BDBM195612 GSK467
SMILES: O=c1[nH]c(Oc2cnn(Cc3ccccc3)c2)nc2cnccc12
InChI Key: InChIKey=ZTYRLXUTLYBVHH-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 (KDM5A) (Homo sapiens (Human)) | BDBM195612 (GSK467) | PDB GoogleScholar AffyNet | Purchase PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 24 | 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 (Homo sapiens (Human)) | BDBM195612 (GSK467) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid PDB UniChem | PubMed | n/a | n/a | 3.98E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline R&D Curated by ChEMBL | Assay Description Inhibition of human KDM5C transfected in U2OS cells assessed as inhibition of H3K9Me3 demethylation for 24 hrs | J Med Chem 59: 1370-87 (2016) BindingDB Entry DOI: 10.7270/Q26D5VV2 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5C (KDM5C) (Homo sapiens (Human)) | BDBM195612 (GSK467) | PDB GoogleScholar AffyNet | Purchase PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 65 | 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 5D (KDM5D) (Homo sapiens (Human)) | BDBM195612 (GSK467) | PDB GoogleScholar AffyNet | Purchase PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 77 | 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)) | BDBM195612 (GSK467) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 5.10E+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 3A (Homo sapiens (Human)) | BDBM195612 (GSK467) | Reactome pathway KEGG UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid PDB UniChem | Article PubMed | n/a | n/a | 3.39E+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)) | BDBM195612 (GSK467) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid PDB UniChem | PubMed | n/a | n/a | 501 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline R&D Curated by ChEMBL | Assay Description Inhibition of N-terminal his-tagged human KDM4C expressed in Escherichia coli BL21(DE3) using trimethylated peptide substrate by RFMS assay | J Med Chem 59: 1370-87 (2016) BindingDB Entry DOI: 10.7270/Q26D5VV2 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histone Lysine Demethylase (Homo sapiens (Human)) | BDBM195612 (GSK467) | PDB MMDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid PDB UniChem | PubMed | n/a | n/a | 501 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline R&D Curated by ChEMBL | Assay Description Inhibition of KDM4E (unknown origin) by RFMS assay | J Med Chem 59: 1370-87 (2016) BindingDB Entry DOI: 10.7270/Q26D5VV2 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Prolyl hydroxylase EGLN3 (Homo sapiens (Human)) | BDBM195612 (GSK467) | Reactome pathway KEGG UniProtKB/SwissProt DrugBank antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid PDB UniChem | PubMed | n/a | n/a | <1.00E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline R&D Curated by ChEMBL | Assay Description Inhibition of full-length EGLN3 (unknown origin) expressed in Escherichia coli BL21(DE3) cells by HTRF assay | J Med Chem 59: 1370-87 (2016) BindingDB Entry DOI: 10.7270/Q26D5VV2 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5C (Homo sapiens (Human)) | BDBM195612 (GSK467) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid PDB UniChem | PubMed | n/a | n/a | 63 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline R&D Curated by ChEMBL | Assay Description Inhibition of KDM5C catalytic domain (1 -764 aa) (unknown origin) expressed in Sf9 cells using H3K4Me3 peptide as substrate by RFMS assay | J Med Chem 59: 1370-87 (2016) BindingDB Entry DOI: 10.7270/Q26D5VV2 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 4D (Homo sapiens (Human)) | BDBM195612 (GSK467) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase PC cid PC sid PDB UniChem | PubMed | n/a | n/a | 398 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline R&D Curated by ChEMBL | Assay Description Inhibition of KDM4D (unknown origin) by RFMS assay | J Med Chem 59: 1370-87 (2016) BindingDB Entry DOI: 10.7270/Q26D5VV2 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 6B (Homo sapiens (Human)) | BDBM195612 (GSK467) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid PDB UniChem | PubMed | n/a | n/a | <1.00E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline R&D Curated by ChEMBL | Assay Description Inhibition of KDM6B (unknown origin) by RFMS assay | J Med Chem 59: 1370-87 (2016) BindingDB Entry DOI: 10.7270/Q26D5VV2 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 4A (KDM4A) (Homo sapiens (Human)) | BDBM195612 (GSK467) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid PDB UniChem | PubMed | n/a | n/a | 631 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline R&D Curated by ChEMBL | Assay Description Inhibition of KDM4A (unknown origin) by RFMS assay | J Med Chem 59: 1370-87 (2016) BindingDB Entry DOI: 10.7270/Q26D5VV2 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 4C (Homo sapiens (Human)) | BDBM195612 (GSK467) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid PDB UniChem | PubMed | n/a | n/a | 5.01E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline R&D Curated by ChEMBL | Assay Description Inhibition of N-terminal his-tagged full-length human KDM4C transfected in U2OS cells assessed as inhibition of H3K9Me3 demethylation for 24 hrs | J Med Chem 59: 1370-87 (2016) BindingDB Entry DOI: 10.7270/Q26D5VV2 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 4C (Homo sapiens (Human)) | BDBM195612 (GSK467) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid PDB UniChem | PubMed | n/a | n/a | 2.00E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline R&D Curated by ChEMBL | Assay Description Inhibition of N-terminal his-tagged full-length human KDM4C transfected in U2OS cells assessed as inhibition of H3K9Me3 demethylation for 24 hrs | J Med Chem 59: 1370-87 (2016) BindingDB Entry DOI: 10.7270/Q26D5VV2 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5C (Homo sapiens (Human)) | BDBM195612 (GSK467) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid PDB UniChem | PubMed | n/a | n/a | 2.50E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline R&D Curated by ChEMBL | Assay Description Inhibition of human KDM5C transfected in U2OS cells assessed as inhibition of H3K9Me3 demethylation for 24 hrs | J Med Chem 59: 1370-87 (2016) BindingDB Entry DOI: 10.7270/Q26D5VV2 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Lysine-specific demethylase 5B (Homo sapiens (Human)) | BDBM195612 (GSK467) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 26 | 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) |