ChEMBL ligand: CHEMBL2170016
leucine rich repeat kinase 2/Leucine-rich repeat serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL1075104] [GtoPdb: 2059] [UniProtKB: Q5S007] There should be some charts here, you may need to enable JavaScript!
MAPK interacting serine/threonine kinase 2/MAP kinase signal-integrating kinase 2 in Human [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase kinase 9/Mitogen-activated protein kinase kinase kinase 9 in Human [ChEMBL: CHEMBL2872] [GtoPdb: 2084] [UniProtKB: P80192] There should be some charts here, you may need to enable JavaScript!
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] There should be some charts here, you may need to enable JavaScript!

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 35:

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]