pemrametostat [Ligand Id: 13679] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4466233 (EPZ-015938, EPZ015938, Gsk 3326595, Gsk-3326595, Gsk3326595, GSK3326595, GSK-3326595A, Pemrametostat)
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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 - - 7.33 pIC50 46.9 nM IC50 J Med Chem (2025) 68: 108-134 [PMID:39722476]
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]
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 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]