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 |
|---|---|---|---|---|---|---|---|---|
| PHD finger protein 8/Histone lysine demethylase PHF8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938212] [GtoPdb: 2698] [UniProtKB: Q9UPP1] | ||||||||
| ChEMBL | Inhibition of PHF8 (1 to 1024 residues)(unknown origin) by Alphalisa assay | B | 4.55 | pIC50 | 28000 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| enhancer of zeste 2 polycomb repressive complex 2 subunit/Histone-lysine N-methyltransferase EZH2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189110] [GtoPdb: 2654] [UniProtKB: Q15910] | ||||||||
| ChEMBL | Inhibition of EZH2 Y641F mutant (unknown origin) | B | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (2024) 67: 922-951 [PMID:38214982] |
| lysine demethylase 2B/Lysine-specific demethylase 2B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3779760] [GtoPdb: 2672] [UniProtKB: Q8NHM5] | ||||||||
| ChEMBL | Inhibition of KDM2B (1 to 650 residues)(unknown origin) by Alphalisa assay | B | 4.68 | pIC50 | 21000 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| lysine demethylase 3A/Lysine-specific demethylase 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938209] [GtoPdb: 2673] [UniProtKB: Q9Y4C1] | ||||||||
| ChEMBL | Inhibition of KDM3A (2 to 1322 residues)(unknown origin) by Alphalisa assay | B | 4.12 | pIC50 | >75000 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| ChEMBL | Inhibition of recombinant human JmjD1a using biotinylated H3K9(1-21)me2 as substrate preincubated for 15 mins followed by substrate addition and measured after 5 mins in presence of alpha-KG, FAS and L-ascorbic acid by Alphascreen assay | B | 4.39 | pIC50 | 41000 | nM | IC50 | Nature (2012) 488: 404-408 [PMID:22842901] |
| ChEMBL | Inhibition of KDM3A (unknown origin) | B | 4.4 | pIC50 | 39810.72 | nM | IC50 | Medchemcomm (2014) 5: 1879-1886 [PMID:26682034] |
| lysine demethylase 3B/Lysine-specific demethylase 3B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3784906] [GtoPdb: 2674] [UniProtKB: Q7LBC6] | ||||||||
| ChEMBL | Inhibition of KDM3B (842 to 1761 residues)(unknown origin) by Alphalisa assay | B | 4.12 | pIC50 | >75000 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| lysine demethylase 4A/Lysine-specific demethylase 4A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5896] [GtoPdb: 2675] [UniProtKB: O75164] | ||||||||
| ChEMBL | Inhibition of human JmjD2a using H3K27(me3) as substrate preincubated for 10 mins followed by substrate addition and measured after 7 mins in presence of alpha-KG by RapidFire Mass Spectrometry | B | 4 | pIC50 | >100000 | nM | IC50 | Nature (2012) 488: 404-408 [PMID:22842901] |
| ChEMBL | Inhibition of KDM4A (1 to 350 residues)(unknown origin) by Alphalisa assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| ChEMBL | Inhibition of human JmjD2a by Alphascreen assay | B | 4.35 | pIC50 | 44300 | nM | IC50 | Nature (2012) 488: 404-408 [PMID:22842901] |
| lysine demethylase 4B/Lysine-specific demethylase 4B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3313832] [GtoPdb: 2676] [UniProtKB: O94953] | ||||||||
| ChEMBL | Inhibition of KDM4B (2 to 500 residues)(unknown origin) by Alphalisa assay | B | 4.14 | pIC50 | 73000 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| lysine demethylase 4C/Lysine-specific demethylase 4C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6175] [GtoPdb: 2677] [UniProtKB: Q9H3R0] | ||||||||
| ChEMBL | Inhibition of human JmjD2c using H3K27(me3) as substrate preincubated for 10 mins followed by substrate addition and measured after 7 mins in presence of alpha-KG by RapidFire Mass Spectrometry | B | 4 | pIC50 | >100000 | nM | IC50 | Nature (2012) 488: 404-408 [PMID:22842901] |
| ChEMBL | Inhibition of KDM4C (1 to 349 residues)(unknown origin) by Alphalisa assay | B | 4.47 | pIC50 | 34000 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| lysine demethylase 4D/Lysine-specific demethylase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6138] [GtoPdb: 2678] [UniProtKB: Q6B0I6] | ||||||||
| ChEMBL | Inhibition of human JmjD2d using H3K27(me3) as substrate preincubated for 10 mins followed by substrate addition and measured after 7 mins in presence of alpha-KG by RapidFire Mass Spectrometry | B | 4.1 | pIC50 | 79000 | nM | IC50 | Nature (2012) 488: 404-408 [PMID:22842901] |
| lysine demethylase 4E/Lysine-specific demethylase 4E in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293226] [GtoPdb: 2679] [UniProtKB: B2RXH2] | ||||||||
| ChEMBL | Inhibition of human JmjD2e using H3K27(me3) as substrate preincubated for 10 mins followed by substrate addition and measured after 7 mins in presence of alpha-KG by RapidFire Mass Spectrometry | B | 4.2 | pIC50 | 63000 | nM | IC50 | Nature (2012) 488: 404-408 [PMID:22842901] |
| ChEMBL | Inhibition of KDM4E (unknown origin) | B | 4.7 | pIC50 | 19952.62 | nM | IC50 | Medchemcomm (2014) 5: 1879-1886 [PMID:26682034] |
| ChEMBL | Inhibition of recombinant human JmjD2e using biotinylated H3K9(1-15)me3 as substrate preincubated for 15 mins followed by substrate addition and measured after 20 mins in presence of alpha-KG, FAS and L-ascorbic acid by Alphascreen assay | B | 4.71 | pIC50 | 19600 | nM | IC50 | Nature (2012) 488: 404-408 [PMID:22842901] |
| 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] |
| ChEMBL | Inhibition of KDM5A (1 to 1090 residues)(unknown origin) by Alphalisa assay | B | 5.17 | pIC50 | 6800 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| 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] |
| ChEMBL | Inhibition of KDM5B (1 to 809 residues) (unknown origin) AlphaLISA assay | B | 6.77 | pIC50 | 170 | nM | IC50 | Eur J Med Chem (2024) 272: 116494-116494 [PMID:38749268] |
| ChEMBL | Inhibition of KDM5B (1 to 809 residues)(unknown origin) by Alphalisa assay | B | 6.77 | pIC50 | 170 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| GtoPdb | - | - | 6.77 | pIC50 | 170 | nM | IC50 | Nature (2014) 514: E1-2 [PMID:25279926] |
| lysine demethylase 5C/Lysine-specific demethylase 5C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163176] [GtoPdb: 2682] [UniProtKB: P41229] | ||||||||
| ChEMBL | Inhibition of human Jarid1c by MALDI-TOF analysis | B | 4 | pIC50 | >100000 | nM | IC50 | Nature (2012) 488: 404-408 [PMID:22842901] |
| ChEMBL | Inhibition of KDM5C (2 to 1560 residues)(unknown origin) by Alphalisa assay | B | 6.26 | pIC50 | 550 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| GtoPdb | - | - | 6.26 | pIC50 | 550 | 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] |
| ChEMBL | Inhibition of human UTX using Biotin-KAPRKQLATKAARK(me3)SAPATGG as substrate by MALDI-TOF analysis | B | 4.25 | pIC50 | 56000 | nM | IC50 | Nature (2012) 488: 404-408 [PMID:22842901] |
| ChEMBL | Inhibition of KDM6A (919 to 1401 residues)(unknown origin) by Alphalisa assay | B | 7.28 | pIC50 | 53 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| 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 recombinant human N-terminal His6/Flag-tagged TEV-protease cleavage site fused JMJD3 1637-1675 deletion mutant (1141 to 1682 residues) expressed in baculovirus infected Sf9 insect cells using Biotin-KAPRKQLATKAARK(me3)SAPATGG as substrate by MALDI-TOF analysis | B | 4.74 | pIC50 | 18000 | nM | IC50 | Nature (2012) 488: 404-408 [PMID:22842901] |
| ChEMBL | Inhibition of epitope-tagged KDM6B (1026 to 1682 residues)(unknown origin) transfected in human U2OS cells using H3K27me2 peptide as substrate | B | 4.77 | pIC50 | 17000 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| ChEMBL | Inhibition of recombinant human N-terminal His6/Flag-tagged TEV-protease cleavage site fused JMJD3 1637-1675 deletion mutant (1141 to 1682 residues) expressed in baculovirus infected Sf9 insect cells using H3K27(me3) as substrate preincubated for 10 mins followed by substrate addition and measured after 7 mins in presence of alpha-KG by RapidFire Mass Spectrometry | B | 5.3 | pIC50 | 5000 | nM | IC50 | Nature (2012) 488: 404-408 [PMID:22842901] |
| 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 recombinant human N-terminal His6/Flag-tagged TEV-protease cleavage site fused JMJD3 1637-1675 deletion mutant (1141 to 1682 residues) expressed in baculovirus infected Sf9 insect cells using biotinylated H3K27(14-34)me3 as substrate preincubated for 15 mins followed by substrate addition and measured after 5 mins in presence of alpha-KG, FAS and L-ascorbic acid by Alphascreen assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Nature (2012) 488: 404-408 [PMID:22842901] |
| ChEMBL | Inhibition of KDM6B (unknown origin) | B | 7.22 | pIC50 | 60 | nM | IC50 | Eur J Med Chem (2020) 208: 112760-112760 [PMID:32883639] |
| ChEMBL | Competitive inhibition of KDM6B (unknown origin) using biotinylated H3K27me3 peptide as substrate preincubated for 15 mins followed by substrate addition measured after 5 mins in presence of 2-oxoglutarate/Fe2+/L-ascorbic acid by AlphaScreen assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| 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 KDM6B (1043 to 1643 residues)(unknown origin) by Alphalisa assay | B | 7.55 | pIC50 | 28 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| 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] |
ChEMBL data shown on this page come from version 36:
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]
