navlimetostat [Ligand Id: 12116] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL5075255
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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 Binding affinity to PPRMT5 complexed with MTA - 9.85 pKd 0.14 nM Kd J Med Chem (2022) 65: 1749-1766 [PMID:35041419]
ChEMBL Inhibition of PRMT5/MEP50 (unknown origin) using Histone H2A as substrate B 6.39 pIC50 410 nM IC50 J Med Chem (2022) 65: 1749-1766 [PMID:35041419]
GtoPdb Inhibitory potency in HCT116 MTAP-deleted cells - 7.92 pIC50 12 nM IC50 J Med Chem (2022) 65: 1749-1766 [PMID:35041419]
protein arginine methyltransferase 5 /Protein arginine N-methyltransferase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795116] [GtoPdb: 1256] [UniProtKB: O14744]
GtoPdb Binding affinity to PPRMT5 complexed with MTA - 9.85 pKd 0.14 nM Kd J Med Chem (2022) 65: 1749-1766 [PMID:35041419]
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 5.26 pIC50 >5500 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 5.82 pIC50 1520 nM IC50 J Med Chem (2022) 65: 1749-1766 [PMID:35041419]
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 6.19 pIC50 653 nM IC50 J Med Chem (2022) 65: 1749-1766 [PMID:35041419]
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 In-cell Western analysis B 6.19 pIC50 653 nM IC50 Bioorg Med Chem (2022) 71: 116947-116947 [PMID:35926325]
GtoPdb Inhibitory potency in HCT116 MTAP-deleted cells - 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 8.1 pIC50 8 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 In-cell Western analysis B 8.1 pIC50 8 nM IC50 Bioorg Med Chem (2022) 71: 116947-116947 [PMID:35926325]
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 8.22 pIC50 6 nM IC50 J Med Chem (2022) 65: 1749-1766 [PMID:35041419]

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]