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Patent code US9353066

Compile Data Set for Download or QSAR

Found 228 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
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233627
PNG
(US9353066, 1.80)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(cc1)C(C)(O)[C@H]1CC[C@@H](CC1)C(O)=O
Show InChI InChI=1S/C27H28F3N3O3/c1-16-13-19(15-22(14-16)32-25-31-12-11-23(33-25)27(28,29)30)17-3-7-20(8-4-17)26(2,36)21-9-5-18(6-10-21)24(34)35/h3-4,7-8,11-15,18,21,36H,5-6,9-10H2,1-2H3,(H,34,35)(H,31,32,33)/t18-,21-,26?
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n/an/a 1.30n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233625
PNG
(US9353066, 1.78)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cccc(c1)C(O)=O
Show InChI InChI=1S/C19H14F3N3O2/c1-11-7-14(12-3-2-4-13(9-12)17(26)27)10-15(8-11)24-18-23-6-5-16(25-18)19(20,21)22/h2-10H,1H3,(H,26,27)(H,23,24,25)
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n/an/a 1.90n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233769
PNG
(US9353066, 4.8)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cccc(c1)S(=O)(=O)Nc1ccc(cc1)C(O)=O
Show InChI InChI=1S/C25H19F3N4O4S/c1-15-11-18(13-20(12-15)30-24-29-10-9-22(31-24)25(26,27)28)17-3-2-4-21(14-17)37(35,36)32-19-7-5-16(6-8-19)23(33)34/h2-14,32H,1H3,(H,33,34)(H,29,30,31)
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n/an/a 2.20n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233643
PNG
(US9353066, 1.96)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cc(cc(c1)C(O)=O)C#N
Show InChI InChI=1S/C20H13F3N4O2/c1-11-4-13(14-6-12(10-24)7-15(8-14)18(28)29)9-16(5-11)26-19-25-3-2-17(27-19)20(21,22)23/h2-9H,1H3,(H,28,29)(H,25,26,27)
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n/an/a 2.70n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233645
PNG
(US9353066, 1.98)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cc(F)cc(c1)C(O)=O
Show InChI InChI=1S/C19H13F4N3O2/c1-10-4-11(12-6-13(17(27)28)8-14(20)7-12)9-15(5-10)25-18-24-3-2-16(26-18)19(21,22)23/h2-9H,1H3,(H,27,28)(H,24,25,26)
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n/an/a 2.80n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233650
PNG
(US9353066, 1.103)
Show SMILES COc1ccc(cc1C(O)=O)-c1cc(C)cc(Nc2nccc(n2)C(F)(F)F)c1
Show InChI InChI=1S/C20H16F3N3O3/c1-11-7-13(12-3-4-16(29-2)15(10-12)18(27)28)9-14(8-11)25-19-24-6-5-17(26-19)20(21,22)23/h3-10H,1-2H3,(H,27,28)(H,24,25,26)
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n/an/a 3.20n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233574
PNG
(US9353066, 1.27)
Show SMILES C1CC(CCN1)Oc1ccnc(Nc2cc(cc(c2)-c2ccccc2)N2CCOCC2)n1
Show InChI InChI=1S/C25H29N5O2/c1-2-4-19(5-3-1)20-16-21(18-22(17-20)30-12-14-31-15-13-30)28-25-27-11-8-24(29-25)32-23-6-9-26-10-7-23/h1-5,8,11,16-18,23,26H,6-7,9-10,12-15H2,(H,27,28,29)
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n/an/a 3.30n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233667
PNG
(US9353066, 1.120)
Show SMILES Cc1cc(Nc2nccc(n2)C2CC2)cc(c1)-c1ccc(CCC(O)=O)cc1
Show InChI InChI=1S/C23H23N3O2/c1-15-12-19(17-5-2-16(3-6-17)4-9-22(27)28)14-20(13-15)25-23-24-11-10-21(26-23)18-7-8-18/h2-3,5-6,10-14,18H,4,7-9H2,1H3,(H,27,28)(H,24,25,26)
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n/an/a 4.20n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233626
PNG
(US9353066, 1.79)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cccc(c1)C(=O)NCC(O)=O
Show InChI InChI=1S/C21H17F3N4O3/c1-12-7-15(13-3-2-4-14(9-13)19(31)26-11-18(29)30)10-16(8-12)27-20-25-6-5-17(28-20)21(22,23)24/h2-10H,11H2,1H3,(H,26,31)(H,29,30)(H,25,27,28)
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n/an/a 4.60n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233765
PNG
(US9353066, 4.4)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cccc(c1)S(=O)(=O)NCCC(O)=O
Show InChI InChI=1S/C21H19F3N4O4S/c1-13-9-15(11-16(10-13)27-20-25-7-5-18(28-20)21(22,23)24)14-3-2-4-17(12-14)33(31,32)26-8-6-19(29)30/h2-5,7,9-12,26H,6,8H2,1H3,(H,29,30)(H,25,27,28)
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n/an/a 4.60n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233649
PNG
(US9353066, 1.102)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(Cl)c(c1)C(O)=O
Show InChI InChI=1S/C19H13ClF3N3O2/c1-10-6-12(11-2-3-15(20)14(9-11)17(27)28)8-13(7-10)25-18-24-5-4-16(26-18)19(21,22)23/h2-9H,1H3,(H,27,28)(H,24,25,26)
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n/an/a 4.80n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233740
PNG
(US9353066, 3.38)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(OCc2cn(C)cn2)c(c1)C(O)=O
Show InChI InChI=1S/C24H20F3N5O3/c1-14-7-16(9-17(8-14)30-23-28-6-5-21(31-23)24(25,26)27)15-3-4-20(19(10-15)22(33)34)35-12-18-11-32(2)13-29-18/h3-11,13H,12H2,1-2H3,(H,33,34)(H,28,30,31)
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n/an/a 5.60n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233646
PNG
(US9353066, 1.99)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(N)c(c1)C(O)=O
Show InChI InChI=1S/C19H15F3N4O2/c1-10-6-12(11-2-3-15(23)14(9-11)17(27)28)8-13(7-10)25-18-24-5-4-16(26-18)19(20,21)22/h2-9H,23H2,1H3,(H,27,28)(H,24,25,26)
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n/an/a 5.60n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233635
PNG
(US9353066, 1.88)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(-c2ccccc2)c(c1)C(O)=O
Show InChI InChI=1S/C25H18F3N3O2/c1-15-11-18(13-19(12-15)30-24-29-10-9-22(31-24)25(26,27)28)17-7-8-20(21(14-17)23(32)33)16-5-3-2-4-6-16/h2-14H,1H3,(H,32,33)(H,29,30,31)
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n/an/a 5.90n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233687
PNG
(US9353066, 1.141)
Show SMILES COc1ccnc(Nc2cc(C)cc(c2)-c2cccc(c2)C(O)=O)n1
Show InChI InChI=1S/C19H17N3O3/c1-12-8-15(13-4-3-5-14(10-13)18(23)24)11-16(9-12)21-19-20-7-6-17(22-19)25-2/h3-11H,1-2H3,(H,23,24)(H,20,21,22)
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n/an/a 6.20n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233695
PNG
(US9353066, 2.3)
Show SMILES CC(=O)Nc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(cc1)[C@@H](O)C(F)F
Show InChI InChI=1S/C21H17F5N4O2/c1-11(31)28-15-8-14(12-2-4-13(5-3-12)18(32)19(22)23)9-16(10-15)29-20-27-7-6-17(30-20)21(24,25)26/h2-10,18-19,32H,1H3,(H,28,31)(H,27,29,30)/t18-/m1/s1
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n/an/a 6.30n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233686
PNG
(US9353066, 1.140)
Show SMILES Cc1cc(Nc2nccc(n2)C2CC2)cc(c1)-c1cccc(CCC(O)=O)c1
Show InChI InChI=1S/C23H23N3O2/c1-15-11-19(18-4-2-3-16(13-18)5-8-22(27)28)14-20(12-15)25-23-24-10-9-21(26-23)17-6-7-17/h2-4,9-14,17H,5-8H2,1H3,(H,27,28)(H,24,25,26)
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n/an/a 6.40n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233666
PNG
(US9353066, 1.119)
Show SMILES Cc1cc(Nc2nccc(C)n2)cc(c1)-c1ccc(cc1)C(C)(O)[C@H]1CC[C@@H](CC1)C(O)=O
Show InChI InChI=1S/C27H31N3O3/c1-17-14-21(16-24(15-17)30-26-28-13-12-18(2)29-26)19-4-8-22(9-5-19)27(3,33)23-10-6-20(7-11-23)25(31)32/h4-5,8-9,12-16,20,23,33H,6-7,10-11H2,1-3H3,(H,31,32)(H,28,29,30)/t20-,23-,27?
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n/an/a 6.5n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233659
PNG
(US9353066, 1.112)
Show SMILES OC(=O)c1cc(cc(c1)-c1cccc(Nc2nccc(n2)C(F)(F)F)c1)C#N
Show InChI InChI=1S/C19H11F3N4O2/c20-19(21,22)16-4-5-24-18(26-16)25-15-3-1-2-12(9-15)13-6-11(10-23)7-14(8-13)17(27)28/h1-9H,(H,27,28)(H,24,25,26)
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n/an/a 6.60n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233706
PNG
(US9353066, 3.4)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(OCCF)c(c1)C(O)=O
Show InChI InChI=1S/C21H17F4N3O3/c1-12-8-14(13-2-3-17(31-7-5-22)16(11-13)19(29)30)10-15(9-12)27-20-26-6-4-18(28-20)21(23,24)25/h2-4,6,8-11H,5,7H2,1H3,(H,29,30)(H,26,27,28)
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n/an/a 6.90n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233631
PNG
(US9353066, 1.84)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(CCC(O)=O)cc1
Show InChI InChI=1S/C21H18F3N3O2/c1-13-10-16(15-5-2-14(3-6-15)4-7-19(28)29)12-17(11-13)26-20-25-9-8-18(27-20)21(22,23)24/h2-3,5-6,8-12H,4,7H2,1H3,(H,28,29)(H,25,26,27)
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n/an/a 7.10n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233764
PNG
(US9353066, 4.3)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cccc(c1)S(=O)(=O)NCCCC(O)=O
Show InChI InChI=1S/C22H21F3N4O4S/c1-14-10-16(12-17(11-14)28-21-26-9-7-19(29-21)22(23,24)25)15-4-2-5-18(13-15)34(32,33)27-8-3-6-20(30)31/h2,4-5,7,9-13,27H,3,6,8H2,1H3,(H,30,31)(H,26,28,29)
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n/an/a 7.40n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233630
PNG
(US9353066, 1.83)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cccc(CCC(O)=O)c1
Show InChI InChI=1S/C21H18F3N3O2/c1-13-9-16(15-4-2-3-14(11-15)5-6-19(28)29)12-17(10-13)26-20-25-8-7-18(27-20)21(22,23)24/h2-4,7-12H,5-6H2,1H3,(H,28,29)(H,25,26,27)
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n/an/a 7.60n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233661
PNG
(US9353066, 1.114)
Show SMILES OC(=O)c1cc(F)cc(c1)-c1cccc(Nc2nccc(n2)C(F)(F)F)c1
Show InChI InChI=1S/C18H11F4N3O2/c19-13-7-11(6-12(8-13)16(26)27)10-2-1-3-14(9-10)24-17-23-5-4-15(25-17)18(20,21)22/h1-9H,(H,26,27)(H,23,24,25)
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n/an/a 8n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233671
PNG
(US9353066, 1.124)
Show SMILES COc1ccnc(Nc2cc(C)cc(c2)-c2cccc(CCC(O)=O)c2)n1
Show InChI InChI=1S/C21H21N3O3/c1-14-10-17(16-5-3-4-15(12-16)6-7-20(25)26)13-18(11-14)23-21-22-9-8-19(24-21)27-2/h3-5,8-13H,6-7H2,1-2H3,(H,25,26)(H,22,23,24)
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Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233762
PNG
(US9353066, 4.1)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cccc(c1)S(O)(=O)=O
Show InChI InChI=1S/C18H14F3N3O3S/c1-11-7-13(12-3-2-4-15(10-12)28(25,26)27)9-14(8-11)23-17-22-6-5-16(24-17)18(19,20)21/h2-10H,1H3,(H,22,23,24)(H,25,26,27)
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Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233724
PNG
(US9353066, 3.22)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(OCc2cccnc2)c(c1)C(O)=O
Show InChI InChI=1S/C25H19F3N4O3/c1-15-9-18(11-19(10-15)31-24-30-8-6-22(32-24)25(26,27)28)17-4-5-21(20(12-17)23(33)34)35-14-16-3-2-7-29-13-16/h2-13H,14H2,1H3,(H,33,34)(H,30,31,32)
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Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233739
PNG
(US9353066, 3.37)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(OCc2cncn2C)c(c1)C(O)=O
Show InChI InChI=1S/C24H20F3N5O3/c1-14-7-16(9-17(8-14)30-23-29-6-5-21(31-23)24(25,26)27)15-3-4-20(19(10-15)22(33)34)35-12-18-11-28-13-32(18)2/h3-11,13H,12H2,1-2H3,(H,33,34)(H,29,30,31)
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Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233700
PNG
(US9353066, 2.8)
Show SMILES CCNC(=O)Nc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(cc1)[C@@H](O)C(F)F
Show InChI InChI=1S/C22H20F5N5O2/c1-2-28-21(34)31-16-10-14(12-3-5-13(6-4-12)18(33)19(23)24)9-15(11-16)30-20-29-8-7-17(32-20)22(25,26)27/h3-11,18-19,33H,2H2,1H3,(H2,28,31,34)(H,29,30,32)/t18-/m1/s1
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Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233737
PNG
(US9353066, 3.35)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(OCCCCO)c(c1)C(O)=O
Show InChI InChI=1S/C23H22F3N3O4/c1-14-10-16(12-17(11-14)28-22-27-7-6-20(29-22)23(24,25)26)15-4-5-19(18(13-15)21(31)32)33-9-3-2-8-30/h4-7,10-13,30H,2-3,8-9H2,1H3,(H,31,32)(H,27,28,29)
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Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233736
PNG
(US9353066, 3.34)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(OCCCO)c(c1)C(O)=O
Show InChI InChI=1S/C22H20F3N3O4/c1-13-9-15(14-3-4-18(32-8-2-7-29)17(12-14)20(30)31)11-16(10-13)27-21-26-6-5-19(28-21)22(23,24)25/h3-6,9-12,29H,2,7-8H2,1H3,(H,30,31)(H,26,27,28)
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Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233662
PNG
(US9353066, 1.115)
Show SMILES Nc1ccc(cc1C(O)=O)-c1cccc(Nc2nccc(n2)C(F)(F)F)c1
Show InChI InChI=1S/C18H13F3N4O2/c19-18(20,21)15-6-7-23-17(25-15)24-12-3-1-2-10(8-12)11-4-5-14(22)13(9-11)16(26)27/h1-9H,22H2,(H,26,27)(H,23,24,25)
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Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233713
PNG
(US9353066, 3.11)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(OCc2cccc(F)c2)c(c1)C(O)=O
Show InChI InChI=1S/C26H19F4N3O3/c1-15-9-18(12-20(10-15)32-25-31-8-7-23(33-25)26(28,29)30)17-5-6-22(21(13-17)24(34)35)36-14-16-3-2-4-19(27)11-16/h2-13H,14H2,1H3,(H,34,35)(H,31,32,33)
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Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233703
PNG
(US9353066, 3.1)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cccc(c1)C(=O)NS(C)(=O)=O
Show InChI InChI=1S/C20H17F3N4O3S/c1-12-8-15(13-4-3-5-14(10-13)18(28)27-31(2,29)30)11-16(9-12)25-19-24-7-6-17(26-19)20(21,22)23/h3-11H,1-2H3,(H,27,28)(H,24,25,26)
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Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233648
PNG
(US9353066, 1.101)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cc(N)cc(c1)C(O)=O
Show InChI InChI=1S/C19H15F3N4O2/c1-10-4-11(12-6-13(17(27)28)8-14(23)7-12)9-15(5-10)25-18-24-3-2-16(26-18)19(20,21)22/h2-9H,23H2,1H3,(H,27,28)(H,24,25,26)
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Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233708
PNG
(US9353066, 3.6)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(OCC2CC2)c(c1)C(O)=O
Show InChI InChI=1S/C23H20F3N3O3/c1-13-8-16(10-17(9-13)28-22-27-7-6-20(29-22)23(24,25)26)15-4-5-19(18(11-15)21(30)31)32-12-14-2-3-14/h4-11,14H,2-3,12H2,1H3,(H,30,31)(H,27,28,29)
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Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233710
PNG
(US9353066, 3.8)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(OCc2ccccc2)c(c1)C(O)=O
Show InChI InChI=1S/C26H20F3N3O3/c1-16-11-19(13-20(12-16)31-25-30-10-9-23(32-25)26(27,28)29)18-7-8-22(21(14-18)24(33)34)35-15-17-5-3-2-4-6-17/h2-14H,15H2,1H3,(H,33,34)(H,30,31,32)
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Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233548
PNG
(US9353066, 1.1)
Show SMILES Cc1cc(Nc2nccc(OC3CCNCC3)n2)cc(c1)-c1ccccc1
Show InChI InChI=1S/C22H24N4O/c1-16-13-18(17-5-3-2-4-6-17)15-19(14-16)25-22-24-12-9-21(26-22)27-20-7-10-23-11-8-20/h2-6,9,12-15,20,23H,7-8,10-11H2,1H3,(H,24,25,26)
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Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233709
PNG
(US9353066, 3.7)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(OC2CCCCC2)c(c1)C(O)=O
Show InChI InChI=1S/C25H24F3N3O3/c1-15-11-17(13-18(12-15)30-24-29-10-9-22(31-24)25(26,27)28)16-7-8-21(20(14-16)23(32)33)34-19-5-3-2-4-6-19/h7-14,19H,2-6H2,1H3,(H,32,33)(H,29,30,31)
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Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233699
PNG
(US9353066, 2.7)
Show SMILES O[C@@H](C(F)F)c1ccc(cc1)-c1cc(NC(=O)NS(=O)(=O)c2ccc(Cl)cc2)cc(Nc2nccc(n2)C(F)(F)F)c1
Show InChI InChI=1S/C26H19ClF5N5O4S/c27-17-5-7-20(8-6-17)42(40,41)37-25(39)35-19-12-16(14-1-3-15(4-2-14)22(38)23(28)29)11-18(13-19)34-24-33-10-9-21(36-24)26(30,31)32/h1-13,22-23,38H,(H,33,34,36)(H2,35,37,39)/t22-/m1/s1
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Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233723
PNG
(US9353066, 3.21)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(OCc2ccccn2)c(c1)C(O)=O
Show InChI InChI=1S/C25H19F3N4O3/c1-15-10-17(12-19(11-15)31-24-30-9-7-22(32-24)25(26,27)28)16-5-6-21(20(13-16)23(33)34)35-14-18-4-2-3-8-29-18/h2-13H,14H2,1H3,(H,33,34)(H,30,31,32)
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n/an/a 14.3n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233718
PNG
(US9353066, 3.16)
Show SMILES COCCCOc1ccc(cc1C(O)=O)-c1cc(C)cc(Nc2nccc(n2)C(F)(F)F)c1
Show InChI InChI=1S/C23H22F3N3O4/c1-14-10-16(12-17(11-14)28-22-27-7-6-20(29-22)23(24,25)26)15-4-5-19(18(13-15)21(30)31)33-9-3-8-32-2/h4-7,10-13H,3,8-9H2,1-2H3,(H,30,31)(H,27,28,29)
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n/an/a 15n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233689
PNG
(US9353066, 1.143)
Show SMILES N#Cc1cnc(Nc2cccc(c2)-c2ccccc2)nc1N1CCC2(CCNC2)CC1
Show InChI InChI=1S/C25H26N6/c26-16-21-17-28-24(29-22-8-4-7-20(15-22)19-5-2-1-3-6-19)30-23(21)31-13-10-25(11-14-31)9-12-27-18-25/h1-8,15,17,27H,9-14,18H2,(H,28,29,30)
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n/an/a 15.8n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233688
PNG
(US9353066, 1.142)
Show SMILES Cc1cc(Nc2nccc(C)n2)cc(c1)-c1cccc(c1)C(O)=O
Show InChI InChI=1S/C19H17N3O2/c1-12-8-16(14-4-3-5-15(10-14)18(23)24)11-17(9-12)22-19-20-7-6-13(2)21-19/h3-11H,1-2H3,(H,23,24)(H,20,21,22)
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n/an/a 16n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233725
PNG
(US9353066, 3.23)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(OCc2ccncc2)c(c1)C(O)=O
Show InChI InChI=1S/C25H19F3N4O3/c1-15-10-18(12-19(11-15)31-24-30-9-6-22(32-24)25(26,27)28)17-2-3-21(20(13-17)23(33)34)35-14-16-4-7-29-8-5-16/h2-13H,14H2,1H3,(H,33,34)(H,30,31,32)
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n/an/a 16.3n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233727
PNG
(US9353066, 3.25)
Show SMILES COc1cccc(COc2ccc(cc2C(O)=O)-c2cc(C)cc(Nc3nccc(n3)C(F)(F)F)c2)c1
Show InChI InChI=1S/C27H22F3N3O4/c1-16-10-19(13-20(11-16)32-26-31-9-8-24(33-26)27(28,29)30)18-6-7-23(22(14-18)25(34)35)37-15-17-4-3-5-21(12-17)36-2/h3-14H,15H2,1-2H3,(H,34,35)(H,31,32,33)
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n/an/a 17.4n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233742
PNG
(US9353066, 3.40)
Show SMILES CC(=O)NCCCOc1ccc(cc1C(O)=O)-c1cc(C)cc(Nc2nccc(n2)C(F)(F)F)c1
Show InChI InChI=1S/C24H23F3N4O4/c1-14-10-17(12-18(11-14)30-23-29-8-6-21(31-23)24(25,26)27)16-4-5-20(19(13-16)22(33)34)35-9-3-7-28-15(2)32/h4-6,8,10-13H,3,7,9H2,1-2H3,(H,28,32)(H,33,34)(H,29,30,31)
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n/an/a 17.4n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233705
PNG
(US9353066, 3.3)
Show SMILES CC(C)COc1ccc(cc1C(O)=O)-c1cc(C)cc(Nc2nccc(n2)C(F)(F)F)c1
Show InChI InChI=1S/C23H22F3N3O3/c1-13(2)12-32-19-5-4-15(11-18(19)21(30)31)16-8-14(3)9-17(10-16)28-22-27-7-6-20(29-22)23(24,25)26/h4-11,13H,12H2,1-3H3,(H,30,31)(H,27,28,29)
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n/an/a 18.3n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233647
PNG
(US9353066, 1.100)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(O)c(c1)C(O)=O
Show InChI InChI=1S/C19H14F3N3O3/c1-10-6-12(11-2-3-15(26)14(9-11)17(27)28)8-13(7-10)24-18-23-5-4-16(25-18)19(20,21)22/h2-9,26H,1H3,(H,27,28)(H,23,24,25)
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n/an/a 18.4n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


Citation and Details
More data for this
Ligand-Target Pair
Tyrosine-protein kinase SYK


(Homo sapiens (human))
BDBM233704
PNG
(US9353066, 3.2)
Show SMILES Cc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cccc(c1)-c1nnn[nH]1
Show InChI InChI=1S/C19H14F3N7/c1-11-7-14(12-3-2-4-13(9-12)17-26-28-29-27-17)10-15(8-11)24-18-23-6-5-16(25-18)19(20,21)22/h2-10H,1H3,(H,23,24,25)(H,26,27,28,29)
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n/an/a 18.7n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.; Merck Canada Inc.

US Patent


Assay Description
A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human Syk activity. The recombinant human GST-SYK (Carna Bi...


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