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Patent code US9499534

Compile Data Set for Download or QSAR
Found 42 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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255549
PNG
(US9499534, 1.2)
Show SMILES C[C@@H]1C[C@](O)(CC[C@@H]1C(O)=O)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cn[nH]c1
Show InChI InChI=1S/C25H23F3N6O3S/c1-13-9-24(37,4-2-18(13)21(35)36)22-30-12-19(38-22)15-6-14(16-10-31-32-11-16)7-17(8-15)33-23-29-5-3-20(34-23)25(26,27)28/h3,5-8,10-13,18,37H,2,4,9H2,1H3,(H,31,32)(H,35,36)(H,29,33,34)/t13-,18+,24-/m1/s1
PDB

UniProtKB/SwissProt
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UniChem
US Patent
n/an/a 0.959n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255564
PNG
(US9499534, 2.11)
Show SMILES CC1(C)C[C@](O)(CC[C@@H]1C(O)=O)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccn[nH]1
Show InChI InChI=1S/C26H25F3N6O3S/c1-24(2)13-25(38,6-3-17(24)21(36)37)22-31-12-19(39-22)15-9-14(18-4-8-32-35-18)10-16(11-15)33-23-30-7-5-20(34-23)26(27,28)29/h4-5,7-12,17,38H,3,6,13H2,1-2H3,(H,32,35)(H,36,37)(H,30,33,34)/t17-,25-/m1/s1
PDB

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UniChem
US Patent
n/an/a 1.11n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255553
PNG
(US9499534, 1.6)
Show SMILES COc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cnc(s1)[C@@]1(O)CC[C@@H](CC1)C(O)=O
Show InChI InChI=1S/C22H21F3N4O4S/c1-33-15-9-13(8-14(10-15)28-20-26-7-4-17(29-20)22(23,24)25)16-11-27-19(34-16)21(32)5-2-12(3-6-21)18(30)31/h4,7-12,32H,2-3,5-6H2,1H3,(H,30,31)(H,26,28,29)/t12-,21+
PDB

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UniChem
US Patent
n/an/a 1.29n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255572
PNG
(US9499534, 2.19)
Show SMILES CC1(C)C[C@](O)(CC[C@@H]1C(O)=O)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(N)nc1
Show InChI InChI=1S/C28H27F3N6O3S/c1-26(2)14-27(40,7-5-19(26)23(38)39)24-35-13-20(41-24)17-9-16(15-3-4-22(32)34-12-15)10-18(11-17)36-25-33-8-6-21(37-25)28(29,30)31/h3-4,6,8-13,19,40H,5,7,14H2,1-2H3,(H2,32,34)(H,38,39)(H,33,36,37)/t19-,27-/m1/s1
PDB

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UniChem
US Patent
n/an/a 1.29n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255552
PNG
(US9499534, 1.5)
Show SMILES COc1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cnc(s1)[C@@]1(O)CC[C@H](C(O)=O)C(C)(C)C1
Show InChI InChI=1S/C24H25F3N4O4S/c1-22(2)12-23(34,6-4-16(22)19(32)33)20-29-11-17(36-20)13-8-14(10-15(9-13)35-3)30-21-28-7-5-18(31-21)24(25,26)27/h5,7-11,16,34H,4,6,12H2,1-3H3,(H,32,33)(H,28,30,31)/t16-,23-/m1/s1
PDB

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UniChem
US Patent
n/an/a 1.40n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255558
PNG
(US9499534, 2.5)
Show SMILES CC1(C)C[C@](O)(CC[C@@H]1C(O)=O)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccncc1
Show InChI InChI=1S/C28H26F3N5O3S/c1-26(2)15-27(39,7-3-20(26)23(37)38)24-34-14-21(40-24)18-11-17(16-4-8-32-9-5-16)12-19(13-18)35-25-33-10-6-22(36-25)28(29,30)31/h4-6,8-14,20,39H,3,7,15H2,1-2H3,(H,37,38)(H,33,35,36)/t20-,27-/m1/s1
PDB

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US Patent
n/an/a 1.56n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255563
PNG
(US9499534, 2.10)
Show SMILES CC1(C)C[C@](O)(CC[C@@H]1C(O)=O)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cn[nH]c1
Show InChI InChI=1S/C26H25F3N6O3S/c1-24(2)13-25(38,5-3-18(24)21(36)37)22-31-12-19(39-22)15-7-14(16-10-32-33-11-16)8-17(9-15)34-23-30-6-4-20(35-23)26(27,28)29/h4,6-12,18,38H,3,5,13H2,1-2H3,(H,32,33)(H,36,37)(H,30,34,35)/t18-,25-/m1/s1
PDB

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US Patent
n/an/a 2.38n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255584
PNG
(US9499534, 3.1)
Show SMILES CC1(C)C[C@](O)(CC[C@@H]1C(O)=O)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1nccs1
Show InChI InChI=1S/C26H24F3N5O3S2/c1-24(2)13-25(37,5-3-17(24)21(35)36)22-32-12-18(39-22)14-9-15(20-30-7-8-38-20)11-16(10-14)33-23-31-6-4-19(34-23)26(27,28)29/h4,6-12,17,37H,3,5,13H2,1-2H3,(H,35,36)(H,31,33,34)/t17-,25-/m1/s1
PDB

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US Patent
n/an/a 2.5n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255579
PNG
(US9499534, 2.26)
Show SMILES CC\C=C/c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cnc(s1)[C@@]1(O)CC[C@H](C(O)=O)C(C)(C)C1
Show InChI InChI=1S/C27H29F3N4O3S/c1-4-5-6-16-11-17(13-18(12-16)33-24-31-10-8-21(34-24)27(28,29)30)20-14-32-23(38-20)26(37)9-7-19(22(35)36)25(2,3)15-26/h5-6,8,10-14,19,37H,4,7,9,15H2,1-3H3,(H,35,36)(H,31,33,34)/b6-5-/t19-,26-/m1/s1
PDB

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PC sid
UniChem
US Patent
n/an/a 2.68n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255581
PNG
(US9499534, 2.28)
Show SMILES C\C=C(/C)c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cnc(s1)[C@@]1(O)CC[C@H](C(O)=O)C(C)(C)C1
Show InChI InChI=1S/C27H29F3N4O3S/c1-5-15(2)16-10-17(12-18(11-16)33-24-31-9-7-21(34-24)27(28,29)30)20-13-32-23(38-20)26(37)8-6-19(22(35)36)25(3,4)14-26/h5,7,9-13,19,37H,6,8,14H2,1-4H3,(H,35,36)(H,31,33,34)/b15-5+/t19-,26-/m1/s1
PDB

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UniChem
US Patent
n/an/a 2.75n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255562
PNG
(US9499534, 2.9)
Show SMILES CC1(C)C[C@](O)(CC[C@@H]1C(O)=O)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cccc(c1)C(=O)NC1CC1
Show InChI InChI=1S/C33H32F3N5O4S/c1-31(2)17-32(45,10-8-24(31)28(43)44)29-38-16-25(46-29)21-13-20(18-4-3-5-19(12-18)27(42)39-22-6-7-22)14-23(15-21)40-30-37-11-9-26(41-30)33(34,35)36/h3-5,9,11-16,22,24,45H,6-8,10,17H2,1-2H3,(H,39,42)(H,43,44)(H,37,40,41)/t24-,32-/m1/s1
PDB

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US Patent
n/an/a 2.78n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255550
PNG
(US9499534, 1.3)
Show SMILES C[C@@H]1C[C@](O)(CC[C@@H]1C(N)=O)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cn[nH]c1
Show InChI InChI=1S/C25H24F3N7O2S/c1-13-9-24(37,4-2-18(13)21(29)36)22-31-12-19(38-22)15-6-14(16-10-32-33-11-16)7-17(8-15)34-23-30-5-3-20(35-23)25(26,27)28/h3,5-8,10-13,18,37H,2,4,9H2,1H3,(H2,29,36)(H,32,33)(H,30,34,35)/t13-,18+,24-/m1/s1
PDB

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US Patent
n/an/a 2.95n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255568
PNG
(US9499534, 2.15)
Show SMILES CC1(C)C[C@](O)(CC[C@@H]1C(O)=O)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cncc(F)c1
Show InChI InChI=1S/C28H25F4N5O3S/c1-26(2)14-27(40,5-3-20(26)23(38)39)24-35-13-21(41-24)16-7-15(17-8-18(29)12-33-11-17)9-19(10-16)36-25-34-6-4-22(37-25)28(30,31)32/h4,6-13,20,40H,3,5,14H2,1-2H3,(H,38,39)(H,34,36,37)/t20-,27-/m1/s1
PDB

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PC cid
PC sid
UniChem
US Patent
n/an/a 3.22n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255560
PNG
(US9499534, 2.7)
Show SMILES COc1ccc(cn1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cnc(s1)[C@@]1(O)CC[C@H](C(O)=O)C(C)(C)C1
Show InChI InChI=1S/C29H28F3N5O4S/c1-27(2)15-28(40,8-6-20(27)24(38)39)25-35-14-21(42-25)18-10-17(16-4-5-23(41-3)34-13-16)11-19(12-18)36-26-33-9-7-22(37-26)29(30,31)32/h4-5,7,9-14,20,40H,6,8,15H2,1-3H3,(H,38,39)(H,33,36,37)/t20-,28-/m1/s1
PDB

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UniChem
US Patent
n/an/a 3.68n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255583
PNG
(US9499534, 2.30)
Show SMILES CC(=C)c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cnc(s1)[C@@]1(O)CC[C@H](C(O)=O)C(C)(C)C1
Show InChI InChI=1S/C26H27F3N4O3S/c1-14(2)15-9-16(11-17(10-15)32-23-30-8-6-20(33-23)26(27,28)29)19-12-31-22(37-19)25(36)7-5-18(21(34)35)24(3,4)13-25/h6,8-12,18,36H,1,5,7,13H2,2-4H3,(H,34,35)(H,30,32,33)/t18-,25-/m1/s1
PDB

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US Patent
n/an/a 3.94n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255580
PNG
(US9499534, 2.27)
Show SMILES CC1(C)C[C@](O)(CC[C@@H]1C(O)=O)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(\C=C/C2CC2)c1
Show InChI InChI=1S/C28H29F3N4O3S/c1-26(2)15-27(38,9-7-20(26)23(36)37)24-33-14-21(39-24)18-11-17(6-5-16-3-4-16)12-19(13-18)34-25-32-10-8-22(35-25)28(29,30)31/h5-6,8,10-14,16,20,38H,3-4,7,9,15H2,1-2H3,(H,36,37)(H,32,34,35)/b6-5-/t20-,27-/m1/s1
PDB

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UniChem
US Patent
n/an/a 4.06n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255588
PNG
(US9499534, 1.9)
Show SMILES CC1(C)C[C@@](O)(CC[C@H]1C(O)=O)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)S(C)(=O)=O
Show InChI InChI=1S/C24H25F3N4O5S2/c1-22(2)12-23(34,6-4-16(22)19(32)33)20-29-11-17(37-20)13-8-14(10-15(9-13)38(3,35)36)30-21-28-7-5-18(31-21)24(25,26)27/h5,7-11,16,34H,4,6,12H2,1-3H3,(H,32,33)(H,28,30,31)/t16-,23-/m0/s1
PDB

UniProtKB/SwissProt
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PC cid
PC sid
UniChem
US Patent
n/an/a 5.10n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255587
PNG
(US9499534, 1.8)
Show SMILES CC1(C)C[C@@](O)(CC[C@H]1C(O)=O)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)C#N
Show InChI InChI=1S/C24H22F3N5O3S/c1-22(2)12-23(35,5-3-16(22)19(33)34)20-30-11-17(36-20)14-7-13(10-28)8-15(9-14)31-21-29-6-4-18(32-21)24(25,26)27/h4,6-9,11,16,35H,3,5,12H2,1-2H3,(H,33,34)(H,29,31,32)/t16-,23-/m0/s1
PDB

UniProtKB/SwissProt
UniProtKB/TrEMBL

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PC cid
PC sid
UniChem
US Patent
n/an/a 5.77n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255586
PNG
(US9499534, 1.7)
Show SMILES OC(=O)C1CCC(O)(CC1)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)C#N
Show InChI InChI=1S/C22H18F3N5O3S/c23-22(24,25)17-3-6-27-20(30-17)29-15-8-12(10-26)7-14(9-15)16-11-28-19(34-16)21(33)4-1-13(2-5-21)18(31)32/h3,6-9,11,13,33H,1-2,4-5H2,(H,31,32)(H,27,29,30)
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n/an/a 8.48n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255576
PNG
(US9499534, 2.23)
Show SMILES Cc1ccsc1-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cnc(s1)[C@@]1(O)CC[C@H](C(O)=O)C(C)(C)C1
Show InChI InChI=1S/C28H27F3N4O3S2/c1-15-6-9-39-22(15)17-10-16(11-18(12-17)34-25-32-8-5-21(35-25)28(29,30)31)20-13-33-24(40-20)27(38)7-4-19(23(36)37)26(2,3)14-27/h5-6,8-13,19,38H,4,7,14H2,1-3H3,(H,36,37)(H,32,34,35)/t19-,27-/m1/s1
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n/an/a 10.1n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255566
PNG
(US9499534, 2.13)
Show SMILES COCc1ccc(cc1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cnc(s1)[C@@]1(O)CC[C@H](C(O)=O)C(C)(C)C1
Show InChI InChI=1S/C31H31F3N4O4S/c1-29(2)17-30(41,10-8-23(29)26(39)40)27-36-15-24(43-27)21-12-20(19-6-4-18(5-7-19)16-42-3)13-22(14-21)37-28-35-11-9-25(38-28)31(32,33)34/h4-7,9,11-15,23,41H,8,10,16-17H2,1-3H3,(H,39,40)(H,35,37,38)/t23-,30-/m1/s1
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n/an/a 10.2n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255561
PNG
(US9499534, 2.8)
Show SMILES CC1(C)C[C@](O)(CC[C@@H]1C(O)=O)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccsc1
Show InChI InChI=1S/C27H25F3N4O3S2/c1-25(2)14-26(37,6-3-19(25)22(35)36)23-32-12-20(39-23)17-9-16(15-5-8-38-13-15)10-18(11-17)33-24-31-7-4-21(34-24)27(28,29)30/h4-5,7-13,19,37H,3,6,14H2,1-2H3,(H,35,36)(H,31,33,34)/t19-,26-/m1/s1
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n/an/a 11.7n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255585
PNG
(US9499534, 3.2)
Show SMILES CC1(C)C[C@](O)(CC[C@@H]1C(O)=O)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cccs1
Show InChI InChI=1S/C27H25F3N4O3S2/c1-25(2)14-26(37,7-5-18(25)22(35)36)23-32-13-20(39-23)16-10-15(19-4-3-9-38-19)11-17(12-16)33-24-31-8-6-21(34-24)27(28,29)30/h3-4,6,8-13,18,37H,5,7,14H2,1-2H3,(H,35,36)(H,31,33,34)/t18-,26-/m1/s1
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n/an/a 12.4n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255567
PNG
(US9499534, 2.14)
Show SMILES CC1(C)C[C@](O)(CC[C@@H]1C(O)=O)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cccc(F)c1F
Show InChI InChI=1S/C29H25F5N4O3S/c1-27(2)14-28(41,8-6-19(27)24(39)40)25-36-13-21(42-25)16-10-15(18-4-3-5-20(30)23(18)31)11-17(12-16)37-26-35-9-7-22(38-26)29(32,33)34/h3-5,7,9-13,19,41H,6,8,14H2,1-2H3,(H,39,40)(H,35,37,38)/t19-,28-/m1/s1
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n/an/a 12.9n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255570
PNG
(US9499534, 2.17)
Show SMILES CS(=O)c1ccccc1-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cnc(s1)[C@@]1(O)CC[C@H](C(O)=O)C(C)(C)C1
Show InChI InChI=1S/C30H29F3N4O4S2/c1-28(2)16-29(40,10-8-21(28)25(38)39)26-35-15-22(42-26)18-12-17(20-6-4-5-7-23(20)43(3)41)13-19(14-18)36-27-34-11-9-24(37-27)30(31,32)33/h4-7,9,11-15,21,40H,8,10,16H2,1-3H3,(H,38,39)(H,34,36,37)/t21-,29-,43?/m1/s1
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n/an/a 15.3n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255582
PNG
(US9499534, 2.29)
Show SMILES CC(C)(C)\C=C/c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cnc(s1)[C@@]1(O)CC[C@H](C(O)=O)C(C)(C)C1
Show InChI InChI=1S/C29H33F3N4O3S/c1-26(2,3)9-6-17-12-18(14-19(13-17)35-25-33-11-8-22(36-25)29(30,31)32)21-15-34-24(40-21)28(39)10-7-20(23(37)38)27(4,5)16-28/h6,8-9,11-15,20,39H,7,10,16H2,1-5H3,(H,37,38)(H,33,35,36)/b9-6-/t20-,28-/m1/s1
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n/an/a 16.8n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255574
PNG
(US9499534, 2.21)
Show SMILES CC1(C)C[C@](O)(CC[C@@H]1C(O)=O)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)C1=CCCCC1
Show InChI InChI=1S/C29H31F3N4O3S/c1-27(2)16-28(39,10-8-21(27)24(37)38)25-34-15-22(40-25)19-12-18(17-6-4-3-5-7-17)13-20(14-19)35-26-33-11-9-23(36-26)29(30,31)32/h6,9,11-15,21,39H,3-5,7-8,10,16H2,1-2H3,(H,37,38)(H,33,35,36)/t21-,28-/m1/s1
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n/an/a 17.6n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255559
PNG
(US9499534, 2.6)
Show SMILES CC1(C)C[C@](O)(CC[C@@H]1C(O)=O)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(F)cc1
Show InChI InChI=1S/C29H26F4N4O3S/c1-27(2)15-28(40,9-7-21(27)24(38)39)25-35-14-22(41-25)18-11-17(16-3-5-19(30)6-4-16)12-20(13-18)36-26-34-10-8-23(37-26)29(31,32)33/h3-6,8,10-14,21,40H,7,9,15H2,1-2H3,(H,38,39)(H,34,36,37)/t21-,28-/m1/s1
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n/an/a 20.7n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255577
PNG
(US9499534, 2.24)
Show SMILES Cc1cscc1-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cnc(s1)[C@@]1(O)CC[C@H](C(O)=O)C(C)(C)C1
Show InChI InChI=1S/C28H27F3N4O3S2/c1-15-12-39-13-19(15)16-8-17(10-18(9-16)34-25-32-7-5-22(35-25)28(29,30)31)21-11-33-24(40-21)27(38)6-4-20(23(36)37)26(2,3)14-27/h5,7-13,20,38H,4,6,14H2,1-3H3,(H,36,37)(H,32,34,35)/t20-,27-/m1/s1
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n/an/a 24.6n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255589
PNG
(US9499534, 3.3)
Show SMILES CC1(C)C[C@](O)(CC[C@@H]1C(O)=O)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccc(C#N)c(F)c1
Show InChI InChI=1S/C30H25F4N5O3S/c1-28(2)15-29(42,7-5-21(28)25(40)41)26-37-14-23(43-26)19-9-18(16-3-4-17(13-35)22(31)12-16)10-20(11-19)38-27-36-8-6-24(39-27)30(32,33)34/h3-4,6,8-12,14,21,42H,5,7,15H2,1-2H3,(H,40,41)(H,36,38,39)/t21-,29-/m1/s1
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n/an/a 34.8n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255578
PNG
(US9499534, 2.25)
Show SMILES CC1(C)C[C@](O)(CC[C@@H]1C(O)=O)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccccc1F
Show InChI InChI=1S/C29H26F4N4O3S/c1-27(2)15-28(40,9-7-20(27)24(38)39)25-35-14-22(41-25)17-11-16(19-5-3-4-6-21(19)30)12-18(13-17)36-26-34-10-8-23(37-26)29(31,32)33/h3-6,8,10-14,20,40H,7,9,15H2,1-2H3,(H,38,39)(H,34,36,37)/t20-,28-/m1/s1
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n/an/a 35.2n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255565
PNG
(US9499534, 2.12)
Show SMILES COc1ccc(cc1F)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cnc(s1)[C@@]1(O)CC[C@H](C(O)=O)C(C)(C)C1
Show InChI InChI=1S/C30H28F4N4O4S/c1-28(2)15-29(41,8-6-20(28)25(39)40)26-36-14-23(43-26)18-10-17(16-4-5-22(42-3)21(31)13-16)11-19(12-18)37-27-35-9-7-24(38-27)30(32,33)34/h4-5,7,9-14,20,41H,6,8,15H2,1-3H3,(H,39,40)(H,35,37,38)/t20-,29-/m1/s1
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Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255571
PNG
(US9499534, 2.18)
Show SMILES CC1(C)C[C@](O)(CC[C@@H]1C(O)=O)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1ccccc1Cl
Show InChI InChI=1S/C29H26ClF3N4O3S/c1-27(2)15-28(40,9-7-20(27)24(38)39)25-35-14-22(41-25)17-11-16(19-5-3-4-6-21(19)30)12-18(13-17)36-26-34-10-8-23(37-26)29(31,32)33/h3-6,8,10-14,20,40H,7,9,15H2,1-2H3,(H,38,39)(H,34,36,37)/t20-,28-/m1/s1
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n/an/a 37.1n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255575
PNG
(US9499534, 2.22)
Show SMILES Cc1ccc(F)c(c1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cnc(s1)[C@@]1(O)CC[C@H](C(O)=O)C(C)(C)C1
Show InChI InChI=1S/C30H28F4N4O3S/c1-16-4-5-22(31)20(10-16)17-11-18(13-19(12-17)37-27-35-9-7-24(38-27)30(32,33)34)23-14-36-26(42-23)29(41)8-6-21(25(39)40)28(2,3)15-29/h4-5,7,9-14,21,41H,6,8,15H2,1-3H3,(H,39,40)(H,35,37,38)/t21-,29-/m1/s1
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Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255554
PNG
(US9499534, 2.1)
Show SMILES Cn1cc(cn1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cnc(s1)[C@@]1(O)CC[C@H](C(O)=O)C(C)(C)C1
Show InChI InChI=1S/C27H27F3N6O3S/c1-25(2)14-26(39,6-4-19(25)22(37)38)23-32-12-20(40-23)16-8-15(17-11-33-36(3)13-17)9-18(10-16)34-24-31-7-5-21(35-24)27(28,29)30/h5,7-13,19,39H,4,6,14H2,1-3H3,(H,37,38)(H,31,34,35)/t19-,26-/m1/s1
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n/an/a 48.0n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255557
PNG
(US9499534, 2.4)
Show SMILES CCn1cc(cn1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cnc(s1)[C@@]1(O)CC[C@H](C(O)=O)C(C)(C)C1
Show InChI InChI=1S/C28H29F3N6O3S/c1-4-37-14-18(12-34-37)16-9-17(11-19(10-16)35-25-32-8-6-22(36-25)28(29,30)31)21-13-33-24(41-21)27(40)7-5-20(23(38)39)26(2,3)15-27/h6,8-14,20,40H,4-5,7,15H2,1-3H3,(H,38,39)(H,32,35,36)/t20-,27-/m1/s1
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n/an/a 63.5n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255573
PNG
(US9499534, 2.20)
Show SMILES Cc1ccccc1-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cnc(s1)[C@@]1(O)CC[C@H](C(O)=O)C(C)(C)C1
Show InChI InChI=1S/C30H29F3N4O3S/c1-17-6-4-5-7-21(17)18-12-19(14-20(13-18)36-27-34-11-9-24(37-27)30(31,32)33)23-15-35-26(41-23)29(40)10-8-22(25(38)39)28(2,3)16-29/h4-7,9,11-15,22,40H,8,10,16H2,1-3H3,(H,38,39)(H,34,36,37)/t22-,29-/m1/s1
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n/an/a 70.4n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255551
PNG
(US9499534, 1.4)
Show SMILES OC1(CCC1)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1nnn[nH]1
Show InChI InChI=1S/C19H15F3N8OS/c20-19(21,22)14-2-5-23-17(26-14)25-12-7-10(6-11(8-12)15-27-29-30-28-15)13-9-24-16(32-13)18(31)3-1-4-18/h2,5-9,31H,1,3-4H2,(H,23,25,26)(H,27,28,29,30)
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n/an/a 77.7n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255556
PNG
(US9499534, 2.3)
Show SMILES CC(C)n1cc(cn1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cnc(s1)[C@@]1(O)CC[C@H](C(O)=O)C(C)(C)C1
Show InChI InChI=1S/C29H31F3N6O3S/c1-16(2)38-14-19(12-35-38)17-9-18(11-20(10-17)36-26-33-8-6-23(37-26)29(30,31)32)22-13-34-25(42-22)28(41)7-5-21(24(39)40)27(3,4)15-28/h6,8-14,16,21,41H,5,7,15H2,1-4H3,(H,39,40)(H,33,36,37)/t21-,28-/m1/s1
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n/an/a 149n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255569
PNG
(US9499534, 2.16)
Show SMILES Cc1cc(ccc1F)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cnc(s1)[C@@]1(O)CC[C@H](C(O)=O)C(C)(C)C1
Show InChI InChI=1S/C30H28F4N4O3S/c1-16-10-17(4-5-22(16)31)18-11-19(13-20(12-18)37-27-35-9-7-24(38-27)30(32,33)34)23-14-36-26(42-23)29(41)8-6-21(25(39)40)28(2,3)15-29/h4-5,7,9-14,21,41H,6,8,15H2,1-3H3,(H,39,40)(H,35,37,38)/t21-,29-/m1/s1
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Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255548
PNG
(US9499534, 1.1)
Show SMILES CCOC(=O)[C@H]1CC[C@@](O)(C[C@H]1C)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cn[nH]c1
Show InChI InChI=1S/C27H27F3N6O3S/c1-3-39-23(37)20-4-6-26(38,11-15(20)2)24-32-14-21(40-24)17-8-16(18-12-33-34-13-18)9-19(10-17)35-25-31-7-5-22(36-25)27(28,29)30/h5,7-10,12-15,20,38H,3-4,6,11H2,1-2H3,(H,33,34)(H,31,35,36)/t15-,20+,26-/m1/s1
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n/an/a 162n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
GST-Tyrosine-protein kinase SYK


(Homo sapiens (Human)-Homo sapiens (human))
BDBM255555
PNG
(US9499534, 2.2)
Show SMILES CC(C)(C)n1cc(cn1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)-c1cnc(s1)[C@@]1(O)CC[C@H](C(O)=O)C(C)(C)C1
Show InChI InChI=1S/C30H33F3N6O3S/c1-27(2,3)39-15-19(13-36-39)17-10-18(12-20(11-17)37-26-34-9-7-23(38-26)30(31,32)33)22-14-35-25(43-22)29(42)8-6-21(24(40)41)28(4,5)16-29/h7,9-15,21,42H,6,8,16H2,1-5H3,(H,40,41)(H,34,37,38)/t21-,29-/m1/s1
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n/an/a 285n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

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
* indicates data uncertainty>20%