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Found 691 with Last Name = 'jacoby' and Initial = 'e'
TargetSubstance-P receptor(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50290462(CHEMBL305119 | potassium 2N-[1-benzyl(methyl)carba...)
Affinity DataKi:  1.5nMAssay Description:Binding affinity of the compound for NK-1 receptor was determined in a radioligand binding assay using IM9 human lymphoblastoma cell line.More data for this Ligand-Target Pair
In DepthDetails Article
TargetNeuromedin-K receptor(Rattus norvegicus)
TBA

Curated by ChEMBL
LigandPNGBDBM50290462(CHEMBL305119 | potassium 2N-[1-benzyl(methyl)carba...)
Affinity DataKi:  5nMAssay Description:Binding affinity of the compound for NK-3 receptor was determined in vitro using isolated rat portal vein.More data for this Ligand-Target Pair
In DepthDetails Article
TargetSubstance-K receptor(Oryctolagus cuniculus)
TBA

Curated by ChEMBL
LigandPNGBDBM50290461(CHEMBL65468 | potassium 3,5-di(trifluoromethyl)ben...)
Affinity DataKi:  5.20nMAssay Description:Binding affinity of the compound for NK-2 receptor was determined in vitro using isolated rabbit pulmonary artery.More data for this Ligand-Target Pair
In DepthDetails Article
TargetNeuromedin-K receptor(Rattus norvegicus)
TBA

Curated by ChEMBL
LigandPNGBDBM50290461(CHEMBL65468 | potassium 3,5-di(trifluoromethyl)ben...)
Affinity DataKi:  5.5nMAssay Description:Binding affinity of the compound for NK-3 receptor was determined in vitro using isolated rat portal vein.More data for this Ligand-Target Pair
In DepthDetails Article
TargetSubstance-K receptor(Oryctolagus cuniculus)
TBA

Curated by ChEMBL
LigandPNGBDBM50290462(CHEMBL305119 | potassium 2N-[1-benzyl(methyl)carba...)
Affinity DataKi:  5.60nMAssay Description:Binding affinity of the compound for NK-2 receptor was determined in vitro using isolated rabbit pulmonary artery.More data for this Ligand-Target Pair
In DepthDetails Article
TargetSubstance-P receptor(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50290461(CHEMBL65468 | potassium 3,5-di(trifluoromethyl)ben...)
Affinity DataKi:  9nMAssay Description:Binding affinity of the compound for NK-1 receptor was determined in vitro using isolated rabbit vena cava.More data for this Ligand-Target Pair
In DepthDetails Article
TargetSubstance-P receptor(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50290461(CHEMBL65468 | potassium 3,5-di(trifluoromethyl)ben...)
Affinity DataKi:  9nMAssay Description:Antagonistic potency for NK-1 receptor was determined in a radioligand binding assay, using IM9 human lymphoblastoma cell line.More data for this Ligand-Target Pair
In DepthDetails Article
TargetSubstance-P receptor(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50290462(CHEMBL305119 | potassium 2N-[1-benzyl(methyl)carba...)
Affinity DataKi:  9.60nMAssay Description:Antagonistic potency for NK-2 receptor was determined in vitro, using isolated rabbit pulmonary artery.More data for this Ligand-Target Pair
In DepthDetails Article
TargetSubstance-K receptor(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50290462(CHEMBL305119 | potassium 2N-[1-benzyl(methyl)carba...)
Affinity DataKi:  2.40E+3nMAssay Description:Antagonistic potency for NK-2 receptor was determined in vitro, using isolated rabbit pulmonary artery.More data for this Ligand-Target Pair
In DepthDetails Article
TargetSubstance-K receptor(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50290461(CHEMBL65468 | potassium 3,5-di(trifluoromethyl)ben...)
Affinity DataKi:  4.20E+3nMAssay Description:Binding affinity of the compound for NK-2 receptor was determined in vitro using isolated rabbit pulmonary artery.More data for this Ligand-Target Pair
In DepthDetails Article
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Homo sapiens (Human))
Janssen Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50554026(CHEMBL4744558)
Affinity DataIC50:  0.120nMAssay Description:Inhibition of human DHODHMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Homo sapiens (Human))
Janssen Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50598905(CHEMBL5180161)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of His fused human DHODH expressed in Escherichia coli using DHO as substrate by DCIP absorbance based colorimetry assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Homo sapiens (Human))
Janssen Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50598923(CHEMBL5193821)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of His fused human DHODH expressed in Escherichia coli using DHO as substrate by DCIP absorbance based colorimetry assayMore data for this Ligand-Target Pair
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Homo sapiens (Human))
Janssen Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50598917(CHEMBL5171223)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of His fused human DHODH expressed in Escherichia coli using DHO as substrate by DCIP absorbance based colorimetry assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Homo sapiens (Human))
Janssen Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM15339(6-fluoro-2-[4-(2-fluorophenyl)phenyl]-3-methyl-qui...)
Affinity DataIC50:  0.480nMAssay Description:Inhibition of human DHODHMore data for this Ligand-Target Pair
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Homo sapiens (Human))
Janssen Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50598902(CHEMBL5187184)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of His fused human DHODH expressed in Escherichia coli using DHO as substrate by DCIP absorbance based colorimetry assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Homo sapiens (Human))
Janssen Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50598922(CHEMBL5186161)
Affinity DataIC50:  0.560nMAssay Description:Inhibition of His fused human DHODH expressed in Escherichia coli using DHO as substrate by DCIP absorbance based colorimetry assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Homo sapiens (Human))
Janssen Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50598915(CHEMBL5198030)
Affinity DataIC50:  0.600nMAssay Description:Inhibition of His fused human DHODH expressed in Escherichia coli using DHO as substrate by DCIP absorbance based colorimetry assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetMitogen-activated protein kinase kinase kinase 14(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM523659(US11136311, Compound 149)
Affinity DataIC50:  0.700nMAssay Description:NIK/MAP3K14 auto-phosphorylation activity was measured using the AlphaScreenŽ (αscreen) format (Perkin Elmer). All compounds tested were dissolv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMitogen-activated protein kinase kinase kinase 14(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM523658(US11136311, Compound 148)
Affinity DataIC50:  0.800nMAssay Description:NIK/MAP3K14 auto-phosphorylation activity was measured using the AlphaScreenŽ (αscreen) format (Perkin Elmer). All compounds tested were dissolv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMitogen-activated protein kinase kinase kinase 14(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM527664(US11186589, Compound 30)
Affinity DataIC50:  0.800nMAssay Description:NIK/MAP3K14 auto-phosphorylation activity was measured using the AlphaScreenŽ (αscreen) format (Perkin Elmer). All compounds tested were dissolv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase Mdm2(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM162123(US9051279, 106)
Affinity DataIC50:  0.800nMAssay Description:The inhibition of p53-Hdm2 and p53-Hdm4 interactions is measured by time resolved fluorescence energy transfer (TR-FRET). Fluorescence energy transfe...More data for this Ligand-Target Pair
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Homo sapiens (Human))
Janssen Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50598926(CHEMBL5206111)
Affinity DataIC50:  0.800nMAssay Description:Inhibition of His fused human DHODH expressed in Escherichia coli using DHO as substrate by DCIP absorbance based colorimetry assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetMitogen-activated protein kinase kinase kinase 14(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM523642(US11136311, Compound 132)
Affinity DataIC50:  1nMAssay Description:NIK/MAP3K14 auto-phosphorylation activity was measured using the AlphaScreenŽ (αscreen) format (Perkin Elmer). All compounds tested were dissolv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMitogen-activated protein kinase kinase kinase 14(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM527687(US11186589, Compound 3b)
Affinity DataIC50:  1nMAssay Description:NIK/MAP3K14 auto-phosphorylation activity was measured using the AlphaScreenŽ (αscreen) format (Perkin Elmer). All compounds tested were dissolv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMitogen-activated protein kinase kinase kinase 14(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM527662(US11186589, Compound 28)
Affinity DataIC50:  1.10nMAssay Description:NIK/MAP3K14 auto-phosphorylation activity was measured using the AlphaScreenŽ (αscreen) format (Perkin Elmer). All compounds tested were dissolv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMitogen-activated protein kinase kinase kinase 14(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM523713(US11136311, Compound 204)
Affinity DataIC50:  1.10nMAssay Description:NIK/MAP3K14 auto-phosphorylation activity was measured using the AlphaScreenŽ (αscreen) format (Perkin Elmer). All compounds tested were dissolv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Homo sapiens (Human))
Janssen Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50598920(CHEMBL5209113)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of His fused human DHODH expressed in Escherichia coli using DHO as substrate by DCIP absorbance based colorimetry assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Homo sapiens (Human))
Janssen Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50598913(CHEMBL5193591)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of His fused human DHODH expressed in Escherichia coli using DHO as substrate by DCIP absorbance based colorimetry assayMore data for this Ligand-Target Pair
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Homo sapiens (Human))
Janssen Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM470454(N-(2-chloro-6-fluorophenyl)-4-[4-ethyl-3-(hydroxym...)
Affinity DataIC50:  1.20nMAssay Description:Inhibition of His fused human DHODH expressed in Escherichia coli using DHO as substrate by DCIP absorbance based colorimetry assayMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase kinase kinase 14(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM523587(US11136311, Compound 76)
Affinity DataIC50:  1.20nMAssay Description:NIK/MAP3K14 auto-phosphorylation activity was measured using the AlphaScreenŽ (αscreen) format (Perkin Elmer). All compounds tested were dissolv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase Mdm2(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM162165(US9051279, 148)
Affinity DataIC50:  1.20nMAssay Description:The inhibition of p53-Hdm2 and p53-Hdm4 interactions is measured by time resolved fluorescence energy transfer (TR-FRET). Fluorescence energy transfe...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMitogen-activated protein kinase kinase kinase 14(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM527642(US11186589, Compound 13)
Affinity DataIC50:  1.30nMAssay Description:NIK/MAP3K14 auto-phosphorylation activity was measured using the AlphaScreenŽ (αscreen) format (Perkin Elmer). All compounds tested were dissolv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMitogen-activated protein kinase kinase kinase 14(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM523653(US11136311, Compound 143)
Affinity DataIC50:  1.30nMAssay Description:NIK/MAP3K14 auto-phosphorylation activity was measured using the AlphaScreenŽ (αscreen) format (Perkin Elmer). All compounds tested were dissolv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMitogen-activated protein kinase kinase kinase 14(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM523656(US11136311, Compound 146)
Affinity DataIC50:  1.30nMAssay Description:NIK/MAP3K14 auto-phosphorylation activity was measured using the AlphaScreenŽ (αscreen) format (Perkin Elmer). All compounds tested were dissolv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMitogen-activated protein kinase kinase kinase 14(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM527628(US11186589, Compound 3)
Affinity DataIC50:  1.40nMAssay Description:NIK/MAP3K14 auto-phosphorylation activity was measured using the AlphaScreenŽ (αscreen) format (Perkin Elmer). All compounds tested were dissolv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetDihydroorotate dehydrogenase (quinone), mitochondrial(Homo sapiens (Human))
Janssen Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50554025(CHEMBL4759615)
Affinity DataIC50:  1.40nMAssay Description:Inhibition of human DHODHMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetE3 ubiquitin-protein ligase Mdm2(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM162130(US9051279, 113)
Affinity DataIC50:  1.40nMAssay Description:The inhibition of p53-Hdm2 and p53-Hdm4 interactions is measured by time resolved fluorescence energy transfer (TR-FRET). Fluorescence energy transfe...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase Mdm2(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM162077(US9051279, 84)
Affinity DataIC50:  1.40nMAssay Description:The inhibition of p53-Hdm2 and p53-Hdm4 interactions is measured by time resolved fluorescence energy transfer (TR-FRET). Fluorescence energy transfe...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMitogen-activated protein kinase kinase kinase 14(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM527666(US11186589, Compound 31)
Affinity DataIC50:  1.40nMAssay Description:NIK/MAP3K14 auto-phosphorylation activity was measured using the AlphaScreenŽ (αscreen) format (Perkin Elmer). All compounds tested were dissolv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMitogen-activated protein kinase kinase kinase 14(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM527696(US11186589, Compound 12b)
Affinity DataIC50:  1.5nMAssay Description:NIK/MAP3K14 auto-phosphorylation activity was measured using the AlphaScreenŽ (αscreen) format (Perkin Elmer). All compounds tested were dissolv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMitogen-activated protein kinase kinase kinase 14(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM523569(US11136311, Compound 58)
Affinity DataIC50:  1.5nMAssay Description:NIK/MAP3K14 auto-phosphorylation activity was measured using the AlphaScreenŽ (αscreen) format (Perkin Elmer). All compounds tested were dissolv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMitogen-activated protein kinase kinase kinase 14(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM523655(US11136311, Compound 145)
Affinity DataIC50:  1.5nMAssay Description:NIK/MAP3K14 auto-phosphorylation activity was measured using the AlphaScreenŽ (αscreen) format (Perkin Elmer). All compounds tested were dissolv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMitogen-activated protein kinase kinase kinase 14(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM523606(US11136311, Compound 95)
Affinity DataIC50:  1.60nMAssay Description:NIK/MAP3K14 auto-phosphorylation activity was measured using the AlphaScreenŽ (αscreen) format (Perkin Elmer). All compounds tested were dissolv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMitogen-activated protein kinase kinase kinase 14(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM523607(US11136311, Compound 96)
Affinity DataIC50:  1.60nMAssay Description:NIK/MAP3K14 auto-phosphorylation activity was measured using the AlphaScreenŽ (αscreen) format (Perkin Elmer). All compounds tested were dissolv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMitogen-activated protein kinase kinase kinase 14(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM523633(US11136311, Compound 123)
Affinity DataIC50:  1.60nMAssay Description:NIK/MAP3K14 auto-phosphorylation activity was measured using the AlphaScreenŽ (αscreen) format (Perkin Elmer). All compounds tested were dissolv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMitogen-activated protein kinase kinase kinase 14(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM523578(US11136311, Compound 67)
Affinity DataIC50:  1.60nMAssay Description:NIK/MAP3K14 auto-phosphorylation activity was measured using the AlphaScreenŽ (αscreen) format (Perkin Elmer). All compounds tested were dissolv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetE3 ubiquitin-protein ligase Mdm2(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM162069(US9051279, 79)
Affinity DataIC50:  1.60nMAssay Description:The inhibition of p53-Hdm2 and p53-Hdm4 interactions is measured by time resolved fluorescence energy transfer (TR-FRET). Fluorescence energy transfe...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMitogen-activated protein kinase kinase kinase 14(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM527648(US11186589, Compound 16)
Affinity DataIC50:  1.60nMAssay Description:NIK/MAP3K14 auto-phosphorylation activity was measured using the AlphaScreenŽ (αscreen) format (Perkin Elmer). All compounds tested were dissolv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMitogen-activated protein kinase kinase kinase 14(Homo sapiens (Human))
Janssen Pharmaceutica

US Patent
LigandPNGBDBM527670(US11186589, Compound 48)
Affinity DataIC50:  1.60nMAssay Description:NIK/MAP3K14 auto-phosphorylation activity was measured using the AlphaScreenŽ (αscreen) format (Perkin Elmer). All compounds tested were dissolv...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
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