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Found 11905 hits Enz. Inhib. hit(s) with Target = 'MER intracellular domain/EGFR extracellular domain chimera'   
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
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM270588
PNG
((S)-6-(((2- chlorophenyl)(1-(1- cyanocyclopropyl)-...)
Show SMILES CC(C)(C)CNc1ncnc2c(cc(NC(c3cn(nn3)C3(CC3)C#N)c3ccccc3Cl)cc12)C#N
Show InChI InChI=1S/C27H26ClN9/c1-26(2,3)15-31-25-20-11-18(10-17(12-29)23(20)32-16-33-25)34-24(19-6-4-5-7-21(19)28)22-13-37(36-35-22)27(14-30)8-9-27/h4-7,10-11,13,16,24,34H,8-9,15H2,1-3H3,(H,31,32,33)
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US Patent
n/an/a 3.30n/an/an/an/a7.025



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 US10059695 (2018)

More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM270588
PNG
((S)-6-(((2- chlorophenyl)(1-(1- cyanocyclopropyl)-...)
Show SMILES CC(C)(C)CNc1ncnc2c(cc(NC(c3cn(nn3)C3(CC3)C#N)c3ccccc3Cl)cc12)C#N
Show InChI InChI=1S/C27H26ClN9/c1-26(2,3)15-31-25-20-11-18(10-17(12-29)23(20)32-16-33-25)34-24(19-6-4-5-7-21(19)28)22-13-37(36-35-22)27(14-30)8-9-27/h4-7,10-11,13,16,24,34H,8-9,15H2,1-3H3,(H,31,32,33)
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n/an/an/an/a 35n/an/a7.025



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 US10059695 (2018)

More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM270589
PNG
((S)-8-chloro-N6-((1- (1- (difluoromethyl) cyclopro...)
Show SMILES Cc1nc(F)ccc1[C@H](Nc1cc(Cl)c2ncnc(NCC(C)(C)C)c2c1)c1cn(nn1)C1(CC1)C(F)F
Show InChI InChI=1S/C26H28ClF3N8/c1-14-16(5-6-20(28)34-14)22(19-11-38(37-36-19)26(7-8-26)24(29)30)35-15-9-17-21(18(27)10-15)32-13-33-23(17)31-12-25(2,3)4/h5-6,9-11,13,22,24,35H,7-8,12H2,1-4H3,(H,31,32,33)/t22-/m0/s1
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n/an/a 1.90n/an/an/an/a7.025



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 US10059695 (2018)

More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM234389
PNG
(Mangiferin)
Show SMILES OC[C@H]1OC([C@H](O)[C@@H](O)[C@@H]1O)c1c(O)cc2oc3cc(O)c(O)cc3c(=O)c2c1O
Show InChI InChI=1S/C19H18O11/c20-4-11-15(25)17(27)18(28)19(30-11)12-8(23)3-10-13(16(12)26)14(24)5-1-6(21)7(22)2-9(5)29-10/h1-3,11,15,17-23,25-28H,4H2/t11-,15-,17+,18-,19?/m1/s1
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Article
PubMed
n/an/a>1.00E+4n/an/an/an/a7.0n/a



Gyeongsang National University



Assay Description
Inhibition of kinase activity against a variety of recombinant kinases [FLT3, FLT3 D835Y, anaplastic lymphoma kinase (ALK), insulin receptor, and epi...


J Enzyme Inhib Med Chem 26: 445-8 (2011)


Article DOI: 10.3109/14756366.2010.515215
BindingDB Entry DOI: 10.7270/Q2S46QTV
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM101226
PNG
(US8524722, 5)
Show SMILES Fc1ccc(Nc2ncnc3sc4CN(CCc4c23)C(=O)\C=C\CN2CCCOCC2)cc1Cl
Show InChI InChI=1S/C24H25ClFN5O2S/c25-18-13-16(4-5-19(18)26)29-23-22-17-6-9-31(14-20(17)34-24(22)28-15-27-23)21(32)3-1-7-30-8-2-11-33-12-10-30/h1,3-5,13,15H,2,6-12,14H2,(H,27,28,29)/b3-1+
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US Patent
n/an/a 1n/an/an/an/a7.022



Bayer Intellectual Property GmbH

US Patent


Assay Description
EGFR inhibitory activity of compounds of the present invention is quantified employing the EGFR HTRF assay.


US Patent US8524722 (2013)


BindingDB Entry DOI: 10.7270/Q2B856RQ
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM101227
PNG
(US8524722, 10)
Show SMILES Fc1ccc(Nc2ncnc3sc4CN(CCc4c23)C(=O)\C=C\CN2C3CCC2CC3)cc1Cl
Show InChI InChI=1S/C25H25ClFN5OS/c26-19-12-15(3-8-20(19)27)30-24-23-18-9-11-31(13-21(18)34-25(23)29-14-28-24)22(33)2-1-10-32-16-4-5-17(32)7-6-16/h1-3,8,12,14,16-17H,4-7,9-11,13H2,(H,28,29,30)/b2-1+
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US Patent
n/an/a 1.10n/an/an/an/a7.022



Bayer Intellectual Property GmbH

US Patent


Assay Description
EGFR inhibitory activity of compounds of the present invention is quantified employing the EGFR HTRF assay.


US Patent US8524722 (2013)


BindingDB Entry DOI: 10.7270/Q2B856RQ
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM101228
PNG
(US8524722, 12)
Show SMILES CC(C)(CN1CCOCC1)NC\C=C\C(=O)N1CCc2c(C1)sc1ncnc(Nc3ccc(F)c(Cl)c3)c21
Show InChI InChI=1S/C27H32ClFN6O2S/c1-27(2,16-34-10-12-37-13-11-34)32-8-3-4-23(36)35-9-7-19-22(15-35)38-26-24(19)25(30-17-31-26)33-18-5-6-21(29)20(28)14-18/h3-6,14,17,32H,7-13,15-16H2,1-2H3,(H,30,31,33)/b4-3+
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n/an/a 1n/an/an/an/a7.022



Bayer Intellectual Property GmbH

US Patent


Assay Description
EGFR inhibitory activity of compounds of the present invention is quantified employing the EGFR HTRF assay.


US Patent US8524722 (2013)


BindingDB Entry DOI: 10.7270/Q2B856RQ
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM101229
PNG
(US8524722, 13)
Show SMILES Fc1ccc(Nc2ncnc3sc4CN(CCc4c23)C(=O)\C=C\[C@@H]2CCCN2)cc1Cl
Show InChI InChI=1S/C22H21ClFN5OS/c23-16-10-14(3-5-17(16)24)28-21-20-15-7-9-29(11-18(15)31-22(20)27-12-26-21)19(30)6-4-13-2-1-8-25-13/h3-6,10,12-13,25H,1-2,7-9,11H2,(H,26,27,28)/b6-4+/t13-/m0/s1
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US Patent
n/an/a 2n/an/an/an/a7.022



Bayer Intellectual Property GmbH

US Patent


Assay Description
EGFR inhibitory activity of compounds of the present invention is quantified employing the EGFR HTRF assay.


US Patent US8524722 (2013)


BindingDB Entry DOI: 10.7270/Q2B856RQ
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM101230
PNG
(US8524722, 14)
Show SMILES CN1CCC[C@H]1\C=C\C(=O)N1CCc2c(C1)sc1ncnc(Nc3ccc(F)c(Cl)c3)c21
Show InChI InChI=1S/C23H23ClFN5OS/c1-29-9-2-3-15(29)5-7-20(31)30-10-8-16-19(12-30)32-23-21(16)22(26-13-27-23)28-14-4-6-18(25)17(24)11-14/h4-7,11,13,15H,2-3,8-10,12H2,1H3,(H,26,27,28)/b7-5+/t15-/m0/s1
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US Patent
n/an/a 1n/an/an/an/a7.022



Bayer Intellectual Property GmbH

US Patent


Assay Description
EGFR inhibitory activity of compounds of the present invention is quantified employing the EGFR HTRF assay.


US Patent US8524722 (2013)


BindingDB Entry DOI: 10.7270/Q2B856RQ
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM50330241
PNG
((E)-4-(Dimethylamino)-1-(4-[(1R)-1-phenylethyl]ami...)
Show SMILES C[C@@H](Nc1ncnc2sc3CN(CCc3c12)C(=O)\C=C\CN(C)C)c1ccccc1
Show InChI InChI=1S/C23H27N5OS/c1-16(17-8-5-4-6-9-17)26-22-21-18-11-13-28(20(29)10-7-12-27(2)3)14-19(18)30-23(21)25-15-24-22/h4-10,15-16H,11-14H2,1-3H3,(H,24,25,26)/b10-7+/t16-/m1/s1
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US Patent
n/an/a 4.60n/an/an/an/a7.022



Bayer Intellectual Property GmbH

US Patent


Assay Description
EGFR inhibitory activity of compounds of the present invention is quantified employing the EGFR HTRF assay.


US Patent US8524722 (2013)


BindingDB Entry DOI: 10.7270/Q2B856RQ
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM101231
PNG
(US8524722, 31)
Show SMILES COCCN(CCOC)C\C=C\C(=O)N1CCc2c(C1)sc1ncnc(Nc3ccc(F)c(Cl)c3)c21
Show InChI InChI=1S/C25H29ClFN5O3S/c1-34-12-10-31(11-13-35-2)8-3-4-22(33)32-9-7-18-21(15-32)36-25-23(18)24(28-16-29-25)30-17-5-6-20(27)19(26)14-17/h3-6,14,16H,7-13,15H2,1-2H3,(H,28,29,30)/b4-3+
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n/an/a 1n/an/an/an/a7.022



Bayer Intellectual Property GmbH

US Patent


Assay Description
EGFR inhibitory activity of compounds of the present invention is quantified employing the EGFR HTRF assay.


US Patent US8524722 (2013)


BindingDB Entry DOI: 10.7270/Q2B856RQ
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM101232
PNG
(US8524722, 70)
Show SMILES CN(C)C(=O)N1CCN(C\C=C\C(=O)N2CCc3c(C2)sc2ncnc(Nc4ccc(F)c(Cl)c4)c32)CC1
Show InChI InChI=1S/C26H29ClFN7O2S/c1-32(2)26(37)34-12-10-33(11-13-34)8-3-4-22(36)35-9-7-18-21(15-35)38-25-23(18)24(29-16-30-25)31-17-5-6-20(28)19(27)14-17/h3-6,14,16H,7-13,15H2,1-2H3,(H,29,30,31)/b4-3+
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n/an/a 1n/an/an/an/a7.022



Bayer Intellectual Property GmbH

US Patent


Assay Description
EGFR inhibitory activity of compounds of the present invention is quantified employing the EGFR HTRF assay.


US Patent US8524722 (2013)


BindingDB Entry DOI: 10.7270/Q2B856RQ
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM101233
PNG
(US8524722, 81)
Show SMILES CN(C)C\C=C\C(=O)N1Cc2sc3ncnc(Nc4ccc(F)c(Cl)c4)c3c2C1
Show InChI InChI=1S/C20H19ClFN5OS/c1-26(2)7-3-4-17(28)27-9-13-16(10-27)29-20-18(13)19(23-11-24-20)25-12-5-6-15(22)14(21)8-12/h3-6,8,11H,7,9-10H2,1-2H3,(H,23,24,25)/b4-3+
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US Patent
n/an/a 12n/an/an/an/a7.022



Bayer Intellectual Property GmbH

US Patent


Assay Description
EGFR inhibitory activity of compounds of the present invention is quantified employing the EGFR HTRF assay.


US Patent US8524722 (2013)


BindingDB Entry DOI: 10.7270/Q2B856RQ
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM101234
PNG
(US8524722, 84)
Show SMILES CC(C)N(C)C\C=C\C(=O)N1Cc2sc3ncnc(Nc4ccc(Cl)c(Cl)c4)c3c2C1
Show InChI InChI=1S/C22H23Cl2N5OS/c1-13(2)28(3)8-4-5-19(30)29-10-15-18(11-29)31-22-20(15)21(25-12-26-22)27-14-6-7-16(23)17(24)9-14/h4-7,9,12-13H,8,10-11H2,1-3H3,(H,25,26,27)/b5-4+
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n/an/a 1.40n/an/an/an/a7.022



Bayer Intellectual Property GmbH

US Patent


Assay Description
EGFR inhibitory activity of compounds of the present invention is quantified employing the EGFR HTRF assay.


US Patent US8524722 (2013)


BindingDB Entry DOI: 10.7270/Q2B856RQ
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM101235
PNG
(US8524722, 86)
Show SMILES CN(C)C\C=C\C(=O)N1Cc2sc3ncnc(Nc4ccc(OCc5cccc(F)c5)c(Cl)c4)c3c2C1
Show InChI InChI=1S/C27H25ClFN5O2S/c1-33(2)10-4-7-24(35)34-13-20-23(14-34)37-27-25(20)26(30-16-31-27)32-19-8-9-22(21(28)12-19)36-15-17-5-3-6-18(29)11-17/h3-9,11-12,16H,10,13-15H2,1-2H3,(H,30,31,32)/b7-4+
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n/an/a 5n/an/an/an/a7.022



Bayer Intellectual Property GmbH

US Patent


Assay Description
EGFR inhibitory activity of compounds of the present invention is quantified employing the EGFR HTRF assay.


US Patent US8524722 (2013)


BindingDB Entry DOI: 10.7270/Q2B856RQ
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM101236
PNG
(US8524722, 87)
Show SMILES CN(C)C\C=C\C(=O)N1Cc2sc3ncnc(Nc4ccc(OCc5ccccn5)c(Cl)c4)c3c2C1
Show InChI InChI=1S/C26H25ClN6O2S/c1-32(2)11-5-7-23(34)33-13-19-22(14-33)36-26-24(19)25(29-16-30-26)31-17-8-9-21(20(27)12-17)35-15-18-6-3-4-10-28-18/h3-10,12,16H,11,13-15H2,1-2H3,(H,29,30,31)/b7-5+
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n/an/a 19n/an/an/an/a7.022



Bayer Intellectual Property GmbH

US Patent


Assay Description
EGFR inhibitory activity of compounds of the present invention is quantified employing the EGFR HTRF assay.


US Patent US8524722 (2013)


BindingDB Entry DOI: 10.7270/Q2B856RQ
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM101237
PNG
(US8524722, 90)
Show SMILES CC(C)N(C)C\C=C\C(=O)N1CCc2c(C1)oc1ncnc(Nc3ccc(F)c(Cl)c3)c21
Show InChI InChI=1S/C23H25ClFN5O2/c1-14(2)29(3)9-4-5-20(31)30-10-8-16-19(12-30)32-23-21(16)22(26-13-27-23)28-15-6-7-18(25)17(24)11-15/h4-7,11,13-14H,8-10,12H2,1-3H3,(H,26,27,28)/b5-4+
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n/an/a 1n/an/an/an/a7.022



Bayer Intellectual Property GmbH

US Patent


Assay Description
EGFR inhibitory activity of compounds of the present invention is quantified employing the EGFR HTRF assay.


US Patent US8524722 (2013)


BindingDB Entry DOI: 10.7270/Q2B856RQ
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM101238
PNG
(US8524722, 95)
Show SMILES CN(C)C\C=C\C(=O)N1CCc2c(C1)sc1ncc(C#N)c(Nc3ccc(F)c(Cl)c3)c21
Show InChI InChI=1S/C23H21ClFN5OS/c1-29(2)8-3-4-20(31)30-9-7-16-19(13-30)32-23-21(16)22(14(11-26)12-27-23)28-15-5-6-18(25)17(24)10-15/h3-6,10,12H,7-9,13H2,1-2H3,(H,27,28)/b4-3+
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n/an/a 10n/an/an/an/a7.022



Bayer Intellectual Property GmbH

US Patent


Assay Description
EGFR inhibitory activity of compounds of the present invention is quantified employing the EGFR HTRF assay.


US Patent US8524722 (2013)


BindingDB Entry DOI: 10.7270/Q2B856RQ
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM101239
PNG
(US8524722, 119)
Show SMILES Clc1ccc(Nc2ncnc3sc4CN(CCc4c23)C(=O)\C=C\CNC23CC4CC(CC(C4)C2)C3)cc1Cl
Show InChI InChI=1S/C29H31Cl2N5OS/c30-22-4-3-20(11-23(22)31)35-27-26-21-5-7-36(15-24(21)38-28(26)33-16-32-27)25(37)2-1-6-34-29-12-17-8-18(13-29)10-19(9-17)14-29/h1-4,11,16-19,34H,5-10,12-15H2,(H,32,33,35)/b2-1+
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n/an/a 1n/an/an/an/a7.022



Bayer Intellectual Property GmbH

US Patent


Assay Description
EGFR inhibitory activity of compounds of the present invention is quantified employing the EGFR HTRF assay.


US Patent US8524722 (2013)


BindingDB Entry DOI: 10.7270/Q2B856RQ
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM101240
PNG
(US8524722, 123)
Show SMILES CC(C)C(C)C\C=C\C(=O)N1CCc2c(C1)sc1ncnc(Nc3cc(O)cc(Cl)c3)c21
Show InChI InChI=1S/C24H27ClN4O2S/c1-14(2)15(3)5-4-6-21(31)29-8-7-19-20(12-29)32-24-22(19)23(26-13-27-24)28-17-9-16(25)10-18(30)11-17/h4,6,9-11,13-15,30H,5,7-8,12H2,1-3H3,(H,26,27,28)/b6-4+
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n/an/a 1n/an/an/an/a7.022



Bayer Intellectual Property GmbH

US Patent


Assay Description
EGFR inhibitory activity of compounds of the present invention is quantified employing the EGFR HTRF assay.


US Patent US8524722 (2013)


BindingDB Entry DOI: 10.7270/Q2B856RQ
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM101241
PNG
(US8524722, 134)
Show SMILES CN(C\C=C\C(=O)N1CCc2c(C1)sc1ncnc(Nc3cc(O)c(Cl)c(Cl)c3)c21)C(C)(C)C
Show InChI InChI=1S/C24H27Cl2N5O2S/c1-24(2,3)30(4)8-5-6-19(33)31-9-7-15-18(12-31)34-23-20(15)22(27-13-28-23)29-14-10-16(25)21(26)17(32)11-14/h5-6,10-11,13,32H,7-9,12H2,1-4H3,(H,27,28,29)/b6-5+
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n/an/a 1n/an/an/an/a7.022



Bayer Intellectual Property GmbH

US Patent


Assay Description
EGFR inhibitory activity of compounds of the present invention is quantified employing the EGFR HTRF assay.


US Patent US8524722 (2013)


BindingDB Entry DOI: 10.7270/Q2B856RQ
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM101242
PNG
(US8524722, 139)
Show SMILES CC(C)N(C)C\C=C\C(=O)N1CCc2sc3ncnc(Nc4ccc(Cl)c(Cl)c4)c3c2C1
Show InChI InChI=1S/C23H25Cl2N5OS/c1-14(2)29(3)9-4-5-20(31)30-10-8-19-16(12-30)21-22(26-13-27-23(21)32-19)28-15-6-7-17(24)18(25)11-15/h4-7,11,13-14H,8-10,12H2,1-3H3,(H,26,27,28)/b5-4+
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n/an/a 9.20n/an/an/an/a7.022



Bayer Intellectual Property GmbH

US Patent


Assay Description
EGFR inhibitory activity of compounds of the present invention is quantified employing the EGFR HTRF assay.


US Patent US8524722 (2013)


BindingDB Entry DOI: 10.7270/Q2B856RQ
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM101243
PNG
(US8524722, 143)
Show SMILES Clc1ccc(Nc2ncnc3sc4CN(CCCc4c23)C(=O)\C=C\CN2CCCOCC2)cc1Cl
Show InChI InChI=1S/C25H27Cl2N5O2S/c26-19-7-6-17(14-20(19)27)30-24-23-18-4-1-10-32(15-21(18)35-25(23)29-16-28-24)22(33)5-2-8-31-9-3-12-34-13-11-31/h2,5-7,14,16H,1,3-4,8-13,15H2,(H,28,29,30)/b5-2+
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n/an/a 1n/an/an/an/a7.022



Bayer Intellectual Property GmbH

US Patent


Assay Description
EGFR inhibitory activity of compounds of the present invention is quantified employing the EGFR HTRF assay.


US Patent US8524722 (2013)


BindingDB Entry DOI: 10.7270/Q2B856RQ
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM101244
PNG
(US8524722, 148)
Show SMILES Clc1ccc(Nc2c(cnc3sc4CN(CCc4c23)C(=O)\C=C\CN2CCCOCC2)C#N)cc1Cl
Show InChI InChI=1S/C26H25Cl2N5O2S/c27-20-5-4-18(13-21(20)28)31-25-17(14-29)15-30-26-24(25)19-6-9-33(16-22(19)36-26)23(34)3-1-7-32-8-2-11-35-12-10-32/h1,3-5,13,15H,2,6-12,16H2,(H,30,31)/b3-1+
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n/an/a 4.30n/an/an/an/a7.022



Bayer Intellectual Property GmbH

US Patent


Assay Description
EGFR inhibitory activity of compounds of the present invention is quantified employing the EGFR HTRF assay.


US Patent US8524722 (2013)


BindingDB Entry DOI: 10.7270/Q2B856RQ
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM101245
PNG
(US8524722, 151)
Show SMILES CC(C)N(C)C\C=C\C(=O)N1CCc2c(C1)sc1ncc(C#N)c(Nc3ccc4n(Cc5cccc(F)c5)ncc4c3)c21
Show InChI InChI=1S/C33H32FN7OS/c1-21(2)39(3)12-5-8-30(42)40-13-11-27-29(20-40)43-33-31(27)32(24(16-35)17-36-33)38-26-9-10-28-23(15-26)18-37-41(28)19-22-6-4-7-25(34)14-22/h4-10,14-15,17-18,21H,11-13,19-20H2,1-3H3,(H,36,38)/b8-5+
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n/an/a 6.40n/an/an/an/a7.022



Bayer Intellectual Property GmbH

US Patent


Assay Description
EGFR inhibitory activity of compounds of the present invention is quantified employing the EGFR HTRF assay.


US Patent US8524722 (2013)


BindingDB Entry DOI: 10.7270/Q2B856RQ
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM54680
PNG
((3Z)-5-bromanyl-3-(3-oxidanylidene-1H-indol-2-ylid...)
Show SMILES Brc1ccc2NC(=O)C(=C3Nc4ccccc4C3=O)c2c1
Show InChI InChI=1S/C16H9BrN2O2/c17-8-5-6-12-10(7-8)13(16(21)19-12)14-15(20)9-3-1-2-4-11(9)18-14/h1-7,18H,(H,19,21)
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n/an/a>1.00E+4n/an/an/an/a7.022



Schering AG



Assay Description
Inhibition assay using CDK and selective kinases such as gsk3, EGFR, c-Kit, InsR and KDR.


Chembiochem 6: 531-40 (2005)


Article DOI: 10.1002/cbic.200400108
BindingDB Entry DOI: 10.7270/Q2B56H8H
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM84534
PNG
(Indirubin derivative, 20)
Show SMILES OS(=O)(=O)c1ccc2NC(=O)C(=C3Nc4ccccc4C3=O)c2c1
Show InChI InChI=1S/C16H10N2O5S/c19-15-9-3-1-2-4-11(9)17-14(15)13-10-7-8(24(21,22)23)5-6-12(10)18-16(13)20/h1-7,17H,(H,18,20)(H,21,22,23)
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n/an/a>1.00E+4n/an/an/an/a7.022



Schering AG



Assay Description
Inhibition assay using CDK and selective kinases such as gsk3, EGFR, c-Kit, InsR and KDR.


Chembiochem 6: 531-40 (2005)


Article DOI: 10.1002/cbic.200400108
BindingDB Entry DOI: 10.7270/Q2B56H8H
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM84553
PNG
(Indirubin derivative, 28a | Indirubin derivative, ...)
Show SMILES CN(C)CCN(C)S(=O)(=O)c1ccc2NC(=O)C(C3=Nc4ccccc4C3(C)O)c2c1
Show InChI InChI=1S/C22H26N4O4S/c1-22(28)16-7-5-6-8-18(16)23-20(22)19-15-13-14(9-10-17(15)24-21(19)27)31(29,30)26(4)12-11-25(2)3/h5-10,13,19,28H,11-12H2,1-4H3,(H,24,27)
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n/an/a>1.00E+4n/an/an/an/a7.022



Schering AG



Assay Description
Inhibition assay using CDK and selective kinases such as gsk3, EGFR, c-Kit, InsR and KDR.


Chembiochem 6: 531-40 (2005)


Article DOI: 10.1002/cbic.200400108
BindingDB Entry DOI: 10.7270/Q2B56H8H
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM84553
PNG
(Indirubin derivative, 28a | Indirubin derivative, ...)
Show SMILES CN(C)CCN(C)S(=O)(=O)c1ccc2NC(=O)C(C3=Nc4ccccc4C3(C)O)c2c1
Show InChI InChI=1S/C22H26N4O4S/c1-22(28)16-7-5-6-8-18(16)23-20(22)19-15-13-14(9-10-17(15)24-21(19)27)31(29,30)26(4)12-11-25(2)3/h5-10,13,19,28H,11-12H2,1-4H3,(H,24,27)
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n/an/a>1.00E+4n/an/an/an/a7.022



Schering AG



Assay Description
Inhibition assay using CDK and selective kinases such as gsk3, EGFR, c-Kit, InsR and KDR.


Chembiochem 6: 531-40 (2005)


Article DOI: 10.1002/cbic.200400108
BindingDB Entry DOI: 10.7270/Q2B56H8H
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM84555
PNG
(Indirubin derivative, 30a | Indirubin derivative, ...)
Show SMILES CN(C)CCN(C)S(=O)(=O)c1ccc2NC(=O)C(C3=Nc4ccccc4C3(O)CC=C)c2c1
Show InChI InChI=1S/C24H28N4O4S/c1-5-12-24(30)18-8-6-7-9-20(18)25-22(24)21-17-15-16(10-11-19(17)26-23(21)29)33(31,32)28(4)14-13-27(2)3/h5-11,15,21,30H,1,12-14H2,2-4H3,(H,26,29)
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n/an/a>1.00E+4n/an/an/an/a7.022



Schering AG



Assay Description
Inhibition assay using CDK and selective kinases such as gsk3, EGFR, c-Kit, InsR and KDR.


Chembiochem 6: 531-40 (2005)


Article DOI: 10.1002/cbic.200400108
BindingDB Entry DOI: 10.7270/Q2B56H8H
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM84555
PNG
(Indirubin derivative, 30a | Indirubin derivative, ...)
Show SMILES CN(C)CCN(C)S(=O)(=O)c1ccc2NC(=O)C(C3=Nc4ccccc4C3(O)CC=C)c2c1
Show InChI InChI=1S/C24H28N4O4S/c1-5-12-24(30)18-8-6-7-9-20(18)25-22(24)21-17-15-16(10-11-19(17)26-23(21)29)33(31,32)28(4)14-13-27(2)3/h5-11,15,21,30H,1,12-14H2,2-4H3,(H,26,29)
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n/an/a>1.00E+4n/an/an/an/a7.022



Schering AG



Assay Description
Inhibition assay using CDK and selective kinases such as gsk3, EGFR, c-Kit, InsR and KDR.


Chembiochem 6: 531-40 (2005)


Article DOI: 10.1002/cbic.200400108
BindingDB Entry DOI: 10.7270/Q2B56H8H
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM6619
PNG
(3-[(9bR)-5-oxo-1H,2H,3H,5H,9bH-benzo[a]pyrrolizin-...)
Show SMILES O=C(Nc1ccccn1)Nc1cccc2C(=O)N3CCC[C@@H]3c12
Show InChI InChI=1S/C17H16N4O2/c22-16-11-5-3-6-12(15(11)13-7-4-10-21(13)16)19-17(23)20-14-8-1-2-9-18-14/h1-3,5-6,8-9,13H,4,7,10H2,(H2,18,19,20,23)/t13-/m1/s1
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n/an/a>2.00E+4n/an/an/an/a7.022



Banyu Tsukuba Research Institute



Assay Description
Src, Lck, Flt-1, ZAP, EGFR, FGFR1, and PFGFR-beta were assayed in the Merck research laboratory (Homogeneous proximity tyrosine kinase assays: scinti...


J Med Chem 44: 4628-40 (2001)


Article DOI: 10.1021/jm010326y
BindingDB Entry DOI: 10.7270/Q2BV7DS8
More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM270589
PNG
((S)-8-chloro-N6-((1- (1- (difluoromethyl) cyclopro...)
Show SMILES Cc1nc(F)ccc1[C@H](Nc1cc(Cl)c2ncnc(NCC(C)(C)C)c2c1)c1cn(nn1)C1(CC1)C(F)F
Show InChI InChI=1S/C26H28ClF3N8/c1-14-16(5-6-20(28)34-14)22(19-11-38(37-36-19)26(7-8-26)24(29)30)35-15-9-17-21(18(27)10-15)32-13-33-23(17)31-12-25(2,3)4/h5-6,9-11,13,22,24,35H,7-8,12H2,1-4H3,(H,31,32,33)/t22-/m0/s1
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US Patent
n/an/an/an/a 28n/an/a7.025



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 US10059695 (2018)

More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM270590
PNG
((S)-6-(((1-(1- (difluoromethyl) cyclopropyl)-1H-1,...)
Show SMILES Cc1nc(F)ccc1[C@H](Nc1cc(C#N)c2ncnc(NCC(C)(C)C)c2c1)c1cn(nn1)C1(CC1)C(F)F
Show InChI InChI=1S/C27H28F3N9/c1-15-18(5-6-21(28)35-15)23(20-12-39(38-37-20)27(7-8-27)25(29)30)36-17-9-16(11-31)22-19(10-17)24(34-14-33-22)32-13-26(2,3)4/h5-6,9-10,12,14,23,25,36H,7-8,13H2,1-4H3,(H,32,33,34)/t23-/m0/s1
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n/an/a 1.70n/an/an/an/a7.025



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 US10059695 (2018)

More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM270590
PNG
((S)-6-(((1-(1- (difluoromethyl) cyclopropyl)-1H-1,...)
Show SMILES Cc1nc(F)ccc1[C@H](Nc1cc(C#N)c2ncnc(NCC(C)(C)C)c2c1)c1cn(nn1)C1(CC1)C(F)F
Show InChI InChI=1S/C27H28F3N9/c1-15-18(5-6-21(28)35-15)23(20-12-39(38-37-20)27(7-8-27)25(29)30)36-17-9-16(11-31)22-19(10-17)24(34-14-33-22)32-13-26(2,3)4/h5-6,9-10,12,14,23,25,36H,7-8,13H2,1-4H3,(H,32,33,34)/t23-/m0/s1
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n/an/an/an/a 36n/an/a7.025



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 US10059695 (2018)

More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM270591
PNG
((S)-3-(((8-chloro-4- (neopentylamino) quinazolin-6...)
Show SMILES Cc1c(cccc1[C@H](Nc1cc(Cl)c2ncnc(NCC(C)(C)C)c2c1)c1cn(nn1)C1(CC1)C(F)F)C#N
Show InChI InChI=1S/C28H29ClF2N8/c1-16-17(12-32)6-5-7-19(16)24(22-13-39(38-37-22)28(8-9-28)26(30)31)36-18-10-20-23(21(29)11-18)34-15-35-25(20)33-14-27(2,3)4/h5-7,10-11,13,15,24,26,36H,8-9,14H2,1-4H3,(H,33,34,35)/t24-/m0/s1
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n/an/a 1.60n/an/an/an/a7.025



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 US10059695 (2018)

More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM270592
PNG
((S)-6-(((1-(1- (difluoromethyl) cyclopropyl)-1H-1,...)
Show SMILES Cn1ccc2c(cccc2c1=O)[C@H](Nc1cc(C#N)c2ncnc(NCC(C)(C)C)c2c1)c1cn(nn1)C1(CC1)C(F)F
Show InChI InChI=1S/C31H31F2N9O/c1-30(2,3)16-35-27-23-13-19(12-18(14-34)25(23)36-17-37-27)38-26(24-15-42(40-39-24)31(9-10-31)29(32)33)21-6-5-7-22-20(21)8-11-41(4)28(22)43/h5-8,11-13,15,17,26,29,38H,9-10,16H2,1-4H3,(H,35,36,37)/t26-/m0/s1
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n/an/a 1.20n/an/an/an/a7.025



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 US10059695 (2018)

More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM270592
PNG
((S)-6-(((1-(1- (difluoromethyl) cyclopropyl)-1H-1,...)
Show SMILES Cn1ccc2c(cccc2c1=O)[C@H](Nc1cc(C#N)c2ncnc(NCC(C)(C)C)c2c1)c1cn(nn1)C1(CC1)C(F)F
Show InChI InChI=1S/C31H31F2N9O/c1-30(2,3)16-35-27-23-13-19(12-18(14-34)25(23)36-17-37-27)38-26(24-15-42(40-39-24)31(9-10-31)29(32)33)21-6-5-7-22-20(21)8-11-41(4)28(22)43/h5-8,11-13,15,17,26,29,38H,9-10,16H2,1-4H3,(H,35,36,37)/t26-/m0/s1
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n/an/an/an/a 11.3n/an/a7.025



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 US10059695 (2018)

More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM270593
PNG
((S)-5-(((8-chloro-4- (neopentylamino) quinazolin-6...)
Show SMILES Cn1ccc2c(cccc2c1=O)[C@H](Nc1cc(Cl)c2ncnc(NCC(C)(C)C)c2c1)c1cn(nn1)C1(CC1)C(F)F
Show InChI InChI=1S/C30H31ClF2N8O/c1-29(2,3)15-34-26-21-12-17(13-22(31)24(21)35-16-36-26)37-25(23-14-41(39-38-23)30(9-10-30)28(32)33)19-6-5-7-20-18(19)8-11-40(4)27(20)42/h5-8,11-14,16,25,28,37H,9-10,15H2,1-4H3,(H,34,35,36)/t25-/m0/s1
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n/an/a 2.40n/an/an/an/a7.025



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 US10059695 (2018)

More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM270593
PNG
((S)-5-(((8-chloro-4- (neopentylamino) quinazolin-6...)
Show SMILES Cn1ccc2c(cccc2c1=O)[C@H](Nc1cc(Cl)c2ncnc(NCC(C)(C)C)c2c1)c1cn(nn1)C1(CC1)C(F)F
Show InChI InChI=1S/C30H31ClF2N8O/c1-29(2,3)15-34-26-21-12-17(13-22(31)24(21)35-16-36-26)37-25(23-14-41(39-38-23)30(9-10-30)28(32)33)19-6-5-7-20-18(19)8-11-40(4)27(20)42/h5-8,11-14,16,25,28,37H,9-10,15H2,1-4H3,(H,34,35,36)/t25-/m0/s1
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n/an/an/an/a 25.5n/an/a7.025



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 US10059695 (2018)

More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM270594
PNG
((S)-5-((1- (bicyclo[1.1.1]pentan- 1-yl)-1H-1,2,3- ...)
Show SMILES Cn1ccc2c(cccc2c1=O)[C@H](Nc1cc(Cl)c2ncnc(NCC(C)(C)C)c2c1)c1cn(nn1)C12CC(C1)C2
Show InChI InChI=1S/C31H33ClN8O/c1-30(2,3)16-33-28-23-10-19(11-24(32)26(23)34-17-35-28)36-27(25-15-40(38-37-25)31-12-18(13-31)14-31)21-6-5-7-22-20(21)8-9-39(4)29(22)41/h5-11,15,17-18,27,36H,12-14,16H2,1-4H3,(H,33,34,35)/t18?,27-,31?/m0/s1
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n/an/a 1.70n/an/an/an/a7.025



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 US10059695 (2018)

More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM270594
PNG
((S)-5-((1- (bicyclo[1.1.1]pentan- 1-yl)-1H-1,2,3- ...)
Show SMILES Cn1ccc2c(cccc2c1=O)[C@H](Nc1cc(Cl)c2ncnc(NCC(C)(C)C)c2c1)c1cn(nn1)C12CC(C1)C2
Show InChI InChI=1S/C31H33ClN8O/c1-30(2,3)16-33-28-23-10-19(11-24(32)26(23)34-17-35-28)36-27(25-15-40(38-37-25)31-12-18(13-31)14-31)21-6-5-7-22-20(21)8-9-39(4)29(22)41/h5-11,15,17-18,27,36H,12-14,16H2,1-4H3,(H,33,34,35)/t18?,27-,31?/m0/s1
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n/an/an/an/a 12.1n/an/a7.025



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 US10059695 (2018)

More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM270595
PNG
(US10059695, II-1 | benzyl 4-(4-(((8- chloro-4-((3-...)
Show SMILES Fc1ccc(Nc2ncnc3c(Cl)cc(NC(c4cn(nn4)C4CCN(CC4)C(=O)OCc4ccccc4)c4ccccc4)cc23)cc1Cl
Show InChI InChI=1S/C36H31Cl2FN8O2/c37-29-18-25(11-12-31(29)39)43-35-28-17-26(19-30(38)34(28)40-22-41-35)42-33(24-9-5-2-6-10-24)32-20-47(45-44-32)27-13-15-46(16-14-27)36(48)49-21-23-7-3-1-4-8-23/h1-12,17-20,22,27,33,42H,13-16,21H2,(H,40,41,43)
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n/an/a 8.48E+3n/an/an/an/a7.025



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 US10059695 (2018)

More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM270596
PNG
(8-chloro-N4-(3- chloro-4- fluorophenyl)-N6- (pheny...)
Show SMILES Fc1ccc(Nc2ncnc3c(Cl)cc(NC(c4cn(nn4)C4CCNCC4)c4ccccc4)cc23)cc1Cl
Show InChI InChI=1S/C28H25Cl2FN8/c29-22-13-18(6-7-24(22)31)36-28-21-12-19(14-23(30)27(21)33-16-34-28)35-26(17-4-2-1-3-5-17)25-15-39(38-37-25)20-8-10-32-11-9-20/h1-7,12-16,20,26,32,35H,8-11H2,(H,33,34,36)
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n/an/a 28n/an/an/an/a7.025



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 US10059695 (2018)

More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM270597
PNG
(8-chloro-N4-(3- chloro-4- fluorophenyl)-N6- ((1-(1...)
Show SMILES CCN1CCC(CC1)n1cc(nn1)C(Nc1cc(Cl)c2ncnc(Nc3ccc(F)c(Cl)c3)c2c1)c1ccccc1
Show InChI InChI=1S/C30H29Cl2FN8/c1-2-40-12-10-22(11-13-40)41-17-27(38-39-41)28(19-6-4-3-5-7-19)36-21-14-23-29(25(32)16-21)34-18-35-30(23)37-20-8-9-26(33)24(31)15-20/h3-9,14-18,22,28,36H,2,10-13H2,1H3,(H,34,35,37)
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n/an/a 19n/an/an/an/a7.025



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 US10059695 (2018)

More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM270598
PNG
((S)-8-chloro-N4-(3- chloro-4- fluorophenyl)-N6- ((...)
Show SMILES CCN1CCC(CC1)n1cc(nn1)[C@@H](Nc1cc(Cl)c2ncnc(Nc3ccc(F)c(Cl)c3)c2c1)c1ccccc1
Show InChI InChI=1S/C30H29Cl2FN8/c1-2-40-12-10-22(11-13-40)41-17-27(38-39-41)28(19-6-4-3-5-7-19)36-21-14-23-29(25(32)16-21)34-18-35-30(23)37-20-8-9-26(33)24(31)15-20/h3-9,14-18,22,28,36H,2,10-13H2,1H3,(H,34,35,37)/t28-/m0/s1
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n/an/a 5.90n/an/an/an/a7.025



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 US10059695 (2018)

More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM270598
PNG
((S)-8-chloro-N4-(3- chloro-4- fluorophenyl)-N6- ((...)
Show SMILES CCN1CCC(CC1)n1cc(nn1)[C@@H](Nc1cc(Cl)c2ncnc(Nc3ccc(F)c(Cl)c3)c2c1)c1ccccc1
Show InChI InChI=1S/C30H29Cl2FN8/c1-2-40-12-10-22(11-13-40)41-17-27(38-39-41)28(19-6-4-3-5-7-19)36-21-14-23-29(25(32)16-21)34-18-35-30(23)37-20-8-9-26(33)24(31)15-20/h3-9,14-18,22,28,36H,2,10-13H2,1H3,(H,34,35,37)/t28-/m0/s1
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n/an/an/an/a 254n/an/a7.025



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 US10059695 (2018)

More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM270599
PNG
((S)-N6-((1-(1-(tert- butyl)piperidin-4- yl)-1H-1,2...)
Show SMILES CC(C)(C)N1CCC(CC1)n1cc(nn1)[C@@H](Nc1ccc2ncnc(Nc3ccc(F)c(Cl)c3)c2c1)c1ccc(Cl)cc1
Show InChI InChI=1S/C32H33Cl2FN8/c1-32(2,3)42-14-12-24(13-15-42)43-18-29(40-41-43)30(20-4-6-21(33)7-5-20)38-22-9-11-28-25(16-22)31(37-19-36-28)39-23-8-10-27(35)26(34)17-23/h4-11,16-19,24,30,38H,12-15H2,1-3H3,(H,36,37,39)/t30-/m0/s1
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n/an/a 72n/an/an/an/a7.025



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 US10059695 (2018)

More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM270600
PNG
((S)-N4-(3-chloro-4- fluorophenyl)-N6- ((4-chloroph...)
Show SMILES Fc1ccc(Nc2ncnc3ccc(N[C@H](c4cn(nn4)C4CCNCC4)c4ccc(Cl)cc4)cc23)cc1Cl
Show InChI InChI=1S/C28H25Cl2FN8/c29-18-3-1-17(2-4-18)27(26-15-39(38-37-26)21-9-11-32-12-10-21)35-19-6-8-25-22(13-19)28(34-16-33-25)36-20-5-7-24(31)23(30)14-20/h1-8,13-16,21,27,32,35H,9-12H2,(H,33,34,36)/t27-/m0/s1
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n/an/a 49n/an/an/an/a7.025



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 US10059695 (2018)

More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (Human))
BDBM270601
PNG
((S)-N4-(3-chloro-4- fluorophenyl)-N6- ((4-chloroph...)
Show SMILES Fc1ccc(Nc2ncnc3ccc(N[C@H](c4cn(nn4)C4COC4)c4ccc(Cl)cc4)cc23)cc1Cl
Show InChI InChI=1S/C26H20Cl2FN7O/c27-16-3-1-15(2-4-16)25(24-11-36(35-34-24)19-12-37-13-19)32-17-6-8-23-20(9-17)26(31-14-30-23)33-18-5-7-22(29)21(28)10-18/h1-11,14,19,25,32H,12-13H2,(H,30,31,33)/t25-/m0/s1
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n/an/a 284n/an/an/an/a7.025



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 US10059695 (2018)

More data for this
Ligand-Target Pair
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