ChEMBL ligand: CHEMBL4249337 (Jnj-64619178, JNJ-64619178, JNJ64619178, Onametostat)
protein arginine methyltransferase 5 /PRMT5/MEP50 complex in Human [ChEMBL: CHEMBL3137261] [GtoPdb: 1256] [UniProtKB: O14744, Q9BQA1] There should be some charts here, you may need to enable JavaScript!
protein arginine methyltransferase 5 /Protein arginine N-methyltransferase 5 in Human [ChEMBL: CHEMBL1795116] [GtoPdb: 1256] [UniProtKB: O14744] There should be some charts here, you may need to enable JavaScript!

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	Binding affinity to Full-length human PRMT5/human MEP50 assessed as equilibrium dissociation constant by SPR analysis	B	9.2	pKd	<0.63	nM	Kd	J Med Chem (2023) 66: 8407-8427 [PMID:37366223]
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 (unknown origin)	B	9.11	pIC50	0.77	nM	IC50	Eur J Med Chem (2022) 244: 114842-114842 [PMID:36274274]
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]