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| ChEMBL ligand: CHEMBL4297641 (Sp-2577, SP-2577, Seclidemstat, SP2577) |
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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]