ChEMBL ligand: CHEMBL4466233 (EPZ-015938, EPZ015938, Gsk 3326595, Gsk-3326595, Gsk3326595, GSK3326595, GSK-3326595A, Pemrametostat)
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]
ChEMBL	Uncompetitive inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using [3H]SAM as substrate assessed as apparent inhibition constant incubated for 30 mins by Cheng-Prusoff plot analysis	B	7.37	pKi	43	nM	Ki	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Competitive inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using [3H]SAM as substrate assessed as apparent inhibition constant incubated for 30 mins by Cheng-Prusoff plot analysis	B	7.59	pKi	26	nM	Ki	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using FUBP1 as substrate assessed as apparent inhibition constant preincubated for 60 mins followed by substrate addition and measured after 30 mins by Cheng-Prusoff plot analysis	B	8	pKi	9.9	nM	Ki	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using HNRNPH1 as substrate assessed as apparent inhibition constant preincubated for 60 mins followed by substrate addition and measured after 30 mins by Cheng-Prusoff plot analysis	B	8.02	pKi	9.5	nM	Ki	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using H4 as substrate assessed as apparent inhibition constant preincubated for 60 mins followed by substrate addition and measured after 30 mins by Cheng-Prusoff plot analysis	B	8.51	pKi	3.1	nM	Ki	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using [3H]SAM as substrate assessed as apparent inhibition constant preincubated for 60 mins followed by substrate addition and measured after 30 mins by Cheng-Prusoff plot analysis	B	8.51	pKi	3.1	nM	Ki	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using H2A as substrate assessed as apparent inhibition constant preincubated for 60 mins followed by substrate addition and measured after 30 mins by Cheng-Prusoff plot analysis	B	8.52	pKi	3	nM	Ki	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using Sm3d as substrate assessed as apparent inhibition constant preincubated for 60 mins followed by substrate addition and measured after 30 mins by Cheng-Prusoff plot analysis	B	8.52	pKi	3	nM	Ki	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	PRMT5 Biochemical Assay : 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. Compounds in 100% DMSO (1 ul) were spotted into a polypropylene 384-well V-bottom plates (Greiner) using a Platemate Plus outfitted with a 384-channel head (Thermo Scientific). DMSO (1 ul) was added to Columns 11, 12, 23, 24, rows A-H for the maximum signal control and 1 ul of SAH, a known product and inhibitor of PRMT5/MEP50, was added to columns 11, 12, 23, 24, rows I-P for the minimum signal control. A cocktail (40 ul) containing the PRMT5/MEP50 enzyme and the peptide was added by Multidrop Combi (Thermo-Fisher). The compounds were allowed to incubate with PRMT5/MEP50 for 30 min at 25 degrees Celsius, then a cocktail (10 ul) containing 3H-SAM was added to initiate the reaction (final volume=51 ul). The final concentrations of the components were as follows: PRMT5/MEP50 was 4 nM, 3H-SAM was 75 nM, peptide was 40 nM, SAH in the minimum signal control wells was 100 uM, and the DMSO concentration was 1%. The assays were stopped by the addition of non-radioactive SAM (10 ul) to a final concentration of 600 uM, which dilutes the 3H-SAM to a level where its incorporation into the peptide substrate is no longer detectable. 50 ul of the reaction in the 384-well polypropylene plate was then transferred to a 384-well Flashplate and the biotinylated peptides were allowed to bind to the streptavidin surface for at least 1 hour before being washed three times with 0.1% Tween20 in a Biotek ELx405 plate washer. The plates were then read in a PerkinElmer TopCount plate reader to measure the quantity of 3H-labeled peptide bound to the Flashplate surface, measured as disintegrations per minute (dpm) or alternatively, referred to as counts per minute (cpm).	B	7	pIC50	<100	nM	IC50	US-10307413-B2. Tetrahydro- and dihydro-isoquinoline PRMT5 inhibitors and uses thereof (2019)
ChEMBL	PRMT5/MEP50 Enzyme Assays on Peptide Substrates: 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. Compounds in 100% DMSO (1 ul) were spotted into a polypropylene 384-well V-bottom plates (Greiner) using a Platemate Plus outfitted with a 384-channel head (Thermo Scientific). DMSO (1 ul) was added to Columns 11, 12, 23, 24, rows A-H for the maximum signal control and 1 ul of SAH, a known product and inhibitor of PRMT5/MEP50, was added to columns 11, 12, 23, 24, rows I-P for the minimum signal control. A cocktail (40 ul) containing the PRMT5/MEP50 enzyme and the peptide was added by Multidrop Combi (Thermo-Fisher). The compounds were allowed to incubate with PRMT5/MEP50 for 30 min at 25 degrees Celsius, then a cocktail (10 ul) containing 3H-SAM was added to initiate the reaction (final volume=51 ul). The final concentrations of the components were as follows: PRMT5/MEP50 was 4 nM, 3H-SAM was 75 nM, peptide was 40 nM, SAH in the minimum signal control wells was 100 uM, and the DMSO concentration was 1%. The assays were stopped by the addition of non-radioactive SAM (10 ul) to a final concentration of 600 uM, which dilutes the 3H-SAM to a level where its incorporation into the peptide substrate is no longer detectable. 50 ul of the reaction in the 384-well polypropylene plate was then transferred to a 384-well Flashplate and the biotinylated peptides were allowed to bind to the streptavidin surface for at least 1 hour before being washed three times with 0.1% Tween20 in a Biotek ELx405 μlate washer. The plates were then read in a PerkinElmer TopCount plate reader to measure the quantity of 3H-labeled peptide bound to the Flashplate surface, measured as disintegrations per minute (dpm) or alternatively, referred to as counts per minute (cpm).	B	7	pIC50	<100	nM	IC50	US-10980794-B2. PRMT5 inhibitors and uses thereof (2021)
ChEMBL	Enzyme Assay: 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. Compounds in 100% DMSO (1 ul) were spotted into a polypropylene 384-well V-bottom plates (Greiner) using a Platemate Plus outfitted with a 384-channel head (Thermo Scientific). DMSO (1 ul) was added to Columns 11, 12, 23, 24, rows A-H for the maximum signal control and 1 ul of SAH, a known product and inhibitor of PRMT5/MEP50, was added to columns 11, 12, 23, 24, rows I-P for the minimum signal control. A cocktail (40 ul) containing the PRMT5/MEP50 enzyme and the peptide was added by Multidrop Combi (Thermo-Fisher). The compounds were allowed to incubate with PRMT5/MEP50 for 30 min at 25 degrees Celsius, then a cocktail (10 ul) containing 3H-SAM was added to initiate the reaction (final volume=51 ul). The final concentrations of the components were as follows: PRMT5/MEP50 was 4 nM, 3H-SAM was 75 nM, peptide was 40 nM, SAH in the minimum signal control wells was 100 uM, and the DMSO concentration was 1%. The assays were stopped by the addition of non-radioactive SAM (10 ul) to a final concentration of 600 uM, which dilutes the 3H-SAM to a level where its incorporation into the peptide substrate is no longer detectable. 50 ul of the reaction in the 384-well polypropylene plate was then transferred to a 384-well Flashplate and the biotinylated peptides were allowed to bind to the streptavidin surface for at least 1 hour before being washed three times with 0.1% Tween20 in a Biotek ELx405 plate washer.	B	7	pIC50	<100	nM	IC50	US-10391089-B2. PRMT5 inhibitors and uses therof (2019)
GtoPdb	-	-	7.33	pIC50	46.9	nM	IC50	J Med Chem (2025) 68: 108-134 [PMID:39722476]
ChEMBL	AlphaLISA Enzyme Inhibitory Assay: 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 MgCl2, 50 mM NaCl with 0.01% Tween20 and 1 mM DTT added right before the assay. 2.5 μL of compound solution in the assay buffer with 4% DMSO and 5 μL of PRMT5/MRP50 complex/SAM mixture solution in the assay buffer which was pre-incubated for 30 minutes were added into a white low volume 384 well microtiter plate. This mixture solution was incubated for 15 minutes with gentle shaking at room temperature. Methyl transfer reaction was initiated by adding 2.5 μL of Biotin-H4 (1-21) peptide substrate solution in the assay buffer. Final concentrations of PRMT5/MEP50, SAM, Biotin-H4 peptide substrate, and DMSO were 25 nM, 10 μM, 30 nM, and 1%, respectively. The reaction was allowed to perform for 120 minutes in dark with gentle shaking at room temperature after which 5 μL of Anti-H4R3-Me AlphaLISA acceptor beads in detection buffer from the manufacturer was added into the reaction mixture followed by incubation for 60 minutes. 10 μL of Streptavidin labeled AlphaLISA donor beads in detection buffer was added into the mixture followed by 30 minute incubation. Final acceptor and donor beads concentrations were 10 μg/mL. Plates were read on an Envision multimode plate reader from PerkinElmer (Waltham Mass., USA) with an excitation wavelength of 680 nm and emission wavelength of 615 nm. IC50 values of inhibitors were obtained by fitting the fluorescence intensity vs inhibitor concentrations in a sigmoidal dose-response curve (variable slopes, four parameters) using Prism 7.	B	7.42	pIC50	38	nM	IC50	US-11591326-B2. Inhibitors of protein arginine methyltransferase 5 (PRMT5), pharmaceutical products thereof, and methods thereof (2023)
ChEMBL	Inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using FUBP1 as substrate preincubated for 60 mins followed by substrate addition and measured after 30 mins by Cheng-Prusoff plot analysis	B	7.71	pIC50	19.7	nM	IC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using HNRNPH1 as substrate preincubated for 60 mins followed by substrate addition and measured after 30 mins by Cheng-Prusoff plot analysis	B	7.72	pIC50	18.9	nM	IC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of PRMT5 (unknown origin)/MEP50 (unknown origin) using histone H4 as substrate preincubated for 60 mins in presence of enzyme and SAM	B	8.21	pIC50	6.2	nM	IC50	Bioorg Med Chem Lett (2018) 28: 3693-3699 [PMID:30366617]
ChEMBL	Inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using H4 as substrate preincubated for 60 mins followed by substrate addition and measured after 30 mins by Cheng-Prusoff plot analysis	B	8.21	pIC50	6.2	nM	IC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using [3H]SAM as substrate preincubated for 60 mins followed by substrate addition and measured after 30 mins by Cheng-Prusoff plot analysis	B	8.21	pIC50	6.2	nM	IC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using H2A as substrate preincubated for 60 mins followed by substrate addition and measured after 30 mins by Cheng-Prusoff plot analysis	B	8.22	pIC50	6	nM	IC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using Sm3d as substrate preincubated for 60 mins followed by substrate addition and measured after 30 mins by Cheng-Prusoff plot analysis	B	8.23	pIC50	5.9	nM	IC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
protein arginine methyltransferase 5 /Protein arginine N-methyltransferase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795116] [GtoPdb: 1256] [UniProtKB: O14744]
GtoPdb	-	-	7.33	pIC50	46.9	nM	IC50	J Med Chem (2025) 68: 108-134 [PMID:39722476]
ChEMBL	Inhibition of PRMT5 methyltransferase activity in human HCT-116 cells expressing wild type MTAP assessed as inhibition of PRMT5- mediated SDMA modification level incubated for 96 hrs by Western blot analysis	B	7.92	pIC50	12	nM	IC50	J Med Chem (2022) 65: 1749-1766 [PMID:35041419]
ChEMBL	Inhibition of PRMT5 methyltransferase activity in MTAP knockout human HCT-116 cells assessed as inhibition of PRMT5- mediated SDMA modification level incubated for 96 hrs by Western blot analysis	B	7.96	pIC50	11	nM	IC50	J Med Chem (2022) 65: 1749-1766 [PMID:35041419]
ChEMBL	Inhibition of PRMT5 (unknown origin)	B	8.21	pIC50	6.2	nM	IC50	Bioorg Med Chem Lett (2018) 28: 3693-3699 [PMID:30366617]
ChEMBL	Inhibition of PRMT5 in human Z138 cells assessed as effect on GADD45A expression incubated for 2 to 4 days by Western blot analysis	B	6.49	pEC50	323	nM	EC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of PRMT5 in human Z138 cells assessed as effect on EGR2 expression incubated for 2 to 4 days by Western blot analysis	B	6.67	pEC50	214	nM	EC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of PRMT5 in human Z138 cells assessed as effect on TRIM22 expression incubated for 2 to 4 days by Western blot analysis	B	6.67	pEC50	212	nM	EC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of PRMT5 in human Z138 cells assessed as effect on PHLDA3 expression incubated for 2 to 4 days by Western blot analysis	B	6.75	pEC50	177	nM	EC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of PRMT5 in human Z138 cells assessed as effect on MDM2 expression incubated for 2 to 4 days by Western blot analysis	B	6.78	pEC50	167	nM	EC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of PRMT5 in human Z138 cells assessed as effect on CDKN1 expression incubated for 2 to 4 days by Western blot analysis	B	7.26	pEC50	55	nM	EC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of PRMT5 in human Z138 cells assessed as effect on BAX expression incubated for 2 to 4 days by Western blot analysis	B	7.3	pEC50	50	nM	EC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of PRMT5 in human Z138 cells assessed as effect on SESN1 expression incubated for 2 to 4 days by Western blot analysis	B	7.66	pEC50	22	nM	EC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of PRMT5 in human Z138 cells assessed as effect on SDMA level incubated for 3 days by ELISA analysis	B	8.6	pEC50	2.5	nM	EC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of PRMT5 in human ZR-75-1 cells assessed as decrease in SDMA level incubated for 3 days	B	8.7	pEC50	2	nM	EC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of PRMT5 in human U-2940 cells assessed as decrease in SDMA level incubated for 3 days	B	8.7	pEC50	2	nM	EC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of PRMT5 in human REC1 cells assessed as decrease in SDMA level incubated for 3 days	B	8.7	pEC50	2	nM	EC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of PRMT5 in human BJAB cells assessed as decrease in SDMA level incubated for 3 days	B	8.7	pEC50	2	nM	EC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of PRMT5 in human MINO cells assessed as decrease in SDMA level incubated for 3 days	B	8.7	pEC50	2	nM	EC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of PRMT5 in human MAVER-1 cells assessed as decrease in SDMA level incubated for 3 days	B	8.7	pEC50	2	nM	EC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of PRMT5 in human MCF7 cells assessed as decrease in SDMA level incubated for 3 days	B	8.7	pEC50	2	nM	EC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]
ChEMBL	Inhibition of PRMT5 in human MDA-MB-468 cells assessed as decrease in SDMA level incubated for 3 days	B	8.7	pEC50	2	nM	EC50	Sci Rep (2018) 8: 9711-9711 [PMID:29946150]

ChEMBL data shown on this page come from version 36:

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]