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Patent code US9771369

Compile Data Set for Download or QSAR

Found 502 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 Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342222
PNG
(4-[4-[5-(4-methoxy-3-methyl-phenyl)-4- methyl-1H-i...)
Show SMILES COc1cc(ccn1)-c1cc2c(ncnc2[nH]1)N1CCC(C)(CC1)c1nc(C)c([nH]1)-c1ccc(OC)c(C)c1
Show InChI InChI=1S/C30H33N7O2/c1-18-14-21(6-7-24(18)38-4)26-19(2)34-29(36-26)30(3)9-12-37(13-10-30)28-22-16-23(35-27(22)32-17-33-28)20-8-11-31-25(15-20)39-5/h6-8,11,14-17H,9-10,12-13H2,1-5H3,(H,34,36)(H,32,33,35)
PDB

GoogleScholar
PC cid
PC sid
UniChem
US Patent
500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Mast/stem cell growth factor receptor Kit


(Homo sapiens (Human))
BDBM342225
PNG
(6-(4-fluorophenyl)-4-[4-[5-(4- fluorophenyl)-4-met...)
Show SMILES Cc1nc([nH]c1-c1ccc(F)cc1)C1(C)CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(F)cc1
Show InChI InChI=1S/C28H26F2N6/c1-17-24(19-5-9-21(30)10-6-19)35-27(33-17)28(2)11-13-36(14-12-28)26-22-15-23(34-25(22)31-16-32-26)18-3-7-20(29)8-4-18/h3-10,15-16H,11-14H2,1-2H3,(H,33,35)(H,31,32,34)
PDB

UniProtKB/SwissProt

GoogleScholar
PC cid
PC sid
UniChem
US Patent
500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
Assays for biochemical cell-based activity of c-kit kinase are known in the art, for example, as described in U.S. Pat. Nos. 7,498,342 and 7,846,941,...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342225
PNG
(6-(4-fluorophenyl)-4-[4-[5-(4- fluorophenyl)-4-met...)
Show SMILES Cc1nc([nH]c1-c1ccc(F)cc1)C1(C)CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(F)cc1
Show InChI InChI=1S/C28H26F2N6/c1-17-24(19-5-9-21(30)10-6-19)35-27(33-17)28(2)11-13-36(14-12-28)26-22-15-23(34-25(22)31-16-32-26)18-3-7-20(29)8-4-18/h3-10,15-16H,11-14H2,1-2H3,(H,33,35)(H,31,32,34)
PDB

GoogleScholar
PC cid
PC sid
UniChem
US Patent
500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342231
PNG
(4-[4-[5-(4-methoxyphenyl)-4-methyl- 1H-imidazol-2-...)
Show SMILES COc1ccc(cc1)-c1[nH]c(nc1C)C1(C)CCN(CC1)c1ncnc2[nH]c(C)cc12
Show InChI InChI=1S/C24H28N6O/c1-15-13-19-21(27-15)25-14-26-22(19)30-11-9-24(3,10-12-30)23-28-16(2)20(29-23)17-5-7-18(31-4)8-6-17/h5-8,13-14H,9-12H2,1-4H3,(H,28,29)(H,25,26,27)
PDB

GoogleScholar
PC cid
PC sid
UniChem
US Patent
500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Mast/stem cell growth factor receptor Kit


(Homo sapiens (Human))
BDBM342235
PNG
(4-[4-[5-(4-ethoxy-3-methyl-phenyl)-4- methyl-1H-im...)
Show SMILES CCOc1ccc(cc1C)-c1[nH]c(nc1C)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccnc(OC)c1
Show InChI InChI=1S/C30H33N7O2/c1-5-39-25-7-6-22(14-18(25)2)27-19(3)34-28(36-27)20-9-12-37(13-10-20)30-23-16-24(35-29(23)32-17-33-30)21-8-11-31-26(15-21)38-4/h6-8,11,14-17,20H,5,9-10,12-13H2,1-4H3,(H,34,36)(H,32,33,35)
PDB

UniProtKB/SwissProt

GoogleScholar
PC cid
PC sid
UniChem
US Patent
500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
Assays for biochemical cell-based activity of c-kit kinase are known in the art, for example, as described in U.S. Pat. Nos. 7,498,342 and 7,846,941,...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342237
PNG
(4-[4-[4-[5-(1,3-benzodioxol-5-yl)-4- methyl-1H-imi...)
Show SMILES Cc1nc([nH]c1-c1ccc2OCOc2c1)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(cc1)C#N
Show InChI InChI=1S/C29H25N7O2/c1-17-26(21-6-7-24-25(12-21)38-16-37-24)35-27(33-17)20-8-10-36(11-9-20)29-22-13-23(34-28(22)31-15-32-29)19-4-2-18(14-30)3-5-19/h2-7,12-13,15,20H,8-11,16H2,1H3,(H,33,35)(H,31,32,34)
PDB

GoogleScholar
PC cid
PC sid
UniChem
US Patent
500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Mast/stem cell growth factor receptor Kit


(Homo sapiens (Human))
BDBM342241
PNG
(6-(1,3-dimethylpyrazol-4-yl)-4-[4-(4- methyl-5-phe...)
Show SMILES Cc1nc([nH]c1-c1ccccc1)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1cn(C)nc1C
Show InChI InChI=1S/C26H28N8/c1-16-21(14-33(3)32-16)22-13-20-25(30-22)27-15-28-26(20)34-11-9-19(10-12-34)24-29-17(2)23(31-24)18-7-5-4-6-8-18/h4-8,13-15,19H,9-12H2,1-3H3,(H,29,31)(H,27,28,30)
PDB

UniProtKB/SwissProt

GoogleScholar
PC cid
PC sid
UniChem
US Patent
500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
Assays for biochemical cell-based activity of c-kit kinase are known in the art, for example, as described in U.S. Pat. Nos. 7,498,342 and 7,846,941,...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342241
PNG
(6-(1,3-dimethylpyrazol-4-yl)-4-[4-(4- methyl-5-phe...)
Show SMILES Cc1nc([nH]c1-c1ccccc1)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1cn(C)nc1C
Show InChI InChI=1S/C26H28N8/c1-16-21(14-33(3)32-16)22-13-20-25(30-22)27-15-28-26(20)34-11-9-19(10-12-34)24-29-17(2)23(31-24)18-7-5-4-6-8-18/h4-8,13-15,19H,9-12H2,1-3H3,(H,29,31)(H,27,28,30)
PDB

GoogleScholar
PC cid
PC sid
UniChem
US Patent
500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342244
PNG
(4-[4-[4-[4-(4-methyl-5-phenyl-1H- imidazol-2-yl)-1...)
Show SMILES Cc1nc([nH]c1-c1ccccc1)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccnc(c1)N1CCOCC1
Show InChI InChI=1S/C30H32N8O/c1-20-27(21-5-3-2-4-6-21)36-28(34-20)22-8-11-38(12-9-22)30-24-18-25(35-29(24)32-19-33-30)23-7-10-31-26(17-23)37-13-15-39-16-14-37/h2-7,10,17-19,22H,8-9,11-16H2,1H3,(H,34,36)(H,32,33,35)
PDB

GoogleScholar
PC cid
PC sid
UniChem
US Patent
500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Mast/stem cell growth factor receptor Kit


(Homo sapiens (Human))
BDBM342253
PNG
(6-(4-fluorophenyl)-4-[4-[4-methyl-5-[4- (trifluoro...)
Show SMILES Cc1nc([nH]c1-c1ccc(OC(F)(F)F)cc1)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(F)cc1
Show InChI InChI=1S/C28H24F4N6O/c1-16-24(18-4-8-21(9-5-18)39-28(30,31)32)37-25(35-16)19-10-12-38(13-11-19)27-22-14-23(36-26(22)33-15-34-27)17-2-6-20(29)7-3-17/h2-9,14-15,19H,10-13H2,1H3,(H,35,37)(H,33,34,36)
PDB

UniProtKB/SwissProt

GoogleScholar
PC cid
PC sid
UniChem
US Patent
500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
Assays for biochemical cell-based activity of c-kit kinase are known in the art, for example, as described in U.S. Pat. Nos. 7,498,342 and 7,846,941,...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Mast/stem cell growth factor receptor Kit


(Homo sapiens (Human))
BDBM342263
PNG
(4-[4-[4-[5-(3-ethoxy-4-methyl-phenyl)- 4-methyl-1H...)
Show SMILES CCOc1cc(ccc1C)-c1[nH]c(nc1C)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(cc1)C#N
Show InChI InChI=1S/C31H31N7O/c1-4-39-27-15-24(8-5-19(27)2)28-20(3)35-29(37-28)23-11-13-38(14-12-23)31-25-16-26(36-30(25)33-18-34-31)22-9-6-21(17-32)7-10-22/h5-10,15-16,18,23H,4,11-14H2,1-3H3,(H,35,37)(H,33,34,36)
PDB

UniProtKB/SwissProt

GoogleScholar
PC cid
PC sid
UniChem
US Patent
500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
Assays for biochemical cell-based activity of c-kit kinase are known in the art, for example, as described in U.S. Pat. Nos. 7,498,342 and 7,846,941,...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342264
PNG
(4-[4-[5-(3-ethoxy-4-methyl-phenyl)-4- methyl-1H-im...)
Show SMILES CCOc1cc(ccc1C)-c1[nH]c(nc1C)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccnc(OC)c1
Show InChI InChI=1S/C30H33N7O2/c1-5-39-25-14-22(7-6-18(25)2)27-19(3)34-28(36-27)20-9-12-37(13-10-20)30-23-16-24(35-29(23)32-17-33-30)21-8-11-31-26(15-21)38-4/h6-8,11,14-17,20H,5,9-10,12-13H2,1-4H3,(H,34,36)(H,32,33,35)
PDB

GoogleScholar
PC cid
PC sid
UniChem
US Patent
500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342274
PNG
(4-[4-[4-[5-(3-methoxy-4-methyl- phenyl)-4-methyl-1...)
Show SMILES COc1cc(ccc1C)-c1[nH]c(nc1C)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(cc1)C#N
Show InChI InChI=1S/C30H29N7O/c1-18-4-7-23(14-26(18)38-3)27-19(2)34-28(36-27)22-10-12-37(13-11-22)30-24-15-25(35-29(24)32-17-33-30)21-8-5-20(16-31)6-9-21/h4-9,14-15,17,22H,10-13H2,1-3H3,(H,34,36)(H,32,33,35)
PDB

GoogleScholar
PC cid
PC sid
UniChem
US Patent
500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Mast/stem cell growth factor receptor Kit


(Homo sapiens (Human))
BDBM342282
PNG
(6-[1-(difluoromethyl)pyrazol-4-yl]-4-[4- [5-(3-met...)
Show SMILES COc1cccc(c1)-c1[nH]c(nc1C)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1cnn(c1)C(F)F
Show InChI InChI=1S/C26H26F2N8O/c1-15-22(17-4-3-5-19(10-17)37-2)34-23(32-15)16-6-8-35(9-7-16)25-20-11-21(33-24(20)29-14-30-25)18-12-31-36(13-18)26(27)28/h3-5,10-14,16,26H,6-9H2,1-2H3,(H,32,34)(H,29,30,33)
PDB

UniProtKB/SwissProt

GoogleScholar
PC cid
PC sid
UniChem
US Patent
500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
Assays for biochemical cell-based activity of c-kit kinase are known in the art, for example, as described in U.S. Pat. Nos. 7,498,342 and 7,846,941,...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Mast/stem cell growth factor receptor Kit


(Homo sapiens (Human))
BDBM342292
PNG
(4-[4-[4-[5-(3-methoxyphenyl)-4- (trifluoromethyl)-...)
Show SMILES COc1cccc(c1)-c1[nH]c(nc1C(F)(F)F)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(cc1)C#N
Show InChI InChI=1S/C29H24F3N7O/c1-40-21-4-2-3-20(13-21)24-25(29(30,31)32)38-26(37-24)19-9-11-39(12-10-19)28-22-14-23(36-27(22)34-16-35-28)18-7-5-17(15-33)6-8-18/h2-8,13-14,16,19H,9-12H2,1H3,(H,37,38)(H,34,35,36)
PDB

UniProtKB/SwissProt

GoogleScholar
PC cid
PC sid
UniChem
US Patent
500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
Assays for biochemical cell-based activity of c-kit kinase are known in the art, for example, as described in U.S. Pat. Nos. 7,498,342 and 7,846,941,...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342299
PNG
(4-[4-[5-(3-methoxyphenyl)-4-methyl- 1H-imidazol-2-...)
Show SMILES COc1cccc(c1)-c1[nH]c(nc1C)C1CCN(CC1)c1ncnc2[nH]c(C)cc12
Show InChI InChI=1S/C23H26N6O/c1-14-11-19-22(26-14)24-13-25-23(19)29-9-7-16(8-10-29)21-27-15(2)20(28-21)17-5-4-6-18(12-17)30-3/h4-6,11-13,16H,7-10H2,1-3H3,(H,27,28)(H,24,25,26)
PDB

GoogleScholar
PC cid
PC sid
UniChem
US Patent
500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342300
PNG
(4-[4-[4-[5-(2,3-dihydro-1,4- benzodioxin-6-yl)-4-m...)
Show SMILES Cc1nc([nH]c1-c1ccc2OCCOc2c1)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(cc1)C#N
Show InChI InChI=1S/C30H27N7O2/c1-18-27(22-6-7-25-26(14-22)39-13-12-38-25)36-28(34-18)21-8-10-37(11-9-21)30-23-15-24(35-29(23)32-17-33-30)20-4-2-19(16-31)3-5-20/h2-7,14-15,17,21H,8-13H2,1H3,(H,34,36)(H,32,33,35)
PDB

GoogleScholar
PC cid
PC sid
UniChem
US Patent
500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342304
PNG
(6-(4-fluorophenyl)-4-[4-[4-methyl-5-[4- (trifluoro...)
Show SMILES Cc1nc([nH]c1-c1ccc(cc1)C(F)(F)F)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(F)cc1
Show InChI InChI=1S/C28H24F4N6/c1-16-24(18-2-6-20(7-3-18)28(30,31)32)37-25(35-16)19-10-12-38(13-11-19)27-22-14-23(36-26(22)33-15-34-27)17-4-8-21(29)9-5-17/h2-9,14-15,19H,10-13H2,1H3,(H,35,37)(H,33,34,36)
PDB

GoogleScholar
PC cid
PC sid
UniChem
US Patent
500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Mast/stem cell growth factor receptor Kit


(Homo sapiens (Human))
BDBM342321
PNG
(6-[1-(difluoromethyl)pyrazol-4-yl]-4-[4- [5-(4-met...)
Show SMILES COc1ccc(cc1)-c1[nH]c(nc1C)C1(C)CCN(CC1)c1ncnc2[nH]c(cc12)-c1cnn(c1)C(F)F
Show InChI InChI=1S/C27H28F2N8O/c1-16-22(17-4-6-19(38-3)7-5-17)35-25(33-16)27(2)8-10-36(11-9-27)24-20-12-21(34-23(20)30-15-31-24)18-13-32-37(14-18)26(28)29/h4-7,12-15,26H,8-11H2,1-3H3,(H,33,35)(H,30,31,34)
PDB

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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
Assays for biochemical cell-based activity of c-kit kinase are known in the art, for example, as described in U.S. Pat. Nos. 7,498,342 and 7,846,941,...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Mast/stem cell growth factor receptor Kit


(Homo sapiens (Human))
BDBM342326
PNG
(4-[4-[5-(1,3-benzodioxol-5-yl)-4- methyl-1H-imidaz...)
Show SMILES COc1ccc(cn1)-c1cc2c(ncnc2[nH]1)N1CCC(C)(CC1)c1nc(C)c([nH]1)-c1ccc2OCOc2c1
Show InChI InChI=1S/C29H29N7O3/c1-17-25(18-4-6-22-23(12-18)39-16-38-22)35-28(33-17)29(2)8-10-36(11-9-29)27-20-13-21(34-26(20)31-15-32-27)19-5-7-24(37-3)30-14-19/h4-7,12-15H,8-11,16H2,1-3H3,(H,33,35)(H,31,32,34)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
Assays for biochemical cell-based activity of c-kit kinase are known in the art, for example, as described in U.S. Pat. Nos. 7,498,342 and 7,846,941,...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342328
PNG
(4-[4-[4-[5-(4-ethoxy-3-methyl-phenyl)- 4-methyl-1H...)
Show SMILES CCOc1ccc(cc1C)-c1[nH]c(nc1C)C1(C)CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(cc1)C#N
Show InChI InChI=1S/C32H33N7O/c1-5-40-27-11-10-24(16-20(27)2)28-21(3)36-31(38-28)32(4)12-14-39(15-13-32)30-25-17-26(37-29(25)34-19-35-30)23-8-6-22(18-33)7-9-23/h6-11,16-17,19H,5,12-15H2,1-4H3,(H,36,38)(H,34,35,37)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342333
PNG
(6-methyl-4-[4-methyl-4-[4-methyl-5-[4- (trifluorom...)
Show SMILES Cc1cc2c(ncnc2[nH]1)N1CCC(CC1)c1nc(C)c([nH]1)-c1ccc(cc1)C(F)(F)F
Show InChI InChI=1S/C23H23F3N6/c1-13-11-18-21(29-13)27-12-28-22(18)32-9-7-16(8-10-32)20-30-14(2)19(31-20)15-3-5-17(6-4-15)23(24,25)26/h3-6,11-12,16H,7-10H2,1-2H3,(H,30,31)(H,27,28,29)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342342
PNG
(4-[4-[5-(4-chlorophenyl)-4-methyl-1H- imidazol-2-y...)
Show SMILES Cc1cc2c(ncnc2[nH]1)N1CCC(C)(CC1)c1nc(C)c([nH]1)-c1ccc(Cl)cc1
Show InChI InChI=1S/C23H25ClN6/c1-14-12-18-20(27-14)25-13-26-21(18)30-10-8-23(3,9-11-30)22-28-15(2)19(29-22)16-4-6-17(24)7-5-16/h4-7,12-13H,8-11H2,1-3H3,(H,28,29)(H,25,26,27)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342343
PNG
(4-[4-[5-(4-chlorophenyl)-4-methyl-1H- imidazol-2-y...)
Show SMILES Cc1nc([nH]c1-c1ccc(Cl)cc1)C1(C)CCN(CC1)c1ncnc2[nH]c(cc12)-c1cnn(c1)C(F)F
Show InChI InChI=1S/C26H25ClF2N8/c1-15-21(16-3-5-18(27)6-4-16)35-24(33-15)26(2)7-9-36(10-8-26)23-19-11-20(34-22(19)30-14-31-23)17-12-32-37(13-17)25(28)29/h3-6,11-14,25H,7-10H2,1-2H3,(H,33,35)(H,30,31,34)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Mast/stem cell growth factor receptor Kit


(Homo sapiens (Human))
BDBM342344
PNG
(4-[4-[5-(4-chlorophenyl)-4-methyl-1H- imidazol-2-y...)
Show SMILES COc1ccc(cn1)-c1cc2c(ncnc2[nH]1)N1CCC(C)(CC1)c1nc(C)c([nH]1)-c1ccc(Cl)cc1
Show InChI InChI=1S/C28H28ClN7O/c1-17-24(18-4-7-20(29)8-5-18)35-27(33-17)28(2)10-12-36(13-11-28)26-21-14-22(34-25(21)31-16-32-26)19-6-9-23(37-3)30-15-19/h4-9,14-16H,10-13H2,1-3H3,(H,33,35)(H,31,32,34)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
Assays for biochemical cell-based activity of c-kit kinase are known in the art, for example, as described in U.S. Pat. Nos. 7,498,342 and 7,846,941,...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342346
PNG
(6-(6-methoxy-3-pyridyl)-4-[4-methyl-4- [4-methyl-5...)
Show SMILES COc1ccc(cn1)-c1cc2c(ncnc2[nH]1)N1CCC(C)(CC1)c1nc(C)c([nH]1)-c1ccc(cc1)C(F)(F)F
Show InChI InChI=1S/C29H28F3N7O/c1-17-24(18-4-7-20(8-5-18)29(30,31)32)38-27(36-17)28(2)10-12-39(13-11-28)26-21-14-22(37-25(21)34-16-35-26)19-6-9-23(40-3)33-15-19/h4-9,14-16H,10-13H2,1-3H3,(H,36,38)(H,34,35,37)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Mast/stem cell growth factor receptor Kit


(Homo sapiens (Human))
BDBM342349
PNG
(4-[4-[4-[5-(5-fluoro-6-methoxy-3- pyridyl)-4-methy...)
Show SMILES COc1ncc(cc1F)-c1[nH]c(nc1C)C1(C)CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(cc1)C#N
Show InChI InChI=1S/C29H27FN8O/c1-17-24(20-12-22(30)27(39-3)32-15-20)37-28(35-17)29(2)8-10-38(11-9-29)26-21-13-23(36-25(21)33-16-34-26)19-6-4-18(14-31)5-7-19/h4-7,12-13,15-16H,8-11H2,1-3H3,(H,35,37)(H,33,34,36)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
Assays for biochemical cell-based activity of c-kit kinase are known in the art, for example, as described in U.S. Pat. Nos. 7,498,342 and 7,846,941,...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Mast/stem cell growth factor receptor Kit


(Homo sapiens (Human))
BDBM342355
PNG
(6-[1-(difluoromethyl)pyrazol-4-yl]-4-[4- [5-(3-flu...)
Show SMILES COc1ccc(cc1F)-c1[nH]c(nc1C)C1(C)CCN(CC1)c1ncnc2[nH]c(cc12)-c1cnn(c1)C(F)F
Show InChI InChI=1S/C27H27F3N8O/c1-15-22(16-4-5-21(39-3)19(28)10-16)36-25(34-15)27(2)6-8-37(9-7-27)24-18-11-20(35-23(18)31-14-32-24)17-12-33-38(13-17)26(29)30/h4-5,10-14,26H,6-9H2,1-3H3,(H,34,36)(H,31,32,35)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
Assays for biochemical cell-based activity of c-kit kinase are known in the art, for example, as described in U.S. Pat. Nos. 7,498,342 and 7,846,941,...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342356
PNG
(4-[4-[5-(3-fluoro-4-methoxy-phenyl)-4- methyl-1H-i...)
Show SMILES COc1ccc(cn1)-c1cc2c(ncnc2[nH]1)N1CCC(C)(CC1)c1nc(C)c([nH]1)-c1ccc(OC)c(F)c1
Show InChI InChI=1S/C29H30FN7O2/c1-17-25(18-5-7-23(38-3)21(30)13-18)36-28(34-17)29(2)9-11-37(12-10-29)27-20-14-22(35-26(20)32-16-33-27)19-6-8-24(39-4)31-15-19/h5-8,13-16H,9-12H2,1-4H3,(H,34,36)(H,32,33,35)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342359
PNG
(4-[4-[5-[3-(difluoromethoxy)phenyl]-4- methyl-1H-i...)
Show SMILES Cc1cc2c(ncnc2[nH]1)N1CCC(C)(CC1)c1nc(C)c([nH]1)-c1cccc(OC(F)F)c1
Show InChI InChI=1S/C24H26F2N6O/c1-14-11-18-20(29-14)27-13-28-21(18)32-9-7-24(3,8-10-32)22-30-15(2)19(31-22)16-5-4-6-17(12-16)33-23(25)26/h4-6,11-13,23H,7-10H2,1-3H3,(H,30,31)(H,27,28,29)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342384
PNG
(2-[4-[4-[4-[5-(3-methoxyphenyl)-4- methyl-1H-imida...)
Show SMILES COc1cccc(c1)-c1[nH]c(nc1C)C1(C)CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(OCC(O)=O)cc1
Show InChI InChI=1S/C31H32N6O4/c1-19-27(21-5-4-6-23(15-21)40-3)36-30(34-19)31(2)11-13-37(14-12-31)29-24-16-25(35-28(24)32-18-33-29)20-7-9-22(10-8-20)41-17-26(38)39/h4-10,15-16,18H,11-14,17H2,1-3H3,(H,34,36)(H,38,39)(H,32,33,35)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Mast/stem cell growth factor receptor Kit


(Homo sapiens (Human))
BDBM342387
PNG
(2-[4-[4-[4-[5-(4-ethoxyphenyl)-4- methyl-1H-imidaz...)
Show SMILES CCOc1ccc(cc1)-c1[nH]c(nc1C)C1(C)CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(OCC(O)=O)cc1
Show InChI InChI=1S/C32H34N6O4/c1-4-41-23-11-7-22(8-12-23)28-20(2)35-31(37-28)32(3)13-15-38(16-14-32)30-25-17-26(36-29(25)33-19-34-30)21-5-9-24(10-6-21)42-18-27(39)40/h5-12,17,19H,4,13-16,18H2,1-3H3,(H,35,37)(H,39,40)(H,33,34,36)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
Assays for biochemical cell-based activity of c-kit kinase are known in the art, for example, as described in U.S. Pat. Nos. 7,498,342 and 7,846,941,...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342394
PNG
(4-[4-[4-[5-[3-(difluoromethoxy)phenyl]- 4-methyl-1...)
Show SMILES Cc1nc([nH]c1-c1cccc(OC(F)F)c1)C1(C)CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(cc1)C(N)=O
Show InChI InChI=1S/C30H29F2N7O2/c1-17-24(20-4-3-5-21(14-20)41-29(31)32)38-28(36-17)30(2)10-12-39(13-11-30)27-22-15-23(37-26(22)34-16-35-27)18-6-8-19(9-7-18)25(33)40/h3-9,14-16,29H,10-13H2,1-2H3,(H2,33,40)(H,36,38)(H,34,35,37)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342398
PNG
(5-[4-[4-[5-[4-(difluoromethyl)phenyl]-4- methyl-1H...)
Show SMILES CNC(=O)c1ccc(cn1)-c1cc2c(ncnc2[nH]1)N1CCC(C)(CC1)c1nc(C)c([nH]1)-c1ccc(cc1)C(F)F
Show InChI InChI=1S/C30H30F2N8O/c1-17-24(18-4-6-19(7-5-18)25(31)32)39-29(37-17)30(2)10-12-40(13-11-30)27-21-14-23(38-26(21)35-16-36-27)20-8-9-22(34-15-20)28(41)33-3/h4-9,14-16,25H,10-13H2,1-3H3,(H,33,41)(H,37,39)(H,35,36,38)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Mast/stem cell growth factor receptor Kit


(Homo sapiens (Human))
BDBM342411
PNG
(4-[5-[4-[4-[5-[4- (difluoromethoxy)phenyl]-4-methy...)
Show SMILES Cc1nc([nH]c1-c1ccc(OC(F)F)cc1)C1(C)CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(nc1)N1CCOCC1
Show InChI InChI=1S/C32H34F2N8O2/c1-20-27(21-3-6-23(7-4-21)44-31(33)34)40-30(38-20)32(2)9-11-42(12-10-32)29-24-17-25(39-28(24)36-19-37-29)22-5-8-26(35-18-22)41-13-15-43-16-14-41/h3-8,17-19,31H,9-16H2,1-2H3,(H,38,40)(H,36,37,39)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
Assays for biochemical cell-based activity of c-kit kinase are known in the art, for example, as described in U.S. Pat. Nos. 7,498,342 and 7,846,941,...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Mast/stem cell growth factor receptor Kit


(Homo sapiens (Human))
BDBM342413
PNG
(5-[4-[4-[5-(4-methoxy-3-methyl- phenyl)-4-methyl-1...)
Show SMILES COc1ccc(cc1C)-c1[nH]c(nc1C)C1(C)CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(nc1)C#N
Show InChI InChI=1S/C30H30N8O/c1-18-13-20(6-8-25(18)39-4)26-19(2)35-29(37-26)30(3)9-11-38(12-10-30)28-23-14-24(36-27(23)33-17-34-28)21-5-7-22(15-31)32-16-21/h5-8,13-14,16-17H,9-12H2,1-4H3,(H,35,37)(H,33,34,36)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
Assays for biochemical cell-based activity of c-kit kinase are known in the art, for example, as described in U.S. Pat. Nos. 7,498,342 and 7,846,941,...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342416
PNG
(4-[4-[4-[5-[4-(difluoromethoxy)phenyl]- 4-methyl-1...)
Show SMILES Cc1nc([nH]c1-c1ccc(OC(F)F)cc1)C1(C)CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(cc1)C(N)=O
Show InChI InChI=1S/C30H29F2N7O2/c1-17-24(19-7-9-21(10-8-19)41-29(31)32)38-28(36-17)30(2)11-13-39(14-12-30)27-22-15-23(37-26(22)34-16-35-27)18-3-5-20(6-4-18)25(33)40/h3-10,15-16,29H,11-14H2,1-2H3,(H2,33,40)(H,36,38)(H,34,35,37)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Mast/stem cell growth factor receptor Kit


(Homo sapiens (Human))
BDBM342419
PNG
(5-[4-[4-[5-(3-methoxyphenyl)-4-methyl- 1H-imidazol...)
Show SMILES COc1cccc(c1)-c1[nH]c(nc1C)C1(C)CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(nc1)C#N
Show InChI InChI=1S/C29H28N8O/c1-18-25(19-5-4-6-22(13-19)38-3)36-28(34-18)29(2)9-11-37(12-10-29)27-23-14-24(35-26(23)32-17-33-27)20-7-8-21(15-30)31-16-20/h4-8,13-14,16-17H,9-12H2,1-3H3,(H,34,36)(H,32,33,35)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
Assays for biochemical cell-based activity of c-kit kinase are known in the art, for example, as described in U.S. Pat. Nos. 7,498,342 and 7,846,941,...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Mast/stem cell growth factor receptor Kit


(Homo sapiens (Human))
BDBM342152
PNG
(4-[4-(5-methyl-4-phenyl-1H-imidazol-2- yl)-1-piper...)
Show SMILES Cc1[nH]c(nc1-c1ccccc1)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccncc1
Show InChI InChI=1S/C26H25N7/c1-17-23(19-5-3-2-4-6-19)32-24(30-17)20-9-13-33(14-10-20)26-21-15-22(18-7-11-27-12-8-18)31-25(21)28-16-29-26/h2-8,11-12,15-16,20H,9-10,13-14H2,1H3,(H,30,32)(H,28,29,31)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
Assays for biochemical cell-based activity of c-kit kinase are known in the art, for example, as described in U.S. Pat. Nos. 7,498,342 and 7,846,941,...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Mast/stem cell growth factor receptor Kit


(Homo sapiens (Human))
BDBM342154
PNG
(6-(2-methoxy-4-pyridyl)-4-[4-(4- methyl-5-phenyl-1...)
Show SMILES COc1cc(ccn1)-c1cc2c(ncnc2[nH]1)N1CCC(CC1)c1nc(C)c([nH]1)-c1ccccc1
Show InChI InChI=1S/C27H27N7O/c1-17-24(18-6-4-3-5-7-18)33-25(31-17)19-9-12-34(13-10-19)27-21-15-22(32-26(21)29-16-30-27)20-8-11-28-23(14-20)35-2/h3-8,11,14-16,19H,9-10,12-13H2,1-2H3,(H,31,33)(H,29,30,32)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
Assays for biochemical cell-based activity of c-kit kinase are known in the art, for example, as described in U.S. Pat. Nos. 7,498,342 and 7,846,941,...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342154
PNG
(6-(2-methoxy-4-pyridyl)-4-[4-(4- methyl-5-phenyl-1...)
Show SMILES COc1cc(ccn1)-c1cc2c(ncnc2[nH]1)N1CCC(CC1)c1nc(C)c([nH]1)-c1ccccc1
Show InChI InChI=1S/C27H27N7O/c1-17-24(18-6-4-3-5-7-18)33-25(31-17)19-9-12-34(13-10-19)27-21-15-22(32-26(21)29-16-30-27)20-8-11-28-23(14-20)35-2/h3-8,11,14-16,19H,9-10,12-13H2,1-2H3,(H,31,33)(H,29,30,32)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342165
PNG
(4-[4-[5-[3-(difluoromethoxy)phenyl]- 4H-1,2,4-tria...)
Show SMILES FC(F)Oc1cccc(c1)-c1nnc([nH]1)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(F)cc1
Show InChI InChI=1S/C26H22F3N7O/c27-18-6-4-15(5-7-18)21-13-20-24(32-21)30-14-31-25(20)36-10-8-16(9-11-36)22-33-23(35-34-22)17-2-1-3-19(12-17)37-26(28)29/h1-7,12-14,16,26H,8-11H2,(H,30,31,32)(H,33,34,35)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342181
PNG
(4-[4-[4-[5-(4-fluorophenyl)-4-methyl- 1H-imidazol-...)
Show SMILES Cc1nc([nH]c1-c1ccc(F)cc1)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(cc1)C#N
Show InChI InChI=1S/C28H24FN7/c1-17-25(20-6-8-22(29)9-7-20)35-26(33-17)21-10-12-36(13-11-21)28-23-14-24(34-27(23)31-16-32-28)19-4-2-18(15-30)3-5-19/h2-9,14,16,21H,10-13H2,1H3,(H,33,35)(H,31,32,34)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342182
PNG
(4-[4-[4-[5-(3-methoxyphenyl)-4-methyl- 1H-imidazol...)
Show SMILES COc1cccc(c1)-c1[nH]c(nc1C)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(cc1)C#N
Show InChI InChI=1S/C29H27N7O/c1-18-26(22-4-3-5-23(14-22)37-2)35-27(33-18)21-10-12-36(13-11-21)29-24-15-25(34-28(24)31-17-32-29)20-8-6-19(16-30)7-9-20/h3-9,14-15,17,21H,10-13H2,1-2H3,(H,33,35)(H,31,32,34)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342183
PNG
(4-[4-[5-(3-methoxyphenyl)-4-methyl- 1H-imidazol-2-...)
Show SMILES COc1cccc(c1)-c1[nH]c(nc1C)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccnc(OC)c1
Show InChI InChI=1S/C28H29N7O2/c1-17-25(20-5-4-6-21(13-20)36-2)34-26(32-17)18-8-11-35(12-9-18)28-22-15-23(33-27(22)30-16-31-28)19-7-10-29-24(14-19)37-3/h4-7,10,13-16,18H,8-9,11-12H2,1-3H3,(H,32,34)(H,30,31,33)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Mast/stem cell growth factor receptor Kit


(Homo sapiens (Human))
BDBM342192
PNG
(4-[4-[4-[5-(4-methoxy-3-methyl- phenyl)-4-methyl-1...)
Show SMILES COc1ccc(cc1C)-c1[nH]c(nc1C)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(cc1)C#N
Show InChI InChI=1S/C30H29N7O/c1-18-14-23(8-9-26(18)38-3)27-19(2)34-28(36-27)22-10-12-37(13-11-22)30-24-15-25(35-29(24)32-17-33-30)21-6-4-20(16-31)5-7-21/h4-9,14-15,17,22H,10-13H2,1-3H3,(H,34,36)(H,32,33,35)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
Assays for biochemical cell-based activity of c-kit kinase are known in the art, for example, as described in U.S. Pat. Nos. 7,498,342 and 7,846,941,...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Mast/stem cell growth factor receptor Kit


(Homo sapiens (Human))
BDBM342201
PNG
(4-[4-[5-(4-chlorophenyl)-4-methyl-1H- imidazol-2-y...)
Show SMILES Cc1nc([nH]c1-c1ccc(Cl)cc1)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(F)cc1
Show InChI InChI=1S/C27H24ClFN6/c1-16-24(18-2-6-20(28)7-3-18)34-25(32-16)19-10-12-35(13-11-19)27-22-14-23(33-26(22)30-15-31-27)17-4-8-21(29)9-5-17/h2-9,14-15,19H,10-13H2,1H3,(H,32,34)(H,30,31,33)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
Assays for biochemical cell-based activity of c-kit kinase are known in the art, for example, as described in U.S. Pat. Nos. 7,498,342 and 7,846,941,...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342201
PNG
(4-[4-[5-(4-chlorophenyl)-4-methyl-1H- imidazol-2-y...)
Show SMILES Cc1nc([nH]c1-c1ccc(Cl)cc1)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(F)cc1
Show InChI InChI=1S/C27H24ClFN6/c1-16-24(18-2-6-20(28)7-3-18)34-25(32-16)19-10-12-35(13-11-19)27-22-14-23(33-26(22)30-15-31-27)17-4-8-21(29)9-5-17/h2-9,14-15,19H,10-13H2,1H3,(H,32,34)(H,30,31,33)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Mast/stem cell growth factor receptor Kit


(Homo sapiens (Human))
BDBM342204
PNG
(4-[4-[4-[5-(4-chlorophenyl)-4-methyl- 1H-imidazol-...)
Show SMILES Cc1nc([nH]c1-c1ccc(Cl)cc1)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(cc1)C#N
Show InChI InChI=1S/C28H24ClN7/c1-17-25(20-6-8-22(29)9-7-20)35-26(33-17)21-10-12-36(13-11-21)28-23-14-24(34-27(23)31-16-32-28)19-4-2-18(15-30)3-5-19/h2-9,14,16,21H,10-13H2,1H3,(H,33,35)(H,31,32,34)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
Assays for biochemical cell-based activity of c-kit kinase are known in the art, for example, as described in U.S. Pat. Nos. 7,498,342 and 7,846,941,...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Kit (Kit)(D816V)


(Homo sapiens (Human))
BDBM342216
PNG
(4-[4-[4-(4-methyl-5-phenyl-1H- imidazol-2-yl)-1-pi...)
Show SMILES Cc1nc([nH]c1-c1ccccc1)C1CCN(CC1)c1ncnc2[nH]c(cc12)-c1ccc(cc1)S(N)(=O)=O
Show InChI InChI=1S/C27H27N7O2S/c1-17-24(19-5-3-2-4-6-19)33-25(31-17)20-11-13-34(14-12-20)27-22-15-23(32-26(22)29-16-30-27)18-7-9-21(10-8-18)37(28,35)36/h2-10,15-16,20H,11-14H2,1H3,(H,31,33)(H2,28,35,36)(H,29,30,32)
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500n/an/an/an/an/an/an/an/a



Plexxikon Inc.

US Patent


Assay Description
The c-kit mutant D816V (or kinase domain thereof) is an active kinase in AlphaScreen. IC50 values are determined with respect to inhibition of c-Kit ...


US Patent US9771369 (2017)


BindingDB Entry DOI: 10.7270/Q24J0H7Q
More data for this
Ligand-Target Pair
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* indicates data uncertainty>20%