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Found 243 with Last Name = 'o''connell' and Initial = 'sm'
TargetLysine-specific demethylase 5B(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM264020(2-[5-[(4- cyanophenyl)methoxy]pyrazol-1- yl]pyridi...)
Affinity DataIC50:  0.600nMAssay Description:Inhibition of KDM5B (unknown origin) preincubated with enzymeMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 5B(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM263974(2-(5-(benzyloxy)-1H-pyrazol-1- yl)isonicotinic aci...)
Affinity DataIC50:  1nMAssay Description:Inhibition of KDM5B (unknown origin) preincubated with enzymeMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 5B(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM264012(2-[5-[(4-chloro-2- methoxyphenyl)methoxy]pyrazol- ...)
Affinity DataIC50:  1nMAssay Description:Inhibition of KDM5B (unknown origin) preincubated with enzymeMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 5B(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM264025(2-(4-[2-(dimethylamino)ethyl]- 5-[(4- fluorophenyl...)
Affinity DataIC50:  1nMAssay Description:Inhibition of KDM5B (unknown origin) preincubated with enzymeMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM285038(4-(5-ethylsulfonyl-2-propoxyphenyl)-2-methyl- 6-(1...)
Affinity DataIC50:  2nMAssay Description:Inhibition of BRD4-BD1 in human Raji cells assessed as downregulation of MYC gene expression by PCR methodMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 5B(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM191600(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
Affinity DataIC50:  2nMAssay Description:Inhibition of KDM5B (unknown origin) preincubated with enzymeMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50158627(CHEMBL3787482 | US10023592, Example 81)
Affinity DataIC50:  2nMAssay Description:Inhibition of BRD4-BD1 in human Raji cells assessed as downregulation of MYC gene expression by PCR methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 5B(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM263992(2-{5-[(4-bromobenzyl)oxy]-1H- pyrazol-1-yl}pyridin...)
Affinity DataIC50:  2nMAssay Description:Inhibition of KDM5B (unknown origin) preincubated with enzymeMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 5A(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM264025(2-(4-[2-(dimethylamino)ethyl]- 5-[(4- fluorophenyl...)
Affinity DataIC50:  3nMAssay Description:Inhibition of KDM5A (unknown origin) preincubated with enzymeMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 5B(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM263991(2-{5-[(4-ethylbenzyl)oxy]- 1H-pyrazol-1-yl}pyridin...)
Affinity DataIC50:  3nMAssay Description:Inhibition of KDM5B (unknown origin) preincubated with enzymeMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM285038(4-(5-ethylsulfonyl-2-propoxyphenyl)-2-methyl- 6-(1...)
Affinity DataIC50:  3nMAssay Description:Inhibition of His-tagged human BRD4-BD1 using H4K5acK8acK12acK16ac as substrate preincubated for 30 mins followed by substrate addition measured afte...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Takeda California

Curated by ChEMBL
LigandPNGBDBM50337934((R)-3-(2,3-dihydroxypropoxy)-6-fluoro-5-(2-fluoro-...)
Affinity DataIC50:  3.10nMAssay Description:Inhibition of MEK1 by IMAP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Takeda California

Curated by ChEMBL
LigandPNGBDBM50337926((R)-3-(2,3-dihydroxypropyl)-6-fluoro-5-(2-fluoro-4...)
Affinity DataIC50:  3.20nMAssay Description:Inhibition of MEK1 by IMAP assayMore data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Takeda California

Curated by ChEMBL
LigandPNGBDBM50337929((S)-3-(2,3-dihydroxypropyl)-6-fluoro-5-(2-fluoro-4...)
Affinity DataIC50:  3.20nMAssay Description:Inhibition of MEK1 by IMAP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Takeda California

Curated by ChEMBL
LigandPNGBDBM50337933(3-(1,3-dihydroxypropan-2-yl)-6-fluoro-5-(2-fluoro-...)
Affinity DataIC50:  3.30nMAssay Description:Inhibition of MEK1 by IMAP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Takeda California

Curated by ChEMBL
LigandPNGBDBM1711(CHEMBL1684067 | US8470837, 8)
Affinity DataIC50:  3.80nMAssay Description:Inhibition of MEK1 by IMAP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 5B(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM264001(2-{5-[(4-chloro-2- fluorobenzyl)oxy]-1H-pyrazol-1-...)
Affinity DataIC50:  4nMAssay Description:Inhibition of KDM5B (unknown origin) preincubated with enzymeMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 5B(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM263978(2-{5-[(4-methoxybenzyl)oxy]-1H- pyrazol-1-yl}pyrid...)
Affinity DataIC50:  4nMAssay Description:Inhibition of KDM5B (unknown origin) preincubated with enzymeMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 5B(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM50158703(CHEMBL3785832 | US10173996, Example 53 | US9604961...)
Affinity DataIC50:  4nMAssay Description:Inhibition of KDM5B (unknown origin) preincubated with enzymeMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 5B(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM263990(2-{5-[(4-methylbenzyl)oxy]-1H- pyrazol-1-yl}pyridi...)
Affinity DataIC50:  4nMAssay Description:Inhibition of KDM5B (unknown origin) preincubated with enzymeMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 5B(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM264030(2-[5-[(4-chloro-2- ethoxyphenyl)methoxy]pyrazol-1-...)
Affinity DataIC50:  4nMAssay Description:Inhibition of KDM5B (unknown origin) preincubated with enzymeMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 5B(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM263975(2-{5-[(4-fluorobenzyl)oxy]-1H- pyrazol-1-yl}pyridi...)
Affinity DataIC50:  4nMAssay Description:Inhibition of KDM5B (unknown origin) preincubated with enzymeMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 5B(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM264021(2-[5-[(4-chloro-2- phenylmethoxyphenyl)methoxy] py...)
Affinity DataIC50:  4nMAssay Description:Inhibition of KDM5B (unknown origin) preincubated with enzymeMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 5A(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM264020(2-[5-[(4- cyanophenyl)methoxy]pyrazol-1- yl]pyridi...)
Affinity DataIC50:  4nMAssay Description:Inhibition of KDM5A (unknown origin) preincubated with enzymeMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Takeda California

Curated by ChEMBL
LigandPNGBDBM50337932(5-(2-fluoro-4-iodophenylamino)-3-(2-hydroxyethyl)-...)
Affinity DataIC50:  4nMAssay Description:Inhibition of MEK1 by IMAP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Takeda California

Curated by ChEMBL
LigandPNGBDBM50337920((R)-3-(2,3-dihydroxypropyl)-5-(2-fluoro-4-iodophen...)
Affinity DataIC50:  4.60nMAssay Description:Inhibition of MEK1 by IMAP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Takeda California

Curated by ChEMBL
LigandPNGBDBM50337928((R)-3-(2,3-dihydroxypropyl)-5-(4-ethynyl-2-fluorop...)
Affinity DataIC50:  4.80nMAssay Description:Inhibition of MEK1 by IMAP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Takeda California

Curated by ChEMBL
LigandPNGBDBM50337937(5-(2-fluoro-4-iodophenylamino)-3-(3-hydroxypropyl)...)
Affinity DataIC50:  4.90nMAssay Description:Inhibition of MEK1 by IMAP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Takeda California

Curated by ChEMBL
LigandPNGBDBM1714(CHEMBL1684071 | US8470837, 13)
Affinity DataIC50:  5nMAssay Description:Inhibition of MEK1 by IMAP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM285167(2-methyl-6-(1-methylpyrazol-4-yl)-4-(5- methylsulf...)
Affinity DataIC50:  5nMAssay Description:Inhibition of His-tagged human BRD4-BD1 using H4K5acK8acK12acK16ac as substrate preincubated for 30 mins followed by substrate addition measured afte...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 4C(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM263974(2-(5-(benzyloxy)-1H-pyrazol-1- yl)isonicotinic aci...)
Affinity DataIC50:  5nMAssay Description:Inhibition of KDM4C (unknown origin) preincubated with enzymeMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50158627(CHEMBL3787482 | US10023592, Example 81)
Affinity DataIC50:  5nMAssay Description:Inhibition of His-tagged human BRD4-BD1 using H4K5acK8acK12acK16ac as substrate preincubated for 30 mins followed by substrate addition measured afte...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Takeda California

Curated by ChEMBL
LigandPNGBDBM50337924((R)-6-chloro-3-(2,3-dihydroxypropyl)-5-(2-fluoro-4...)
Affinity DataIC50:  5.90nMAssay Description:Inhibition of MEK1 by IMAP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 5A(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM263992(2-{5-[(4-bromobenzyl)oxy]-1H- pyrazol-1-yl}pyridin...)
Affinity DataIC50:  6nMAssay Description:Inhibition of KDM5A (unknown origin) preincubated with enzymeMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 5B(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM264022(2-[5-[[4-chloro-2- (cyclopropylmethoxy(phenyl] met...)
Affinity DataIC50:  6nMAssay Description:Inhibition of KDM5B (unknown origin) preincubated with enzymeMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 4C(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM321348(3-({[(1R)-6-methoxy-1,2,3,4- tetrahydronaphthalen-...)
Affinity DataIC50:  6nMAssay Description:Inhibition of KDM4C (unknown origin) using biotinylated H3K9me3 peptide and alpha-ketoglutarate as substrate pretreated for 1 hr followed by substrat...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Takeda California

Curated by ChEMBL
LigandPNGBDBM50321576(1-(4-(3-aminoazetidine-1-carbonyl)-5-(2-fluoro-4-i...)
Affinity DataIC50:  7nMAssay Description:Inhibition of MEK1 by cascade assay methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 4C(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM321334(3-{[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl- methyl...)
Affinity DataIC50:  8nMAssay Description:Inhibition of KDM4C (unknown origin) using biotinylated H3K9me3 peptide and alpha-ketoglutarate as substrate pretreated for 1 hr followed by substrat...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 5B(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM264003(2-{5-[(4-cyclopropylbenzyl)oxy]- 1H-pyrazol-1-yl}p...)
Affinity DataIC50:  8nMAssay Description:Inhibition of KDM5B (unknown origin) preincubated with enzymeMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Takeda California

Curated by ChEMBL
LigandPNGBDBM1710(CHEMBL1684064 | US8470837, 5)
Affinity DataIC50:  8.30nMAssay Description:Inhibition of MEK1 by IMAP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Takeda California

Curated by ChEMBL
LigandPNGBDBM1716(CHEMBL1684072 | US8470837, 17)
Affinity DataIC50:  8.60nMAssay Description:Inhibition of MEK1 by IMAP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Takeda California

Curated by ChEMBL
LigandPNGBDBM50380088(CHEMBL2012893)
Affinity DataIC50:  8.90nMAssay Description:Inhibition of MEK1-mediated ERK1 phosphorylation using IPTTPITTYFFFK-5FAM-COOH as substrate by fluorescent polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM285167(2-methyl-6-(1-methylpyrazol-4-yl)-4-(5- methylsulf...)
Affinity DataIC50:  9nMAssay Description:Inhibition of BRD4-BD1 in human Raji cells assessed as downregulation of MYC gene expression by PCR methodMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 4C(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM293660(3-({[(1S)-6-[methyl(phenyl)amino]-1,2,3,4-tetrahyd...)
Affinity DataIC50:  9nMAssay Description:Inhibition of KDM4C (unknown origin) using biotinylated H3K9me3 peptide and alpha-ketoglutarate as substrate pretreated for 1 hr followed by substrat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM285166(4-(2-ethoxy-5-methylsulfonylphenyl)-2- methyl-6-(1...)
Affinity DataIC50:  9nMAssay Description:Inhibition of His-tagged human BRD4-BD1 using H4K5acK8acK12acK16ac as substrate preincubated for 30 mins followed by substrate addition measured afte...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Takeda California

Curated by ChEMBL
LigandPNGBDBM1665(CHEMBL1684061 | US8470837, 2)
Affinity DataIC50:  9.80nMAssay Description:Inhibition of MEK1 by IMAP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Takeda California

Curated by ChEMBL
LigandPNGBDBM50321567((S)-5-acetyl-N-(2,3-dihydroxypropoxy)-2-(2-fluoro-...)
Affinity DataIC50:  11nMAssay Description:Inhibition of MEK1 by cascade assay methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Takeda California

Curated by ChEMBL
LigandPNGBDBM50321561(1-acetyl-4-(2-fluoro-4-iodophenylamino)-N-(2-hydro...)
Affinity DataIC50:  11nMAssay Description:Inhibition of MEK1 by cascade assay methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Takeda California

Curated by ChEMBL
LigandPNGBDBM50380087(CHEMBL2012894)
Affinity DataIC50:  11nMAssay Description:Inhibition of MEK1-mediated ERK1 phosphorylation using IPTTPITTYFFFK-5FAM-COOH as substrate by fluorescent polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysine-specific demethylase 5A(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM264012(2-[5-[(4-chloro-2- methoxyphenyl)methoxy]pyrazol- ...)
Affinity DataIC50:  12nMAssay Description:Inhibition of KDM5A (unknown origin) preincubated with enzymeMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
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