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4 similar compounds to monomer 29906

Wt: 557.8
BDBM21926
Wt: 486.2
BDBM29901
Wt: 528.8
BDBM29904
Wt: 563.8
BDBM29908

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 5 hits for monomerid = 21926,29901,29904,29908   
Target
(Institution)
LigandTarget
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kcal/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Mitogen-activated protein kinase kinase kinase 8


(Homo sapiens (human))
BDBM21926
PNG
(8-bromo-4-[(3-chloro-4-fluorophenyl)amino]-6-[({1-...)
Show SMILES CN(C)CCCn1cc(CNc2cc(Br)c3ncc(C#N)c(Nc4ccc(F)c(Cl)c4)c3c2)nn1
Show InChI InChI=1S/C24H23BrClFN8/c1-34(2)6-3-7-35-14-18(32-33-35)13-29-17-8-19-23(31-16-4-5-22(27)21(26)10-16)15(11-28)12-30-24(19)20(25)9-17/h4-5,8-10,12,14,29H,3,6-7,13H2,1-2H3,(H,30,31)
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n/an/a 20n/an/an/an/an/an/a



Wyeth Research



Assay Description
Tpl2/Cot activity was directly assayed using GST-MEK1 as a substrate. The phosphorylation on serine residues was detected by an ELISA. IC50 calculati...


J Med Chem 50: 4728-45 (2007)

More data for this
Ligand-Target Pair
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (human))
BDBM21926
PNG
(8-bromo-4-[(3-chloro-4-fluorophenyl)amino]-6-[({1-...)
Show SMILES CN(C)CCCn1cc(CNc2cc(Br)c3ncc(C#N)c(Nc4ccc(F)c(Cl)c4)c3c2)nn1
Show InChI InChI=1S/C24H23BrClFN8/c1-34(2)6-3-7-35-14-18(32-33-35)13-29-17-8-19-23(31-16-4-5-22(27)21(26)10-16)15(11-28)12-30-24(19)20(25)9-17/h4-5,8-10,12,14,29H,3,6-7,13H2,1-2H3,(H,30,31)
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MMDB

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PubMed
n/an/a>5.00E+3n/an/an/an/an/an/a



Wyeth Research



Assay Description
EGFR kinase activity was assayed using poly(Glu4-Tyr) as a substrate. The phosphorylation of tyrosine residue was detected by an ELISA. IC50 calculat...


J Med Chem 50: 4728-45 (2007)

More data for this
Ligand-Target Pair
Mitogen-activated protein kinase kinase kinase 8


(Homo sapiens (human))
BDBM29908
PNG
(substituted 6-aminoquinoline-3-carbonitrile, 19)
Show SMILES Fc1ccc(Nc2c(cnc3c(Br)cc(NCc4cn(Cc5cccnc5)nn4)cc23)C#N)cc1Cl
Show InChI InChI=1S/C25H17BrClFN8/c26-21-7-18(31-12-19-14-36(35-34-19)13-15-2-1-5-30-10-15)6-20-24(16(9-29)11-32-25(20)21)33-17-3-4-23(28)22(27)8-17/h1-8,10-11,14,31H,12-13H2,(H,32,33)
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n/an/a 20n/an/an/an/a7.230



Wyeth Research



Assay Description
Tpl2/Cot activity was directly assayed using GST-MEK1 as a substrate. The phosphorylation on serine residues 217 and 221 of GST-MEK1 was detected by ...


Bioorg Med Chem Lett 19: 3485-8 (2009)

More data for this
Ligand-Target Pair
Mitogen-activated protein kinase kinase kinase 8


(Homo sapiens (human))
BDBM29904
PNG
(substituted 6-aminoquinoline-3-carbonitrile, 15)
Show SMILES CC(C)(C)n1cc(CNc2cc(Br)c3ncc(C#N)c(Nc4ccc(F)c(Cl)c4)c3c2)nn1
Show InChI InChI=1S/C23H20BrClFN7/c1-23(2,3)33-12-16(31-32-33)11-28-15-6-17-21(30-14-4-5-20(26)19(25)8-14)13(9-27)10-29-22(17)18(24)7-15/h4-8,10,12,28H,11H2,1-3H3,(H,29,30)
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n/an/a 61n/an/an/an/a7.230



Wyeth Research



Assay Description
Tpl2/Cot activity was directly assayed using GST-MEK1 as a substrate. The phosphorylation on serine residues 217 and 221 of GST-MEK1 was detected by ...


Bioorg Med Chem Lett 19: 3485-8 (2009)

More data for this
Ligand-Target Pair
Mitogen-activated protein kinase kinase kinase 8


(Homo sapiens (human))
BDBM29901
PNG
(substituted 6-aminoquinoline-3-carbonitrile, 12)
Show SMILES OC(=O)Cn1cc(CNc2cc(Cl)c3ncc(C#N)c(Nc4ccc(F)c(Cl)c4)c3c2)nn1
Show InChI InChI=1S/C21H14Cl2FN7O2/c22-16-4-12(1-2-18(16)24)28-20-11(6-25)7-27-21-15(20)3-13(5-17(21)23)26-8-14-9-31(30-29-14)10-19(32)33/h1-5,7,9,26H,8,10H2,(H,27,28)(H,32,33)
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PubMed
n/an/a 9.60n/an/an/an/a7.230



Wyeth Research



Assay Description
Tpl2/Cot activity was directly assayed using GST-MEK1 as a substrate. The phosphorylation on serine residues 217 and 221 of GST-MEK1 was detected by ...


Bioorg Med Chem Lett 19: 3485-8 (2009)

More data for this
Ligand-Target Pair