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 6B (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 16 | n/a | n/a | n/a | n/a | n/a | n/a |
Kyoto Prefectural University of Medicine Curated by ChEMBL | Assay Description Inhibition of C-terminal FLAG-tagged human KDM6B expressed in expressed in Sf9 cells pre-incubated for 4 hrs before substrate addition and measured a... | Bioorg Med Chem Lett 29: 1173-1176 (2019) Article DOI: 10.1016/j.bmcl.2019.03.028 BindingDB Entry DOI: 10.7270/Q2H70K7V | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Lysine-specific demethylase 6B (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 63 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Oxford Curated by ChEMBL | Assay Description Inhibition of KDM6B (unknown origin) | Medchemcomm 5: 1879-1886 (2014) Article DOI: 10.1039/C4MD00291A BindingDB Entry DOI: 10.7270/Q2KH0RBN | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Lysine-specific demethylase 6B (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 150 | n/a | n/a | n/a | n/a | n/a | n/a |
Chinese Academy of Sciences Curated by ChEMBL | Assay Description Inhibition of JMJD3 (unknown origin) using biotinylated H3K27me3 peptide as substrate after 1 hr by AlphaLISA assay | Bioorg Med Chem Lett 26: 721-5 (2016) Article DOI: 10.1016/j.bmcl.2016.01.006 BindingDB Entry DOI: 10.7270/Q2P55QC2 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Lysine-specific demethylase 6B (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 160 | n/a | n/a | n/a | n/a | 7.5 | n/a |
University of Oxford | Assay Description The demethylase AlphaScreen assay was performed in 384-well plate format using white proxiplates (PerkinElmer), and transfer of compound (100 nl) was... | Nat Chem Biol 12: 539-45 (2016) Article DOI: 10.1038/nchembio.2087 BindingDB Entry DOI: 10.7270/Q27P8X6K | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Lysine-specific demethylase 5B (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 210 | 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 | 3D Structure (crystal) | ||||||||||||
Lysine-specific demethylase 5B (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 550 | n/a | n/a | n/a | n/a | 7.5 | n/a |
University of Oxford | Assay Description The demethylase AlphaScreen assay was performed in 384-well plate format using white proxiplates (PerkinElmer), and transfer of compound (100 nl) was... | Nat Chem Biol 12: 539-45 (2016) Article DOI: 10.1038/nchembio.2087 BindingDB Entry DOI: 10.7270/Q27P8X6K | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Lysine-specific demethylase 5C (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | 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 | 1.20E+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 5D [1-775] (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 1.50E+3 | n/a | n/a | n/a | n/a | 7.5 | n/a |
University of Oxford | Assay Description The demethylase AlphaScreen assay was performed in 384-well plate format using white proxiplates (PerkinElmer), and transfer of compound (100 nl) was... | Nat Chem Biol 12: 539-45 (2016) Article DOI: 10.1038/nchembio.2087 BindingDB Entry DOI: 10.7270/Q27P8X6K | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5C [1-765] (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 1.50E+3 | n/a | n/a | n/a | n/a | 7.5 | n/a |
University of Oxford | Assay Description The demethylase AlphaScreen assay was performed in 384-well plate format using white proxiplates (PerkinElmer), and transfer of compound (100 nl) was... | Nat Chem Biol 12: 539-45 (2016) Article DOI: 10.1038/nchembio.2087 BindingDB Entry DOI: 10.7270/Q27P8X6K | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5A (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | 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 | 2.90E+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 | 3D Structure (crystal) | ||||||||||||
Lysine-specific demethylase 6A (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 3.20E+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 | 3D Structure (crystal) | ||||||||||||
Lysine-specific demethylase 5A [1-801] (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 3.90E+3 | n/a | n/a | n/a | n/a | 7.5 | n/a |
University of Oxford | Assay Description The demethylase AlphaScreen assay was performed in 384-well plate format using white proxiplates (PerkinElmer), and transfer of compound (100 nl) was... | Nat Chem Biol 12: 539-45 (2016) Article DOI: 10.1038/nchembio.2087 BindingDB Entry DOI: 10.7270/Q27P8X6K | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Lysine-specific demethylase 4C [1-350] (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 1.33E+4 | 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 | |||||||||||||
Prolyl 4-hydroxylase (Paramecium bursaria Chlorella virus 1) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/TrEMBL B.MOAD DrugBank GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 1.59E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Oxford Curated by ChEMBL | Assay Description Inhibition of N-terminal His6-tagged recombinant Paramecium bursaria chlorella virus 1 CPH expressed in Escherichia coli Rosetta 2 (DE3) cells pre-in... | Bioorg Med Chem 27: 2405-2412 (2019) Article DOI: 10.1016/j.bmc.2019.01.018 BindingDB Entry DOI: 10.7270/Q2KK9G4R | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 4E (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | PDB MMDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 2.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Oxford Curated by ChEMBL | Assay Description Inhibition of KDM4E (unknown origin) | Medchemcomm 5: 1879-1886 (2014) Article DOI: 10.1039/C4MD00291A BindingDB Entry DOI: 10.7270/Q2KH0RBN | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 2B (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | 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 | |||||||||||||
Histone lysine demethylase PHF8 (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | 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 | |||||||||||||
Lysine-specific demethylase 3B (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | 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 3A (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | Reactome pathway KEGG UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 3.98E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Oxford Curated by ChEMBL | Assay Description Inhibition of KDM3A (unknown origin) | Medchemcomm 5: 1879-1886 (2014) Article DOI: 10.1039/C4MD00291A BindingDB Entry DOI: 10.7270/Q2KH0RBN | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 3A (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | Reactome pathway KEGG UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 4.60E+4 | n/a | n/a | n/a | n/a | 7.5 | n/a |
University of Oxford | Assay Description The demethylase AlphaScreen assay was performed in 384-well plate format using white proxiplates (PerkinElmer), and transfer of compound (100 nl) was... | Nat Chem Biol 12: 539-45 (2016) Article DOI: 10.1038/nchembio.2087 BindingDB Entry DOI: 10.7270/Q27P8X6K | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 4C (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 6.49E+4 | n/a | n/a | n/a | n/a | 7.5 | n/a |
University of Oxford | Assay Description The demethylase AlphaScreen assay was performed in 384-well plate format using white proxiplates (PerkinElmer), and transfer of compound (100 nl) was... | Nat Chem Biol 12: 539-45 (2016) Article DOI: 10.1038/nchembio.2087 BindingDB Entry DOI: 10.7270/Q27P8X6K | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 6A (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 6.90E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
The University of Texas M.D. Anderson Cancer Center Curated by ChEMBL | Assay Description Inhibition of KDM6A (880 to 1401 residues) (unknown origin) using H3 ( 21 to 44 residues) K27me3 as substrate preincubated for 15 min followed by sub... | J Med Chem 61: 10588-10601 (2018) Article DOI: 10.1021/acs.jmedchem.8b01219 BindingDB Entry DOI: 10.7270/Q2R49TGF | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Lysine-specific demethylase 5A (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | 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 | 1.10E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
The University of Texas M.D. Anderson Cancer Center Curated by ChEMBL | Assay Description Inhibition of KDM5A ARID/PhD1 domain deletion mutant (1 to 739 residues) (unknown origin) using H3 ( 1 to 24 residues) K4me3 as substrate preincubate... | J Med Chem 61: 10588-10601 (2018) Article DOI: 10.1021/acs.jmedchem.8b01219 BindingDB Entry DOI: 10.7270/Q2R49TGF | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Lysine-specific demethylase 4A (Homo sapiens (Human)) | BDBM60875 (3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 4.00E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
The University of Texas M.D. Anderson Cancer Center Curated by ChEMBL | Assay Description Inhibition of KDM4A (1 to 350 residues) (unknown origin) using H3 ( 1 to 15 residues) K9me3 as substrate preincubated for 15 min followed by substrat... | J Med Chem 61: 10588-10601 (2018) Article DOI: 10.1021/acs.jmedchem.8b01219 BindingDB Entry DOI: 10.7270/Q2R49TGF | |||||||||||
More data for this Ligand-Target Pair |