BDBM195608 CPI-455
SMILES: CC(C)c1c([nH]c2c(cnn2c1=O)C#N)-c1ccccc1
InChI Key: InChIKey=DHXKRMSKXLDZGY-UHFFFAOYSA-N
Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kcal/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Lysine-specific demethylase 5A (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 10 | n/a | n/a | n/a | n/a | 7.0 | n/a |
Genentech Inc | Assay Description Time-resolved fluorescence resonance energy transfer (TR-FRET) assays were carried out using full-length KDM5 enzymes in 384-well black ProxiPlates (... | Nat Chem Biol 12: 531-8 (2016) Article DOI: 10.1038/nchembio.2085 BindingDB Entry DOI: 10.7270/Q2CF9NXW | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Lysine-specific demethylase 5B (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | n/a | n/a | 11 | n/a | n/a | n/a | n/a | n/a | n/a | |
TBA | Citation and Details | ||||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5B (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 3 | n/a | n/a | n/a | n/a | 7.0 | n/a |
Genentech Inc | Assay Description Time-resolved fluorescence resonance energy transfer (TR-FRET) assays were carried out using full-length KDM5 enzymes in 384-well black ProxiPlates (... | Nat Chem Biol 12: 531-8 (2016) Article DOI: 10.1038/nchembio.2085 BindingDB Entry DOI: 10.7270/Q2CF9NXW | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5C (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 14 | n/a | n/a | n/a | n/a | 7.0 | n/a |
Genentech Inc | Assay Description Time-resolved fluorescence resonance energy transfer (TR-FRET) assays were carried out using full-length KDM5 enzymes in 384-well black ProxiPlates (... | Nat Chem Biol 12: 531-8 (2016) Article DOI: 10.1038/nchembio.2085 BindingDB Entry DOI: 10.7270/Q2CF9NXW | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 2B (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | >2.50E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Inc | Assay Description TR-FRET assays similar to those described above for KDM5 enzymes were carried out with full-length KDM2B, KDM3B, KDM4C, KDM6A and KDM7B. | Nat Chem Biol 12: 531-8 (2016) Article DOI: 10.1038/nchembio.2085 BindingDB Entry DOI: 10.7270/Q2CF9NXW | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 2B (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 9.10E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Inc | Assay Description TR-FRET assays similar to those described above for KDM5 enzymes were carried out with full-length KDM2B, KDM3B, KDM4C, KDM6A and KDM7B. | Nat Chem Biol 12: 531-8 (2016) Article DOI: 10.1038/nchembio.2085 BindingDB Entry DOI: 10.7270/Q2CF9NXW | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 3B (KDM3B) (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | >2.50E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Inc | Assay Description TR-FRET assays similar to those described above for KDM5 enzymes were carried out with full-length KDM2B, KDM3B, KDM4C, KDM6A and KDM7B. | Nat Chem Biol 12: 531-8 (2016) Article DOI: 10.1038/nchembio.2085 BindingDB Entry DOI: 10.7270/Q2CF9NXW | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 3B (KDM3B) (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 1.53E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Inc | Assay Description TR-FRET assays similar to those described above for KDM5 enzymes were carried out with full-length KDM2B, KDM3B, KDM4C, KDM6A and KDM7B. | Nat Chem Biol 12: 531-8 (2016) Article DOI: 10.1038/nchembio.2085 BindingDB Entry DOI: 10.7270/Q2CF9NXW | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 4C (KDM4C) (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 2.00E+3 | n/a | n/a | n/a | n/a | 7.5 | n/a |
Genentech Inc | Assay Description High-throughput MS assays were carried out using truncated KDM4C in 384-well V-bottom polypropylene plates (Greiner, Inc.). His-tagged recombinant KD... | Nat Chem Biol 12: 531-8 (2016) Article DOI: 10.1038/nchembio.2085 BindingDB Entry DOI: 10.7270/Q2CF9NXW | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 6A (KDM6A) (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | >2.50E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Inc | Assay Description TR-FRET assays similar to those described above for KDM5 enzymes were carried out with full-length KDM2B, KDM3B, KDM4C, KDM6A and KDM7B. | Nat Chem Biol 12: 531-8 (2016) Article DOI: 10.1038/nchembio.2085 BindingDB Entry DOI: 10.7270/Q2CF9NXW | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histone lysine demethylase PHF8 (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 7.70E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Genentech Inc | Assay Description TR-FRET assays similar to those described above for KDM5 enzymes were carried out with full-length KDM2B, KDM3B, KDM4C, KDM6A and KDM7B. | Nat Chem Biol 12: 531-8 (2016) Article DOI: 10.1038/nchembio.2085 BindingDB Entry DOI: 10.7270/Q2CF9NXW | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5B (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 337 | n/a | n/a | n/a | n/a | n/a | n/a |
Kyoto Prefectural University of Medicine Curated by ChEMBL | Assay Description Inhibition of human N-terminal FLAG/His-tagged KDM5B (2 to 751 residues) expressed in baculovirus infected Sf9 insect cells using H3(1-21)K4(Me3)-GGK... | Bioorg Med Chem 27: 1119-1129 (2019) Article DOI: 10.1016/j.bmc.2019.02.006 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5C (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 3.01E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Kyoto Prefectural University of Medicine Curated by ChEMBL | Assay Description Inhibition of full-length human N-terminal FLAG/His-tagged KDM5C (2 to 1560 residues) expressed in baculovirus infected Sf9 insect cells using H3(1-2... | Bioorg Med Chem 27: 1119-1129 (2019) Article DOI: 10.1016/j.bmc.2019.02.006 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5A (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 506 | n/a | n/a | n/a | n/a | n/a | n/a |
Kyoto Prefectural University of Medicine Curated by ChEMBL | Assay Description Inhibition of human C-terminal FLAG-tagged KDM5A (1 to 1090 residues) expressed in baculovirus infected Sf9 insect cells using H3(1-21)K4(Me3)-GGK(Bi... | Bioorg Med Chem 27: 1119-1129 (2019) Article DOI: 10.1016/j.bmc.2019.02.006 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Lysine-specific demethylase 6B (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 1.43E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Kyoto Prefectural University of Medicine Curated by ChEMBL | Assay Description Inhibition of human C-terminal FLAG-tagged KDM6B (1043 to end residues) expressed in baculovirus infected Sf9 insect cells using H3(21-44)-K27(Me3)-G... | Bioorg Med Chem 27: 1119-1129 (2019) Article DOI: 10.1016/j.bmc.2019.02.006 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5A (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 20 | n/a | n/a | n/a | n/a | n/a | n/a |
Constellation Pharmaceuticals, Inc. Curated by ChEMBL | Assay Description Inhibition of KDM5A (unknown origin) using ART(Kme3)QTARKSTGGKAPRKQLA-NovaTagPEG-biotin/20 uM 2-OG as substrate/co-factor by TR-FRET assay | Bioorg Med Chem Lett 26: 4350-4 (2016) Article DOI: 10.1016/j.bmcl.2016.07.026 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Lysine-specific demethylase 5B (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 3 | n/a | n/a | n/a | n/a | n/a | n/a |
Constellation Pharmaceuticals, Inc. Curated by ChEMBL | Assay Description Inhibition of KDM5B (unknown origin) using ART(Kme3)QTARKSTGGKAPRKQLA-NovaTagPEG-biotin/2-OG as substrate/co-factor by TR-FRET assay | Bioorg Med Chem Lett 26: 4350-4 (2016) Article DOI: 10.1016/j.bmcl.2016.07.026 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 4C (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 2.00E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Constellation Pharmaceuticals, Inc. Curated by ChEMBL | Assay Description Inhibition of KDM4C (unknown origin) using ARTKQTAR(KMe3)STGGKAPRKQLA-NovaTagPEG-biotin/2-OG as substrate/co-factor by TR-FRET assay | Bioorg Med Chem Lett 26: 4350-4 (2016) Article DOI: 10.1016/j.bmcl.2016.07.026 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 7A/7B (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 7.70E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Constellation Pharmaceuticals, Inc. Curated by ChEMBL | Assay Description Inhibition of KDM7B (unknown origin) ARTKQTAR(KMe1)STGGKAPRKQLA-NovaTagPEG-biotin/2-OG as substrate/co-factor by TR-FRET assay | Bioorg Med Chem Lett 26: 4350-4 (2016) Article DOI: 10.1016/j.bmcl.2016.07.026 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 3B (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | >1.53E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Constellation Pharmaceuticals, Inc. Curated by ChEMBL | Assay Description Inhibition of KDM3B (unknown origin) using ARTKQTAR(KMe1)STGGKAPRKQLA -NovaTagPEG-biotin/2-OG as substrate/co-factor by TR-FRET assay | Bioorg Med Chem Lett 26: 4350-4 (2016) Article DOI: 10.1016/j.bmcl.2016.07.026 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 2B (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | >9.10E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Constellation Pharmaceuticals, Inc. Curated by ChEMBL | Assay Description Inhibition of KDM2B (unknown origin) using RKSAPATGGV(KMe2)KPHRYRPGTV-NovaTagPEG-biotin/2-OG as substrate/co-factor by TR-FRET assay | Bioorg Med Chem Lett 26: 4350-4 (2016) Article DOI: 10.1016/j.bmcl.2016.07.026 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5C (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 14 | n/a | n/a | n/a | n/a | n/a | n/a |
Constellation Pharmaceuticals, Inc. Curated by ChEMBL | Assay Description Inhibition of KDM5C (unknown origin) using ART(Kme3)QTARKSTGGKAPRKQLA-NovaTagPEG-biotin/2-OG as substrate/co-factor by TR-FRET assay | Bioorg Med Chem Lett 26: 4350-4 (2016) Article DOI: 10.1016/j.bmcl.2016.07.026 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5A (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 10 | n/a | n/a | n/a | n/a | n/a | n/a |
Constellation Pharmaceuticals, Inc. Curated by ChEMBL | Assay Description Inhibition of KDM5A (unknown origin) using ART(Kme3)QTARKSTGGKAPRKQLA-NovaTagPEG-biotin/1 uM 2-OG as substrate/co-factor by TR-FRET assay | Bioorg Med Chem Lett 26: 4350-4 (2016) Article DOI: 10.1016/j.bmcl.2016.07.026 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Lysine-specific demethylase 7A/7B (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 7.70E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Constellation Pharmaceuticals, Inc. Curated by ChEMBL | Assay Description Inhibition of KDM7B (unknown origin) ARTKQTAR(KMe1)STGGKAPRKQLA-NovaTagPEG-biotin/2-OG as substrate/co-factor by TR-FRET assay | Bioorg Med Chem Lett 26: 4350-4 (2016) Article DOI: 10.1016/j.bmcl.2016.07.026 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 3B (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | >1.53E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Constellation Pharmaceuticals, Inc. Curated by ChEMBL | Assay Description Inhibition of KDM3B (unknown origin) using ARTKQTAR(KMe1)STGGKAPRKQLA -NovaTagPEG-biotin/2-OG as substrate/co-factor by TR-FRET assay | Bioorg Med Chem Lett 26: 4350-4 (2016) Article DOI: 10.1016/j.bmcl.2016.07.026 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 2B (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | >9.10E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Constellation Pharmaceuticals, Inc. Curated by ChEMBL | Assay Description Inhibition of KDM2B (unknown origin) using RKSAPATGGV(KMe2)KPHRYRPGTV-NovaTagPEG-biotin/2-OG as substrate/co-factor by TR-FRET assay | Bioorg Med Chem Lett 26: 4350-4 (2016) Article DOI: 10.1016/j.bmcl.2016.07.026 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5A (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 10 | n/a | n/a | n/a | n/a | n/a | n/a |
Constellation Pharmaceuticals, Inc. Curated by ChEMBL | Assay Description Inhibition of KDM5A (unknown origin) using ART(Kme3)QTARKSTGGKAPRKQLA-NovaTagPEG-biotin/1 uM 2-OG as substrate/co-factor by TR-FRET assay | Bioorg Med Chem Lett 26: 4350-4 (2016) Article DOI: 10.1016/j.bmcl.2016.07.026 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Lysine-specific demethylase 4C (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 2.00E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Constellation Pharmaceuticals, Inc. Curated by ChEMBL | Assay Description Inhibition of KDM4C (unknown origin) using ARTKQTAR(KMe3)STGGKAPRKQLA-NovaTagPEG-biotin/2-OG as substrate/co-factor by TR-FRET assay | Bioorg Med Chem Lett 26: 4350-4 (2016) Article DOI: 10.1016/j.bmcl.2016.07.026 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5C (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 14 | n/a | n/a | n/a | n/a | n/a | n/a |
Constellation Pharmaceuticals, Inc. Curated by ChEMBL | Assay Description Inhibition of KDM5C (unknown origin) using ART(Kme3)QTARKSTGGKAPRKQLA-NovaTagPEG-biotin/2-OG as substrate/co-factor by TR-FRET assay | Bioorg Med Chem Lett 26: 4350-4 (2016) Article DOI: 10.1016/j.bmcl.2016.07.026 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5B (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 3 | n/a | n/a | n/a | n/a | n/a | n/a |
Constellation Pharmaceuticals, Inc. Curated by ChEMBL | Assay Description Inhibition of KDM5B (unknown origin) using ART(Kme3)QTARKSTGGKAPRKQLA-NovaTagPEG-biotin/2-OG as substrate/co-factor by TR-FRET assay | Bioorg Med Chem Lett 26: 4350-4 (2016) Article DOI: 10.1016/j.bmcl.2016.07.026 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5A (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | n/a | n/a | 5.20E+3 | n/a | n/a | n/a | n/a |
Constellation Pharmaceuticals, Inc. Curated by ChEMBL | Assay Description Inhibition of KDM5A in human PC9 cells assessed as increase in H3K4me3 levels preincubated for 4 days measured up to 24 hrs by ELISA | Bioorg Med Chem Lett 26: 4350-4 (2016) Article DOI: 10.1016/j.bmcl.2016.07.026 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Lysine-specific demethylase 5A (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 20 | n/a | n/a | n/a | n/a | n/a | n/a |
Constellation Pharmaceuticals, Inc. Curated by ChEMBL | Assay Description Inhibition of KDM5A (unknown origin) using ART(Kme3)QTARKSTGGKAPRKQLA-NovaTagPEG-biotin/20 uM 2-OG as substrate/co-factor by TR-FRET assay | Bioorg Med Chem Lett 26: 4350-4 (2016) Article DOI: 10.1016/j.bmcl.2016.07.026 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Lysine-specific demethylase 5A (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | n/a | n/a | 5.20E+3 | n/a | n/a | n/a | n/a |
Constellation Pharmaceuticals, Inc. Curated by ChEMBL | Assay Description Inhibition of KDM5A in human PC9 cells assessed as increase in H3K4me3 levels preincubated for 4 days measured up to 24 hrs by ELISA | Bioorg Med Chem Lett 26: 4350-4 (2016) Article DOI: 10.1016/j.bmcl.2016.07.026 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Lysine-specific demethylase 5B (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PubMed | n/a | n/a | 10 | n/a | n/a | n/a | n/a | n/a | n/a |
Zhengzhou University Curated by ChEMBL | Assay Description Inhibition of KDM5B (unknown origin) | Eur J Med Chem 161: 131-140 (2019) | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5A (Homo sapiens (Human)) | BDBM195608 (CPI-455) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 20 | n/a | n/a | n/a | n/a | 7.0 | n/a |
Genentech Inc | Assay Description Time-resolved fluorescence resonance energy transfer (TR-FRET) assays were carried out using full-length KDM5 enzymes in 384-well black ProxiPlates (... | Nat Chem Biol 12: 531-8 (2016) Article DOI: 10.1038/nchembio.2085 BindingDB Entry DOI: 10.7270/Q2CF9NXW | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) |