BDBM190179 EPZ005030::US10273223, Compound A-2::US9175331, 4::US9637472, Compound A-2
SMILES: CC(C)n1ncc2c(cc(nc12)-c1ccc(CN2CCOCC2)cc1)C(=O)NCc1c(C)cc(C)[nH]c1=O
InChI Key: InChIKey=WGDUEUOSWFHQIH-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 |
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human)) | BDBM190179 (EPZ005030 | US10273223, Compound A-2 | US9175331, ...) | PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem Similars | 180 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a | |
TBA | Citation and Details | ||||||||||||
More data for this Ligand-Target Pair | |||||||||||||
EZH2(Y641F) (Homo sapiens (Human)) | BDBM190179 (EPZ005030 | US10273223, Compound A-2 | US9175331, ...) | PDB MMDB KEGG B.MOAD DrugBank GoogleScholar AffyNet | PC cid PC sid UniChem Similars | US Patent | n/a | n/a | 185 | n/a | n/a | n/a | n/a | n/a | n/a |
Epizyme, Inc. US Patent | Assay Description Test compounds were serially diluted 3-fold in DMSO in a 10 point-curve and 1 uL was spotted into a 384-well microplate in duplicate using a Platemat... | US Patent US9175331 (2015) BindingDB Entry DOI: 10.7270/Q2ZW1JQP | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histone-lysine N-methyltransferase EZH2 (A677G) (Homo sapiens (Human)) | BDBM190179 (EPZ005030 | US10273223, Compound A-2 | US9175331, ...) | PDB GoogleScholar AffyNet | PC cid PC sid UniChem Similars | US Patent | n/a | n/a | 41.8 | n/a | n/a | n/a | n/a | n/a | n/a |
Epizyme, Inc. US Patent | Assay Description Test compounds were serially diluted 3-fold in DMSO in a 10 point-curve and 1 uL was spotted into a 384-well microplate in duplicate using a Platemat... | US Patent US9175331 (2015) BindingDB Entry DOI: 10.7270/Q2ZW1JQP | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histone-lysine N-methyltransferase EZH2 (A687V) (Homo sapiens (Human)) | BDBM190179 (EPZ005030 | US10273223, Compound A-2 | US9175331, ...) | PDB GoogleScholar AffyNet | PC cid PC sid UniChem Similars | US Patent | n/a | n/a | 50.4 | n/a | n/a | n/a | n/a | n/a | n/a |
Epizyme, Inc. US Patent | Assay Description Test compounds were serially diluted 3-fold in DMSO in a 10 point-curve and 1 uL was spotted into a 384-well microplate in duplicate using a Platemat... | US Patent US9175331 (2015) BindingDB Entry DOI: 10.7270/Q2ZW1JQP | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human)) | BDBM190179 (EPZ005030 | US10273223, Compound A-2 | US9175331, ...) | PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem Similars | PubMed | n/a | n/a | >3.00E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Epizyme Curated by ChEMBL | Assay Description Inhibition of methyltransferase activity of EZH2 in human lymphoma cells assessed as H3K27 methylation | J Med Chem 59: 1556-64 (2016) BindingDB Entry DOI: 10.7270/Q2B56MM7 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human)) | BDBM190179 (EPZ005030 | US10273223, Compound A-2 | US9175331, ...) | PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem Similars | PubMed | n/a | n/a | 400 | n/a | n/a | n/a | n/a | n/a | n/a |
Epizyme Curated by ChEMBL | Assay Description Inhibition of methyltransferase activity of human EZH2 using chicken oligonucleotide as substrate by pull down assay | J Med Chem 59: 1556-64 (2016) BindingDB Entry DOI: 10.7270/Q2B56MM7 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human)) | BDBM190179 (EPZ005030 | US10273223, Compound A-2 | US9175331, ...) | PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem Similars | US Patent | n/a | n/a | 650 | n/a | n/a | n/a | n/a | n/a | n/a |
Epizyme, Inc. US Patent | Assay Description Recombinant PRC2 Enzymes. Human PRC2 enzymes were purified as 4-component enzyme complexes co-expressed in Spodoptera frugiperda (sf9) cells using a ... | US Patent US9637472 (2017) BindingDB Entry DOI: 10.7270/Q2X0693B | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human)) | BDBM190179 (EPZ005030 | US10273223, Compound A-2 | US9175331, ...) | PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem Similars | US Patent | n/a | n/a | 650 | n/a | n/a | n/a | n/a | n/a | n/a |
IRBM/Merck | Assay Description eneral Procedure for Wild-Type PRC2 Enzyme Assay on Oligonucleosome Substrate. The assays was performed in a buffer consisting of 20 mM bicine (pH=7.... | J Med Chem 51: 2350-3 (2008) BindingDB Entry DOI: 10.7270/Q28P62V9 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human)) | BDBM190179 (EPZ005030 | US10273223, Compound A-2 | US9175331, ...) | PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem Similars | US Patent | n/a | n/a | 260 | n/a | n/a | n/a | n/a | n/a | n/a |
Epizyme, Inc. US Patent | Assay Description Test compounds were serially diluted 3-fold in DMSO in a 10 point-curve and 1 uL was spotted into a 384-well microplate in duplicate using a Platemat... | US Patent US9175331 (2015) BindingDB Entry DOI: 10.7270/Q2ZW1JQP | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histone-lysine N-methyltransferase EZH2 (Homo sapiens (Human)) | BDBM190179 (EPZ005030 | US10273223, Compound A-2 | US9175331, ...) | PDB KEGG UniProtKB/SwissProt B.MOAD antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem Similars | PubMed | n/a | n/a | n/a | n/a | 1.05E+4 | n/a | n/a | n/a | n/a |
Epizyme Curated by ChEMBL | Assay Description Inhibition of methyltransferase activity of EZH2 in human G401 cells assessed as H3K27 trimethylation after 4 hrs by ELISA | J Med Chem 59: 1556-64 (2016) BindingDB Entry DOI: 10.7270/Q2B56MM7 | |||||||||||
More data for this Ligand-Target Pair |