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TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50235302(CHEMBL4099771)
Affinity DataKi:  0.00200nMAssay Description:Competitive inhibition of DOT1L (2 to 416 residues) (unknown origin) using biotinylated nucleosomes as substrate preincubated for 30 mins followed by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50075098(CHEMBL3414626 | US10143704, Compound A2 | US944606...)
Affinity DataKi:  0.0120nMAssay Description:Competitive inhibition of DOT1L (2 to 416 residues) (unknown origin) using biotinylated nucleosomes as substrate preincubated for 30 mins followed by...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50536826(CHEMBL4590355)
Affinity DataKi:  0.0800nMAssay Description:Inhibition of DOT1L (2 to 416 residues) (unknown origin) using biotinylated nucleosomes as substrate preincubated for 30 mins followed by substrate a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50536819(CHEMBL4534250)
Affinity DataKi:  0.360nMAssay Description:Inhibition of DOT1L (2 to 416 residues) (unknown origin) using biotinylated nucleosomes as substrate preincubated for 30 mins followed by substrate a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50075098(CHEMBL3414626 | US10143704, Compound A2 | US944606...)
Affinity DataIC50: <0.100nMAssay Description:Inhibition of DOT1L (2 to 416 residues) (unknown origin) using biotinylated nucleosomes as substrate preincubated for 30 mins followed by substrate a...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50235302(CHEMBL4099771)
Affinity DataIC50: <0.100nMAssay Description:Inhibition of DOT1L (2 to 416 residues) (unknown origin) using biotinylated nucleosomes as substrate preincubated for 30 mins followed by substrate a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50235301(CHEMBL4081752)
Affinity DataIC50:  0.150nMAssay Description:Inhibition of DOT1L (2 to 416 residues) (unknown origin) using biotinylated nucleosomes as substrate preincubated for 30 mins followed by substrate a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1 [866-1154](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM294911(US10112907, Example 00020 | US10766894, Compound T...)
Affinity DataIC50:  0.200nMpH: 7.5Assay Description:A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), J...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM294911(US10112907, Example 00020 | US10766894, Compound T...)
Affinity DataIC50:  0.200nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK1 [866-1154](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM294911(US10112907, Example 00020 | US10766894, Compound T...)
Affinity DataIC50:  0.200nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCathepsin E(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50305527((4S)-4-[(1R)-1-hydroxy-2-({1-[3-(1-methylethyl)phe...)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of cathepsin EMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50536826(CHEMBL4590355)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of DOT1L (2 to 416 residues) (unknown origin) using biotinylated nucleosomes as substrate preincubated for 30 mins followed by substrate a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM50021656(BARICITINIB | INCB-028050 | LY-3009104 | US1011290...)
Affinity DataIC50:  0.700nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM294911(US10112907, Example 00020 | US10766894, Compound T...)
Affinity DataIC50:  0.700nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK1 [866-1154](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM50021656(BARICITINIB | INCB-028050 | LY-3009104 | US1011290...)
Affinity DataIC50:  0.700nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK2 [808-1132](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM294911(US10112907, Example 00020 | US10766894, Compound T...)
Affinity DataIC50:  0.700nMpH: 7.5Assay Description:A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), J...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK1 [866-1154](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM50021656(BARICITINIB | INCB-028050 | LY-3009104 | US1011290...)
Affinity DataIC50:  0.700nMpH: 7.5Assay Description:A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), J...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK2 [808-1132](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM294911(US10112907, Example 00020 | US10766894, Compound T...)
Affinity DataIC50:  0.700nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBeta-secretase 2(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM116254(US10035794, Example 31 | US10683287, Example 31 | ...)
Affinity DataIC50:  1nMpH: 4.5 T: 2°CAssay Description:Recombinant BACE-2 (extracellular domain, expressed in baculovirus and purified using standard methods) at 0.1 to 10 nM concentrations is incubated w...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBeta-secretase 2(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM116254(US10035794, Example 31 | US10683287, Example 31 | ...)
Affinity DataIC50:  1nMAssay Description:Inhibition of human recombinant BACE2 catalytic domain using FRET substrate with BACE-cleavable sequenceMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50305544((S)-4-{(R)-1-Hydroxy-2-[1-(3-isopropyl-phenyl)-cyc...)
Affinity DataIC50:  1nMAssay Description:Inhibition of human recombinant BACE1 expressed in Escherichia coliMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1 [866-1154](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM50402074(CHEMBL2206059 | US10112907, Example 00024 | US1076...)
Affinity DataIC50:  1nMpH: 7.5Assay Description:A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), J...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK1 [866-1154](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM294916(US10112907, Example 00027 | US10206907, Compound 1...)
Affinity DataIC50:  1nMpH: 7.5Assay Description:A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), J...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCathepsin D(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50294218((3S,14R,16S)-16-((R)-1-hydroxy-2-((S)-6-isopropyl-...)
Affinity DataIC50:  1nMAssay Description:Inhibition of human cathepsin DMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin D(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50305527((4S)-4-[(1R)-1-hydroxy-2-({1-[3-(1-methylethyl)phe...)
Affinity DataIC50:  1nMAssay Description:Inhibition of cathepsin DMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1 [866-1154](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataIC50:  1nMpH: 7.5Assay Description:A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), J...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBeta-secretase 2(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM116254(US10035794, Example 31 | US10683287, Example 31 | ...)
Affinity DataIC50:  1nMpH: 4.5 T: 2°CAssay Description:Recombinant BACE-2 (extracellular domain, expressed in baculovirus and purified using standard methods) at 0.1 to 10 nM concentrations is incubated w...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM50402074(CHEMBL2206059 | US10112907, Example 00024 | US1076...)
Affinity DataIC50:  1nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM294916(US10112907, Example 00027 | US10206907, Compound 1...)
Affinity DataIC50:  1nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK1 [866-1154](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataIC50:  1nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK1 [866-1154](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM50402074(CHEMBL2206059 | US10112907, Example 00024 | US1076...)
Affinity DataIC50:  1nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
TargetBeta-secretase 2(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM116254(US10035794, Example 31 | US10683287, Example 31 | ...)
Affinity DataIC50:  1nMAssay Description:Recombinant BACE-2 (extracellular domain, expressed in baculovirus and purified using standard methods) at 0.1 to 10 nM concentrations is incubated w...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50305542(CHEMBL595016 | Propane-1-sulfonic acid{(S)-4-[(R)-...)
Affinity DataIC50:  1nMAssay Description:Inhibition of human recombinant BACE1 expressed in Escherichia coliMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataIC50:  1nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
In DepthDetails US PatentDrugBank

TargetTyrosine-protein kinase JAK1 [866-1154](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM294916(US10112907, Example 00027 | US10206907, Compound 1...)
Affinity DataIC50:  1nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50536819(CHEMBL4534250)
Affinity DataIC50:  1.40nMAssay Description:Inhibition of DOT1L (2 to 416 residues) (unknown origin) using biotinylated nucleosomes as substrate preincubated for 30 mins followed by substrate a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50386481(CHEMBL2048058)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant BACE1 ectodomain after 1 hr by fluorescence analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM294911(US10112907, Example 00020 | US10766894, Compound T...)
Affinity DataIC50:  2nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50294218((3S,14R,16S)-16-((R)-1-hydroxy-2-((S)-6-isopropyl-...)
Affinity DataIC50:  2nMAssay Description:Inhibition of BACE1More data for this Ligand-Target Pair
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50305531(CHEMBL595136 | Propane-1-sulfonic acid((S)-4-{(R)-...)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant BACE1 expressed in Escherichia coliMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNon-receptor tyrosine-protein kinase TYK2 [888-1187](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM294911(US10112907, Example 00020 | US10766894, Compound T...)
Affinity DataIC50:  2nMpH: 7.5Assay Description:A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), J...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK1 [866-1154](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM294915(US10112907, Example 00026)
Affinity DataIC50:  2nMpH: 7.5Assay Description:A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), J...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK2 [808-1132](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataIC50:  2nMpH: 7.5Assay Description:A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), J...More data for this Ligand-Target Pair
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50386487(CHEMBL2048047)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant BACE1 ectodomain after 1 hr by fluorescence analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50386513(CHEMBL2048051)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant BACE1 ectodomain after 1 hr by fluorescence analysisMore data for this Ligand-Target Pair
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50386515(CHEMBL2048053)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant BACE1 ectodomain after 1 hr by fluorescence analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50386482(CHEMBL2048059)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant BACE1 ectodomain after 1 hr by fluorescence analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM116236(US10035794, Example 11 | US10683287, Example 11 | ...)
Affinity DataIC50:  2nMAssay Description:Chinese hamster ovary cells are transfected with the human gene for amyloid precursor protein. The cells are plated at a density of 8000 cells/well i...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM462294(US10766894, Compound TABLE 1.11 | US11203595, TABL...)
Affinity DataIC50:  2nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetTyrosine-protein kinase JAK2 [808-1132](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM50355501(INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE ...)
Affinity DataIC50:  2nMAssay Description:The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by ...More data for this Ligand-Target Pair
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