seclidemstat [Ligand Id: 14466] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4297641 (Sp-2577, SP-2577, Seclidemstat, SP2577)
  • lysine demethylase 1A/Lysine-specific histone demethylase 1A in Human [ChEMBL: CHEMBL6136] [GtoPdb: 2669] [UniProtKB: O60341]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
lysine demethylase 1A/Lysine-specific histone demethylase 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6136] [GtoPdb: 2669] [UniProtKB: O60341]
ChEMBL Inhibition of LSD1 (unknown origin) assessed as inhibition constant by peroxidase-coupled assay B 7.51 pKi 31 nM Ki J Med Chem (2023) 66: 71-94 [PMID:36537915]
GtoPdb - - 7.51 pKi 31 nM Ki J Med Chem (2023) 66: 71-94 [PMID:36537915]
ChEMBL Inhibition of LSD1 (unknown origin) B 6.9 pIC50 127 nM IC50 J Med Chem (2023) 66: 4275-4293 [PMID:37014989]
ChEMBL Inhibition of human recombinant LSD1 expressed in Escherichia coli using H3K4me2 peptide as substrate incubated for 60 mins by AlphaLISA assay B 7.58 pIC50 26.2 nM IC50 ACS Med Chem Lett (2023) 14: 1389-1395 [PMID:37849536]
ChEMBL Inhibition of LSD1 (unknown origin) B 7.89 pIC50 13 nM IC50 J Med Chem (2023) 66: 71-94 [PMID:36537915]
ChEMBL Inhibition of LSD1 (unknown origin) B 7.89 pIC50 13 nM IC50 Eur J Med Chem (2022) 240: 114564-114564 [PMID:35820351]
ChEMBL Inhibition of human recombinant LSD1 expressed in Escherichia coli BL21 (DE3) using H3K4me2 peptide as substrate incubated for 1 hr by fluorescence based analysis B 7.89 pIC50 13 nM IC50 J Med Chem (2024) 67: 922-951 [PMID:38214982]
ChEMBL Inhibition of human recombinant LSD1 expressed in Escherichia coli BL21 (DE3) measured after 1 hr by fluorescence based analysis B 7.89 pIC50 13 nM IC50 J Med Chem (2024) 67: 922-951 [PMID:38214982]
ChEMBL Inhibition of human LSD1 B 7.89 pIC50 13 nM IC50 Bioorg Med Chem Lett (2024) 114: 129982-129982 [PMID:39384076]
GtoPdb Inhibition of LSD1 enzymatic activity in a biochemical assay - 7.89 pIC50 13 nM IC50 PLoS One (2020) 15: e0235705 [PMID:32649682]

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]