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ChEMBL ligand: CHEMBL2170016 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 31:
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]