Found 11 hits Enz. Inhib. hit(s) with Target = 'Lysine-specific demethylase 5A' and Ligand = 'BDBM195608' Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kJ/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)Show InChI InChI=1S/C16H14N4O/c1-10(2)13-14(11-6-4-3-5-7-11)19-15-12(8-17)9-18-20(15)16(13)21/h3-7,9-10,19H,1-2H3 | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar AffyNet
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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 5A
(Homo sapiens (Human)) | BDBM195608
(CPI-455)Show InChI InChI=1S/C16H14N4O/c1-10(2)13-14(11-6-4-3-5-7-11)19-15-12(8-17)9-18-20(15)16(13)21/h3-7,9-10,19H,1-2H3 | 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 BindingDB Entry DOI: 10.7270/Q2MW2MNW |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Lysine-specific demethylase 5A
(Homo sapiens (Human)) | BDBM195608
(CPI-455)Show InChI InChI=1S/C16H14N4O/c1-10(2)13-14(11-6-4-3-5-7-11)19-15-12(8-17)9-18-20(15)16(13)21/h3-7,9-10,19H,1-2H3 | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar AffyNet
| Purchase
MCE PC cid PC sid PDB UniChem
| PDB
| n/a | n/a | 10 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
|
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Lysine-specific demethylase 5A
(Homo sapiens (Human)) | BDBM195608
(CPI-455)Show InChI InChI=1S/C16H14N4O/c1-10(2)13-14(11-6-4-3-5-7-11)19-15-12(8-17)9-18-20(15)16(13)21/h3-7,9-10,19H,1-2H3 | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar AffyNet
| Purchase
MCE PC cid PC sid PDB UniChem
| PDB
| n/a | n/a | 10 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
|
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Lysine-specific demethylase 5A
(Homo sapiens (Human)) | BDBM195608
(CPI-455)Show InChI InChI=1S/C16H14N4O/c1-10(2)13-14(11-6-4-3-5-7-11)19-15-12(8-17)9-18-20(15)16(13)21/h3-7,9-10,19H,1-2H3 | 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 BindingDB Entry DOI: 10.7270/Q2MW2MNW |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Lysine-specific demethylase 5A
(Homo sapiens (Human)) | BDBM195608
(CPI-455)Show InChI InChI=1S/C16H14N4O/c1-10(2)13-14(11-6-4-3-5-7-11)19-15-12(8-17)9-18-20(15)16(13)21/h3-7,9-10,19H,1-2H3 | 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 BindingDB Entry DOI: 10.7270/Q2MW2MNW |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Lysine-specific demethylase 5A
(Homo sapiens (Human)) | BDBM195608
(CPI-455)Show InChI InChI=1S/C16H14N4O/c1-10(2)13-14(11-6-4-3-5-7-11)19-15-12(8-17)9-18-20(15)16(13)21/h3-7,9-10,19H,1-2H3 | 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 BindingDB Entry DOI: 10.7270/Q2MW2MNW |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Lysine-specific demethylase 5A
(Homo sapiens (Human)) | BDBM195608
(CPI-455)Show InChI InChI=1S/C16H14N4O/c1-10(2)13-14(11-6-4-3-5-7-11)19-15-12(8-17)9-18-20(15)16(13)21/h3-7,9-10,19H,1-2H3 | 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) |
Lysine-specific demethylase 5A
(Homo sapiens (Human)) | BDBM195608
(CPI-455)Show InChI InChI=1S/C16H14N4O/c1-10(2)13-14(11-6-4-3-5-7-11)19-15-12(8-17)9-18-20(15)16(13)21/h3-7,9-10,19H,1-2H3 | 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 BindingDB Entry DOI: 10.7270/Q2668HPR |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Lysine-specific demethylase 5A
(Homo sapiens (Human)) | BDBM195608
(CPI-455)Show InChI InChI=1S/C16H14N4O/c1-10(2)13-14(11-6-4-3-5-7-11)19-15-12(8-17)9-18-20(15)16(13)21/h3-7,9-10,19H,1-2H3 | 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 BindingDB Entry DOI: 10.7270/Q2MW2MNW |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Lysine-specific demethylase 5A
(Homo sapiens (Human)) | BDBM195608
(CPI-455)Show InChI InChI=1S/C16H14N4O/c1-10(2)13-14(11-6-4-3-5-7-11)19-15-12(8-17)9-18-20(15)16(13)21/h3-7,9-10,19H,1-2H3 | 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 BindingDB Entry DOI: 10.7270/Q2MW2MNW |
More data for this Ligand-Target Pair | 3D Structure (crystal) |