onametostat [Ligand Id: 11749] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4249337 (Jnj-64619178, JNJ-64619178, JNJ64619178, Onametostat)
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  • protein arginine methyltransferase 5 /Protein arginine N-methyltransferase 5 in Human [ChEMBL: CHEMBL1795116] [GtoPdb: 1256] [UniProtKB: O14744]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
protein arginine methyltransferase 5 /PRMT5/MEP50 complex in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3137261] [GtoPdb: 1256] [UniProtKB: O14744, Q9BQA1]
GtoPdb Equilibrium dissociation constant determined by surface plasmon resonance spectroscopy, using immobilized Avi-tagged PRMT5:MEP50 protein on streptavidin coated sensors. - 9.2 pKd <0.63 nM Kd Mol Cancer Ther (2021) 20: 2317-2328 [PMID:34583982]
ChEMBL Displacement of fluorophore-labeled RIOK1 from human PRMT5/WDR77 hetero octameric complex expressed in Sf9 cells by competition fluorescence polarization (FP) assay B 4 pIC50 >100000 nM IC50 J Med Chem (2021) 64: 11148-11168 [PMID:34342224]
ChEMBL Inhibition of full-length human N-terminal FLAG-tagged PRMT5/full length N-terminal His6-tagged MEP50 (unknown origin) expressed in baculovirus infected Sf9 insect cells assessed as reduction of S-adenosyl-L-homocysteine formation using human recombinant histone H2A (1 to 130 residues) as substrate after 1 hr in the presence of S-adenosyl-L-methionine by high throughput mass spectrometry B 9.89 pIC50 0.13 nM IC50 Bioorg Med Chem Lett (2019) 29: 1264-1269 [PMID:30956011]
protein arginine methyltransferase 5 /Protein arginine N-methyltransferase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795116] [GtoPdb: 1256] [UniProtKB: O14744]
GtoPdb Equilibrium dissociation constant determined by surface plasmon resonance spectroscopy, using immobilized Avi-tagged PRMT5:MEP50 protein on streptavidin coated sensors. - 9.2 pKd <0.63 nM Kd Mol Cancer Ther (2021) 20: 2317-2328 [PMID:34583982]
ChEMBL Inhibition of human N-terminal FLAG-tagged PRMT5 (2 to end) expressed in HEK293 cells using biotinylated H2A as substrate measured after 60 mins in presence of SAM by high throughput mass spectrometer assay B 8.2 pIC50 6.3 nM IC50 J Med Chem (2018) 61: 9429-9441 [PMID:29870258]
ChEMBL Inhibition of PRMT5 in human A549 cells assessed as reduction in sDMA production after 48 hrs by Hoechst Stain/HCS CellMask Deep Red Stain based immunohistochemistry method B 9.6 pIC50 0.25 nM IC50 Bioorg Med Chem Lett (2019) 29: 1264-1269 [PMID:30956011]
ChEMBL Inhibition of full-length human N-terminal FLAG-tagged PRMT5 expressed in Sf9 insect cells using histone H2A as peptide after 120 mins in presence of SAM by high throughput mass spectrometer assay B 9.85 pIC50 0.14 nM IC50 Bioorg Med Chem Lett (2018) 28: 3693-3699 [PMID:30366617]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]