ChEMBL ligand: CHEMBL2178134
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!
TTK protein kinase in Human [GtoPdb: 2264] [UniProtKB: P33981] 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]
ChEMBL	LabChip Assay: This assay was used to determine a compound's potency in inhibiting activity of LRRK2 by determining, Kiapp, IC50, or percent inhibition values. In a polypropylene plate, LRRK2, fluorescently-labeled peptide substrate, ATP and test compound were incubated together. Using a LabChip 3000 (Caliper Life Sciences), after the reaction the substrate was separated by capillary electrophoresis into two populations: phosphorylated and unphosphorylated. The relative amounts of each were quantitated by fluorescence intensity.	B	8.7	pKi	2	nM	Ki	US-8802674-B2. Aminopyrimidine derivatives as LRRK2 modulators (2014)
GtoPdb	-	-	9	pKi	1	nM	Ki	J Med Chem (2014) 57: 921-36 [PMID:24354345]
ChEMBL	Inhibition of LRRK2 using FAM-LRRKtide as substrate after 120 mins by microfluidic capillary electrophoresis assay	B	9	pKi	1	nM	Ki	J Med Chem (2012) 55: 9416-9433 [PMID:22985112]
ChEMBL	Inhibition of LRRK2 G2019S mutant (unknown origin)	B	9	pKi	1	nM	Ki	J Med Chem (2020) 63: 11330-11361 [PMID:32352776]
ChEMBL	Inhibition of recombinant human wild type GST-tagged LRRK2 (970 to 2527 residues) preincubated for 30 mins followed by fluorescein-LRRKtide substrate addition after 2 hrs by TR-FRET assay	B	7.01	pIC50	97	nM	IC50	Bioorg Med Chem Lett (2017) 27: 4500-4505 [PMID:28802631]
ChEMBL	Inhibition of recombinant human LRRK2 (970 to 2527 residues) G2019S mutant expressed in baculovirus preincubated for 30 mins followed by fluorescein-LRRKtide substrate addition after 2 hrs by TR-FRET assay	B	7.34	pIC50	46	nM	IC50	Bioorg Med Chem Lett (2017) 27: 4500-4505 [PMID:28802631]
ChEMBL	Inhibition of autophosphorylation of LRRK2 in human HEK293 cells	B	8.05	pIC50	9	nM	IC50	J Med Chem (2012) 55: 9416-9433 [PMID:22985112]
ChEMBL	Inhibition of LRRK2 (unknown origin) phosphorylation	B	8.05	pIC50	9	nM	IC50	Eur J Med Chem (2023) 256: 115475-115475 [PMID:37201428]
GtoPdb	Inhibition of autophosphorylation in a cellular assay.	-	8.05	pIC50	9	nM	IC50	J Med Chem (2014) 57: 921-36 [PMID:24354345]
ChEMBL	Inhibition of LRRK2 G2019S mutant (unknown origin)	B	9	pIC50	1	nM	IC50	Eur J Med Chem (2023) 256: 115475-115475 [PMID:37201428]
TTK protein kinase in Human [GtoPdb: 2264] [UniProtKB: P33981]
GtoPdb	-	-	7.28	pKi	53	nM	Ki	J Med Chem (2014) 57: 921-36 [PMID:24354345]

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]