PRMT5 inhibitor D3 [Ligand Id: 13678] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL5398215
  • coactivator associated arginine methyltransferase 1/Histone-arginine methyltransferase CARM1 in Human [ChEMBL: CHEMBL5406] [GtoPdb: 1255] [UniProtKB: Q86X55]
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  • protein arginine methyltransferase 1 /Protein arginine N-methyltransferase 1 in Human [ChEMBL: CHEMBL5524] [GtoPdb: 1252] [UniProtKB: Q99873]
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  • protein arginine methyltransferase 3/Protein arginine N-methyltransferase 3 in Human [ChEMBL: CHEMBL5891] [GtoPdb: 1254] [UniProtKB: O60678]
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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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  • protein arginine methyltransferase 6/Protein arginine N-methyltransferase 6 in Human [ChEMBL: CHEMBL1275221] [GtoPdb: 1257] [UniProtKB: Q96LA8]
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  • protein arginine methyltransferase 7 /Protein arginine N-methyltransferase 7 in Human [ChEMBL: CHEMBL3562175] [GtoPdb: 1258] [UniProtKB: Q9NVM4]
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  • protein arginine methyltransferase 8/Protein arginine N-methyltransferase 8 in Human [ChEMBL: CHEMBL3108648] [GtoPdb: 1259] [UniProtKB: Q9NR22]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
coactivator associated arginine methyltransferase 1/Histone-arginine methyltransferase CARM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5406] [GtoPdb: 1255] [UniProtKB: Q86X55]
ChEMBL Inhibition of PRMT4 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2025) 68: 108-134 [PMID:39722476]
protein arginine methyltransferase 5 /PRMT5/MEP50 complex in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3137261] [GtoPdb: 1256] [UniProtKB: O14744Q9BQA1]
ChEMBL Binding affinity to PRMT5/MEP50 (unknown origin) assessed as dissociation constant by SPR analysis B 6.98 pKd 104 nM Kd J Med Chem (2025) 68: 108-134 [PMID:39722476]
GtoPdb - - 7.68 pIC50 20.7 nM IC50 J Med Chem (2025) 68: 108-134 [PMID:39722476]
ChEMBL Inhibition of recombinant N-terminal FLAG-tagged human full-length PRMT5/full length human MEP50 extracted from baculovirus expression system using [3H]-SAM as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by multimode plate reader analysis B 7.68 pIC50 20.7 nM IC50 J Med Chem (2025) 68: 108-134 [PMID:39722476]
protein arginine methyltransferase 1 /Protein arginine N-methyltransferase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5524] [GtoPdb: 1252] [UniProtKB: Q99873]
ChEMBL Inhibition of PRMT1 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2025) 68: 108-134 [PMID:39722476]
protein arginine methyltransferase 3/Protein arginine N-methyltransferase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5891] [GtoPdb: 1254] [UniProtKB: O60678]
ChEMBL Inhibition of PRMT3 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2025) 68: 108-134 [PMID:39722476]
protein arginine methyltransferase 5 /Protein arginine N-methyltransferase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795116] [GtoPdb: 1256] [UniProtKB: O14744]
ChEMBL Inhibition of PRMT5 (unknown origin) using H4(1-21)S1ac as substrate preincubated for 15 mins followed by substrate addition and measured for 60 mins by scintillation counting analysis B 7.3 pIC50 49.7 nM IC50 J Med Chem (2023) 66: 8407-8427 [PMID:37366223]
GtoPdb - - 7.68 pIC50 20.7 nM IC50 J Med Chem (2025) 68: 108-134 [PMID:39722476]
protein arginine methyltransferase 6/Protein arginine N-methyltransferase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1275221] [GtoPdb: 1257] [UniProtKB: Q96LA8]
ChEMBL Inhibition of PRMT6 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2025) 68: 108-134 [PMID:39722476]
protein arginine methyltransferase 7 /Protein arginine N-methyltransferase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3562175] [GtoPdb: 1258] [UniProtKB: Q9NVM4]
ChEMBL Inhibition of PRMT7 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2025) 68: 108-134 [PMID:39722476]
protein arginine methyltransferase 8/Protein arginine N-methyltransferase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108648] [GtoPdb: 1259] [UniProtKB: Q9NR22]
ChEMBL Inhibition of PRMT8 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2025) 68: 108-134 [PMID:39722476]

ChEMBL data shown on this page come from version 37:

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]