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ChEMBL ligand: CHEMBL257167 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
ChEMBL | Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate | B | 5.71 | pIC50 | 1967 | nM | IC50 | HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators |
inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa B kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920] | ||||||||
ChEMBL | Inhibition of IKK-beta | B | 7.7 | pIC50 | 19.95 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2255-2258 [PMID:21429745] |
ChEMBL | Inhibition of IKK-beta | B | 7.71 | pIC50 | 19.5 | nM | IC50 | J Med Chem (2008) 51: 7898-7914 [PMID:19035792] |
ChEMBL | Inhibition of IKK beta at 300 uM by K-ELISA | B | 7.74 | pIC50 | 18 | nM | IC50 | J Nat Prod (2008) 71: 106-111 [PMID:18088098] |
ChEMBL | Inhibition of IKK-beta by TR-FRET assay | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem (2009) 17: 2759-2766 [PMID:19285872] |
GtoPdb | FRET measurement using recombinant human IKK2 (residues 1-756) | - | 7.75 | pIC50 | 17.9 | nM | IC50 | J Pharmacol Exp Ther (2005) 312: 373-81 [PMID:15316093] |
eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525] | ||||||||
ChEMBL | Inhibition of human recombinant PKR autophosphorylation using poly[I:C] after 10 mins by luminescent assay | B | 6.6 | pIC50 | 250 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4108-4114 [PMID:21632247] |
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
ChEMBL | Binding affinity to human JAK2 | B | 7.66 | pKd | 22 | nM | Kd | J Med Chem (2008) 51: 7898-7914 [PMID:19035792] |
ChEMBL | Inhibition of JAK2 | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2008) 51: 7898-7914 [PMID:19035792] |
Venus kinase receptor 2 in Schistosoma mansoni (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5169215] [UniProtKB: D5JEH1] | ||||||||
ChEMBL | Binding affinity to Schistosoma mansoni N-terminal His6-tagged full-length VKR2 kinase domain expressed in baculovirus infected Sf9 insect cells in presence of ATPgammaS by SPR analysis | B | 4.8 | pKd | 16000 | nM | Kd | ACS Med Chem Lett (2022) 13: 1715-1722 [PMID:36385939] |
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]