GSK-J4 [Ligand Id: 8979] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3183531
  • lysine demethylase 5B/Lysine-specific demethylase 5B in Human [ChEMBL: CHEMBL3774295] [GtoPdb: 2681] [UniProtKB: Q9UGL1]
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  • lysine demethylase 6A/Lysine-specific demethylase 6A in Human [ChEMBL: CHEMBL2069164] [GtoPdb: 2684] [UniProtKB: O15550]
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  • lysine demethylase 6B/Lysine-specific demethylase 6B in Human [ChEMBL: CHEMBL1938211] [GtoPdb: 2685] [UniProtKB: O15054]
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  • lysine demethylase 5C in Human [GtoPdb: 2682] [UniProtKB: P41229]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]
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
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) by Alphascreen assay B 5.07 pIC50 8600 nM IC50 Bioorg Med Chem Lett (2023) 94: 129466-129466 [PMID:37660833]
GtoPdb - - 5.07 pIC50 8600 nM IC50 Nature (2014) 514: E1-2 [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]
lysine demethylase 5C in Human [GtoPdb: 2682] [UniProtKB: P41229]
GtoPdb - - 4.82 pIC50 15000 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]