-7-20/h2-4,6-7,11-12,14-15,17-18,23,27,40-42,44H,5,8-10H2,1H3,(H,37,39)/t27-,32-/m1/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505421
PNG
(8-chloro-4-(((R)-3-cyano-1- phenylpropyl)amino)-6-...)
Show SMILES Clc1cc(N[C@H](C2=CN(NN2)C2CC2)c2csc3CN(CCc23)C2COC2)cc2c(N[C@H](CCC#N)c3ccccc3)c(cnc12)C#N
Show InChI InChI=1S/C36H36ClN9OS/c37-30-14-24(13-28-34(23(15-39)16-40-35(28)30)42-31(7-4-11-38)22-5-2-1-3-6-22)41-36(32-17-46(44-43-32)25-8-9-25)29-21-48-33-18-45(12-10-27(29)33)26-19-47-20-26/h1-3,5-6,13-14,16-17,21,25-26,31,36,41,43-44H,4,7-10,12,18-20H2,(H,40,42)/t31-,36+/m1/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM506222
PNG
(6-(((1S)-(6-fluoro-2-methylpyridin-3-yl)(1- (spiro...)
Show SMILES Cc1nc(F)ccc1[C@H](Nc1cc(C#N)c2ncc(C#N)c(NCC(C)(C)C)c2c1)C1=CN(NN1)C1CC11CC1
Show InChI InChI=1S/C30H32FN9/c1-17-21(5-6-25(31)36-17)28(23-15-40(39-38-23)24-11-30(24)7-8-30)37-20-9-18(12-32)26-22(10-20)27(19(13-33)14-34-26)35-16-29(2,3)4/h5-6,9-10,14-15,24,28,37-39H,7-8,11,16H2,1-4H3,(H,34,35)/t24?,28-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM504535
PNG
((S)-6-((benzo[d]thiazol-7-yl(1- cyclopropyl-1H-1,2...)
Show SMILES CC(C)(C)CNc1c(cnc2c(cc(N[C@H](C3=CN(NN3)C3CC3)c3cccc4ncsc34)cc12)C#N)C#N
Show InChI InChI=1S/C29H29N9S/c1-29(2,3)15-33-26-18(12-31)13-32-25-17(11-30)9-19(10-22(25)26)35-27(24-14-38(37-36-24)20-7-8-20)21-5-4-6-23-28(21)39-16-34-23/h4-6,9-10,13-14,16,20,27,35-37H,7-8,15H2,1-3H3,(H,32,33)/t27-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505405
PNG
(8-chloro-4-(((R)-3-cyano-1-phenyl- propyl)amino)-6...)
Show SMILES Clc1cc(N[C@H](C2=CN(NN2)C2CC2)c2cccc3CNCc23)cc2c(N[C@H](CCC#N)c3ccccc3)c(cnc12)C#N
Show InChI InChI=1S/C34H32ClN9/c35-29-15-24(40-34(31-20-44(43-42-31)25-11-12-25)26-9-4-8-22-17-38-19-28(22)26)14-27-32(23(16-37)18-39-33(27)29)41-30(10-5-13-36)21-6-2-1-3-7-21/h1-4,6-9,14-15,18,20,25,30,34,38,40,42-43H,5,10-12,17,19H2,(H,39,41)/t30-,34+/m1/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505411
PNG
(8-chloro-4-(((R)-3-cyano-1- phenylpropyl)amino)- 6...)
Show SMILES Cc1ncccc1[C@H](Nc1cc(Cl)c2ncc(C#N)c(N[C@H](CCC#N)c3ccccc3)c2c1)C1=CN(NN1)C1CC1
Show InChI InChI=1S/C32H30ClN9/c1-20-25(9-6-14-36-20)32(29-19-42(41-40-29)24-11-12-24)38-23-15-26-30(22(17-35)18-37-31(26)27(33)16-23)39-28(10-5-13-34)21-7-3-2-4-8-21/h2-4,6-9,14-16,18-19,24,28,32,38,40-41H,5,10-12H2,1H3,(H,37,39)/t28-,32+/m1/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505760
PNG
((S)-1-(4-(benzo[d]thiazol-7-yl((3,8- dicyano-4-(ne...)
Show SMILES CC(C)(C)CNc1c(cnc2c(cc(N[C@H](C3=CN(NN3)C3(CC3)C(N)=O)c3cccc4ncsc34)cc12)C#N)C#N
Show InChI InChI=1S/C30H30N10OS/c1-29(2,3)15-35-25-18(12-32)13-34-24-17(11-31)9-19(10-21(24)25)37-26(20-5-4-6-22-27(20)42-16-36-22)23-14-40(39-38-23)30(7-8-30)28(33)41/h4-6,9-10,13-14,16,26,37-39H,7-8,15H2,1-3H3,(H2,33,41)(H,34,35)/t26-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505765
PNG
(4-(((R)-3-cyano-1-phenylpropyl)amino)- 6-(((S)-(1-...)
Show SMILES N#CCC[C@@H](Nc1c(cnc2c(cc(N[C@H](C3=CN(NN3)C3CC3)c3csc4CN(CCc34)C3COC3)cc12)C#N)C#N)c1ccccc1
Show InChI InChI=1S/C37H36N10OS/c38-11-4-7-32(23-5-2-1-3-6-23)43-36-25(16-40)17-41-35-24(15-39)13-26(14-30(35)36)42-37(33-18-47(45-44-33)27-8-9-27)31-22-49-34-19-46(12-10-29(31)34)28-20-48-21-28/h1-3,5-6,13-14,17-18,22,27-28,32,37,42,44-45H,4,7-10,12,19-21H2,(H,41,43)/t32-,37+/m1/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505819
PNG
((S)-6-(((1-cyclopropyl-1H-1,2,3-triazol-4- yl)(iso...)
Show SMILES CC(C)(C)CNc1c(cnc2c(cc(N[C@H](C3=CN(NN3)C3CC3)c3cccc4cnccc34)cc12)C#N)C#N
Show InChI InChI=1S/C31H31N9/c1-31(2,3)18-36-29-21(14-33)16-35-28-20(13-32)11-22(12-26(28)29)37-30(27-17-40(39-38-27)23-7-8-23)25-6-4-5-19-15-34-10-9-24(19)25/h4-6,9-12,15-17,23,30,37-39H,7-8,18H2,1-3H3,(H,35,36)/t30-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505845
PNG
((S)-1-(4-(((3,8-dicyano-4-(neopentyl- amino)quinol...)
Show SMILES Cc1nc(F)ccc1[C@H](Nc1cc(C#N)c2ncc(C#N)c(NCC(C)(C)C)c2c1)C1=CN(NN1)C1(CCC1)C(N)=O
Show InChI InChI=1S/C30H33FN10O/c1-17-21(6-7-24(31)37-17)27(23-15-41(40-39-23)30(28(34)42)8-5-9-30)38-20-10-18(12-32)25-22(11-20)26(19(13-33)14-35-25)36-16-29(2,3)4/h6-7,10-11,14-15,27,38-40H,5,8-9,16H2,1-4H3,(H2,34,42)(H,35,36)/t27-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505890
PNG
(8-chloro-6-(((S)-(1-(1-(difluoromethyl)- cycloprop...)
Show SMILES Cc1nc(F)ccc1[C@H](Nc1cc(Cl)c2ncc(C#N)c(N[C@@H]3CCOCC3(C)C)c2c1)C1=CN(NN1)C1(CC1)C(F)F
Show InChI InChI=1S/C30H32ClF3N8O/c1-16-19(4-5-24(32)37-16)27(22-14-42(41-40-22)30(7-8-30)28(33)34)38-18-10-20-25(39-23-6-9-43-15-29(23,2)3)17(12-35)13-36-26(20)21(31)11-18/h4-5,10-11,13-14,23,27-28,38,40-41H,6-9,15H2,1-3H3,(H,36,39)/t23-,27+/m1/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505926
PNG
((S)-1-(4-(((3,8-dicyano-4-(neopentylamino)- quinol...)
Show SMILES CC(C)(C)CNc1c(cnc2c(cc(N[C@H](C3=CN(NN3)C3(CC3)C(N)=O)c3cccc4ncccc34)cc12)C#N)C#N
Show InChI InChI=1S/C32H32N10O/c1-31(2,3)18-38-28-20(15-34)16-37-27-19(14-33)12-21(13-24(27)28)39-29(23-6-4-8-25-22(23)7-5-11-36-25)26-17-42(41-40-26)32(9-10-32)30(35)43/h4-8,11-13,16-17,29,39-41H,9-10,18H2,1-3H3,(H2,35,43)(H,37,38)/t29-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505927
PNG
((S)-1-(4-(((3,8-dicyano-4-(neopentyl- amino)quinol...)
Show SMILES CC(C)(C)CNc1c(cnc2c(cc(N[C@H](C3=CN(NN3)C3(CCC3)C(N)=O)c3cccc4ncccc34)cc12)C#N)C#N
Show InChI InChI=1S/C33H34N10O/c1-32(2,3)19-39-29-21(16-35)17-38-28-20(15-34)13-22(14-25(28)29)40-30(24-7-4-9-26-23(24)8-5-12-37-26)27-18-43(42-41-27)33(31(36)44)10-6-11-33/h4-5,7-9,12-14,17-18,30,40-42H,6,10-11,19H2,1-3H3,(H2,36,44)(H,38,39)/t30-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM506020
PNG
(US11066414, Compound 669 | bi(cyclopropan)]-1-yl)-...)
Show SMILES Cc1nc(F)ccc1[C@H](Nc1cc(Cl)c2ncc(C#N)c(N[C@@H]3CCOCC3(C)C)c2c1)C1=CN(NN1)C1(CC1)C1CC1
Show InChI InChI=1S/C32H36ClFN8O/c1-18-22(6-7-27(34)37-18)30(25-16-42(41-40-25)32(9-10-32)20-4-5-20)38-21-12-23-28(39-26-8-11-43-17-31(26,2)3)19(14-35)15-36-29(23)24(33)13-21/h6-7,12-13,15-16,20,26,30,38,40-41H,4-5,8-11,17H2,1-3H3,(H,36,39)/t26-,30+/m1/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM506221
PNG
((S)-6-(( (Ml-(difluoromethyl)cyclopropyl)- 1H-1,2,...)
Show SMILES Cn1ccc2c(cccc2c1=O)[C@H](Nc1cc(C#N)c2ncc(C#N)c(NCC(C)(C)C)c2c1)C1=CN(NN1)C1(CC1)C(F)F
Show InChI InChI=1S/C33H33F2N9O/c1-32(2,3)18-39-28-20(15-37)16-38-27-19(14-36)12-21(13-25(27)28)40-29(26-17-44(42-41-26)33(9-10-33)31(34)35)23-6-5-7-24-22(23)8-11-43(4)30(24)45/h5-8,11-13,16-17,29,31,40-42H,9-10,18H2,1-4H3,(H,38,39)/t29-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505413
PNG
((S)-6-(((1-cyclopropyl-1H-1,2,3- triazol-4-yl)(1-o...)
Show SMILES CC(C)(C)CNc1c(cnc2c(cc(N[C@H](C3=CN(NN3)C3CC3)c3cccc4C(=O)NCc34)cc12)C#N)C#N
Show InChI InChI=1S/C30H31N9O/c1-30(2,3)16-35-27-18(12-32)13-33-26-17(11-31)9-19(10-23(26)27)36-28(25-15-39(38-37-25)20-7-8-20)21-5-4-6-22-24(21)14-34-29(22)40/h4-6,9-10,13,15,20,28,36-38H,7-8,14,16H2,1-3H3,(H,33,35)(H,34,40)/t28-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505442
PNG
((S)-8-chloro-6-(((1-cyclopropyl-1H- 1,2,3-triazol-...)
Show SMILES CC(C)(C)CNc1c(cnc2c(Cl)cc(N[C@@H](C3=CN(NN3)C3CC3)c3cccnc3F)cc12)C#N
Show InChI InChI=1S/C26H28ClFN8/c1-26(2,3)14-32-22-15(11-29)12-31-23-19(22)9-16(10-20(23)27)33-24(18-5-4-8-30-25(18)28)21-13-36(35-34-21)17-6-7-17/h4-5,8-10,12-13,17,24,33-35H,6-7,14H2,1-3H3,(H,31,32)/t24-/m1/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505938
PNG
((S)-1-(4-(((3,8-dicyano-4- (neopentylamino)- quino...)
Show SMILES CC(C)(C)CNc1c(cnc2c(cc(N[C@H](C3=CN(NN3)C3(CCC3)C(N)=O)c3cccc4cnccc34)cc12)C#N)C#N
Show InChI InChI=1S/C33H34N10O/c1-32(2,3)19-39-29-22(15-35)17-38-28-21(14-34)12-23(13-26(28)29)40-30(25-7-4-6-20-16-37-11-8-24(20)25)27-18-43(42-41-27)33(31(36)44)9-5-10-33/h4,6-8,11-13,16-18,30,40-42H,5,9-10,19H2,1-3H3,(H2,36,44)(H,38,39)/t30-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505972
PNG
((S)-6-(((1-([1,1'-bi(cyclopropan)]- 1-yl)-1H-1,2,3...)
Show SMILES Cc1nc(F)ccc1[C@H](Nc1cc(C#N)c2ncc(C#N)c(NCC(C)(C)C)c2c1)C1=CN(NN1)C1(CC1)C1CC1
Show InChI InChI=1S/C31H34FN9/c1-18-23(7-8-26(32)37-18)29(25-16-41(40-39-25)31(9-10-31)21-5-6-21)38-22-11-19(13-33)27-24(12-22)28(20(14-34)15-35-27)36-17-30(2,3)4/h7-8,11-12,15-16,21,29,38-40H,5-6,9-10,17H2,1-4H3,(H,35,36)/t29-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM506206
PNG
((S)-6-(((1-cyclopropyl-1H-1,2,3-triazol-4- yl)(thi...)
Show SMILES CC(C)(C)CNc1c(cnc2c(cc(N[C@H](C3=CN(NN3)C3CC3)c3csc4cnccc34)cc12)C#N)C#N
Show InChI InChI=1S/C29H29N9S/c1-29(2,3)16-34-27-18(11-31)12-33-26-17(10-30)8-19(9-22(26)27)35-28(24-14-38(37-36-24)20-4-5-20)23-15-39-25-13-32-7-6-21(23)25/h6-9,12-15,20,28,35-37H,4-5,16H2,1-3H3,(H,33,34)/t28-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505786
PNG
((S)-6-((benzo[d]thiazol-7-yl(1-(1- methylcycloprop...)
Show SMILES CC(C)(C)CNc1c(cnc2c(cc(N[C@H](C3=CN(NN3)C3(C)CC3)c3cccc4ncsc34)cc12)C#N)C#N
Show InChI InChI=1S/C30H31N9S/c1-29(2,3)16-34-26-19(13-32)14-33-25-18(12-31)10-20(11-22(25)26)36-27(21-6-5-7-23-28(21)40-17-35-23)24-15-39(38-37-24)30(4)8-9-30/h5-7,10-11,14-15,17,27,36-38H,8-9,16H2,1-4H3,(H,33,34)/t27-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505855
PNG
((S)-8-chloro-6-(((1-cyclopropyl-1H-1,2,3- triazol-...)
Show SMILES CC(C)(C)CNc1c(cnc2c(Cl)cc(N[C@H](C3=CN(NN3)C3CC3)c3cccc4ccncc34)cc12)C#N
Show InChI InChI=1S/C30H31ClN8/c1-30(2,3)17-35-27-19(13-32)14-34-28-23(27)11-20(12-25(28)31)36-29(26-16-39(38-37-26)21-7-8-21)22-6-4-5-18-9-10-33-15-24(18)22/h4-6,9-12,14-16,21,29,36-38H,7-8,17H2,1-3H3,(H,34,35)/t29-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM506048
PNG
((S)-6-(((1-(bicyclo[1.1.1)pentan- 1-yl)-1H-1,2,3- ...)
Show SMILES CC(C)(C)CNc1c(cnc2c(cc(N[C@H](C3=CN(NN3)C34CC(C3)C4)c3cccc4ncccc34)cc12)C#N)C#N
Show InChI InChI=1S/C33H33N9/c1-32(2,3)19-38-30-22(16-35)17-37-29-21(15-34)10-23(11-26(29)30)39-31(25-6-4-8-27-24(25)7-5-9-36-27)28-18-42(41-40-28)33-12-20(13-33)14-33/h4-11,17-18,20,31,39-41H,12-14,19H2,1-3H3,(H,37,38)/t20?,31-,33?/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM506055
PNG
(6-(((SHH(1S,2S)-2- fluorocyclopropyl)-1H-1,2,3- tr...)
Show SMILES CC(C)(C)CNc1c(cnc2c(cc(N[C@H](C3=CN(NN3)C3C[C@@H]3F)c3cccc4cnccc34)cc12)C#N)C#N
Show InChI InChI=1S/C31H30FN9/c1-31(2,3)17-37-29-20(13-34)15-36-28-19(12-33)9-21(10-24(28)29)38-30(26-16-41(40-39-26)27-11-25(27)32)23-6-4-5-18-14-35-8-7-22(18)23/h4-10,14-16,25,27,30,38-40H,11,17H2,1-3H3,(H,36,37)/t25-,27?,30-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM506241
PNG
((S)-6-(((1-(bicyclo[1.1.1]pentan-1-yl)-1H- 1,2,3-t...)
Show SMILES Cn1ccc2c(cccc2c1=O)[C@H](Nc1cc(C#N)c2ncc(C#N)c(NCC(C)(C)C)c2c1)C1=CN(NN1)C12CC(C1)C2
Show InChI InChI=1S/C34H35N9O/c1-33(2,3)19-38-30-22(16-36)17-37-29-21(15-35)10-23(11-27(29)30)39-31(28-18-43(41-40-28)34-12-20(13-34)14-34)25-6-5-7-26-24(25)8-9-42(4)32(26)44/h5-11,17-18,20,31,39-41H,12-14,19H2,1-4H3,(H,37,38)/t20?,31-,34?/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505427
PNG
(8-chloro-4-((3-cyano-1-phenyl- propyl)amino)-6-(((...)
Show SMILES Clc1cc(N[C@H](C2=CN(NN2)C2CC2)c2csc3CN(CCc23)C2COC2)cc2c(NC(CCC#N)c3ccccc3)c(cnc12)C#N
Show InChI InChI=1S/C36H36ClN9OS/c37-30-14-24(13-28-34(23(15-39)16-40-35(28)30)42-31(7-4-11-38)22-5-2-1-3-6-22)41-36(32-17-46(44-43-32)25-8-9-25)29-21-48-33-18-45(12-10-27(29)33)26-19-47-20-26/h1-3,5-6,13-14,16-17,21,25-26,31,36,41,43-44H,4,7-10,12,18-20H2,(H,40,42)/t31?,36-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505815
PNG
((S)-6-((benzo[d]thiazol-7- yl(1-(1-(pyridin-4- yl)...)
Show SMILES CC(C)(C)CNc1c(cnc2c(cc(N[C@H](C3=CN(NN3)C3(CC3)c3ccncc3)c3cccc4ncsc34)cc12)C#N)C#N
Show InChI InChI=1S/C34H32N10S/c1-33(2,3)19-39-30-22(16-36)17-38-29-21(15-35)13-24(14-26(29)30)41-31(25-5-4-6-27-32(25)45-20-40-27)28-18-44(43-42-28)34(9-10-34)23-7-11-37-12-8-23/h4-8,11-14,17-18,20,31,41-43H,9-10,19H2,1-3H3,(H,38,39)/t31-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM505838
PNG
((S)-1-(4-(((3-cyano-8-fluoro-4-(neopentyl- amino)q...)
Show SMILES Cc1nc(F)ccc1[C@H](Nc1cc(F)c2ncc(C#N)c(NCC(C)(C)C)c2c1)C1=CN(NN1)C1(CCC1)C(N)=O
Show InChI InChI=1S/C29H33F2N9O/c1-16-19(6-7-23(31)36-16)26(22-14-40(39-38-22)29(27(33)41)8-5-9-29)37-18-10-20-24(35-15-28(2,3)4)17(12-32)13-34-25(20)21(30)11-18/h6-7,10-11,13-14,26,37-39H,5,8-9,15H2,1-4H3,(H2,33,41)(H,34,35)/t26-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

More data for this
Ligand-Target Pair
Epidermal growth factor receptor


(Homo sapiens (Human))
BDBM504587
PNG
((S)-8-chloro-6-(((1-cyclopropyl- 1H-1,2,3-triazol-...)
Show SMILES CC(C)(C)CNc1c(cnc2c(Cl)cc(N[C@H](C3=CN(NN3)C3CC3)c3cccc4CNCc34)cc12)C#N
Show InChI InChI=1S/C29H33ClN8/c1-29(2,3)16-34-26-18(11-31)13-33-27-22(26)9-19(10-24(27)30)35-28(25-15-38(37-36-25)20-7-8-20)21-6-4-5-17-12-32-14-23(17)21/h4-6,9-10,13,15,20,28,32,35-37H,7-8,12,14,16H2,1-3H3,(H,33,34)/t28-/m0/s1
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Gilead Sciences, Inc.

US Patent


Assay Description
EGFR activity was measured using KinEASE (Cisbio), a time-resolved fluorescence resonance energy transfer (TR-FRET) immunoassay. In this assay, EGFR-...


US Patent US11066414 (2021)

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