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 |
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Histone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12/Zinc finger protein AEBP2 (365/366 > 99%)† (Homo sapiens (Human)) | BDBM225230 (EED226 | US11013745, Compound EED226) | PDB UniProtKB/SwissProt antibodypedia 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 |
Novartis Institutes for BioMedical Research | Assay Description All HMT reactions were performed as described previously [Nasveschuk et al., ACS Med. Chem. Lett., 5:378-383]. | Nat Chem Biol 13: 381-388 (2017) Article DOI: 10.1038/nchembio.2304 BindingDB Entry DOI: 10.7270/Q2S75F64 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Histone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12/Zinc finger protein AEBP2 (365/366 > 99%)† (Homo sapiens (Human)) | BDBM225230 (EED226 | US11013745, Compound EED226) | PDB UniProtKB/SwissProt antibodypedia antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 23.4 | n/a | n/a | n/a | n/a | 8.0 | n/a |
Novartis Institutes for BioMedical Research | Assay Description To assess the compounds potency in the H3K27me0 peptide (2144)-based PRC2 enzymatic assay, compounds were serially diluted three-fold in DMSO t... | Nat Chem Biol 13: 381-388 (2017) Article DOI: 10.1038/nchembio.2304 BindingDB Entry DOI: 10.7270/Q2S75F64 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Histone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH1/Polycomb protein EED/Polycomb protein SUZ12/Zinc finger protein AEBP2 (365/366 > 99%)† (Homo sapiens (Human)) | BDBM225230 (EED226 | US11013745, Compound EED226) | PDB Reactome pathway KEGG UniProtKB/SwissProt DrugBank antibodypedia antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 50 | n/a | n/a | n/a | n/a | n/a | n/a |
Novartis Institutes for BioMedical Research | Assay Description All HMT reactions were performed as described previously [Nasveschuk et al., ACS Med. Chem. Lett., 5:378-383]. | Nat Chem Biol 13: 381-388 (2017) Article DOI: 10.1038/nchembio.2304 BindingDB Entry DOI: 10.7270/Q2S75F64 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Histone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12/Zinc finger protein AEBP2 (365/366 > 99%)† (Homo sapiens (Human)) | BDBM225230 (EED226 | US11013745, Compound EED226) | PDB UniProtKB/SwissProt antibodypedia antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 53.5 | n/a | n/a | n/a | n/a | 8.0 | n/a |
Novartis Institutes for BioMedical Research | Assay Description To assess the compounds potency in the H3K27me0 peptide (2144)-based PRC2 enzymatic assay, compounds were serially diluted three-fold in DMSO t... | Nat Chem Biol 13: 381-388 (2017) Article DOI: 10.1038/nchembio.2304 BindingDB Entry DOI: 10.7270/Q2S75F64 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Polycomb protein EED (365/366 > 99%)† (Homo sapiens (Human)) | BDBM225230 (EED226 | US11013745, Compound EED226) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 220 | n/a | n/a | n/a | n/a | n/a | n/a |
Novartis Institutes for BioMedical Research Curated by ChEMBL | Assay Description Agonist activity was determined against hPR (human progesterone receptor) compared to that of progesterone (100%) | J Med Chem 60: 2215-2226 (2017) Article DOI: 10.1021/acs.jmedchem.6b01576 BindingDB Entry DOI: 10.7270/Q20G3NDT | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Polycomb protein EED (365/366 > 99%)† (Homo sapiens (Human)) | BDBM225230 (EED226 | US11013745, Compound EED226) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 220 | n/a | n/a | n/a | n/a | n/a | n/a |
Novartis Institutes for BioMedical Research Curated by ChEMBL | Assay Description Inhibition of EED in human G401 cells assessed as reduction in global H3K27me3 level after 48 hrs by ELISA | J Med Chem 60: 2215-2226 (2017) Article DOI: 10.1021/acs.jmedchem.6b01576 BindingDB Entry DOI: 10.7270/Q20G3NDT | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Polycomb protein EED (365/366 > 99%)† (Homo sapiens (Human)) | BDBM225230 (EED226 | US11013745, Compound EED226) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | n/a | 82 | n/a | n/a | n/a | 8.0 | 1,390.75 |
Novartis Institutes for BioMedical Research | Assay Description ITC experiments were performed by Auto ITC200 (Microcal) at 25 °C. ITC sample cell was filled with 10 μM PRC2 in titration buffer (25 mM HEPES p... | Nat Chem Biol 13: 381-388 (2017) Article DOI: 10.1038/nchembio.2304 BindingDB Entry DOI: 10.7270/Q2S75F64 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Histone-lysine N-methyltransferase EZH2/Polycomb protein EED [40-441]/Polycomb protein SUZ12 [559-739] (365/366 > 99%)† (Homo sapiens (Human)) | BDBM225230 (EED226 | US11013745, Compound EED226) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | n/a | 114 | n/a | n/a | n/a | 8.0 | 1,390.75 |
Novartis Institutes for BioMedical Research | Assay Description ITC experiments were performed by Auto ITC200 (Microcal) at 25 °C. ITC sample cell was filled with 10 μM PRC2 in titration buffer (25 mM HEPES p... | Nat Chem Biol 13: 381-388 (2017) Article DOI: 10.1038/nchembio.2304 BindingDB Entry DOI: 10.7270/Q2S75F64 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Polycomb protein EED (365/366 > 99%)† (Homo sapiens (Human)) | BDBM225230 (EED226 | US11013745, Compound EED226) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | n/a | 82 | n/a | n/a | n/a | n/a | n/a |
University of Connecticut Curated by ChEMBL | Assay Description Binding affinity to EED (unknown origin) by ITC method | Eur J Med Chem 136: 14-35 (2017) Article DOI: 10.1016/j.ejmech.2017.04.047 BindingDB Entry DOI: 10.7270/Q2F76G3G | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) |