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Found 188 with Last Name = 'pappano' and Initial = 'wn'
TargetPolycomb protein EED(Homo sapiens (Human))
Abbvie

LigandPNGBDBM223987(A-395 (5) | rac-(3R,4S)-1-(7-fluoro-2,3-dihydro-1H...)
Affinity DataKi:  0.400nM ΔG°:  -53.6kJ/molepH: 7.5 T: 2°CAssay Description:For the assay, compounds were dispensed in assay-ready plates using a three-fold serial dilution from 50 μM to ~850 pM using an Echo 550 Acousti...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPolycomb protein EED(Homo sapiens (Human))
Abbvie

LigandPNGBDBM223987(A-395 (5) | rac-(3R,4S)-1-(7-fluoro-2,3-dihydro-1H...)
Affinity DataKi:  0.5nM ΔG°:  -53.1kJ/molepH: 7.5 T: 2°CAssay Description:For the assay, compounds were dispensed in assay-ready plates using a three-fold serial dilution from 50 μM to ~850 pM using an Echo 550 Acousti...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPolycomb protein EED(Homo sapiens (Human))
Abbvie

LigandPNGBDBM223986((3R,4S)-1-[(1S)-7-fluoroindan-1-yl]-N,N-dimethyl-4...)
Affinity DataKi:  1nM ΔG°:  -51.4kJ/molepH: 7.5 T: 2°CAssay Description:For the assay, compounds were dispensed in assay-ready plates using a three-fold serial dilution from 50 μM to ~850 pM using an Echo 550 Acousti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetPolycomb protein EED(Homo sapiens (Human))
Abbvie

LigandPNGBDBM223985(rac-(3R,4S)-1-(2-fluoro-6-methylbenzyl)-N,N-dimeth...)
Affinity DataKi:  4nM ΔG°:  -47.9kJ/molepH: 7.5 T: 2°CAssay Description:For the assay, compounds were dispensed in assay-ready plates using a three-fold serial dilution from 50 μM to ~850 pM using an Echo 550 Acousti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetN-lysine methyltransferase KMT5A(Homo sapiens (Human))
Abbvie

Curated by ChEMBL
LigandPNGBDBM50201571(CHEMBL3934996)
Affinity DataKi:  50nMAssay Description:Competitive inhibition of human SETD8 (186 to 352 residues) using biotin-labeled H4K20 (1 to 24 residues) as substrate after 1 hr in presence of 3H-S...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPolycomb protein EED(Homo sapiens (Human))
Abbvie

LigandPNGBDBM223984(rac-(3R,4S)-1-(2-methoxybenzyl)-N,N-dimethyl-4-(1-...)
Affinity DataKi:  1.20E+3nM ΔG°:  -33.8kJ/molepH: 7.5 T: 2°CAssay Description:For the assay, compounds were dispensed in assay-ready plates using a three-fold serial dilution from 50 μM to ~850 pM using an Echo 550 Acousti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetPolycomb protein EED(Homo sapiens (Human))
Abbvie

LigandPNGBDBM223989(A-395N (6))
Affinity DataKi:  1.83E+3nM ΔG°:  -32.7kJ/molepH: 7.5 T: 2°CAssay Description:For the assay, compounds were dispensed in assay-ready plates using a three-fold serial dilution from 50 μM to ~850 pM using an Echo 550 Acousti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetN-lysine methyltransferase KMT5A(Homo sapiens (Human))
Abbvie

Curated by ChEMBL
LigandPNGBDBM50051116(CHEMBL3318284)
Affinity DataKi:  2.00E+3nMAssay Description:Competitive inhibition of SETD8 (unknown origin) using biotin-labeled H4 (1 to 24 residues) as substrate after 1 hr in presence of varying levels of ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
Abbvie

Curated by ChEMBL
LigandPNGBDBM50446378(CHEMBL3109639)
Affinity DataIC50:  0.900nMAssay Description:Inhibition of G9a (unknown origin) using biotinylated-histone H3(1-21) peptide as substrate after 3 hrs by AlphaLISA assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
Abbvie

Curated by ChEMBL
LigandPNGBDBM50446386(CHEMBL3109631)
Affinity DataIC50:  1nMAssay Description:Inhibition of G9a (unknown origin) using biotinylated-histone H3(1-21) peptide as substrate after 3 hrs by AlphaLISA assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetN-lysine methyltransferase SMYD2(Homo sapiens (Human))
Abbvie

Curated by ChEMBL
LigandPNGBDBM50095537(CHEMBL3590526 | US9598381, 1a (S enantiomer))
Affinity DataIC50:  2.80nMAssay Description:Inhibition of SMYD2 (unknown origin) using biotinylated GSRAHSSHLKSKKGQSTSRH as substrate assessed as incorporation of tritium labeled methyl group f...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
Abbvie

Curated by ChEMBL
LigandPNGBDBM50446376(CHEMBL3109630)
Affinity DataIC50:  3nMAssay Description:Inhibition of G9a (unknown origin)-mediated incorporation of methyl group from [3H]-SAM into peptide substrate by scintillation proximity assayMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
Abbvie

Curated by ChEMBL
LigandPNGBDBM50446376(CHEMBL3109630)
Affinity DataIC50:  3.30nMAssay Description:Inhibition of G9a (unknown origin) using biotinylated-histone H3(1-21) peptide as substrate after 3 hrs by AlphaLISA assayMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
Abbvie

Curated by ChEMBL
LigandPNGBDBM50446380(CHEMBL3109637)
Affinity DataIC50:  3.70nMAssay Description:Inhibition of G9a (unknown origin) using biotinylated-histone H3(1-21) peptide as substrate after 3 hrs by AlphaLISA assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315895(CHEMBL1090357 | N-(3-(5-(2-(4-(2-(dimethylamino)et...)
Affinity DataIC50:  4.30nMAssay Description:Inhibition of ErbB2 by time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
Abbvie

Curated by ChEMBL
LigandPNGBDBM50446383(CHEMBL3109634)
Affinity DataIC50:  4.80nMAssay Description:Inhibition of G9a (unknown origin) using biotinylated-histone H3(1-21) peptide as substrate after 3 hrs by AlphaLISA assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315905(CHEMBL1090350 | N-(3-(5-(2-(4-morpholinophenylamin...)
Affinity DataIC50:  4.80nMAssay Description:Inhibition of ErbB2 by time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
Abbvie

Curated by ChEMBL
LigandPNGBDBM50446385(CHEMBL3109632)
Affinity DataIC50:  5nMAssay Description:Inhibition of G9a (unknown origin) using biotinylated-histone H3(1-21) peptide as substrate after 3 hrs by AlphaLISA assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetN-lysine methyltransferase SMYD2(Homo sapiens (Human))
Abbvie

Curated by ChEMBL
LigandPNGBDBM50095536(CHEMBL3590527 | US9598381, 1 (racemate))
Affinity DataIC50:  5.60nMAssay Description:Inhibition of SMYD2 (unknown origin) using biotinylated GSRAHSSHLKSKKGQSTSRH as substrate assessed as incorporation of tritium labeled methyl group f...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315903(CHEMBL1093234 | N-(3-(5-(2-(phenylamino)pyrimidin-...)
Affinity DataIC50:  6.30nMAssay Description:Inhibition of ErbB2 by time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315897(2,6-difluoro-N-(3-(5-(2-(1,2,3,4-tetrahydroisoquin...)
Affinity DataIC50:  7.20nMAssay Description:Inhibition of ErbB2 by time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPolycomb protein EED(Homo sapiens (Human))
Abbvie

LigandPNGBDBM223987(A-395 (5) | rac-(3R,4S)-1-(7-fluoro-2,3-dihydro-1H...)
Affinity DataIC50:  7.51nMpH: 7.5 T: 2°CAssay Description:For the assay, compounds or nonbiotinylated H3(23-34) peptide were dispensed in assay-ready plates using a three-fold serial dilution from 50 μM...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315896(CHEMBL1090358 | N-(3-(5-(2-(4-(4-ethylpiperazin-1-...)
Affinity DataIC50:  14nMAssay Description:Inhibition of ErbB2 by time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetN-lysine methyltransferase SMYD2(Homo sapiens (Human))
Abbvie

Curated by ChEMBL
LigandPNGBDBM50075102(CHEMBL3414623)
Affinity DataIC50: <15nMAssay Description:Inhibition of SMYD2 (unknown origin) using p53 (361 to 380) as substrate assessed as incorporation of tritium labeled methyl group from [3H]-SAM to p...More data for this Ligand-Target Pair
TargetPolycomb protein EED(Homo sapiens (Human))
Abbvie

LigandPNGBDBM223987(A-395 (5) | rac-(3R,4S)-1-(7-fluoro-2,3-dihydro-1H...)
Affinity DataIC50:  18nMT: 2°CAssay Description:IC50 values were determined for compounds A-395 and A-395N at 75 nM of EZH2 trimeric complex (EZH2-EED-SUZ12), 3 μM of human nucleosome and 1 &#...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
Abbvie

Curated by ChEMBL
LigandPNGBDBM50446379(CHEMBL3109638)
Affinity DataIC50:  18nMAssay Description:Inhibition of G9a (unknown origin) using biotinylated-histone H3(1-21) peptide as substrate after 3 hrs by AlphaLISA assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-4(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315888(CHEMBL1090360 | N-(3-(5-(2-(3-morpholinophenylamin...)
Affinity DataIC50:  18nMAssay Description:Inhibition of ErRB4More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315887((1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidaz...)
Affinity DataIC50:  18nMAssay Description:Inhibition of human recombinant IGF1R expressed in Sf21 cells by time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetN-lysine methyltransferase SMYD2(Homo sapiens (Human))
Abbvie

Curated by ChEMBL
LigandPNGBDBM50095537(CHEMBL3590526 | US9598381, 1a (S enantiomer))
Affinity DataIC50:  23nMAssay Description:Binding affinity of compounds having formula (I) to SMYD2 is indicia of their inhibition of the activity of this protein lysine methyltransferase. To...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase KMT5B(Homo sapiens (Human))
Abbvie

LigandPNGBDBM223981(6,7-Dichloro-N-cyclopentyl-4-(pyridin-4-yl)phthala...)
Affinity DataIC50:  25nMpH: 8.0 T: 2°CAssay Description:Experiments were performed in triplicate at room temperature with 1 h incubation of 10 μl reaction mixture in buffer of 20 mM Tris-HCl, pH 8.0, ...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase Lyn(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315888(CHEMBL1090360 | N-(3-(5-(2-(3-morpholinophenylamin...)
Affinity DataIC50:  26nMAssay Description:Inhibition of LynMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315886(2-phenyl-N-(3-(5-(2-(1,2,3,4-tetrahydroisoquinolin...)
Affinity DataIC50:  27nMAssay Description:Inhibition of human recombinant IGF1R expressed in Sf21 cells by time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315895(CHEMBL1090357 | N-(3-(5-(2-(4-(2-(dimethylamino)et...)
Affinity DataIC50:  27nMAssay Description:Inhibition of ErbB2 intracellular phosphorylation in human N87 cells by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315888(CHEMBL1090360 | N-(3-(5-(2-(3-morpholinophenylamin...)
Affinity DataIC50:  29nMAssay Description:Inhibition of KDRMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM5446(CHEMBL553 | ERLOTINIB HYDROCHLORIDE | Erlotinib | ...)
Affinity DataIC50:  34nMAssay Description:Inhibition of EGFR intracellular phosphorylation in human A431 cells by ELISAMore data for this Ligand-Target Pair
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315902(2-chloro-N-(3-(5-(2-(phenylamino)pyrimidin-4-yl)im...)
Affinity DataIC50:  35nMAssay Description:Inhibition of ErbB2 by time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EHMT1(Homo sapiens (Human))
Abbvie

Curated by ChEMBL
LigandPNGBDBM50446376(CHEMBL3109630)
Affinity DataIC50:  38nMAssay Description:Inhibition of GLP (unknown origin)-mediated incorporation of methyl group from [3H]-SAM into peptide substrate by scintillation proximity assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315885(CHEMBL1090362 | N-(3-(5-(2-(4-(4-ethylpiperazin-1-...)
Affinity DataIC50:  41nMAssay Description:Inhibition of human recombinant IGF1R expressed in Sf21 cells by time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315899(CHEMBL1090363 | N-(3-(5-(2-(3-(2-(dimethylamino)et...)
Affinity DataIC50:  46nMAssay Description:Inhibition of human recombinant IGF1R expressed in Sf21 cells by time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315896(CHEMBL1090358 | N-(3-(5-(2-(4-(4-ethylpiperazin-1-...)
Affinity DataIC50:  50nMAssay Description:Inhibition of EGFR intracellular phosphorylation in human A431 cells by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315885(CHEMBL1090362 | N-(3-(5-(2-(4-(4-ethylpiperazin-1-...)
Affinity DataIC50:  52nMAssay Description:Inhibition of human recombinant IGF1R expressed in Sf21 cells by time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  52nMAssay Description:Inhibition of EGFR intracellular phosphorylation in human A431 cells by ELISAMore data for this Ligand-Target Pair
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315886(2-phenyl-N-(3-(5-(2-(1,2,3,4-tetrahydroisoquinolin...)
Affinity DataIC50:  55nMAssay Description:Inhibition of ErbB2 by time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAurora kinase A(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315888(CHEMBL1090360 | N-(3-(5-(2-(3-morpholinophenylamin...)
Affinity DataIC50:  65nMAssay Description:Inhibition of Aurora1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 3(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315888(CHEMBL1090360 | N-(3-(5-(2-(3-morpholinophenylamin...)
Affinity DataIC50:  65nMAssay Description:Inhibition of Flt4More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetN-lysine methyltransferase SMYD2(Homo sapiens (Human))
Abbvie

Curated by ChEMBL
LigandPNGBDBM50095536(CHEMBL3590527 | US9598381, 1 (racemate))
Affinity DataIC50:  65nMAssay Description:Binding affinity of compounds having formula (I) to SMYD2 is indicia of their inhibition of the activity of this protein lysine methyltransferase. To...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315896(CHEMBL1090358 | N-(3-(5-(2-(4-(4-ethylpiperazin-1-...)
Affinity DataIC50:  69nMAssay Description:Inhibition of ErbB2 intracellular phosphorylation in human N87 cells by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Lck(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315888(CHEMBL1090360 | N-(3-(5-(2-(3-morpholinophenylamin...)
Affinity DataIC50:  71nMAssay Description:Inhibition of LCKMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315888(CHEMBL1090360 | N-(3-(5-(2-(3-morpholinophenylamin...)
Affinity DataIC50:  73nMAssay Description:Inhibition of ErbB2 by time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInsulin receptor(Homo sapiens (Human))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50315888(CHEMBL1090360 | N-(3-(5-(2-(3-morpholinophenylamin...)
Affinity DataIC50:  80nMAssay Description:Inhibition of InsRMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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