ChEMBL ligand: CHEMBL2140523
cyclin dependent kinase 2/CDK2/Cyclin A2 in Human [ChEMBL: CHEMBL3038469] [GtoPdb: 1973] [UniProtKB: P20248, P24941] There should be some charts here, you may need to enable JavaScript!
TTK protein kinase/Dual specificity protein kinase TTK in Human [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981] There should be some charts here, you may need to enable JavaScript!
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] 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
cyclin dependent kinase 2/CDK2/Cyclin A2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038469] [GtoPdb: 1973] [UniProtKB: P20248, P24941]
ChEMBL	Inhibition of full length CDK2/Cyclin A (unknown origin) using 5FAMQSPKKG-CONH2 as substrate after 60 mins by fluorescence assay	B	4.44	pIC50	36000	nM	IC50	J Med Chem (2013) 56: 10045-10065 [PMID:24256217]
TTK protein kinase/Dual specificity protein kinase TTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981]
ChEMBL	Inhibition of human full-length N-terminal GST-tagged MPS1 using FITC-labeled peptide as substrate incubated for 1 hr by Fluorescence based analysis	B	4.46	pIC50	35000	nM	IC50	J Med Chem (2016) 59: 9305-9320 [PMID:27559828]
ChEMBL	Inhibition of Myc-tagged wild type MPS1 autophosphorylation in human HCT116 cells after 2 hrs in presence of proteosome inhibitor MG132	B	6.14	pIC50	720	nM	IC50	J Med Chem (2013) 56: 10045-10065 [PMID:24256217]
ChEMBL	Displacement of tracer K9 from NanoLuc-fused MPS1 (unknown origin) expressed in HEK293T cells measured after 2 hrs by NanoBRET assay	B	6.37	pIC50	429	nM	IC50	J Med Chem (2022) 65: 3173-3192 [PMID:35167750]
ChEMBL	Inhibition of N-terminal GST-tagged full-length human Mps1 expressed in insect cells using FITC-DHTGFLTEYVATR-CONH2 as substrate after 25 mins by fluorescence assay	B	7.46	pIC50	35	nM	IC50	Eur J Med Chem (2019) 175: 247-268 [PMID:31121430]
ChEMBL	Inhibition of Mps1 (unknown origin) pretreated for 10 mins followed by substrate addition and measured after 60 mins in presence of ATP by ADP-glo kinase assay	B	7.46	pIC50	35	nM	IC50	Eur J Med Chem (2023) 253: 115334-115334 [PMID:37037136]
ChEMBL	Inhibition of GST-fused full length human TTK compound pre-incubated for 15 mins prior ATP addition by MBP-based assay	B	7.46	pIC50	35	nM	IC50	Bioorg Med Chem (2014) 22: 4968-4997 [PMID:25043312]
ChEMBL	Inhibition of human His-tagged TTK (510 to 857)-mediated MBP phosphorylation after 20 mins by scintillation counting analysis in presence of gamma-[32P]ATP	B	7.46	pIC50	35	nM	IC50	J Med Chem (2015) 58: 3366-3392 [PMID:25763473]
GtoPdb	In vitro assay using a His-tagged catalytic domain fragment of MPS1 (amino acids 510–857).	-	7.46	pIC50	~35	nM	IC50	J Cell Biol (2010) 190: 25-34 [PMID:20624899]
ChEMBL	Inhibition of recombinant human full length N-terminal GST-fused MPS1 (1 to 857 residues) using histone H3 as substrate by TR-FRET assay	B	8.01	pIC50	9.79	nM	IC50	J Med Chem (2022) 65: 3173-3192 [PMID:35167750]
ChEMBL	Inhibition of N-terminal 6XHis-tagged/GST-tagged full length human MPS1 expressed in recombinant baculovirus infected sf9 insect cells using 5FAM-DHTGFLTEYVATRCONH2 as substrate after 60 to 90 mins by fluorescence assay	B	8.15	pIC50	7	nM	IC50	J Med Chem (2013) 56: 10045-10065 [PMID:24256217]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL	Inhibition of N-terminal His-tagged Aurora A (unknown origin) using 5FAM-LRRASLG-CONH2 as substrate after 60 mins by fluorescence assay	B	4.68	pIC50	21000	nM	IC50	J Med Chem (2013) 56: 10045-10065 [PMID:24256217]

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]