ChEMBL ligand: CHEMBL188381 (GW806742X)
mixed lineage kinase domain like pseudokinase/Mixed lineage kinase domain-like protein in Human [ChEMBL: CHEMBL1938217] [GtoPdb: 2106] [UniProtKB: Q8NB16] mixed lineage kinase domain like pseudokinase/Mixed lineage kinase domain-like protein in Mouse [ChEMBL: CHEMBL5465354] [GtoPdb: 2106] [UniProtKB: Q9D2Y4] There should be some charts here, you may need to enable JavaScript!
receptor interacting serine/threonine kinase 1/Receptor-interacting serine/threonine-protein kinase 1 in Human [ChEMBL: CHEMBL5464] [GtoPdb: 2189] [UniProtKB: Q13546] There should be some charts here, you may need to enable JavaScript!
receptor interacting serine/threonine kinase 3/Receptor-interacting serine/threonine-protein kinase 3 in Human [ChEMBL: CHEMBL1795199] [GtoPdb: 2191] [UniProtKB: Q9Y572] 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!
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] 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
mixed lineage kinase domain like pseudokinase/Mixed lineage kinase domain-like protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938217] [GtoPdb: 2106] [UniProtKB: Q8NB16]
GtoPdb	Surface plasmon resonance (SPR) assay.	-	5.03	pKd	9300	nM	Kd	Proc Natl Acad Sci USA (2014) 111: 15072-7 [PMID:25288762]
ChEMBL	Binding affinity to MLKL (unknown origin)	B	5.03	pKd	9300	nM	Kd	J Med Chem (2020) 63: 1490-1510 [PMID:31622096]
ChEMBL	Binding affinity to full length human MLKL pseudokinase domain by Kinomescan method	B	6.28	pKd	530	nM	Kd	J Med Chem (2022) 65: 14971-14999 [PMID:36346971]
ChEMBL	Binding affinity to full length MLKL (unknown origin) expressed in human HEK293 cells assessed as dissociation constant incubated for 30 mins by Competition Binding Assay	B	6.28	pKd	530	nM	Kd	J Med Chem (2023) 66: 2361-2385 [PMID:36781172]
ChEMBL	Binding affinity to full length human MLKL assessed as dissociation constant	B	6.28	pKd	530	nM	Kd	J Med Chem (2023) 66: 2361-2385 [PMID:36781172]
GtoPdb	Inhibition of TSQ-induced necroptosis in cellular assays.	-	7	pIC50	100	nM	IC50	Proc Natl Acad Sci USA (2014) 111: 15072-7 [PMID:25288762]
mixed lineage kinase domain like pseudokinase/Mixed lineage kinase domain-like protein in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5465354] [GtoPdb: 2106] [UniProtKB: Q9D2Y4]
ChEMBL	Binding affinity to recombinant mouse MLKL pseudokinase domain (179 to 464 residues) expressed in Sf21 insect cells assessed as dissociation constant by Surface plasmon resonance assay	B	5.03	pKd	9300	nM	Kd	J Med Chem (2023) 66: 2361-2385 [PMID:36781172]
receptor interacting serine/threonine kinase 1/Receptor-interacting serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5464] [GtoPdb: 2189] [UniProtKB: Q13546]
ChEMBL	Binding affinity to RIPK1 (unknown origin) by Kinomescan method	B	7.19	pKd	64	nM	Kd	J Med Chem (2022) 65: 14971-14999 [PMID:36346971]
ChEMBL	Binding affinity to RIPK1 (unknown origin) assessed as dissociation constant	B	7.19	pKd	64	nM	Kd	J Med Chem (2023) 66: 2361-2385 [PMID:36781172]
receptor interacting serine/threonine kinase 3/Receptor-interacting serine/threonine-protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795199] [GtoPdb: 2191] [UniProtKB: Q9Y572]
ChEMBL	Binding affinity to RIPK3 (unknown origin) by Kinomescan method	B	6.17	pKd	680	nM	Kd	J Med Chem (2022) 65: 14971-14999 [PMID:36346971]
ChEMBL	Binding affinity to RIPK3 (unknown origin) assessed as dissociation constant	B	6.17	pKd	680	nM	Kd	J Med Chem (2023) 66: 2361-2385 [PMID:36781172]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL	Further kinetic evaluation of compounds supplied by Sanofi against AuroraA within a BIAcore3000 instrument	B	4.9	pKd	12461.05	nM	Kd	K4DD drug target binding kinetics data
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL	Inhibitory concentration against human VEGFR2 kinase	B	8.7	pIC50	2	nM	IC50	Bioorg Med Chem Lett (2005) 15: 3519-3523 [PMID:15990302]
GtoPdb	-	-	8.7	pIC50	2	nM	IC50	Bioorg Med Chem Lett (2005) 15: 3519-23 [PMID:15990302]

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]