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Found 1283 with Last Name = 'george' and Initial = 'n'
TargetGlutamate receptor ionotropic, NMDA 2B(Rattus norvegicus (Rat))
Bristol-Myers Squibb Research and Development

Curated by ChEMBL
LigandPNGBDBM198694(US9221796, 23b)
Affinity DataKi:  1.40nMAssay Description:Displacement of [3H]Ro 25-6981 from GluN2B receptor in Sprague-Dawley rat forebrain membranes incubated for 1 hr by topcount micro scintillation coun...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, NMDA 2B(Rattus norvegicus (Rat))
Bristol-Myers Squibb Research and Development

Curated by ChEMBL
LigandPNGBDBM198665(US9221796, 2b)
Affinity DataKi:  1.40nMAssay Description:Displacement of [3H]Ro 25-6981 from GluN2B receptor in Sprague-Dawley rat forebrain membranes incubated for 1 hr by topcount micro scintillation coun...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, NMDA 2B(Rattus norvegicus (Rat))
Bristol-Myers Squibb Research and Development

Curated by ChEMBL
LigandPNGBDBM198728(US9221796, 46, P-4)
Affinity DataKi:  4nMAssay Description:Displacement of [3H]Ro 25-6981 from GluN2B receptor in Sprague-Dawley rat forebrain membranes incubated for 1 hr by topcount micro scintillation coun...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, NMDA 2B(Rattus norvegicus (Rat))
Bristol-Myers Squibb Research and Development

Curated by ChEMBL
LigandPNGBDBM198726(US9221796, 46, P-2)
Affinity DataKi:  4.30nMAssay Description:Displacement of [3H]Ro 25-6981 from GluN2B receptor in Sprague-Dawley rat forebrain membranes incubated for 1 hr by topcount micro scintillation coun...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, NMDA 2B(Rattus norvegicus (Rat))
Bristol-Myers Squibb Research and Development

Curated by ChEMBL
LigandPNGBDBM50330324(CHEMBL4170867)
Affinity DataKi:  4.40nMAssay Description:Displacement of [3H]Ro 25-6981 from GluN2B receptor in Sprague-Dawley rat forebrain membranes incubated for 1 hr by topcount micro scintillation coun...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, NMDA 2B(Homo sapiens (Human))
Bristol-Myers Squibb Research and Development

Curated by ChEMBL
LigandPNGBDBM198728(US9221796, 46, P-4)
Affinity DataKi:  6.30nMAssay Description:Binding affinity to GluN2B receptor in human cortexMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, NMDA 2B(Rattus norvegicus (Rat))
Bristol-Myers Squibb Research and Development

Curated by ChEMBL
LigandPNGBDBM50330409(CHEMBL4168402)
Affinity DataKi:  7.70nMAssay Description:Displacement of [3H]Ro 25-6981 from GluN2B receptor in Sprague-Dawley rat forebrain membranes incubated for 1 hr by topcount micro scintillation coun...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, NMDA 2B(Rattus norvegicus (Rat))
Bristol-Myers Squibb Research and Development

Curated by ChEMBL
LigandPNGBDBM50330410(CHEMBL4161899)
Affinity DataKi:  8.40nMAssay Description:Displacement of [3H]Ro 25-6981 from GluN2B receptor in Sprague-Dawley rat forebrain membranes incubated for 1 hr by topcount micro scintillation coun...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, NMDA 2B(Rattus norvegicus (Rat))
Bristol-Myers Squibb Research and Development

Curated by ChEMBL
LigandPNGBDBM198735(US9221796, 48, P-3)
Affinity DataKi:  11nMAssay Description:Displacement of [3H]Ro 25-6981 from GluN2B receptor in Sprague-Dawley rat forebrain membranes incubated for 1 hr by topcount micro scintillation coun...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetReceptor-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50513015(CHEMBL4537171)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of human GST/His-tagged RIP1 (1 to 375 residues) expressed in baculovirus expression system assessed as reduction in autophosphorylation m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetDual specificity protein kinase CLK2(Homo sapiens (Human))TBA
LigandPNGBDBM50613087(CHEMBL5091238)
Affinity DataIC50:  0.600nMAssay Description:Inhibition of recombinant human CLK2 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scinti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails PubMed
TargetReceptor-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50507336(CHEMBL4514271)
Affinity DataIC50:  1nMAssay Description:Inhibition of human GST/His-tagged RIP1 (1 to 375 residues) expressed in baculovirus expression system assessed as reduction in autophosphorylation m...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50530417(CHEMBL4441878)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of recombinant human DYRK1A expressed in Escherichia coli using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
LigandPNGBDBM50530417(CHEMBL4441878)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of recombinant human DYRK1B expressed in Sf9 insect cells using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
LigandPNGBDBM50583755(CHEMBL5070553)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of recombinant human DYRK1B expressed in Sf9 insect cells using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetDual specificity protein kinase CLK2(Homo sapiens (Human))TBA
LigandPNGBDBM25036(CHEMBL393525 | N'-[(1E)-{6-bromoimidazo[1,2-a]pyri...)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of recombinant human CLK2 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scinti...More data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM50613087(CHEMBL5091238)
Affinity DataIC50:  1.20nMAssay Description:Inhibition of recombinant human DYRK1A expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scin...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails PubMed
LigandPNGBDBM50538084(CHEMBL4647659)
Affinity DataIC50:  1.20nMAssay Description:Inhibition of recombinant human DYRK1A expressed in Escherichia coli using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetReceptor-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50513040(CHEMBL4593226)
Affinity DataIC50:  1.30nMAssay Description:Inhibition of human GST/His-tagged RIP1 (1 to 375 residues) expressed in baculovirus expression system assessed as reduction in autophosphorylation m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM293424(US10106527, Compound 10 | US10106527, Compound 142...)
Affinity DataIC50:  1.40nMAssay Description:Inhibition of recombinant human DYRK1A expressed in Escherichia coli using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetReceptor-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50513011(CHEMBL4455042)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of human GST/His-tagged RIP1 (1 to 375 residues) expressed in baculovirus expression system assessed as reduction in autophosphorylation m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetReceptor-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50513004(CHEMBL4521353)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of human GST/His-tagged RIP1 (1 to 375 residues) expressed in baculovirus expression system assessed as reduction in autophosphorylation m...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50513024(CHEMBL4471642)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of human GST/His-tagged RIP1 (1 to 375 residues) expressed in baculovirus expression system assessed as reduction in autophosphorylation m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM385170(US10287267, Compound 330 | US10508099, Compound 33...)
Affinity DataIC50:  1.80nMAssay Description:Inhibition of recombinant human DYRK1A expressed in Escherichia coli using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
LigandPNGBDBM50613087(CHEMBL5091238)
Affinity DataIC50:  1.80nMAssay Description:Inhibition of recombinant human DYRK1B expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scin...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails PubMed
LigandPNGBDBM50335638(5-(3-Chlorophenylamino)benzo[c][2,6]naphthyridine-...)
Affinity DataIC50:  1.90nMAssay Description:Inhibition of recombinant human DYRK1A expressed in Escherichia coli using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by...More data for this Ligand-Target Pair
TargetReceptor-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50513034(CHEMBL4541955)
Affinity DataIC50:  2nMAssay Description:Inhibition of RIP1 in human U937 cells assessed as reduction in TNFalpha/QVD-Oph-induced necroptosis measured after 24 hrs by cell titer-glo luminesc...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetReceptor-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50513013(CHEMBL4450890)
Affinity DataIC50:  2nMAssay Description:Inhibition of human GST/His-tagged RIP1 (1 to 375 residues) expressed in baculovirus expression system assessed as reduction in autophosphorylation m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetReceptor-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50513016(CHEMBL4514028)
Affinity DataIC50:  2nMAssay Description:Inhibition of human GST/His-tagged RIP1 (1 to 375 residues) expressed in baculovirus expression system assessed as reduction in autophosphorylation m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50097869(CHEMBL3589662)
Affinity DataIC50:  2.30nMAssay Description:Inhibition of recombinant human DYRK1A expressed in Escherichia coli using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by...More data for this Ligand-Target Pair
TargetReceptor-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50512996(CHEMBL4454462)
Affinity DataIC50:  2.5nMAssay Description:Inhibition of human GST/His-tagged RIP1 (1 to 375 residues) expressed in baculovirus expression system assessed as reduction in autophosphorylation m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetReceptor-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50513034(CHEMBL4541955)
Affinity DataIC50:  2.5nMAssay Description:Inhibition of human GST/His-tagged RIP1 (1 to 375 residues) expressed in baculovirus expression system assessed as reduction in autophosphorylation m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetReceptor-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50513016(CHEMBL4514028)
Affinity DataIC50:  2.5nMAssay Description:Inhibition of RIP1 in human U937 cells assessed as reduction in TNFalpha/QVD-Oph-induced necroptosis measured after 24 hrs by cell titer-glo luminesc...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetReceptor-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50512998(CHEMBL4575848)
Affinity DataIC50:  2.5nMAssay Description:Inhibition of human GST/His-tagged RIP1 (1 to 375 residues) expressed in baculovirus expression system assessed as reduction in autophosphorylation m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetReceptor-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50513030(CHEMBL4548784)
Affinity DataIC50:  2.5nMAssay Description:Inhibition of human GST/His-tagged RIP1 (1 to 375 residues) expressed in baculovirus expression system assessed as reduction in autophosphorylation m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetDual specificity protein kinase CLK4(Homo sapiens (Human))TBA
LigandPNGBDBM50335638(5-(3-Chlorophenylamino)benzo[c][2,6]naphthyridine-...)
Affinity DataIC50:  2.60nMAssay Description:Inhibition of recombinant human CLK4 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scinti...More data for this Ligand-Target Pair
LigandPNGBDBM50613085(CHEMBL5081787)
Affinity DataIC50:  2.60nMAssay Description:Inhibition of recombinant human DYRK1A expressed in Escherichia coli using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
LigandPNGBDBM50583755(CHEMBL5070553)
Affinity DataIC50:  2.70nMAssay Description:Inhibition of recombinant human DYRK1B expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scin...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetDual specificity protein kinase CLK2(Homo sapiens (Human))TBA
LigandPNGBDBM50335638(5-(3-Chlorophenylamino)benzo[c][2,6]naphthyridine-...)
Affinity DataIC50:  2.80nMAssay Description:Inhibition of recombinant human CLK2 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scinti...More data for this Ligand-Target Pair
TargetReceptor-interacting serine/threonine-protein kinase 1(Mus musculus)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50512997(CHEMBL4545939)
Affinity DataIC50:  3.20nMAssay Description:Inhibition of RIP1 in mouse L929 cells assessed as reduction in TNF/zVAD.fmk-induced necrotic death measured after 24 hrs by cell titer-glo luminesce...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetAP2-associated protein kinase 1(Homo sapiens (Human))
Bristol-Myers Squibb

US Patent
LigandPNGBDBM335593(3-((5-((4-aminopiperidin-1-yl)methyl)pyrrolo[2,1-f...)
Affinity DataIC50:  3.30nMAssay Description:The assays were performed in U-bottom 384-well plates. The final assay volume was 30 μl prepared from 15 μl additions of enzyme and substra...More data for this Ligand-Target Pair
LigandPNGBDBM25036(CHEMBL393525 | N'-[(1E)-{6-bromoimidazo[1,2-a]pyri...)
Affinity DataIC50:  3.40nMAssay Description:Inhibition of recombinant human DYRK1B expressed in Sf9 insect cells using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by...More data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM50110183(Abemaciclib | LY-2835219 | US10626107, Example LY2...)
Affinity DataIC50:  3.5nMAssay Description:Inhibition of recombinant human DYRK1B expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scin...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetDual specificity protein kinase CLK2(Homo sapiens (Human))TBA
LigandPNGBDBM293424(US10106527, Compound 10 | US10106527, Compound 142...)
Affinity DataIC50:  3.60nMAssay Description:Inhibition of recombinant human CLK2 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scinti...More data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM293424(US10106527, Compound 10 | US10106527, Compound 142...)
Affinity DataIC50:  3.60nMAssay Description:Inhibition of recombinant human DYRK1B expressed in Sf9 insect cells using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by...More data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM25036(CHEMBL393525 | N'-[(1E)-{6-bromoimidazo[1,2-a]pyri...)
Affinity DataIC50:  3.70nMAssay Description:Inhibition of recombinant human DYRK1B expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scin...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetGlycogen synthase kinase-3 beta(Homo sapiens (Human))TBA
LigandPNGBDBM50538084(CHEMBL4647659)
Affinity DataIC50:  3.80nMAssay Description:Inhibition of recombinant human GSK-3beta expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric s...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetReceptor-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50507336(CHEMBL4514271)
Affinity DataIC50:  4nMAssay Description:Inhibition of RIP1 in human U937 cells assessed as reduction in TNFalpha/QVD-Oph-induced necroptosis measured after 24 hrs by cell titer-glo luminesc...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50513015(CHEMBL4537171)
Affinity DataIC50:  4nMAssay Description:Inhibition of RIP1 in human U937 cells assessed as reduction in TNFalpha/QVD-Oph-induced necroptosis measured after 24 hrs by cell titer-glo luminesc...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetReceptor-interacting serine/threonine-protein kinase 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50513004(CHEMBL4521353)
Affinity DataIC50:  4nMAssay Description:Inhibition of RIP1 in human U937 cells assessed as reduction in TNFalpha/QVD-Oph-induced necroptosis measured after 24 hrs by cell titer-glo luminesc...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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