ChEMBL ligand: CHEMBL1825141
7,8-dihydro-8-oxoguanine triphosphatase in Human [ChEMBL: CHEMBL3708265] [UniProtKB: P36639] There should be some charts here, you may need to enable JavaScript!
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73] There should be some charts here, you may need to enable JavaScript!
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase kinase kinase 3/Mitogen-activated protein kinase kinase kinase kinase 3 in Human [ChEMBL: CHEMBL5432] [GtoPdb: 2087] [UniProtKB: Q8IVH8] 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
7,8-dihydro-8-oxoguanine triphosphatase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3708265] [UniProtKB: P36639]
ChEMBL	Binding affinity to recombinant His-tagged MTH1 isoform p18 (M1 to V156 residues) (unknown origin) assessed as dissociation constant by surface plasmon resonance analysis	B	7.41	pKd	39	nM	Kd	J Med Chem (2016) 59: 2346-2361 [PMID:26878898]
ChEMBL	Inhibition of recombinant C-terminal 6xHis-tagged MTH1 (3 to 156 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using dGTP as substrate measured after 30 mins by malachite green dye based inorganic phosphatase coupled absorbance assay	B	5.74	pIC50	1800	nM	IC50	Eur J Med Chem (2019) 167: 153-160 [PMID:30771603]
ChEMBL	Inhibition of His-tagged human MTH1 expressed in Escherichia coli BL21 (DE3) using 2-OH-dATP as substrate preincubated with protein followed by substrate addition measured over 15 mins by luminescence-based assay	B	6.39	pIC50	408	nM	IC50	Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261]
ChEMBL	Inhibition of human recombinant human His-tagged MTH1 expressed in Escherichia coli BL21 (DE3) using 8-oxo-dGTP as substrate incubated for 15 mins followed by substrate addition and measured after 3 hrs by PPiLight Inorganic Pyrophosphate assay kit method	B	6.44	pIC50	366	nM	IC50	ACS Med Chem Lett (2020) 11: 358-364 [PMID:32184970]
ChEMBL	Inhibition of His-tagged human MTH1 expressed in Escherichia coli BL21 (DE3) using 8-oxo-dGTP as substrate preincubated with protein followed by substrate addition measured over 15 mins by luminescence-based assay	B	6.48	pIC50	330	nM	IC50	Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261]
ChEMBL	Inhibition of recombinant human MTH1 expressed in Escherichia coli BL21 DE3 cells preincubated for 15 mins followed by 8-oxo-dGTP substrate addition measured after 15 mins by luminescence based assay	B	6.48	pIC50	330	nM	IC50	J Med Chem (2016) 59: 2343-2345 [PMID:26924380]
ChEMBL	Inhibition of human recombinant human His-tagged MTH1 expressed in Escherichia coli BL21 (DE3) using 8-oxo-dGTP as substrate incubated for 15 mins followed by substrate addition and measured after 15 mins by PPiLight Inorganic Pyrophosphate assay kit method	B	6.48	pIC50	330	nM	IC50	ACS Med Chem Lett (2020) 11: 358-364 [PMID:32184970]
ChEMBL	Inhibition of MTH1 (unknown origin) using 8-oxo-dGTP as substrate preincubated for 15 mins followed by substrate addition and measured after 20 mins by PPiLight detection reagent based luminescence assay	B	6.86	pIC50	138	nM	IC50	J Med Chem (2016) 59: 2346-2361 [PMID:26878898]
ChEMBL	Binding affinity to MTH1 in human K562 cells assessed as thermal stabilization preincubated for 30 mins followed by heating at 52 degree C for 3 mins by CETSA-based Western blot analysis	B	5.44	pEC50	3600	nM	EC50	J Med Chem (2016) 59: 2346-2361 [PMID:26878898]
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
ChEMBL	Binding affinity to ALK (unknown origin)	B	6.28	pKd	525	nM	Kd	Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261]
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
ChEMBL	Binding affinity to MET (unknown origin)	B	7.43	pKd	37.5	nM	Kd	Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261]
ChEMBL	Binding affinity to human recombinant c-MET assessed as inhibition of autophosphorylation by continuous fluorometric assay	B	6.79	pKi	161	nM	Ki	J Med Chem (2011) 54: 6342-6363 [PMID:21812414]
mitogen-activated protein kinase kinase kinase kinase 3/Mitogen-activated protein kinase kinase kinase kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5432] [GtoPdb: 2087] [UniProtKB: Q8IVH8]
ChEMBL	Inhibition of GLK (unknown origin) by alphascreen assay	B	6.17	pIC50	680	nM	IC50	Bioorg Med Chem Lett (2018) 28: 1964-1971 [PMID:29636220]

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]