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Patent code US10214545

Compile Data Set for Download or QSAR
Found 36 hits of Enzyme Inhibition Constant Data   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358869
PNG
(3-(1-Benzofuran-2-yl)-N-[(2S)-1-hydroxy-3-methylbu...)
Show SMILES CC(C)[C@@H](CO)NC(=O)c1ccc2ncc(-c3cc4ccccc4o3)n2n1
Show InChI InChI=1S/C20H20N4O3/c1-12(2)15(11-25)22-20(26)14-7-8-19-21-10-16(24(19)23-14)18-9-13-5-3-4-6-17(13)27-18/h3-10,12,15,25H,11H2,1-2H3,(H,22,26)/t15-/m1/s1
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US Patent
n/an/a 1.30n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity of compounds of the present invention was quantified employing the MKNK1 TR-FRET assay as described in the following paragr...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358860
PNG
(N-[3-(dimethylamino)propyl]-3-[4-(morpholin-4-yl)f...)
Show SMILES CN(C)CCCNC(=O)c1ccc2ncc(-c3cc4c(nccc4o3)N3CCOCC3)n2n1
Show InChI InChI=1S/C23H27N7O3/c1-28(2)9-3-7-25-23(31)17-4-5-21-26-15-18(30(21)27-17)20-14-16-19(33-20)6-8-24-22(16)29-10-12-32-13-11-29/h4-6,8,14-15H,3,7,9-13H2,1-2H3,(H,25,31)
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US Patent
n/an/a 1.5n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity of compounds of the present invention was quantified employing the MKNK1 TR-FRET assay as described in the following paragr...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358868
PNG
(3-(1-Benzofuran-2-yl)-N-[2-(dimethylamino)ethyl]im...)
Show SMILES CN(C)CCNC(=O)c1ccc2ncc(-c3cc4ccccc4o3)n2n1
Show InChI InChI=1S/C19H19N5O2/c1-23(2)10-9-20-19(25)14-7-8-18-21-12-15(24(18)22-14)17-11-13-5-3-4-6-16(13)26-17/h3-8,11-12H,9-10H2,1-2H3,(H,20,25)
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US Patent
n/an/a 1.70n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity of compounds of the present invention was quantified employing the MKNK1 TR-FRET assay as described in the following paragr...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358856
PNG
(N-(2-methoxyethyl)-N-methyl-3-[4-(morpholin-4-yl)f...)
Show SMILES COCCN(C)C(=O)c1ccc2ncc(-c3cc4c(nccc4o3)N3CCOCC3)n2n1
Show InChI InChI=1S/C22H24N6O4/c1-26(7-10-30-2)22(29)16-3-4-20-24-14-17(28(20)25-16)19-13-15-18(32-19)5-6-23-21(15)27-8-11-31-12-9-27/h3-6,13-14H,7-12H2,1-2H3
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US Patent
n/an/a 2.60n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity of compounds of the present invention was quantified employing the MKNK1 TR-FRET assay as described in the following paragr...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358858
PNG
(N-[(2R)-1-hydroxypropan-2-yl]-3-[4-(morpholin-4-yl...)
Show SMILES C[C@H](CO)NC(=O)c1ccc2ncc(-c3cc4c(nccc4o3)N3CCOCC3)n2n1
Show InChI InChI=1S/C21H22N6O4/c1-13(12-28)24-21(29)15-2-3-19-23-11-16(27(19)25-15)18-10-14-17(31-18)4-5-22-20(14)26-6-8-30-9-7-26/h2-5,10-11,13,28H,6-9,12H2,1H3,(H,24,29)/t13-/m1/s1
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US Patent
n/an/a 2.80n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity of compounds of the present invention was quantified employing the MKNK1 TR-FRET assay as described in the following paragr...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358861
PNG
(3-(1-Benzofuran-2-yl)-N-[3-(dimethylamino)propyl]i...)
Show SMILES CN(C)CCCNC(=O)c1ccc2ncc(-c3cc4ccccc4o3)n2n1
Show InChI InChI=1S/C20H21N5O2/c1-24(2)11-5-10-21-20(26)15-8-9-19-22-13-16(25(19)23-15)18-12-14-6-3-4-7-17(14)27-18/h3-4,6-9,12-13H,5,10-11H2,1-2H3,(H,21,26)
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US Patent
n/an/a 3.30n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity of compounds of the present invention was quantified employing the MKNK1 TR-FRET assay as described in the following paragr...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358853
PNG
(N-(3-methoxypropyl)-3-[4-(morpholin-4-yl)furo[3,2-...)
Show SMILES COCCCNC(=O)c1ccc2ncc(-c3cc4c(nccc4o3)N3CCOCC3)n2n1
Show InChI InChI=1S/C22H24N6O4/c1-30-10-2-6-24-22(29)16-3-4-20-25-14-17(28(20)26-16)19-13-15-18(32-19)5-7-23-21(15)27-8-11-31-12-9-27/h3-5,7,13-14H,2,6,8-12H2,1H3,(H,24,29)
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US Patent
n/an/a 3.80n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity of compounds of the present invention was quantified employing the MKNK1 TR-FRET assay as described in the following paragr...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358862
PNG
(3-(1-Benzofuran-2-yl)-N-[(2R)-1-hydroxypropan-2-yl...)
Show SMILES C[C@H](CO)NC(=O)c1ccc2ncc(-c3cc4ccccc4o3)n2n1
Show InChI InChI=1S/C18H16N4O3/c1-11(10-23)20-18(24)13-6-7-17-19-9-14(22(17)21-13)16-8-12-4-2-3-5-15(12)25-16/h2-9,11,23H,10H2,1H3,(H,20,24)/t11-/m1/s1
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US Patent
n/an/a 4.10n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity of compounds of the present invention was quantified employing the MKNK1 TR-FRET assay as described in the following paragr...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358852
PNG
(N-benzyl-3-[4-(morpholin-4-yl)furo[3,2-c]pyridin-2...)
Show SMILES O=C(NCc1ccccc1)c1ccc2ncc(-c3cc4c(nccc4o3)N3CCOCC3)n2n1
Show InChI InChI=1S/C25H22N6O3/c32-25(28-15-17-4-2-1-3-5-17)19-6-7-23-27-16-20(31(23)29-19)22-14-18-21(34-22)8-9-26-24(18)30-10-12-33-13-11-30/h1-9,14,16H,10-13,15H2,(H,28,32)
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US Patent
n/an/a 4.40n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity of compounds of the present invention was quantified employing the MKNK1 TR-FRET assay as described in the following paragr...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358860
PNG
(N-[3-(dimethylamino)propyl]-3-[4-(morpholin-4-yl)f...)
Show SMILES CN(C)CCCNC(=O)c1ccc2ncc(-c3cc4c(nccc4o3)N3CCOCC3)n2n1
Show InChI InChI=1S/C23H27N7O3/c1-28(2)9-3-7-25-23(31)17-4-5-21-26-15-18(30(21)27-17)20-14-16-19(33-20)6-8-24-22(16)29-10-12-32-13-11-29/h4-6,8,14-15H,3,7,9-13H2,1-2H3,(H,25,31)
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US Patent
n/an/a 4.5n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358857
PNG
(N-(2-methoxyethyl)-3-[4-(morpholin-4-yl)furo[3,2-c...)
Show SMILES COCCNC(=O)c1ccc2ncc(-c3cc4c(nccc4o3)N3CCOCC3)n2n1
Show InChI InChI=1S/C21H22N6O4/c1-29-9-6-23-21(28)15-2-3-19-24-13-16(27(19)25-15)18-12-14-17(31-18)4-5-22-20(14)26-7-10-30-11-8-26/h2-5,12-13H,6-11H2,1H3,(H,23,28)
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US Patent
n/an/a 4.60n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity of compounds of the present invention was quantified employing the MKNK1 TR-FRET assay as described in the following paragr...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358863
PNG
(3-(1-Benzofuran-2-yl)-N-(3-methoxypropyl)imidazo[1...)
Show SMILES COCCCNC(=O)c1ccc2ncc(-c3cc4ccccc4o3)n2n1
Show InChI InChI=1S/C19H18N4O3/c1-25-10-4-9-20-19(24)14-7-8-18-21-12-15(23(18)22-14)17-11-13-5-2-3-6-16(13)26-17/h2-3,5-8,11-12H,4,9-10H2,1H3,(H,20,24)
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US Patent
n/an/a 4.90n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity of compounds of the present invention was quantified employing the MKNK1 TR-FRET assay as described in the following paragr...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358865
PNG
(3-(1-Benzofuran-2-yl)-N-benzylimidazo[1,2-b]pyrida...)
Show SMILES O=C(NCc1ccccc1)c1ccc2ncc(-c3cc4ccccc4o3)n2n1
Show InChI InChI=1S/C22H16N4O2/c27-22(24-13-15-6-2-1-3-7-15)17-10-11-21-23-14-18(26(21)25-17)20-12-16-8-4-5-9-19(16)28-20/h1-12,14H,13H2,(H,24,27)
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US Patent
n/an/a 5.20n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity of compounds of the present invention was quantified employing the MKNK1 TR-FRET assay as described in the following paragr...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358852
PNG
(N-benzyl-3-[4-(morpholin-4-yl)furo[3,2-c]pyridin-2...)
Show SMILES O=C(NCc1ccccc1)c1ccc2ncc(-c3cc4c(nccc4o3)N3CCOCC3)n2n1
Show InChI InChI=1S/C25H22N6O3/c32-25(28-15-17-4-2-1-3-5-17)19-6-7-23-27-16-20(31(23)29-19)22-14-18-21(34-22)8-9-26-24(18)30-10-12-33-13-11-30/h1-9,14,16H,10-13,15H2,(H,28,32)
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US Patent
n/an/a 5.60n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358858
PNG
(N-[(2R)-1-hydroxypropan-2-yl]-3-[4-(morpholin-4-yl...)
Show SMILES C[C@H](CO)NC(=O)c1ccc2ncc(-c3cc4c(nccc4o3)N3CCOCC3)n2n1
Show InChI InChI=1S/C21H22N6O4/c1-13(12-28)24-21(29)15-2-3-19-23-11-16(27(19)25-15)18-10-14-17(31-18)4-5-22-20(14)26-6-8-30-9-7-26/h2-5,10-11,13,28H,6-9,12H2,1H3,(H,24,29)/t13-/m1/s1
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UniChem
US Patent
n/an/a 5.80n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358864
PNG
(3-(1-Benzofuran-2-yl)-N-[(2R)-1-hydroxy-3-methylbu...)
Show SMILES CC(C)[C@H](CO)NC(=O)c1ccc2ncc(-c3cc4ccccc4o3)n2n1
Show InChI InChI=1S/C20H20N4O3/c1-12(2)15(11-25)22-20(26)14-7-8-19-21-10-16(24(19)23-14)18-9-13-5-3-4-6-17(13)27-18/h3-10,12,15,25H,11H2,1-2H3,(H,22,26)/t15-/m0/s1
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PC sid
UniChem
US Patent
n/an/a 6.80n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity of compounds of the present invention was quantified employing the MKNK1 TR-FRET assay as described in the following paragr...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358853
PNG
(N-(3-methoxypropyl)-3-[4-(morpholin-4-yl)furo[3,2-...)
Show SMILES COCCCNC(=O)c1ccc2ncc(-c3cc4c(nccc4o3)N3CCOCC3)n2n1
Show InChI InChI=1S/C22H24N6O4/c1-30-10-2-6-24-22(29)16-3-4-20-25-14-17(28(20)26-16)19-13-15-18(32-19)5-7-23-21(15)27-8-11-31-12-9-27/h3-5,7,13-14H,2,6,8-12H2,1H3,(H,24,29)
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PC sid
UniChem
US Patent
n/an/a 7n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358859
PNG
(N-[(2S)-1-hydroxypropan-2-yl]-3-[4-(morpholin-4-yl...)
Show SMILES C[C@@H](CO)NC(=O)c1ccc2ncc(-c3cc4c(nccc4o3)N3CCOCC3)n2n1
Show InChI InChI=1S/C21H22N6O4/c1-13(12-28)24-21(29)15-2-3-19-23-11-16(27(19)25-15)18-10-14-17(31-18)4-5-22-20(14)26-6-8-30-9-7-26/h2-5,10-11,13,28H,6-9,12H2,1H3,(H,24,29)/t13-/m0/s1
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PC sid
UniChem
US Patent
n/an/a 7.30n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity of compounds of the present invention was quantified employing the MKNK1 TR-FRET assay as described in the following paragr...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358861
PNG
(3-(1-Benzofuran-2-yl)-N-[3-(dimethylamino)propyl]i...)
Show SMILES CN(C)CCCNC(=O)c1ccc2ncc(-c3cc4ccccc4o3)n2n1
Show InChI InChI=1S/C20H21N5O2/c1-24(2)11-5-10-21-20(26)15-8-9-19-22-13-16(25(19)23-15)18-12-14-6-3-4-7-17(14)27-18/h3-4,6-9,12-13H,5,10-11H2,1-2H3,(H,21,26)
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PC sid
UniChem
US Patent
n/an/a 7.90n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358866
PNG
(3-(1-Benzofuran-2-yl)-N-(2-methoxyethyl)imidazo[1,...)
Show SMILES COCCNC(=O)c1ccc2ncc(-c3cc4ccccc4o3)n2n1
Show InChI InChI=1S/C18H16N4O3/c1-24-9-8-19-18(23)13-6-7-17-20-11-14(22(17)21-13)16-10-12-4-2-3-5-15(12)25-16/h2-7,10-11H,8-9H2,1H3,(H,19,23)
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US Patent
n/an/a 8n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity of compounds of the present invention was quantified employing the MKNK1 TR-FRET assay as described in the following paragr...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358856
PNG
(N-(2-methoxyethyl)-N-methyl-3-[4-(morpholin-4-yl)f...)
Show SMILES COCCN(C)C(=O)c1ccc2ncc(-c3cc4c(nccc4o3)N3CCOCC3)n2n1
Show InChI InChI=1S/C22H24N6O4/c1-26(7-10-30-2)22(29)16-3-4-20-24-14-17(28(20)25-16)19-13-15-18(32-19)5-6-23-21(15)27-8-11-31-12-9-27/h3-6,13-14H,7-12H2,1-2H3
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PC sid
UniChem
US Patent
n/an/a 8.70n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358867
PNG
(3-(1-Benzofuran-2-yl)-N-benzyl-N-methylimidazo[1,2...)
Show SMILES CN(Cc1ccccc1)C(=O)c1ccc2ncc(-c3cc4ccccc4o3)n2n1
Show InChI InChI=1S/C23H18N4O2/c1-26(15-16-7-3-2-4-8-16)23(28)18-11-12-22-24-14-19(27(22)25-18)21-13-17-9-5-6-10-20(17)29-21/h2-14H,15H2,1H3
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PC cid
PC sid
UniChem
US Patent
n/an/a 8.80n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity of compounds of the present invention was quantified employing the MKNK1 TR-FRET assay as described in the following paragr...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358862
PNG
(3-(1-Benzofuran-2-yl)-N-[(2R)-1-hydroxypropan-2-yl...)
Show SMILES C[C@H](CO)NC(=O)c1ccc2ncc(-c3cc4ccccc4o3)n2n1
Show InChI InChI=1S/C18H16N4O3/c1-11(10-23)20-18(24)13-6-7-17-19-9-14(22(17)21-13)16-8-12-4-2-3-5-15(12)25-16/h2-9,11,23H,10H2,1H3,(H,20,24)/t11-/m1/s1
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n/an/a 8.80n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358863
PNG
(3-(1-Benzofuran-2-yl)-N-(3-methoxypropyl)imidazo[1...)
Show SMILES COCCCNC(=O)c1ccc2ncc(-c3cc4ccccc4o3)n2n1
Show InChI InChI=1S/C19H18N4O3/c1-25-10-4-9-20-19(24)14-7-8-18-21-12-15(23(18)22-14)17-11-13-5-2-3-6-16(13)26-17/h2-3,5-8,11-12H,4,9-10H2,1H3,(H,20,24)
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n/an/a 9.5n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358865
PNG
(3-(1-Benzofuran-2-yl)-N-benzylimidazo[1,2-b]pyrida...)
Show SMILES O=C(NCc1ccccc1)c1ccc2ncc(-c3cc4ccccc4o3)n2n1
Show InChI InChI=1S/C22H16N4O2/c27-22(24-13-15-6-2-1-3-7-15)17-10-11-21-23-14-18(26(21)25-17)20-12-16-8-4-5-9-19(16)28-20/h1-12,14H,13H2,(H,24,27)
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n/an/a 12n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358864
PNG
(3-(1-Benzofuran-2-yl)-N-[(2R)-1-hydroxy-3-methylbu...)
Show SMILES CC(C)[C@H](CO)NC(=O)c1ccc2ncc(-c3cc4ccccc4o3)n2n1
Show InChI InChI=1S/C20H20N4O3/c1-12(2)15(11-25)22-20(26)14-7-8-19-21-10-16(24(19)23-14)18-9-13-5-3-4-6-17(13)27-18/h3-10,12,15,25H,11H2,1-2H3,(H,22,26)/t15-/m0/s1
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US Patent
n/an/a 12n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358857
PNG
(N-(2-methoxyethyl)-3-[4-(morpholin-4-yl)furo[3,2-c...)
Show SMILES COCCNC(=O)c1ccc2ncc(-c3cc4c(nccc4o3)N3CCOCC3)n2n1
Show InChI InChI=1S/C21H22N6O4/c1-29-9-6-23-21(28)15-2-3-19-24-13-16(27(19)25-15)18-12-14-17(31-18)4-5-22-20(14)26-7-10-30-11-8-26/h2-5,12-13H,6-11H2,1H3,(H,23,28)
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n/an/a 12n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358866
PNG
(3-(1-Benzofuran-2-yl)-N-(2-methoxyethyl)imidazo[1,...)
Show SMILES COCCNC(=O)c1ccc2ncc(-c3cc4ccccc4o3)n2n1
Show InChI InChI=1S/C18H16N4O3/c1-24-9-8-19-18(23)13-6-7-17-20-11-14(22(17)21-13)16-10-12-4-2-3-5-15(12)25-16/h2-7,10-11H,8-9H2,1H3,(H,19,23)
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n/an/a 15n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358859
PNG
(N-[(2S)-1-hydroxypropan-2-yl]-3-[4-(morpholin-4-yl...)
Show SMILES C[C@@H](CO)NC(=O)c1ccc2ncc(-c3cc4c(nccc4o3)N3CCOCC3)n2n1
Show InChI InChI=1S/C21H22N6O4/c1-13(12-28)24-21(29)15-2-3-19-23-11-16(27(19)25-15)18-10-14-17(31-18)4-5-22-20(14)26-6-8-30-9-7-26/h2-5,10-11,13,28H,6-9,12H2,1H3,(H,24,29)/t13-/m0/s1
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n/an/a 21n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358867
PNG
(3-(1-Benzofuran-2-yl)-N-benzyl-N-methylimidazo[1,2...)
Show SMILES CN(Cc1ccccc1)C(=O)c1ccc2ncc(-c3cc4ccccc4o3)n2n1
Show InChI InChI=1S/C23H18N4O2/c1-26(15-16-7-3-2-4-8-16)23(28)18-11-12-22-24-14-19(27(22)25-18)21-13-17-9-5-6-10-20(17)29-21/h2-14H,15H2,1H3
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n/an/a 23n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358868
PNG
(3-(1-Benzofuran-2-yl)-N-[2-(dimethylamino)ethyl]im...)
Show SMILES CN(C)CCNC(=O)c1ccc2ncc(-c3cc4ccccc4o3)n2n1
Show InChI InChI=1S/C19H19N5O2/c1-23(2)10-9-20-19(25)14-7-8-18-21-12-15(24(18)22-14)17-11-13-5-3-4-6-16(13)26-17/h3-8,11-12H,9-10H2,1-2H3,(H,20,25)
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n/an/a 34n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358869
PNG
(3-(1-Benzofuran-2-yl)-N-[(2S)-1-hydroxy-3-methylbu...)
Show SMILES CC(C)[C@@H](CO)NC(=O)c1ccc2ncc(-c3cc4ccccc4o3)n2n1
Show InChI InChI=1S/C20H20N4O3/c1-12(2)15(11-25)22-20(26)14-7-8-19-21-10-16(24(19)23-14)18-9-13-5-3-4-6-17(13)27-18/h3-10,12,15,25H,11H2,1-2H3,(H,22,26)/t15-/m1/s1
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n/an/a 42n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358854
PNG
(N-[2-(dimethylamino)ethyl]-N-methyl-3-[4-(morpholi...)
Show SMILES CN(C)CCN(C)C(=O)c1ccc2ncc(-c3cc4c(nccc4o3)N3CCOCC3)n2n1
Show InChI InChI=1S/C23H27N7O3/c1-27(2)8-9-28(3)23(31)17-4-5-21-25-15-18(30(21)26-17)20-14-16-19(33-20)6-7-24-22(16)29-10-12-32-13-11-29/h4-7,14-15H,8-13H2,1-3H3
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n/an/a 88n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity of compounds of the present invention was quantified employing the MKNK1 TR-FRET assay as described in the following paragr...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358855
PNG
((4-Methylpiperazin-1-yl){3-[4-(morpholin-4-yl)furo...)
Show SMILES CN1CCN(CC1)C(=O)c1ccc2ncc(-c3cc4c(nccc4o3)N3CCOCC3)n2n1
Show InChI InChI=1S/C23H25N7O3/c1-27-6-8-29(9-7-27)23(31)17-2-3-21-25-15-18(30(21)26-17)20-14-16-19(33-20)4-5-24-22(16)28-10-12-32-13-11-28/h2-5,14-15H,6-13H2,1H3
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n/an/a 110n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity of compounds of the present invention was quantified employing the MKNK1 TR-FRET assay as described in the following paragr...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358854
PNG
(N-[2-(dimethylamino)ethyl]-N-methyl-3-[4-(morpholi...)
Show SMILES CN(C)CCN(C)C(=O)c1ccc2ncc(-c3cc4c(nccc4o3)N3CCOCC3)n2n1
Show InChI InChI=1S/C23H27N7O3/c1-27(2)8-9-28(3)23(31)17-4-5-21-25-15-18(30(21)26-17)20-14-16-19(33-20)6-7-24-22(16)29-10-12-32-13-11-29/h4-7,14-15H,8-13H2,1-3H3
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US Patent
n/an/a 140n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...


US Patent US10214545 (2019)

More data for this
Ligand-Target Pair
MAP Kinase interacting Kinase


(Homo sapiens (Human))
BDBM358855
PNG
((4-Methylpiperazin-1-yl){3-[4-(morpholin-4-yl)furo...)
Show SMILES CN1CCN(CC1)C(=O)c1ccc2ncc(-c3cc4c(nccc4o3)N3CCOCC3)n2n1
Show InChI InChI=1S/C23H25N7O3/c1-27-6-8-29(9-7-27)23(31)17-2-3-21-25-15-18(30(21)26-17)20-14-16-19(33-20)4-5-24-22(16)28-10-12-32-13-11-28/h2-5,14-15H,6-13H2,1H3
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US Patent
n/an/a 280n/an/an/an/an/an/a



BAYER PHARMA AKTIENGESELLSCHAFT

US Patent


Assay Description
MKNK1-inhibitory activity at high ATP of compounds of the present invention after their preincubation with MKNK1 was quantified employing the TR-FRET...


US Patent US10214545 (2019)

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