GSK-J4 [Ligand Id: 8979] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3183531 |
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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 | 5.38 | pIC50 | 4200 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| 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 | 5.68 | pIC50 | 2100 | 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 | 5.07 | pIC50 | 8500 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| 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 | 5.16 | pIC50 | 6900 | 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 KDM4A (1 to 350 residues)(unknown origin) by Alphalisa assay | B | 5.12 | pIC50 | 7500 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| 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 | 5.42 | pIC50 | 3800 | 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 epitope-tagged full length KDM4C (unknown origin) transfected in human U2OS cells using H3K9me3 peptide as substrate | B | 5.14 | pIC50 | 7300 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| ChEMBL | Inhibition of KDM4C (1 to 349 residues)(unknown origin) by Alphalisa assay | B | 5.26 | pIC50 | 5500 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| lysine demethylase 5B/Lysine-specific demethylase 5B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3774295] [GtoPdb: 2681] [UniProtKB: Q9UGL1] | ||||||||
| GtoPdb | - | - | 5.01 | pIC50 | 9700 | nM | IC50 | Nature (2014) 514: E1-2 [PMID:25279926] |
| ChEMBL | Inhibition of KDM5B (unknown origin) | B | 5.01 | pIC50 | 9700 | nM | IC50 | Eur J Med Chem (2020) 208: 112760-112760 [PMID:32883639] |
| ChEMBL | Inhibition of KDM5B (1 to 809 residues)(unknown origin) by Alphalisa assay | B | 5.01 | pIC50 | 9700 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| lysine demethylase 5C/Lysine-specific demethylase 5C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163176] [GtoPdb: 2682] [UniProtKB: P41229] | ||||||||
| GtoPdb | - | - | 4.82 | pIC50 | 15000 | nM | IC50 | Nature (2014) 514: E1-2 [PMID:25279926] |
| ChEMBL | Inhibition of KDM5C (2 to 1560 residues)(unknown origin) by Alphalisa assay | B | 4.82 | pIC50 | 15000 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| lysine demethylase 6A/Lysine-specific demethylase 6A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069164] [GtoPdb: 2684] [UniProtKB: O15550] | ||||||||
| ChEMBL | Affinity Phenotypic Cellular interaction (Inhibition of TNF release (in LPS stimulated human macrophages derived from PBMC)) EUB0000217b KDM6A/UTX | F | 5.05 | pIC50 | 9000 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3 |
| GtoPdb | - | - | 5.18 | pIC50 | 6600 | nM | IC50 | Nature (2014) 514: E1-2 [PMID:25279926] |
| ChEMBL | Affinity Biochemical interaction (AlphaLISA based assay) EUB0000217b KDM6A/UTX | B | 5.18 | pIC50 | 6600 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Inhibition of KDM6A (919 to 1401 residues)(unknown origin) by Alphalisa assay | B | 5.18 | pIC50 | 6600 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| lysine demethylase 6B/Lysine-specific demethylase 6B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938211] [GtoPdb: 2685] [UniProtKB: O15054] | ||||||||
| ChEMBL | Inhibition of KDM6B (unknown origin) by mass spectrometry | B | 4.3 | pIC50 | >50000 | 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 | 4.3 | pIC50 | >50000 | nM | IC50 | Nature (2012) 488: 404-408 [PMID:22842901] |
| ChEMBL | Inhibition of JMJD3 (unknown origin) by Alphascreen assay | B | 5.07 | pIC50 | 8600 | nM | IC50 | Bioorg Med Chem Lett (2023) 94: 129466-129466 [PMID:37660833] |
| ChEMBL | Inhibition of KDM6B (1043 to 1643 residues)(unknown origin) by Alphalisa assay | B | 5.07 | pIC50 | 8600 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| GtoPdb | - | - | 5.07 | pIC50 | 8600 | nM | IC50 | Nature (2014) 514: E1-2 [PMID:25279926] |
| ChEMBL | Inhibition of epitope-tagged KDM6B (1026 to 1682 residues)(unknown origin) transfected in human U2OS cells using H3K27me2 peptide as substrate | B | 5.51 | pIC50 | 3100 | nM | IC50 | Nature (2014) 514: 1-2 [PMID:25279926] |
| Methylcytosine dioxygenase TET1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523402] [UniProtKB: Q8NFU7] | ||||||||
| 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 | 4.8 | pEC50 | 16000 | nM | EC50 | 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 | 4.8 | pEC50 | 15848.93 | nM | EC50 | J Med Chem (2024) 67: 4525-4540 [PMID:38294854] |
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]
