HG-10-102-01 [Ligand Id: 9392] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2170016
  • leucine rich repeat kinase 2/Leucine-rich repeat serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL1075104] [GtoPdb: 2059] [UniProtKB: Q5S007]
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  • MAPK interacting serine/threonine kinase 2/MAP kinase signal-integrating kinase 2 in Human [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9]
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  • mitogen-activated protein kinase kinase kinase 9/Mitogen-activated protein kinase kinase kinase 9 in Human [ChEMBL: CHEMBL2872] [GtoPdb: 2084] [UniProtKB: P80192]
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  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
leucine rich repeat kinase 2/Leucine-rich repeat serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075104] [GtoPdb: 2059] [UniProtKB: Q5S007]
GtoPdb - - 8.52 pKi 3 nM Ki J Med Chem (2012) 55: 5536-45 [PMID:22591441]
ChEMBL Inhibition of LRRK2 B 8.52 pKi 3 nM Ki J. Med. Chem. (2012) 55: 5536-5545 [PMID:22591441]
ChEMBL Inhibition of LRRK2 using FAM-LRRKtide as substrate after 120 mins by microfluidic capillary electrophoresis assay B 8.52 pKi 3 nM Ki J. Med. Chem. (2012) 55: 9416-9433 [PMID:22985112]
ChEMBL Inhibition of LRRK2 A2016T mutant expressed in HEK293 cells using nictide as substrate and [gamma32P]ATP after 15 mins by Cerenkov counting method B 6.81 pIC50 153.7 nM IC50 ACS Med. Chem. Lett. (2012) 3: 658-662 [PMID:23066449]
ChEMBL Inhibition of LRRK2 G2019S/A2016T mutant expressed in HEK293 cells using nictide as substrate and [gamma32P]ATP after 15 mins by Cerenkov counting method B 7.02 pIC50 95.9 nM IC50 ACS Med. Chem. Lett. (2012) 3: 658-662 [PMID:23066449]
ChEMBL Inhibition of autophosphorylation of LRRK2 in human HEK293 cells B 7.54 pIC50 29 nM IC50 J. Med. Chem. (2012) 55: 9416-9433 [PMID:22985112]
GtoPdb Inhibition of LRRK2G2019S in vitro - 7.61 pIC50 24.3 nM IC50 chemrxiv (2022) :
ChEMBL Inhibition of LRRK2 expressed in HEK293 cells using nictide as substrate and [gamma32P]ATP after 15 mins by Cerenkov counting method B 7.69 pIC50 20.3 nM IC50 ACS Med. Chem. Lett. (2012) 3: 658-662 [PMID:23066449]
GtoPdb Inhibition of WT hLRRK2 in vitro - 7.91 pIC50 12.4 nM IC50 chemrxiv (2022) :
ChEMBL Inhibition of LRRK2 G2019S mutant expressed in HEK293 cells using nictide as substrate and [gamma32P]ATP after 15 mins by Cerenkov counting method B 8.49 pIC50 3.2 nM IC50 ACS Med. Chem. Lett. (2012) 3: 658-662 [PMID:23066449]
ChEMBL Inhibition of LRRK2 G2019S mutant (unknown origin) using biotinylated ezrin/radaxin/meosin peptide as substrate measured after 1 hr B 8.49 pIC50 3.2 nM IC50 Bioorg Med Chem Lett (2017) 27: 2520-2527 [PMID:28408230]
MAPK interacting serine/threonine kinase 2/MAP kinase signal-integrating kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9]
ChEMBL Inhibition of MNK2 by radiometric assay B 6.22 pIC50 600 nM IC50 ACS Med. Chem. Lett. (2012) 3: 658-662 [PMID:23066449]
mitogen-activated protein kinase kinase kinase 9/Mitogen-activated protein kinase kinase kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2872] [GtoPdb: 2084] [UniProtKB: P80192]
ChEMBL Inhibition of MLK1 by radiometric assay B 5.68 pIC50 2100 nM IC50 ACS Med. Chem. Lett. (2012) 3: 658-662 [PMID:23066449]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
GtoPdb - - 5.49 pKi >3200 nM Ki J Med Chem (2012) 55: 5536-45 [PMID:22591441]
ChEMBL Inhibition of JAK2 B 5.49 pKi >3200 nM Ki J. Med. Chem. (2012) 55: 5536-5545 [PMID:22591441]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]