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Patent code US10273222

Compile Data Set for Download or QSAR

Found 604 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
Homo sapiens lysine demethylase 2B (KDM2B)


(Homo sapiens (Human))
BDBM382050
PNG
(2-[1-(4-fluoro-2,3-dihydro-1H- inden-1-yl)imidazol...)
Show SMILES OC(=O)c1ccnc(c1)-c1cn(cn1)C1CCc2c1cccc2F
Show InChI InChI=1S/C18H14FN3O2/c19-14-3-1-2-13-12(14)4-5-17(13)22-9-16(21-10-22)15-8-11(18(23)24)6-7-20-15/h1-3,6-10,17H,4-5H2,(H,23,24)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of FBXL10 was determined in 384-well plate format under the following reaction conditions: 0.3 ...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5A


(Homo sapiens (Human))
BDBM382052
PNG
(2-[1-(2-naphthalen-1- ylethyl)imidazol-4-yl]pyridi...)
Show SMILES OC(=O)c1ccnc(c1)-c1cn(CCc2cccc3ccccc23)cn1
Show InChI InChI=1S/C21H17N3O2/c25-21(26)17-8-10-22-19(12-17)20-13-24(14-23-20)11-9-16-6-3-5-15-4-1-2-7-18(15)16/h1-8,10,12-14H,9,11H2,(H,25,26)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The enzymatic assay of Jarid1A activity is based upon Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) detection. The ability of test c...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5A


(Homo sapiens (Human))
BDBM381935
PNG
(2-{1-methyl-5-[4- (trifluoromethyl)phenyl]-1H- imi...)
Show SMILES Cn1cnc(c1-c1ccc(cc1)C(F)(F)F)-c1cc(ccn1)C(O)=O
Show InChI InChI=1S/C17H12F3N3O2/c1-23-9-22-14(13-8-11(16(24)25)6-7-21-13)15(23)10-2-4-12(5-3-10)17(18,19)20/h2-9H,1H3,(H,24,25)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The enzymatic assay of Jarid1A activity is based upon Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) detection. The ability of test c...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5A


(Homo sapiens (Human))
BDBM381936
PNG
(2-[5-(4-cyclopropylphenyl)-1- methyl-1H-imidazol-4...)
Show SMILES Cn1cnc(c1-c1ccc(cc1)C1CC1)-c1cc(ccn1)C(O)=O
Show InChI InChI=1S/C19H17N3O2/c1-22-11-21-17(16-10-15(19(23)24)8-9-20-16)18(22)14-6-4-13(5-7-14)12-2-3-12/h4-12H,2-3H2,1H3,(H,23,24)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The enzymatic assay of Jarid1A activity is based upon Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) detection. The ability of test c...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5B


(Homo sapiens (Human))
BDBM382067
PNG
(2-[1-[(2- chlorophenyl)methyl]imidazol-4- yl]-4-(2...)
Show SMILES Clc1ccccc1Cn1cnc(c1)-c1cc(ccn1)-c1nn[nH]n1
Show InChI InChI=1S/C16H12ClN7/c17-13-4-2-1-3-12(13)8-24-9-15(19-10-24)14-7-11(5-6-18-14)16-20-22-23-21-16/h1-7,9-10H,8H2,(H,20,21,22,23)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of Jarid1B was determined in 384-well plate format under the following reaction conditions: 0.8...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Homo sapiens lysine demethylase 2B (KDM2B)


(Homo sapiens (Human))
BDBM382069
PNG
(2-[1-[(4- chlorophenyl)methyl]imidazol-4- yl]-4-(2...)
Show SMILES Clc1ccc(Cn2cnc(c2)-c2cc(ccn2)-c2nn[nH]n2)cc1
Show InChI InChI=1S/C16H12ClN7/c17-13-3-1-11(2-4-13)8-24-9-15(19-10-24)14-7-12(5-6-18-14)16-20-22-23-21-16/h1-7,9-10H,8H2,(H,20,21,22,23)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of FBXL10 was determined in 384-well plate format under the following reaction conditions: 0.3 ...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Homo sapiens lysine demethylase 2B (KDM2B)


(Homo sapiens (Human))
BDBM382072
PNG
(2-[5-(4-fluorophenyl)-1-(2,2,2- trifluoroethyl)imi...)
Show SMILES Fc1ccc(cc1)-c1c(ncn1CC(F)(F)F)-c1cc(ccn1)-c1nn[nH]n1
Show InChI InChI=1S/C17H11F4N7/c18-12-3-1-10(2-4-12)15-14(23-9-28(15)8-17(19,20)21)13-7-11(5-6-22-13)16-24-26-27-25-16/h1-7,9H,8H2,(H,24,25,26,27)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of FBXL10 was determined in 384-well plate format under the following reaction conditions: 0.3 ...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5A


(Homo sapiens (Human))
BDBM381945
PNG
(2-(5-{4-[1- (hydroxymethyl)cyclopropyl]- phenyl}-1...)
Show SMILES Cn1cnc(c1-c1ccc(cc1)C1(CO)CC1)-c1cc(ccn1)C(O)=O
Show InChI InChI=1S/C20H19N3O3/c1-23-12-22-17(16-10-14(19(25)26)6-9-21-16)18(23)13-2-4-15(5-3-13)20(11-24)7-8-20/h2-6,9-10,12,24H,7-8,11H2,1H3,(H,25,26)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The enzymatic assay of Jarid1A activity is based upon Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) detection. The ability of test c...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5B


(Homo sapiens (Human))
BDBM381946
PNG
(2-{1-methyl-5-[4-(pyrrolidin-1- yl)phenyl]-1H-imid...)
Show SMILES Cn1cnc(c1-c1ccc(cc1)N1CCCC1)-c1cc(ccn1)C(O)=O
Show InChI InChI=1S/C20H20N4O2/c1-23-13-22-18(17-12-15(20(25)26)8-9-21-17)19(23)14-4-6-16(7-5-14)24-10-2-3-11-24/h4-9,12-13H,2-3,10-11H2,1H3,(H,25,26)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of Jarid1B was determined in 384-well plate format under the following reaction conditions: 0.8...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Homo sapiens lysine demethylase 2B (KDM2B)


(Homo sapiens (Human))
BDBM381948
PNG
(2-[5-(3-chlorophenyl)-1-methyl- 1H-imidazol-4-yl]p...)
Show SMILES Cn1cnc(c1-c1cccc(Cl)c1)-c1cc(ccn1)C(O)=O
Show InChI InChI=1S/C16H12ClN3O2/c1-20-9-19-14(13-8-11(16(21)22)5-6-18-13)15(20)10-3-2-4-12(17)7-10/h2-9H,1H3,(H,21,22)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of FBXL10 was determined in 384-well plate format under the following reaction conditions: 0.3 ...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5B


(Homo sapiens (Human))
BDBM382082
PNG
(2-[1-(1-phenylpropyl)imidazol-4- yl]-4-(2H-tetrazo...)
Show SMILES CCC(c1ccccc1)n1cnc(c1)-c1cc(ccn1)-c1nn[nH]n1
Show InChI InChI=1/C18H17N7/c1-2-17(13-6-4-3-5-7-13)25-11-16(20-12-25)15-10-14(8-9-19-15)18-21-23-24-22-18/h3-12,17H,2H2,1H3,(H,21,22,23,24)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of Jarid1B was determined in 384-well plate format under the following reaction conditions: 0.8...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Homo sapiens lysine demethylase 2B (KDM2B)


(Homo sapiens (Human))
BDBM382083
PNG
(2-[1-(2-methyl-1- phenylpropyl)imidazol-4-yl]-4- (...)
Show SMILES CC(C)C(c1ccccc1)n1cnc(c1)-c1cc(ccn1)-c1nn[nH]n1
Show InChI InChI=1/C19H19N7/c1-13(2)18(14-6-4-3-5-7-14)26-11-17(21-12-26)16-10-15(8-9-20-16)19-22-24-25-23-19/h3-13,18H,1-2H3,(H,22,23,24,25)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of FBXL10 was determined in 384-well plate format under the following reaction conditions: 0.3 ...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5B


(Homo sapiens (Human))
BDBM382088
PNG
(2-[5-[2-(cyclopropylmethoxy)-4- fluorophenyl]-1-me...)
Show SMILES Cn1cnc(c1-c1ccc(F)cc1OCC1CC1)-c1cc(ccn1)-c1nn[nH]n1
Show InChI InChI=1S/C20H18FN7O/c1-28-11-23-18(16-8-13(6-7-22-16)20-24-26-27-25-20)19(28)15-5-4-14(21)9-17(15)29-10-12-2-3-12/h4-9,11-12H,2-3,10H2,1H3,(H,24,25,26,27)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of Jarid1B was determined in 384-well plate format under the following reaction conditions: 0.8...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5B


(Homo sapiens (Human))
BDBM382092
PNG
(2-[1-[[2-chloro-3- (trifluoromethyl)phenyl]methyl]...)
Show SMILES FC(F)(F)c1cccc(Cn2cnc(c2)-c2cc(ccn2)-c2nn[nH]n2)c1Cl
Show InChI InChI=1S/C17H11ClF3N7/c18-15-11(2-1-3-12(15)17(19,20)21)7-28-8-14(23-9-28)13-6-10(4-5-22-13)16-24-26-27-25-16/h1-6,8-9H,7H2,(H,24,25,26,27)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of Jarid1B was determined in 384-well plate format under the following reaction conditions: 0.8...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5A


(Homo sapiens (Human))
BDBM381973
PNG
(2-{5-[4-chloro-3- (trifluoromethyl)phenyl]-1- meth...)
Show SMILES Cn1cnc(c1-c1ccc(Cl)c(c1)C(F)(F)F)-c1cc(ccn1)C(O)=O
Show InChI InChI=1S/C17H11ClF3N3O2/c1-24-8-23-14(13-7-10(16(25)26)4-5-22-13)15(24)9-2-3-12(18)11(6-9)17(19,20)21/h2-8H,1H3,(H,25,26)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The enzymatic assay of Jarid1A activity is based upon Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) detection. The ability of test c...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5B


(Homo sapiens (Human))
BDBM381974
PNG
(2-[5-(4-chloro-2-ethoxyphenyl)- 1-methyl-1H-imidaz...)
Show SMILES CCOc1cc(Cl)ccc1-c1c(ncn1C)-c1cc(ccn1)C(O)=O
Show InChI InChI=1S/C18H16ClN3O3/c1-3-25-15-9-12(19)4-5-13(15)17-16(21-10-22(17)2)14-8-11(18(23)24)6-7-20-14/h4-10H,3H2,1-2H3,(H,23,24)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of Jarid1B was determined in 384-well plate format under the following reaction conditions: 0.8...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5B


(Homo sapiens (Human))
BDBM381975
PNG
(2-[5-(2,4-dichlorophenyl)-1- methyl-1H-imidazol-4-...)
Show SMILES Cn1cnc(c1-c1ccc(Cl)cc1Cl)-c1cc(ccn1)C(O)=O
Show InChI InChI=1S/C16H11Cl2N3O2/c1-21-8-20-14(13-6-9(16(22)23)4-5-19-13)15(21)11-3-2-10(17)7-12(11)18/h2-8H,1H3,(H,22,23)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of Jarid1B was determined in 384-well plate format under the following reaction conditions: 0.8...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Homo sapiens lysine demethylase 2B (KDM2B)


(Homo sapiens (Human))
BDBM382102
PNG
(2-[5-(4-fluoronaphthalen-1-yl)-1- methylimidazol-4...)
Show SMILES Cn1cnc(c1-c1ccc(F)c2ccccc12)-c1cc(ccn1)-c1nn[nH]n1
Show InChI InChI=1S/C20H14FN7/c1-28-11-23-18(17-10-12(8-9-22-17)20-24-26-27-25-20)19(28)15-6-7-16(21)14-5-3-2-4-13(14)15/h2-11H,1H3,(H,24,25,26,27)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of FBXL10 was determined in 384-well plate format under the following reaction conditions: 0.3 ...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5B


(Homo sapiens (Human))
BDBM381983
PNG
(2-(1-propyl-1H-imidazol-4- yl)pyridine-4-carboxyli...)
Show SMILES CCCn1cnc(c1)-c1cc(ccn1)C(O)=O
Show InChI InChI=1S/C12H13N3O2/c1-2-5-15-7-11(14-8-15)10-6-9(12(16)17)3-4-13-10/h3-4,6-8H,2,5H2,1H3,(H,16,17)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of Jarid1B was determined in 384-well plate format under the following reaction conditions: 0.8...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5A


(Homo sapiens (Human))
BDBM381984
PNG
(2-{1-[3-(dimethylamino)propyl]- 1H-imidazol-4-yl}p...)
Show SMILES CN(C)CCCn1cnc(c1)-c1cc(ccn1)C(O)=O
Show InChI InChI=1S/C14H18N4O2/c1-17(2)6-3-7-18-9-13(16-10-18)12-8-11(14(19)20)4-5-15-12/h4-5,8-10H,3,6-7H2,1-2H3,(H,19,20)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The enzymatic assay of Jarid1A activity is based upon Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) detection. The ability of test c...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5B


(Homo sapiens (Human))
BDBM381984
PNG
(2-{1-[3-(dimethylamino)propyl]- 1H-imidazol-4-yl}p...)
Show SMILES CN(C)CCCn1cnc(c1)-c1cc(ccn1)C(O)=O
Show InChI InChI=1S/C14H18N4O2/c1-17(2)6-3-7-18-9-13(16-10-18)12-8-11(14(19)20)4-5-15-12/h4-5,8-10H,3,6-7H2,1-2H3,(H,19,20)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of Jarid1B was determined in 384-well plate format under the following reaction conditions: 0.8...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Homo sapiens lysine demethylase 2B (KDM2B)


(Homo sapiens (Human))
BDBM381988
PNG
(2-[1-(pyridin-2-ylmethyl)-1H- imidazol-4-yl]pyridi...)
Show SMILES OC(=O)c1ccnc(c1)-c1cn(Cc2ccccn2)cn1
Show InChI InChI=1S/C15H12N4O2/c20-15(21)11-4-6-17-13(7-11)14-9-19(10-18-14)8-12-3-1-2-5-16-12/h1-7,9-10H,8H2,(H,20,21)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of FBXL10 was determined in 384-well plate format under the following reaction conditions: 0.3 ...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5A


(Homo sapiens (Human))
BDBM381989
PNG
(2-(1-{2-[2- (dimethylamino)ethoxy]ethyl}- 1H-imida...)
Show SMILES CN(C)CCOCCn1cnc(c1)-c1cc(ccn1)C(O)=O
Show InChI InChI=1S/C15H20N4O3/c1-18(2)5-7-22-8-6-19-10-14(17-11-19)13-9-12(15(20)21)3-4-16-13/h3-4,9-11H,5-8H2,1-2H3,(H,20,21)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The enzymatic assay of Jarid1A activity is based upon Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) detection. The ability of test c...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5B


(Homo sapiens (Human))
BDBM381989
PNG
(2-(1-{2-[2- (dimethylamino)ethoxy]ethyl}- 1H-imida...)
Show SMILES CN(C)CCOCCn1cnc(c1)-c1cc(ccn1)C(O)=O
Show InChI InChI=1S/C15H20N4O3/c1-18(2)5-7-22-8-6-19-10-14(17-11-19)13-9-12(15(20)21)3-4-16-13/h3-4,9-11H,5-8H2,1-2H3,(H,20,21)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of Jarid1B was determined in 384-well plate format under the following reaction conditions: 0.8...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 4C


(Homo sapiens (Human))
BDBM381996
PNG
(2-{1-[(1-methylpiperidin-3- yl)methyl]-1H-imidazol...)
Show SMILES CN1CCCC(Cn2cnc(c2)-c2cc(ccn2)C(O)=O)C1
Show InChI InChI=1S/C16H20N4O2/c1-19-6-2-3-12(8-19)9-20-10-15(18-11-20)14-7-13(16(21)22)4-5-17-14/h4-5,7,10-12H,2-3,6,8-9H2,1H3,(H,21,22)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of JMJD2C was determined in 384-well plate format under the following reaction conditions: 0.3 ...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5B


(Homo sapiens (Human))
BDBM382000
PNG
(2-{1-[2-(2-oxopyrrolidin-1- yl)ethyl]-1H-imidazol-...)
Show SMILES OC(=O)c1ccnc(c1)-c1cn(CCN2CCCC2=O)cn1
Show InChI InChI=1S/C15H16N4O3/c20-14-2-1-5-19(14)7-6-18-9-13(17-10-18)12-8-11(15(21)22)3-4-16-12/h3-4,8-10H,1-2,5-7H2,(H,21,22)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of Jarid1B was determined in 384-well plate format under the following reaction conditions: 0.8...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5B


(Homo sapiens (Human))
BDBM382001
PNG
(2-{1-[2-(pyrrolidin-1-yl)propyl]- 1H-imidazol-4-yl...)
Show SMILES CC(Cn1cnc(c1)-c1cc(ccn1)C(O)=O)N1CCCC1
Show InChI InChI=1S/C16H20N4O2/c1-12(20-6-2-3-7-20)9-19-10-15(18-11-19)14-8-13(16(21)22)4-5-17-14/h4-5,8,10-12H,2-3,6-7,9H2,1H3,(H,21,22)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of Jarid1B was determined in 384-well plate format under the following reaction conditions: 0.8...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 4A


(Homo sapiens (Human))
BDBM382007
PNG
(2-[1-[2-[methyl-[(4- methylphenyl)methyl]amino]eth...)
Show SMILES CN(CCn1cnc(c1)-c1cc(ccn1)C(O)=O)Cc1ccc(C)cc1
Show InChI InChI=1S/C20H22N4O2/c1-15-3-5-16(6-4-15)12-23(2)9-10-24-13-19(22-14-24)18-11-17(20(25)26)7-8-21-18/h3-8,11,13-14H,9-10,12H2,1-2H3,(H,25,26)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of JMJD2A was determined in 384-well plate format under the following reaction conditions: 2 nM...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5A


(Homo sapiens (Human))
BDBM382008
PNG
(2-[1-[2-[methyl-[[4- (trifluoromethyl)phenyl]methy...)
Show SMILES CN(CCn1cnc(c1)-c1cc(ccn1)C(O)=O)Cc1ccc(cc1)C(F)(F)F
Show InChI InChI=1S/C20H19F3N4O2/c1-26(11-14-2-4-16(5-3-14)20(21,22)23)8-9-27-12-18(25-13-27)17-10-15(19(28)29)6-7-24-17/h2-7,10,12-13H,8-9,11H2,1H3,(H,28,29)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The enzymatic assay of Jarid1A activity is based upon Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) detection. The ability of test c...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5A


(Homo sapiens (Human))
BDBM382010
PNG
(2-[1-[2-[ethyl-[(4- fluorophenyl)methyl]amino]ethy...)
Show SMILES CCN(CCn1cnc(c1)-c1cc(ccn1)C(O)=O)Cc1ccc(F)cc1
Show InChI InChI=1S/C20H21FN4O2/c1-2-24(12-15-3-5-17(21)6-4-15)9-10-25-13-19(23-14-25)18-11-16(20(26)27)7-8-22-18/h3-8,11,13-14H,2,9-10,12H2,1H3,(H,26,27)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The enzymatic assay of Jarid1A activity is based upon Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) detection. The ability of test c...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5A


(Homo sapiens (Human))
BDBM382011
PNG
(2-[1-[2-[cyclopropyl-[(4- fluorophenyl)methyl]amin...)
Show SMILES OC(=O)c1ccnc(c1)-c1cn(CCN(Cc2ccc(F)cc2)C2CC2)cn1
Show InChI InChI=1S/C21H21FN4O2/c22-17-3-1-15(2-4-17)12-26(18-5-6-18)10-9-25-13-20(24-14-25)19-11-16(21(27)28)7-8-23-19/h1-4,7-8,11,13-14,18H,5-6,9-10,12H2,(H,27,28)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The enzymatic assay of Jarid1A activity is based upon Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) detection. The ability of test c...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Homo sapiens lysine demethylase 2B (KDM2B)


(Homo sapiens (Human))
BDBM382012
PNG
(2-[1-[2-[(4,4- difluorocyclohexyl)methylamino] eth...)
Show SMILES OC(=O)c1ccnc(c1)-c1cn(CCNCC2CCC(F)(F)CC2)cn1
Show InChI InChI=1S/C18H22F2N4O2/c19-18(20)4-1-13(2-5-18)10-21-7-8-24-11-16(23-12-24)15-9-14(17(25)26)3-6-22-15/h3,6,9,11-13,21H,1-2,4-5,7-8,10H2,(H,25,26)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of FBXL10 was determined in 384-well plate format under the following reaction conditions: 0.3 ...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Homo sapiens lysine demethylase 2B (KDM2B)


(Homo sapiens (Human))
BDBM382016
PNG
(2-[1-[2-(1,3-dihydroisoindol-2- yl)ethyl]imidazol-...)
Show SMILES OC(=O)c1ccnc(c1)-c1cn(CCN2Cc3ccccc3C2)cn1
Show InChI InChI=1S/C19H18N4O2/c24-19(25)14-5-6-20-17(9-14)18-12-23(13-21-18)8-7-22-10-15-3-1-2-4-16(15)11-22/h1-6,9,12-13H,7-8,10-11H2,(H,24,25)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of FBXL10 was determined in 384-well plate format under the following reaction conditions: 0.3 ...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 4C


(Homo sapiens (Human))
BDBM382018
PNG
(2-[1-[2-[(2- chlorophenyl)methylamino]ethyl] imida...)
Show SMILES OC(=O)c1ccnc(c1)-c1cn(CCNCc2ccccc2Cl)cn1
Show InChI InChI=1S/C18H17ClN4O2/c19-15-4-2-1-3-14(15)10-20-7-8-23-11-17(22-12-23)16-9-13(18(24)25)5-6-21-16/h1-6,9,11-12,20H,7-8,10H2,(H,24,25)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of JMJD2C was determined in 384-well plate format under the following reaction conditions: 0.3 ...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Homo sapiens lysine demethylase 2B (KDM2B)


(Homo sapiens (Human))
BDBM382019
PNG
(2-[1-[2-(5-fluoro-1,3- dihydroisoindol-2- yl)ethyl...)
Show SMILES OC(=O)c1ccnc(c1)-c1cn(CCN2Cc3ccc(F)cc3C2)cn1
Show InChI InChI=1S/C19H17FN4O2/c20-16-2-1-14-9-23(10-15(14)7-16)5-6-24-11-18(22-12-24)17-8-13(19(25)26)3-4-21-17/h1-4,7-8,11-12H,5-6,9-10H2,(H,25,26)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of FBXL10 was determined in 384-well plate format under the following reaction conditions: 0.3 ...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Homo sapiens lysine demethylase 2B (KDM2B)


(Homo sapiens (Human))
BDBM382028
PNG
(2-[1-[2-(3,4-dihydro-2H-quinolin- 1-yl)ethyl]imida...)
Show SMILES OC(=O)c1ccnc(c1)-c1cn(CCN2CCCc3ccccc23)cn1
Show InChI InChI=1S/C20H20N4O2/c25-20(26)16-7-8-21-17(12-16)18-13-23(14-22-18)10-11-24-9-3-5-15-4-1-2-6-19(15)24/h1-2,4,6-8,12-14H,3,5,9-11H2,(H,25,26)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of FBXL10 was determined in 384-well plate format under the following reaction conditions: 0.3 ...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5B


(Homo sapiens (Human))
BDBM382033
PNG
(2-[1-[2-(2- fluorophenyl)ethyl]imidazol-4- yl]pyri...)
Show SMILES OC(=O)c1ccnc(c1)-c1cn(CCc2ccccc2F)cn1
Show InChI InChI=1S/C17H14FN3O2/c18-14-4-2-1-3-12(14)6-8-21-10-16(20-11-21)15-9-13(17(22)23)5-7-19-15/h1-5,7,9-11H,6,8H2,(H,22,23)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of Jarid1B was determined in 384-well plate format under the following reaction conditions: 0.8...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 4C


(Homo sapiens (Human))
BDBM382033
PNG
(2-[1-[2-(2- fluorophenyl)ethyl]imidazol-4- yl]pyri...)
Show SMILES OC(=O)c1ccnc(c1)-c1cn(CCc2ccccc2F)cn1
Show InChI InChI=1S/C17H14FN3O2/c18-14-4-2-1-3-12(14)6-8-21-10-16(20-11-21)15-9-13(17(22)23)5-7-19-15/h1-5,7,9-11H,6,8H2,(H,22,23)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of JMJD2C was determined in 384-well plate format under the following reaction conditions: 0.3 ...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Homo sapiens lysine demethylase 2B (KDM2B)


(Homo sapiens (Human))
BDBM382033
PNG
(2-[1-[2-(2- fluorophenyl)ethyl]imidazol-4- yl]pyri...)
Show SMILES OC(=O)c1ccnc(c1)-c1cn(CCc2ccccc2F)cn1
Show InChI InChI=1S/C17H14FN3O2/c18-14-4-2-1-3-12(14)6-8-21-10-16(20-11-21)15-9-13(17(22)23)5-7-19-15/h1-5,7,9-11H,6,8H2,(H,22,23)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of FBXL10 was determined in 384-well plate format under the following reaction conditions: 0.3 ...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 4A


(Homo sapiens (Human))
BDBM382037
PNG
(2-[1-[2-(2- chlorophenyl)ethyl]imidazol-4- yl]pyri...)
Show SMILES OC(=O)c1ccnc(c1)-c1cn(CCc2ccccc2Cl)cn1
Show InChI InChI=1S/C17H14ClN3O2/c18-14-4-2-1-3-12(14)6-8-21-10-16(20-11-21)15-9-13(17(22)23)5-7-19-15/h1-5,7,9-11H,6,8H2,(H,22,23)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of JMJD2A was determined in 384-well plate format under the following reaction conditions: 2 nM...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5A


(Homo sapiens (Human))
BDBM382040
PNG
(2-(1-benzylimidazol-4- yl)pyridine-4-carboxylic ac...)
Show SMILES OC(=O)c1ccnc(c1)-c1cn(Cc2ccccc2)cn1
Show InChI InChI=1S/C16H13N3O2/c20-16(21)13-6-7-17-14(8-13)15-10-19(11-18-15)9-12-4-2-1-3-5-12/h1-8,10-11H,9H2,(H,20,21)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The enzymatic assay of Jarid1A activity is based upon Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) detection. The ability of test c...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5A


(Homo sapiens (Human))
BDBM382047
PNG
(2-[1-(1-phenylpropyl)imidazol-4- yl]pyridine-4-car...)
Show SMILES CCC(c1ccccc1)n1cnc(c1)-c1cc(ccn1)C(O)=O
Show InChI InChI=1S/C18H17N3O2/c1-2-17(13-6-4-3-5-7-13)21-11-16(20-12-21)15-10-14(18(22)23)8-9-19-15/h3-12,17H,2H2,1H3,(H,22,23)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The enzymatic assay of Jarid1A activity is based upon Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) detection. The ability of test c...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5B


(Homo sapiens (Human))
BDBM382048
PNG
(2-[1-(2-methyl-1- phenylpropyl)imidazol-4- yl]pyri...)
Show SMILES CC(C)C(c1ccccc1)n1cnc(c1)-c1cc(ccn1)C(O)=O
Show InChI InChI=1S/C19H19N3O2/c1-13(2)18(14-6-4-3-5-7-14)22-11-17(21-12-22)16-10-15(19(23)24)8-9-20-16/h3-13,18H,1-2H3,(H,23,24)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of Jarid1B was determined in 384-well plate format under the following reaction conditions: 0.8...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Homo sapiens lysine demethylase 2B (KDM2B)


(Homo sapiens (Human))
BDBM382048
PNG
(2-[1-(2-methyl-1- phenylpropyl)imidazol-4- yl]pyri...)
Show SMILES CC(C)C(c1ccccc1)n1cnc(c1)-c1cc(ccn1)C(O)=O
Show InChI InChI=1S/C19H19N3O2/c1-13(2)18(14-6-4-3-5-7-14)22-11-17(21-12-22)16-10-15(19(23)24)8-9-20-16/h3-13,18H,1-2H3,(H,23,24)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of FBXL10 was determined in 384-well plate format under the following reaction conditions: 0.3 ...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5A


(Homo sapiens (Human))
BDBM382050
PNG
(2-[1-(4-fluoro-2,3-dihydro-1H- inden-1-yl)imidazol...)
Show SMILES OC(=O)c1ccnc(c1)-c1cn(cn1)C1CCc2c1cccc2F
Show InChI InChI=1S/C18H14FN3O2/c19-14-3-1-2-13-12(14)4-5-17(13)22-9-16(21-10-22)15-8-11(18(23)24)6-7-20-15/h1-3,6-10,17H,4-5H2,(H,23,24)
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CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The enzymatic assay of Jarid1A activity is based upon Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) detection. The ability of test c...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5B


(Homo sapiens (Human))
BDBM382051
PNG
(2-[1-[(3- phenylphenyl)methyl]imidazol-4- yl]pyrid...)
Show SMILES OC(=O)c1ccnc(c1)-c1cn(Cc2cccc(c2)-c2ccccc2)cn1
Show InChI InChI=1S/C22H17N3O2/c26-22(27)19-9-10-23-20(12-19)21-14-25(15-24-21)13-16-5-4-8-18(11-16)17-6-2-1-3-7-17/h1-12,14-15H,13H2,(H,26,27)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of Jarid1B was determined in 384-well plate format under the following reaction conditions: 0.8...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Homo sapiens lysine demethylase 2B (KDM2B)


(Homo sapiens (Human))
BDBM382051
PNG
(2-[1-[(3- phenylphenyl)methyl]imidazol-4- yl]pyrid...)
Show SMILES OC(=O)c1ccnc(c1)-c1cn(Cc2cccc(c2)-c2ccccc2)cn1
Show InChI InChI=1S/C22H17N3O2/c26-22(27)19-9-10-23-20(12-19)21-14-25(15-24-21)13-16-5-4-8-18(11-16)17-6-2-1-3-7-17/h1-12,14-15H,13H2,(H,26,27)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of FBXL10 was determined in 384-well plate format under the following reaction conditions: 0.3 ...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5A


(Homo sapiens (Human))
BDBM382055
PNG
(2-[1-(cyclohexylmethyl)imidazol- 4-yl]pyridine-4-c...)
Show SMILES OC(=O)c1ccnc(c1)-c1cn(CC2CCCCC2)cn1
Show InChI InChI=1S/C16H19N3O2/c20-16(21)13-6-7-17-14(8-13)15-10-19(11-18-15)9-12-4-2-1-3-5-12/h6-8,10-12H,1-5,9H2,(H,20,21)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The enzymatic assay of Jarid1A activity is based upon Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) detection. The ability of test c...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5B


(Homo sapiens (Human))
BDBM382056
PNG
(2-[1-(1,2,3,4- tetrahydronaphthalen-1- ylmethyl)im...)
Show SMILES OC(=O)c1ccnc(c1)-c1cn(CC2CCCc3ccccc23)cn1
Show InChI InChI=1S/C20H19N3O2/c24-20(25)15-8-9-21-18(10-15)19-12-23(13-22-19)11-16-6-3-5-14-4-1-2-7-17(14)16/h1-2,4,7-10,12-13,16H,3,5-6,11H2,(H,24,25)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The ability of test compounds to inhibit the activity of Jarid1B was determined in 384-well plate format under the following reaction conditions: 0.8...


US Patent US10273222 (2019)

More data for this
Ligand-Target Pair
Lysine-specific demethylase 5A


(Homo sapiens (Human))
BDBM381931
PNG
(2-(5-bromo-1-methyl-1H- imidazol-4-yl)pyridine-4- ...)
Show SMILES Cn1cnc(c1Br)-c1cc(ccn1)C(O)=O
Show InChI InChI=1S/C10H8BrN3O2/c1-14-5-13-8(9(14)11)7-4-6(10(15)16)2-3-12-7/h2-5H,1H3,(H,15,16)
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n/an/a<100n/an/an/an/an/an/a



CELGENE QUANTSCEL RESEARCH, INC.

US Patent


Assay Description
The enzymatic assay of Jarid1A activity is based upon Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) detection. The ability of test c...


US Patent US10273222 (2019)

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