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 |
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Methylosome protein 50/Protein arginine N-methyltransferase 5 (Homo sapiens (Human)) | BDBM177922 (US10307413, Compound 337 | US10391089, Compound 16...) | PDB UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 22 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Inhibition of human full length FLAG-tagged PRMT5/human His6-tagged MEP50 expressed in baculovirus-infected Sf9 cells assessed as reduction in tritiu... | Citation and Details Article DOI: 10.1021/acsmedchemlett.5b00380 BindingDB Entry DOI: 10.7270/Q2SQ941H | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Methylosome protein 50/Protein arginine N-methyltransferase 5 (Homo sapiens (Human)) | BDBM177922 (US10307413, Compound 337 | US10391089, Compound 16...) | PDB UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 22 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Jinan Curated by ChEMBL | Assay Description Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 i... | Bioorg Med Chem Lett 28: 1476-1483 (2018) Article DOI: 10.1016/j.bmcl.2018.03.087 BindingDB Entry DOI: 10.7270/Q2CN76D3 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Methylosome protein 50/Protein arginine N-methyltransferase 5 (Homo sapiens (Human)) | BDBM177922 (US10307413, Compound 337 | US10391089, Compound 16...) | PDB UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 22 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Jinan Curated by ChEMBL | Assay Description Inhibition of human recombinant PRMT5/MEP50 expressed in 293-F cells using histone 4 peptide as substrate after 90 mins in presence of [3H]SAM by aut... | Bioorg Med Chem Lett 28: 3693-3699 (2018) Article DOI: 10.1016/j.bmcl.2018.10.026 BindingDB Entry DOI: 10.7270/Q2SB490F | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Methylosome protein 50/Protein arginine N-methyltransferase 5 (Homo sapiens (Human)) | BDBM177922 (US10307413, Compound 337 | US10391089, Compound 16...) | PDB UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 30 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Inhibition of human PRMT5/MEP50 assessed as reduction in methyltransferase activity using histone 4 peptide as substrate in presence of [3H]SAM incub... | Citation and Details Article DOI: 10.1021/acs.jmedchem.0c01111 BindingDB Entry DOI: 10.7270/Q2765K17 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Methylosome protein 50/Protein arginine N-methyltransferase 5 (Homo sapiens (Human)) | BDBM177922 (US10307413, Compound 337 | US10391089, Compound 16...) | PDB UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 47 | n/a | n/a | n/a | n/a | n/a | n/a |
Shanghai Institute of Materia Medica Curated by ChEMBL | Assay Description Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (2 to end residues)/human N-terminal His-tagged MEP50 (2 to end residues) expressed in H... | Eur J Med Chem 164: 317-333 (2019) Article DOI: 10.1016/j.ejmech.2018.12.065 BindingDB Entry DOI: 10.7270/Q2RR22Q1 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Methylosome protein 50/Protein arginine N-methyltransferase 5 (Homo sapiens (Human)) | BDBM177922 (US10307413, Compound 337 | US10391089, Compound 16...) | PDB UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 47 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Jinan Curated by ChEMBL | Assay Description Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (2 to end residues) /human N-terminal His-tagged MEP50 (2 to end residues) expressed in ... | Bioorg Med Chem Lett 28: 3693-3699 (2018) Article DOI: 10.1016/j.bmcl.2018.10.026 BindingDB Entry DOI: 10.7270/Q2SB490F | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Methylosome protein 50/Protein arginine N-methyltransferase 5 (Homo sapiens (Human)) | BDBM177922 (US10307413, Compound 337 | US10391089, Compound 16...) | PDB UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | 47 | n/a | n/a | n/a | n/a | n/a | n/a |
Shanghai Institute of Materia Medica Curated by ChEMBL | Assay Description Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (2 to end residues)/human N-terminal His-tagged MEP50 (2 to end residues) expressed in H... | Eur J Med Chem 164: 317-333 (2019) Article DOI: 10.1016/j.ejmech.2018.12.065 BindingDB Entry DOI: 10.7270/Q2RR22Q1 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Methylosome protein 50/Protein arginine N-methyltransferase 5 (Homo sapiens (Human)) | BDBM177922 (US10307413, Compound 337 | US10391089, Compound 16...) | PDB UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB US Patent | n/a | n/a | 85 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description General Procedure for PRMT5/MEP50 AlphaLISA Enzyme Inhibitory Assays: Assays were performed in the buffer consisting of 50 mM Tris, pH 8.5, 5 mM MgCl... | Citation and Details BindingDB Entry DOI: 10.7270/Q28K7F1F | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Methylosome protein 50/Protein arginine N-methyltransferase 5 (Homo sapiens (Human)) | BDBM177922 (US10307413, Compound 337 | US10391089, Compound 16...) | PDB UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB US Patent | n/a | n/a | <100 | n/a | n/a | n/a | n/a | n/a | n/a |
Epizyme, Inc. US Patent | Assay Description The assays were all performed in a buffer consisting of 20 mM Bicine (pH=7.6), 1 mM TCEP, 0.005% BSG, and 0.002% Tween20, prepared on the day of use.... | US Patent US10391089 (2019) BindingDB Entry DOI: 10.7270/Q2RN3B7D | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Methylosome protein 50/Protein arginine N-methyltransferase 5 (Homo sapiens (Human)) | BDBM177922 (US10307413, Compound 337 | US10391089, Compound 16...) | PDB UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid PDB UniChem | PDB Article PubMed | n/a | n/a | >1.00E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Displacement of fluorophore-labeled RIOK1 from human PRMT5/WDR77 hetero octameric complex expressed in Sf9 cells by competition fluorescence polariza... | Citation and Details Article DOI: 10.1021/acs.jmedchem.1c00507 BindingDB Entry DOI: 10.7270/Q26977DH | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) |