GSK-J1 [Ligand Id: 7027] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3188597 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| lysine demethylase 3A/Lysine-specific demethylase 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938209] [GtoPdb: 2673] [UniProtKB: Q9Y4C1] | ||||||||
| ChEMBL | Inhibition of KDM3A (unknown origin) | B | 4.4 | pIC50 | 39810.72 | nM | IC50 | Medchemcomm (2014) 5: 1879-1886 [PMID:26682034] |
| 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) | B | 4.7 | pIC50 | 19952.62 | nM | IC50 | Medchemcomm (2014) 5: 1879-1886 [PMID:26682034] |
| lysine demethylase 5A/Lysine-specific demethylase 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2424504] [GtoPdb: 2680] [UniProtKB: P29375] | ||||||||
| ChEMBL | Binding affinity to KDM5A ARID/PhD1 domain deletion mutant (1 to 588 residues) (unknown origin) by ITC assay | B | 4.92 | pKd | 12000 | nM | Kd | J Med Chem (2018) 61: 10588-10601 [PMID:30392349] |
| ChEMBL | Inhibition of KDM5A (unknown origin ) by TR-FRET assay | B | 5.17 | pIC50 | 6800 | nM | IC50 | Eur J Med Chem (2021) 226: 113855-113855 [PMID:34555614] |
| GtoPdb | - | - | 5.17 | pIC50 | 6800 | nM | IC50 | Nature (2014) 514: E1-2 [PMID:25279926] |
| lysine demethylase 5B/Lysine-specific demethylase 5B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3774295] [GtoPdb: 2681] [UniProtKB: Q9UGL1] | ||||||||
| ChEMBL | Inhibition of KDM5B (unknown origin) | B | 5.77 | pIC50 | 1700 | nM | IC50 | Eur J Med Chem (2020) 208: 112760-112760 [PMID:32883639] |
| ChEMBL | Inhibition of KDM5B (unknown origin) | B | 5.77 | pIC50 | 1700 | nM | IC50 | Eur J Med Chem (2023) 251: 115250-115250 [PMID:36931124] |
| ChEMBL | Inhibition of KDM5B (unknown origin ) by TR-FRET assay | B | 6.77 | pIC50 | 170 | nM | IC50 | Eur J Med Chem (2021) 226: 113855-113855 [PMID:34555614] |
| GtoPdb | - | - | 6.77 | pIC50 | 170 | nM | IC50 | Nature (2014) 514: E1-2 [PMID:25279926] |
| lysine demethylase 6A/Lysine-specific demethylase 6A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069164] [GtoPdb: 2684] [UniProtKB: O15550] | ||||||||
| ChEMBL | Inhibition of KDM6A (880 to 1401 residues) (unknown origin) using H3 ( 21 to 44 residues) K27me3 as substrate preincubated for 15 min followed by substrate addition measured after 15 mins by FDH-coupled demethylase assay | B | 4.16 | pIC50 | 69000 | nM | IC50 | J Med Chem (2018) 61: 10588-10601 [PMID:30392349] |
| GtoPdb | - | - | 7.28 | pIC50 | 53 | nM | IC50 | Nature (2014) 514: E1-2 [PMID:25279926] |
| lysine demethylase 6B/Lysine-specific demethylase 6B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938211] [GtoPdb: 2685] [UniProtKB: O15054] | ||||||||
| ChEMBL | Inhibition of JMJD3 (unknown origin) using biotinylated H3K27me3 peptide as substrate after 1 hr by AlphaLISA assay | B | 6.82 | pIC50 | 150 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 721-725 [PMID:26776360] |
| ChEMBL | Inhibition of KDM6B (unknown origin) | B | 7.2 | pIC50 | 63.1 | nM | IC50 | Medchemcomm (2014) 5: 1879-1886 [PMID:26682034] |
| ChEMBL | Inhibition of KDM6B (unknown origin) | B | 7.22 | pIC50 | 60 | nM | IC50 | Eur J Med Chem (2020) 208: 112760-112760 [PMID:32883639] |
| ChEMBL | Inhibition of JMJD3 (unknown origin) by Alphascreen assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem Lett (2023) 94: 129466-129466 [PMID:37660833] |
| GtoPdb | - | - | 7.55 | pIC50 | 28 | nM | IC50 |
Nature (2012) 488: 404-8 [PMID:22842901]; Nature (2014) 514: E1-2 [PMID:25279926] |
| ChEMBL | Inhibition of KDM6B (unknown origin ) by TR-FRET assay | B | 7.55 | pIC50 | 28 | nM | IC50 | Eur J Med Chem (2021) 226: 113855-113855 [PMID:34555614] |
| ChEMBL | Inhibition of C-terminal FLAG-tagged human KDM6B expressed in expressed in Sf9 cells pre-incubated for 4 hrs before substrate addition and measured after 1 hr by AlphaScreen assay | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1173-1176 [PMID:30928196] |
| 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 | 4 | pIC50 | >100000 | nM | IC50 | 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 | 4 | pIC50 | >100000 | 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 | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2024) 67: 4525-4540 [PMID:38294854] |
| 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 | 4.8 | pIC50 | 15900 | nM | IC50 | Bioorg Med Chem (2019) 27: 2405-2412 [PMID:30737136] |
| lysine demethylase 5C in Human [GtoPdb: 2682] [UniProtKB: P41229] | ||||||||
| GtoPdb | - | - | 6.26 | pIC50 | 550 | nM | IC50 | Nature (2014) 514: E1-2 [PMID:25279926] |
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]
