AMG28 [Ligand Id: 12186] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2334586
  • mitogen-activated protein kinase kinase kinase 14/Mitogen-activated protein kinase kinase kinase 14 in Human [ChEMBL: CHEMBL5888] [GtoPdb: 2074] [UniProtKB: Q99558]
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  • p21 (RAC1) activated kinase 4 in Human [GtoPdb: 2136] [UniProtKB: O96013]
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  • p21 (RAC1) activated kinase 6 in Human [GtoPdb: 2137] [UniProtKB: Q9NQU5]
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  • p21 (RAC1) activated kinase 5 in Human [GtoPdb: 2138] [UniProtKB: Q9P286]
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  • TAO kinase 1 in Human [GtoPdb: 2233] [UniProtKB: Q7L7X3]
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  • TAO kinase 2 in Human [GtoPdb: 2234] [UniProtKB: Q9UL54]
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  • TAO kinase 3 in Human [GtoPdb: 2235] [UniProtKB: Q9H2K8]
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  • tau tubulin kinase 1 in Human [GtoPdb: 2262] [UniProtKB: Q5TCY1]
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  • phosphoinositide kinase, FYVE-type zinc finger containing in Human [GtoPdb: 2857] [UniProtKB: Q9Y2I7]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mitogen-activated protein kinase kinase kinase 14/Mitogen-activated protein kinase kinase kinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5888] [GtoPdb: 2074] [UniProtKB: Q99558]
GtoPdb Enzymatic inhibition determined in a homogenous time resolved fluorescence (HTRF) assay for NIK (MAP3K14) - 6 pKi <1000 nM Ki WO2009158011A1. Alkynyl alcohols as kinase inhibitors (2009)
ChEMBL Inhibition of NIK in human HT-29 cells assessed as LTalpha/beta2-induced p100 processing to NFkappaB2 preincubated for 30 mins before LTalpha/beta2 stimulation measured after 5 hrs B 6.77 pIC50 170 nM IC50 Bioorg Med Chem Lett (2013) 23: 1238-1244 [PMID:23374866]
ChEMBL Inhibition of NIK (unknown origin) autophosphorylation after 1 hr by chemiluminescent assay B 7.39 pIC50 41 nM IC50 Bioorg Med Chem Lett (2013) 23: 1238-1244 [PMID:23374866]
p21 (RAC1) activated kinase 4 in Human [GtoPdb: 2136] [UniProtKB: O96013]
GtoPdb - - 6.96 pIC50 110 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
p21 (RAC1) activated kinase 6 in Human [GtoPdb: 2137] [UniProtKB: Q9NQU5]
GtoPdb - - 7.22 pIC50 60 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
p21 (RAC1) activated kinase 5 in Human [GtoPdb: 2138] [UniProtKB: Q9P286]
GtoPdb - - 7.02 pIC50 96 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
TAO kinase 1 in Human [GtoPdb: 2233] [UniProtKB: Q7L7X3]
GtoPdb - - 7.7 pIC50 20 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
TAO kinase 2 in Human [GtoPdb: 2234] [UniProtKB: Q9UL54]
GtoPdb - - 7.04 pIC50 91 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
TAO kinase 3 in Human [GtoPdb: 2235] [UniProtKB: Q9H2K8]
GtoPdb - - 7.35 pIC50 45 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
tau tubulin kinase 1 in Human [GtoPdb: 2262] [UniProtKB: Q5TCY1]
GtoPdb - - 6.7 pIC50 199 nM IC50 J Med Chem (2021) 64: 6358-6380 [PMID:33944571]
phosphoinositide kinase, FYVE-type zinc finger containing in Human [GtoPdb: 2857] [UniProtKB: Q9Y2I7]
GtoPdb - - 8.66 pIC50 2.2 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]