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

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ChEMBL ligand: CHEMBL2334586
  • phosphoinositide kinase, FYVE-type zinc finger containing/1-phosphatidylinositol 3-phosphate 5-kinase in Human [ChEMBL: CHEMBL1938222] [GtoPdb: 2857] [UniProtKB: Q9Y2I7]
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  • 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/Serine/threonine-protein kinase PAK 4 in Human [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013]
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  • p21 (RAC1) activated kinase 6/Serine/threonine-protein kinase PAK6 in Human [ChEMBL: CHEMBL4311] [GtoPdb: 2137] [UniProtKB: Q9NQU5]
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  • p21 (RAC1) activated kinase 5/Serine/threonine-protein kinase PAK7 in Human [ChEMBL: CHEMBL4524] [GtoPdb: 2138] [UniProtKB: Q9P286]
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  • protein kinase X-linked/Serine/threonine-protein kinase PRKX in Human [ChEMBL: CHEMBL5818] [GtoPdb: 2175] [UniProtKB: P51817]
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  • TAO kinase 1/Serine/threonine-protein kinase TAO1 in Human [ChEMBL: CHEMBL5261] [GtoPdb: 2233] [UniProtKB: Q7L7X3]
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  • TAO kinase 2/Serine/threonine-protein kinase TAO2 in Human [ChEMBL: CHEMBL1075195] [GtoPdb: 2234] [UniProtKB: Q9UL54]
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  • TAO kinase 3/Serine/threonine-protein kinase TAO3 in Human [ChEMBL: CHEMBL5701] [GtoPdb: 2235] [UniProtKB: Q9H2K8]
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  • testis specific serine kinase 1B/Testis-specific serine/threonine-protein kinase 1 in Human [ChEMBL: CHEMBL6003] [GtoPdb: 2257] [UniProtKB: Q9BXA7]
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  • testis specific serine kinase 3/Testis-specific serine/threonine-protein kinase 3 in Human [ChEMBL: CHEMBL3414416] [GtoPdb: 2259] [UniProtKB: Q96PN8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
phosphoinositide kinase, FYVE-type zinc finger containing/1-phosphatidylinositol 3-phosphate 5-kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938222] [GtoPdb: 2857] [UniProtKB: Q9Y2I7]
ChEMBL Inhibition of PIKFYVE in HEK293 cells by NanoBRET assay B 7.85 pIC50 14.1 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
ChEMBL Inhibition of human wild type partial length PIKfyve (F1512 to C2098 residues) expressed in mammalian expression system by Kinomescan assay B 8.66 pIC50 2.2 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
ChEMBL Inhibition of human GST tagged PIKFYVE (1493 to end residues) expressed in baculovirus-infected Sf9 cells using PI(3)P:PS as substrate incubated for 60 mins in presence of ATP by ADP-Glo assay B 8.66 pIC50 2.2 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
GtoPdb - - 8.66 pIC50 2.2 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
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 (unknown origin) B 6.5 pIC50 316 nM IC50 J Med Chem (2021) 64: 6358-6380 [PMID:33944571]
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/Serine/threonine-protein kinase PAK 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013]
ChEMBL Inhibition of human wild type partial length PAK4 (Q144 to R438 residues) expressed in bacterial expression system by Kinomescan assay B 6.96 pIC50 110 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
GtoPdb - - 6.96 pIC50 110 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
p21 (RAC1) activated kinase 6/Serine/threonine-protein kinase PAK6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4311] [GtoPdb: 2137] [UniProtKB: Q9NQU5]
GtoPdb - - 7.22 pIC50 60 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
ChEMBL Inhibition of human wild type partial length PAK6 (N298 to C681 residues) expressed in bacterial expression system by Kinomescan assay B 7.22 pIC50 60 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
p21 (RAC1) activated kinase 5/Serine/threonine-protein kinase PAK7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4524] [GtoPdb: 2138] [UniProtKB: Q9P286]
ChEMBL Inhibition of human wild type partial length PAK5 (Y400 to H719 residues) expressed in bacterial expression system by Kinomescan assay B 7.02 pIC50 96 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
GtoPdb - - 7.02 pIC50 96 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
protein kinase X-linked/Serine/threonine-protein kinase PRKX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5818] [GtoPdb: 2175] [UniProtKB: P51817]
ChEMBL Inhibition of human wild type partial length PRKX (M1 to F358 residues) expressed in bacterial expression system by Kinomescan assay B 6.24 pIC50 580 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
TAO kinase 1/Serine/threonine-protein kinase TAO1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5261] [GtoPdb: 2233] [UniProtKB: Q7L7X3]
ChEMBL Inhibition of human wild type TAOK1 (M1 to A320 residues) expressed in mammalian expression system by Kinomescan assay B 7.7 pIC50 20 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
GtoPdb - - 7.7 pIC50 20 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
TAO kinase 2/Serine/threonine-protein kinase TAO2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075195] [GtoPdb: 2234] [UniProtKB: Q9UL54]
GtoPdb - - 7.04 pIC50 91 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
ChEMBL Inhibition of human wild type partial length TAOK2 (M1 to A320 residues) expressed in mammalian expression system by Kinomescan assay B 7.05 pIC50 89 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
TAO kinase 3/Serine/threonine-protein kinase TAO3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5701] [GtoPdb: 2235] [UniProtKB: Q9H2K8]
ChEMBL Inhibition of human wild type partial length TAOK3 (M1 to T316 residues) expressed in mammalian expression system by Kinomescan assay B 7.35 pIC50 45 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
GtoPdb - - 7.35 pIC50 45 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
tau tubulin kinase 1/Tau-tubulin kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1926492] [GtoPdb: 2262] [UniProtKB: Q5TCY1]
ChEMBL Inhibition of TTBK1 in human HEK293T cells incubated for 1 hrs by HTRF assay B 5.73 pIC50 1850 nM IC50 J Med Chem (2021) 64: 6358-6380 [PMID:33944571]
GtoPdb - - 6.7 pIC50 199 nM IC50 J Med Chem (2021) 64: 6358-6380 [PMID:33944571]
ChEMBL Inhibition of GST-tagged TTBK1 (1 to 421) (unknown origin) using DNA Topoisomerase 2-alpha-Thr1342 as substrate incubated for 15 mins followed by ATP addition and further incubated for 120 mins by TR-FRET assay B 6.7 pIC50 199 nM IC50 J Med Chem (2021) 64: 6358-6380 [PMID:33944571]
testis specific serine kinase 1B/Testis-specific serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6003] [GtoPdb: 2257] [UniProtKB: Q9BXA7]
ChEMBL Inhibition of human wild type TSSK1 B 6.68 pIC50 210 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]
testis specific serine kinase 3/Testis-specific serine/threonine-protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3414416] [GtoPdb: 2259] [UniProtKB: Q96PN8]
ChEMBL Inhibition of wild-type human full length TSSK3 (M1 to T268 residues) expressed in mammalian expression system by Kinomescan method B 7.04 pIC50 91 nM IC50 J Med Chem (2022) 65: 12860-12882 [PMID:36111834]

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]