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ChEMBL ligand: CHEMBL2164243 (N-(Dimethylamino)Succinamic Acid) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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egl-9 family hypoxia inducible factor 1/Egl nine homolog 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5697] [GtoPdb: 2833] [UniProtKB: Q9GZT9] | ||||||||
ChEMBL | Inhibition of human PHD2 expressed in Escherichia coli by fluorescence based assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2012) 55: 6639-6643 [PMID:22724510] |
Gamma-butyrobetaine dioxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163175] [UniProtKB: O75936] | ||||||||
ChEMBL | Inhibition of human BBOX1 by fluorescence based assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2012) 55: 6639-6643 [PMID:22724510] |
PHD finger protein 8/Histone lysine demethylase PHF8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938212] [GtoPdb: 2698] [UniProtKB: Q9UPP1] | ||||||||
ChEMBL | Inhibition of KDM7B (unknown origin) using H3K4me3K9me2 and 2-oxoglutarate as substrate after 1 hr by matrix-assisted laser desorption ionization time of flight mass spectrometry | B | 4.72 | pIC50 | 19000 | nM | IC50 | J Med Chem (2013) 56: 7222-7231 [PMID:23964788] |
ChEMBL | Inhibition of human PHF8 expressed in Escherichia coli using methyl lysine peptide substrate by AlphaScreen assay | B | 6.26 | pIC50 | 550 | nM | IC50 | J Med Chem (2012) 55: 6639-6643 [PMID:22724510] |
ChEMBL | Inhibition of KDM7B (unknown origin) by alphascreen assay | B | 6.26 | pIC50 | 550 | nM | IC50 | J Med Chem (2013) 56: 7222-7231 [PMID:23964788] |
GtoPdb | - | - | 6.26 | pIC50 | 550 | nM | IC50 | J Med Chem (2012) 55: 6639-43 [PMID:22724510] |
Hypoxia-inducible factor 1-alpha inhibitor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5909] [UniProtKB: Q9NWT6] | ||||||||
ChEMBL | Inhibition of human FIH expressed in Escherichia coli by MALDI assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2012) 55: 6639-6643 [PMID:22724510] |
lysine demethylase 2A/Lysine-specific demethylase 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938210] [GtoPdb: 2671] [UniProtKB: Q9Y2K7] | ||||||||
ChEMBL | Mixed type inhibition of human KDM2A expressed in Escherichia coli assessed inhibition constant for compound-enzyme-substrate complex using methyl lysine peptide substrate by enzyme kinetic assay | B | 4.07 | pKi | 85000 | nM | Ki | J Med Chem (2012) 55: 6639-6643 [PMID:22724510] |
ChEMBL | Competitive inhibition of human KDM2A expressed in Escherichia coli using 2-oxoglutarate by enzyme kinetic assay | B | 5.71 | pKi | 1970 | nM | Ki | J Med Chem (2012) 55: 6639-6643 [PMID:22724510] |
GtoPdb | - | - | 5.82 | pIC50 | 1500 | nM | IC50 | J Med Chem (2012) 55: 6639-43 [PMID:22724510] |
ChEMBL | Inhibition of human KDM2A expressed in Escherichia coli by formaldehyde dehydrogenase coupled assay | B | 5.82 | pIC50 | 1500 | nM | IC50 | J Med Chem (2012) 55: 6639-6643 [PMID:22724510] |
ChEMBL | Inhibition of human KDM2A expressed in Escherichia coli using methyl lysine peptide substrate by AlphaScreen assay | B | 5.82 | pIC50 | 1500 | nM | IC50 | J Med Chem (2012) 55: 6639-6643 [PMID:22724510] |
ChEMBL | Inhibition of KDM2A (unknown origin) | B | 5.82 | pIC50 | 1500 | nM | IC50 | J Med Chem (2013) 56: 7222-7231 [PMID:23964788] |
lysine demethylase 4E/Lysine-specific demethylase 4D-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293226] [GtoPdb: 2679] [UniProtKB: B2RXH2] | ||||||||
ChEMBL | Inhibition of human KDM4E expressed in Escherichia coli using methyl lysine peptide substrate by AlphaScreen assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2012) 55: 6639-6643 [PMID:22724510] |
lysine demethylase 5C/Lysine-specific demethylase 5C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163176] [GtoPdb: 2682] [UniProtKB: P41229] | ||||||||
ChEMBL | Inhibition of human KDM5C catalytic domain expressed in Sf9 cells using methyl lysine peptide substrate by AlphaScreen assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2012) 55: 6639-6643 [PMID:22724510] |
lysine demethylase 6A/Lysine-specific demethylase 6A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069164] [GtoPdb: 2684] [UniProtKB: O15550] | ||||||||
ChEMBL | Inhibition of human recombinant KDM6A after 1 hr | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2013) 56: 7222-7231 [PMID:23964788] |
lysine demethylase 6B/Lysine-specific demethylase 6B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938211] [GtoPdb: 2685] [UniProtKB: O15054] | ||||||||
ChEMBL | Inhibition of human KDM6B catalytic domain expressed in Escherichia coli using methyl lysine peptide substrate by AlphaScreen assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2012) 55: 6639-6643 [PMID:22724510] |
lysine demethylase 7A/Lysine-specific demethylase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163177] [GtoPdb: 2686] [UniProtKB: Q6ZMT4] | ||||||||
ChEMBL | Inhibition of human KDM7A catalytic domain expressed in Escherichia coli by MALDI assay | B | 5.68 | pIC50 | 2100 | nM | IC50 | J Med Chem (2012) 55: 6639-6643 [PMID:22724510] |
GtoPdb | - | - | 5.68 | pIC50 | 2100 | nM | IC50 | J Med Chem (2012) 55: 6639-43 [PMID:22724510] |
Prolyl 4-hydroxylase in Paramecium bursaria Chlorella virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523368] [UniProtKB: Q84406] | ||||||||
ChEMBL | Inhibition of N-terminal His6-tagged recombinant Paramecium bursaria chlorella virus 1 CPH expressed in Escherichia coli Rosetta 2 (DE3) cells pre-incubated for 5 mins before 2OG as substrate and Fe2 as co-factor addition in presence of L-ascorbate and measured after 5 mins MALDI TOF MS analysis | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2019) 27: 2405-2412 [PMID:30737136] |
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]