null
SMILES CC(C)c1cc([nH]n1)C(=O)N1CC[C@H](C1)NC(=O)C1CC1
InChI Key InChIKey=CXEXTVGTDZRKJS-LLVKDONJSA-N
PDB links: 3 PDB IDs match this monomer.
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 20 hits for monomerid = 281089
TargetLysine-specific demethylase 5A(Homo sapiens (Human))
GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS INC.
US Patent
GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS INC.
US Patent
Affinity DataIC50: 0.0490nMpH: 7.0 T: 2°CAssay Description:Full length KDM5A enzyme was expressed and purified inhouse. Biotin-H3K4me3 peptide was purchased from New England Biolabs. HTRF reagents (containing...More data for this Ligand-Target Pair
3D Structure (crystal)In DepthDetails
TargetLysine-specific demethylase 5A(Homo sapiens (Human))
GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS INC.
US Patent
GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS INC.
US Patent
Affinity DataIC50: 570nMAssay Description:Inhibition of recombinant human C-terminal FLAG-tagged KDM5A (1 to 1090 residues) expressed in baculovirus infected sf9 cells using biotinylated H3K4...More data for this Ligand-Target Pair
TargetLysine-specific demethylase 5A(Homo sapiens (Human))
GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS INC.
US Patent
GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS INC.
US Patent
Affinity DataIC50: 2.20E+4nMAssay Description:Inhibition of ARID/PHD1 domain truncated human N-terminal His-SUMO-tagged KDM5A (1 to 588 residues) expressed in Escherichia coli using H3K4me3 as su...More data for this Ligand-Target Pair
TargetLysine-specific demethylase 5A(Homo sapiens (Human))
GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS INC.
US Patent
GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS INC.
US Patent
Affinity DataIC50: 2.40E+3nMAssay Description:Binding affinity at [3H]QNB radiolabeled muscarinic M2 receptor in rat heart.More data for this Ligand-Target Pair
TargetLysine-specific demethylase 5A(Homo sapiens (Human))
GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS INC.
US Patent
GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS INC.
US Patent
Affinity DataIC50: 500nMAssay Description:Inhibition of ARID/PHD1 domain truncated human N-terminal His-SUMO-tagged KDM5A (1 to 588 residues) expressed in Escherichia coli using H3K4me3 as su...More data for this Ligand-Target Pair
TargetLysine-specific demethylase 5A(Homo sapiens (Human))
GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS INC.
US Patent
GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS INC.
US Patent
Affinity DataIC50: 45nMAssay Description:Inhibition of KDM5A in human PC9 cells assessed as increase in H3K4me3 level after 5 days by mass-spectrometric methodMore data for this Ligand-Target Pair
TargetLysine-specific histone demethylase 1A(Homo sapiens (Human))
Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: liang.jun@gene.com.
Curated by ChEMBL
Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: liang.jun@gene.com.
Curated by ChEMBL
Affinity DataIC50: 2.50E+4nMAssay Description:Inhibition of KDM1A (unknown origin)More data for this Ligand-Target Pair
TargetLysine-specific demethylase 3B(Homo sapiens (Human))
Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: liang.jun@gene.com.
Curated by ChEMBL
Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: liang.jun@gene.com.
Curated by ChEMBL
Affinity DataIC50: 2.50E+4nMAssay Description:Inhibition of recombinant human N-terminal FLAG-tagged KDM3B expressed in baculovirus infected Sf9 insect cells using H3K9me1 peptide as substrate af...More data for this Ligand-Target Pair
TargetLysine-specific demethylase 4C(Homo sapiens (Human))
Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: liang.jun@gene.com.
Curated by ChEMBL
Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: liang.jun@gene.com.
Curated by ChEMBL
Affinity DataIC50: 4.10E+3nMAssay Description:Inhibition of recombinant human N-terminal FLAG-tagged KDM4C expressed in baculovirus infected Sf9 insect cells using H3K9me3 peptide as substrate af...More data for this Ligand-Target Pair
TargetLysine-specific demethylase 6A(Homo sapiens (Human))
Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: liang.jun@gene.com.
Curated by ChEMBL
Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: liang.jun@gene.com.
Curated by ChEMBL
Affinity DataIC50: 2.50E+4nMAssay Description:Inhibition of recombinant human N-terminal FLAG-tagged KDM6A expressed in baculovirus infected Sf9 insect cells using H3K27me3 peptide as substrate a...More data for this Ligand-Target Pair
TargetHistone lysine demethylase PHF8(Homo sapiens (Human))
Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: liang.jun@gene.com.
Curated by ChEMBL
Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: liang.jun@gene.com.
Curated by ChEMBL
Affinity DataIC50: 2.50E+4nMAssay Description:Inhibition of recombinant human N-terminal FLAG-tagged KDM7B expressed in baculovirus infected Sf9 insect cells using H3K9me1 peptide as substrate af...More data for this Ligand-Target Pair
TargetLysine-specific demethylase 5B(Homo sapiens (Human))
Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: liang.jun@gene.com.
Curated by ChEMBL
Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: liang.jun@gene.com.
Curated by ChEMBL
Affinity DataIC50: 56nMAssay Description:Inhibition of recombinant human N-terminal FLAG-tagged KDM5B expressed in baculovirus infected Sf9 insect cells using H3K4me3 peptide as substrate af...More data for this Ligand-Target Pair
Affinity DataIC50: 55nMAssay Description:Inhibition of recombinant human N-terminal FLAG-tagged KDM5C expressed in baculovirus infected Sf9 insect cells using H3K4me3 peptide as substrate af...More data for this Ligand-Target Pair
TargetLysine-specific demethylase 2B(Homo sapiens (Human))
Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: liang.jun@gene.com.
Curated by ChEMBL
Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: liang.jun@gene.com.
Curated by ChEMBL
Affinity DataIC50: 2.50E+4nMAssay Description:Inhibition of recombinant human N-terminal FLAG-tagged KDM2B expressed in baculovirus infected Sf9 insect cells using H3K36me2 peptide as substrate a...More data for this Ligand-Target Pair
TargetLysine-specific demethylase 5A(Homo sapiens (Human))
GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS INC.
US Patent
GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS INC.
US Patent
Affinity DataEC50: 960nMAssay Description:Inhibition of KDM5A in human PC9 cells assessed as increase in H3K4me3 level after 5 days by mass-spectrometric methodMore data for this Ligand-Target Pair
TargetLysine-specific demethylase 5B(Homo sapiens (Human))
Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: liang.jun@gene.com.
Curated by ChEMBL
Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: liang.jun@gene.com.
Curated by ChEMBL
TargetLysine-specific demethylase 5A(Homo sapiens (Human))
GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS INC.
US Patent
GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS INC.
US Patent
TargetLysine-specific demethylase 5B(Homo sapiens (Human))
Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: liang.jun@gene.com.
Curated by ChEMBL
Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: liang.jun@gene.com.
Curated by ChEMBL
TargetLysine-specific demethylase 5A(Homo sapiens (Human))
GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS INC.
US Patent
GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS INC.
US Patent
Affinity DataKd: 2.40E+3nMAssay Description:Binding affinity to ARID/PHD1/Zn binding domain truncated human N-terminal His-SUMO-tagged KDM5A (1 to 588 residues) expressed in Escherichia coli by...More data for this Ligand-Target Pair