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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 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]