Compile Data Set for Download or QSAR
Report error Found 362 Enz. Inhib. hit(s) with Target = 'Mitogen-activated protein kinase kinase kinase 8'
LigandPNGBDBM29923(substituted 6-aminoquinoline-3-carbonitrile, 34 | ...)
Affinity DataIC50: 1.60nMAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2009
Entry Details Article
PubMed
LigandPNGBDBM21922(8-chloro-4-[(3-chloro-4-fluorophenyl)amino]-6-[(2H...)
Affinity DataIC50: 2nMpH: 7.2 T: 2°CAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/30/2008
Entry Details Article
PubMed
LigandPNGBDBM29910(substituted 6-aminoquinoline-3-carbonitrile, 21)
Affinity DataIC50: 2nMpH: 7.2 T: 2°CAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2009
Entry Details Article
PubMed
LigandPNGBDBM50173838(4-(4-benzylphenylamino)-6-(2-morpholinoethylamino)...)
Affinity DataIC50: 2nMAssay Description:Inhibitory activity against human Tpl2 kinase via quantification of MEK phosphorylationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM29922(substituted 6-aminoquinoline-3-carbonitrile, 33)
Affinity DataIC50: 2.20nMAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2009
Entry Details Article
PubMed
LigandPNGBDBM29912(substituted 6-aminoquinoline-3-carbonitrile, 23)
Affinity DataIC50: 3nMpH: 7.2 T: 2°CAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2009
Entry Details Article
PubMed
LigandPNGBDBM50194988(4-(3-chloro-4-fluorophenylamino)-6-((1,5-dimethyl-...)
Affinity DataIC50: 3nMAssay Description:Inhibition of Tpl2 kinase by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50194998(4-(3-chloro-4-fluorophenylamino)-6-((5-methyl-1H-i...)
Affinity DataIC50: 3nMAssay Description:Inhibition of Tpl2 kinase by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM29909(substituted 6-aminoquinoline-3-carbonitrile, 20)
Affinity DataIC50: 4nMpH: 7.2 T: 2°CAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2009
Entry Details Article
PubMed
LigandPNGBDBM50191770(CHEMBL3912476)
Affinity DataIC50: 4nMAssay Description:Inhibition of human COT (66 to 395 residues) expressed in Sf21 cells using 5-Fluo-Ahx-AGAGSGQLIDSNleANSFVGTR-NH2 as substrate after 60 mins by calipe...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/27/2018
Entry Details Article
PubMed
LigandPNGBDBM29921(substituted 6-aminoquinoline-3-carbonitrile, 32)
Affinity DataIC50: 5.30nMAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2009
Entry Details Article
PubMed
LigandPNGBDBM50173833(6-(2-morpholinoethylamino)-4-(4-(phenylthio)phenyl...)
Affinity DataIC50: 6nMAssay Description:Inhibitory activity against human Tpl2 kinase via quantification of MEK phosphorylationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50191681(CHEMBL3939592)
Affinity DataIC50: 6nMAssay Description:Inhibition of human COT (66 to 395 residues) expressed in Sf21 cells using 5-Fluo-Ahx-AGAGSGQLIDSNleANSFVGTR-NH2 as substrate after 60 mins by calipe...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/27/2018
Entry Details Article
PubMed
LigandPNGBDBM29906(substituted 6-aminoquinoline-3-carbonitrile, 17)
Affinity DataIC50: 7nMpH: 7.2 T: 2°CAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2009
Entry Details Article
PubMed
LigandPNGBDBM29911(substituted 6-aminoquinoline-3-carbonitrile, 22)
Affinity DataIC50: 7.60nMpH: 7.2 T: 2°CAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2009
Entry Details Article
PubMed
LigandPNGBDBM29918(substituted 6-aminoquinoline-3-carbonitrile, 29)
Affinity DataIC50: 8nMpH: 7.2 T: 2°CAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2009
Entry Details Article
PubMed
LigandPNGBDBM29924(substituted 6-aminoquinoline-3-carbonitrile, 35)
Affinity DataIC50: 8.20nMAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2009
Entry Details Article
PubMed
LigandPNGBDBM50191769(CHEMBL3927501)
Affinity DataIC50: 9nMAssay Description:Inhibition of human COT (66 to 395 residues) expressed in Sf21 cells using 5-Fluo-Ahx-AGAGSGQLIDSNleANSFVGTR-NH2 as substrate after 60 mins by calipe...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/27/2018
Entry Details Article
PubMed
LigandPNGBDBM50191771(CHEMBL3890505)
Affinity DataIC50: 9nMAssay Description:Inhibition of human COT (66 to 395 residues) expressed in Sf21 cells using 5-Fluo-Ahx-AGAGSGQLIDSNleANSFVGTR-NH2 as substrate after 60 mins by calipe...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/27/2018
Entry Details Article
PubMed
LigandPNGBDBM29925(substituted 6-aminoquinoline-3-carbonitrile, 36)
Affinity DataIC50: 9.10nMAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2009
Entry Details Article
PubMed
LigandPNGBDBM29901(substituted 6-aminoquinoline-3-carbonitrile, 12)
Affinity DataIC50: 9.60nMpH: 7.2 T: 2°CAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2009
Entry Details Article
PubMed
LigandPNGBDBM21899(8-bromo-4-[(3-chloro-4-fluorophenyl)amino]-6-[(1H-...)
Affinity DataIC50: 10nMpH: 7.2 T: 2°CAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/30/2008
Entry Details Article
PubMed
LigandPNGBDBM29903(substituted 6-aminoquinoline-3-carbonitrile, 14)
Affinity DataIC50: 10nMpH: 7.2 T: 2°CAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2009
Entry Details Article
PubMed
LigandPNGBDBM29926(substituted 6-aminoquinoline-3-carbonitrile, 37)
Affinity DataIC50: 10nMAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2009
Entry Details Article
PubMed
LigandPNGBDBM50264866(4'-(2-(2H-tetrazol-5-yl)thieno[2,3-c]pyridin-4-ylo...)
Affinity DataIC50: 10nMAssay Description:Inhibition of human recombinant COT by HTRF-based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
LigandPNGBDBM50173834((R)-4-(3-chloro-4-fluorophenylamino)-6-(1-phenylet...)
Affinity DataIC50: 12nMAssay Description:Inhibitory activity against human Tpl2 kinase via quantification of MEK phosphorylationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM21898(8-chloro-4-[(3-chloro-4-fluorophenyl)amino]-6-[(1H...)
Affinity DataIC50: 12nMAssay Description:Inhibition of human Tpl2 by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
LigandPNGBDBM29915(substituted 6-aminoquinoline-3-carbonitrile, 26)
Affinity DataIC50: 13nMpH: 7.2 T: 2°CAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2009
Entry Details Article
PubMed
LigandPNGBDBM50195006(4-(3-chloro-4-fluorophenylamino)-6-((5-methyl-1-(2...)
Affinity DataIC50: 14nMAssay Description:Inhibition of Tpl2 kinase by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM21915(8-chloro-4-[(3-chloro-4-fluorophenyl)amino]-6-[(py...)
Affinity DataIC50: 16nMpH: 7.2 T: 2°CAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/30/2008
Entry Details Article
PubMed
LigandPNGBDBM21928(8-chloro-4-[(3-chloro-4-fluorophenyl)amino]-6-({[4...)
Affinity DataIC50: 16nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/30/2008
Entry Details Article
PubMed
LigandPNGBDBM21930(8-chloro-4-[(3-chloro-4-fluorophenyl)amino]-6-{[(4...)
Affinity DataIC50: 16nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/30/2008
Entry Details Article
PubMed
LigandPNGBDBM50173834((R)-4-(3-chloro-4-fluorophenylamino)-6-(1-phenylet...)
Affinity DataIC50: 16nMAssay Description:Inhibition of human Tpl2 by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
LigandPNGBDBM50191774(CHEMBL3899461)
Affinity DataIC50: 16nMAssay Description:Inhibition of human COT (66 to 395 residues) expressed in Sf21 cells using 5-Fluo-Ahx-AGAGSGQLIDSNleANSFVGTR-NH2 as substrate after 60 mins by calipe...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/27/2018
Entry Details Article
PubMed
LigandPNGBDBM29913(substituted 6-aminoquinoline-3-carbonitrile, 24)
Affinity DataIC50: 17nMpH: 7.2 T: 2°CAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2009
Entry Details Article
PubMed
LigandPNGBDBM21920(2-[({8-chloro-4-[(3-chloro-4-fluorophenyl)amino]-3...)
Affinity DataIC50: 18nMpH: 7.2 T: 2°CAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/30/2008
Entry Details Article
PubMed
LigandPNGBDBM21925(8-bromo-4-[(3-chloro-4-fluorophenyl)amino]-6-[(1H-...)
Affinity DataIC50: 18nMpH: 7.2 T: 2°CAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/30/2008
Entry Details Article
PubMed
LigandPNGBDBM21925(8-bromo-4-[(3-chloro-4-fluorophenyl)amino]-6-[(1H-...)
Affinity DataIC50: 18nMpH: 7.2 T: 2°CAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2009
Entry Details Article
PubMed
LigandPNGBDBM29920(substituted 6-aminoquinoline-3-carbonitrile, 31)
Affinity DataIC50: 18nMAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2009
Entry Details Article
PubMed
LigandPNGBDBM21896(BMCL193485 Compound 2 | CHEMBL220037 | 4-[(3-chlor...)
Affinity DataIC50: 19nMpH: 7.2 T: 2°CAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2009
Entry Details Article
PubMed
LigandPNGBDBM21896(BMCL193485 Compound 2 | CHEMBL220037 | 4-[(3-chlor...)
Affinity DataIC50: 19nMAssay Description:Inhibition of Tpl2 kinase by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM21896(BMCL193485 Compound 2 | CHEMBL220037 | 4-[(3-chlor...)
Affinity DataIC50: 20nMpH: 7.2 T: 2°CAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/30/2008
Entry Details Article
PubMed
LigandPNGBDBM21897(4-[(3-chloro-4-fluorophenyl)amino]-8-fluoro-6-[(1H...)
Affinity DataIC50: 20nMpH: 7.2 T: 2°CAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/30/2008
Entry Details Article
PubMed
LigandPNGBDBM21898(8-chloro-4-[(3-chloro-4-fluorophenyl)amino]-6-[(1H...)
Affinity DataIC50: 20nMpH: 7.2 T: 2°CAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/30/2008
Entry Details Article
PubMed
LigandPNGBDBM21903(4-[(3-chloro-4-fluorophenyl)amino]-6-[(1H-imidazol...)
Affinity DataIC50: 20nMpH: 7.2 T: 2°CAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/30/2008
Entry Details Article
PubMed
LigandPNGBDBM21926(8-bromo-4-[(3-chloro-4-fluorophenyl)amino]-6-[({1-...)
Affinity DataIC50: 20nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/30/2008
Entry Details Article
PubMed
LigandPNGBDBM28043(7-amino-4-(3-phenylphenyl)thieno[2,3-c]pyridine-2-...)
Affinity DataIC50: 20nMpH: 7.5 T: 2°CAssay Description:The COT direct HTRF assay was carried out using biotin-MEK1 as a substrate. The reaction was carried out in black 96 half-well plates. At designated...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/4/2009
Entry Details Article
PubMed
LigandPNGBDBM29908(substituted 6-aminoquinoline-3-carbonitrile, 19)
Affinity DataIC50: 20nMpH: 7.2 T: 2°CAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2009
Entry Details Article
PubMed
LigandPNGBDBM29914(substituted 6-aminoquinoline-3-carbonitrile, 25)
Affinity DataIC50: 20nMpH: 7.2 T: 2°CAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2009
Entry Details Article
PubMed
LigandPNGBDBM50191677(CHEMBL3910848)
Affinity DataIC50: 20nMAssay Description:Inhibition of human COT (66 to 395 residues) expressed in Sf21 cells using 5-Fluo-Ahx-AGAGSGQLIDSNleANSFVGTR-NH2 as substrate after 60 mins by calipe...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/27/2018
Entry Details Article
PubMed
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