ML324 [Ligand Id: 9584] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1398529 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| lysine demethylase 4E/Lysine-specific demethylase 4D-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293226] [GtoPdb: 2679] [UniProtKB: B2RXH2] | ||||||||
| ChEMBL | Inhibition of KDM4E (unknown origin) measured by Alphascreen assay | B | 6.04 | pIC50 | 920 | nM | IC50 | J Med Chem (2022) 65: 9564-9579 [PMID:35838529] |
| GtoPdb | - | - | 6.04 | pIC50 | 920 | nM | IC50 | Probe Reports from the NIH Molecular Libraries Program (2010) : [PMID:24260783] |
| Methylcytosine dioxygenase TET1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523402] [UniProtKB: Q8NFU7] | ||||||||
| ChEMBL | Inhibition of N-terminal 3xFlag-tagged human TET1 catalytic domain (E1418 to V2136 residues) expressed in Sf9 cells using 5-methylcytosine as substrate preincubated for 10 mins followed by DNA-cofactor addition and measured after 30 mins by Alphascreen assay | B | 5.89 | pIC50 | 1288.25 | nM | IC50 | J Med Chem (2024) 67: 4525-4540 [PMID:38294854] |
| ChEMBL | Inhibition of tetracyclin/Dox-inducible N-terminal 3xFLAG/C-terminal GFP tagged human TET1 catalytic domain (1481 to 2136 residues) expressed in human U2OS cells assessed as reduction in 5-hydroxymethylcytosine level incubated for 24 hrs by immunofluorescence analysis | B | 4.28 | pEC50 | 52480.75 | nM | EC50 | J Med Chem (2024) 67: 4525-4540 [PMID:38294854] |
| Methylcytosine dioxygenase TET2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523344] [UniProtKB: Q6N021] | ||||||||
| ChEMBL | Inhibition of His10-FLAG tagged human TET2 catalytic domain (Q969 to I2002 residues) expressed in Sf9 cells using 5-methylcytosine as substrate preincubated for 10 mins followed by DNA-cofactor addition and measured after 10 mins by Alphascreen assay | B | 5.81 | pIC50 | 1548.82 | nM | IC50 | J Med Chem (2024) 67: 4525-4540 [PMID:38294854] |
| Methylcytosine dioxygenase TET3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4879414] [UniProtKB: O43151] | ||||||||
| ChEMBL | Inhibition of human TET3 catalytic domain (E824 to I1795 residues) expressed in mammalian cells using 5-methylcytosine as substrate preincubated for 10 mins followed by DNA-cofactor addition and measured after 10 mins by Alphascreen assay | B | 5.9 | pIC50 | 1258.93 | nM | IC50 | J Med Chem (2024) 67: 4525-4540 [PMID:38294854] |
| lysine demethylase 4A in Human [GtoPdb: 2675] [UniProtKB: O75164] | ||||||||
| GtoPdb | - | - | 6 | pIC50 | <1000 | nM | IC50 | Probe Reports from the NIH Molecular Libraries Program (2010) : [PMID:24260783] |
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]
