ChEMBL ligand: CHEMBL4452233

receptor interacting serine/threonine kinase 1/Receptor-interacting serine/threonine-protein kinase 1 in Human [ChEMBL: CHEMBL5464] [GtoPdb: 2189] [UniProtKB: Q13546] receptor interacting serine/threonine kinase 1/Receptor-interacting serine/threonine-protein kinase 1 in Mouse [ChEMBL: CHEMBL3784911] [GtoPdb: 2189] [UniProtKB: Q60855] 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
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 RIP1 (unknown origin) by fluorescence polarization assay	B	7.7	pIC50	19.95	nM	IC50	ACS Med Chem Lett (2018) 9: 1160-1161 [PMID:30613318]
GtoPdb	Inhibition of enzyme activity of recombinant human RIPK1 (aa 1 to 375)	-	8.2	pIC50	6.3	nM	IC50	ACS Med Chem Lett (2019) 10: 857-862 [PMID:31223438]
ChEMBL	Inhibition of RIP1 in human U937 cells assessed as reduction in necroptosis incubated for 24 hrs by cell titer-glo luminescent cell viability assay	B	8.2	pIC50	6.3	nM	IC50	ACS Med Chem Lett (2019) 10: 857-862 [PMID:31223438]
ChEMBL	Inhibition of pDEST8HisGSTTev-tagged human RIP1 (1 to 375 residues) expressed in baculovirus infected insect cells preincubated with enzyme for 1 hr followed by ATP addition and measured after 5 hrs by ADP-Glo kinase assay	B	8.2	pIC50	6.3	nM	IC50	ACS Med Chem Lett (2019) 10: 857-862 [PMID:31223438]
ChEMBL	Inhibition of RIP1 in human whole blood assessed as inhibition of TNF-alpha/QVD-Oph/RMT5265-stimulated MIP-1 beta cytokine overproduction incubated for 6 hrs by sandwich ELISA	B	8.3	pIC50	5	nM	IC50	ACS Med Chem Lett (2019) 10: 857-862 [PMID:31223438]
ChEMBL	Inhibition of RIP1 in human neutrophils assessed as inhibition of TNF-alpha/QVD-Oph/RMT5265-stimulated necroptosis by measuring cellular ATP levels measured at 21 hrs post stimulation by cell-Titer Glo luminescent cell viability assay	B	8.8	pIC50	1.6	nM	IC50	ACS Med Chem Lett (2019) 10: 857-862 [PMID:31223438]
GtoPdb	Cellular activity: inhibition of TNFα-induced necroptosis of human neutrophils	-	9.3	pIC50	0.5	nM	IC50	ACS Med Chem Lett (2019) 10: 857-862 [PMID:31223438]
ChEMBL	Inhibition of RIP1 in human neutrophils assessed as inhibition of TNF-alpha/QVD-Oph/RMT5265-stimulated necroptosis by measuring LDH release measured at 21 hrs post stimulation by LDH assay	B	9.3	pIC50	0.5	nM	IC50	ACS Med Chem Lett (2019) 10: 857-862 [PMID:31223438]
ChEMBL	Inhibition of RIP1 in human neutrophils assessed as inhibition of TNF-alpha/QVD-Oph/RMT5265-stimulated MIP-1 beta cytokine overproduction measured at 21 hrs post stimulation by sandwich ELISA	B	9.4	pIC50	0.4	nM	IC50	ACS Med Chem Lett (2019) 10: 857-862 [PMID:31223438]
ChEMBL	Inhibition of RIP1 in human neutrophils assessed as inhibition of TNF-alpha/QVD-Oph/RMT5265-stimulated MIP-1 beta mRNA overexpression measured at 21 hrs post-stimulation	B	9.4	pIC50	0.4	nM	IC50	ACS Med Chem Lett (2019) 10: 857-862 [PMID:31223438]
receptor interacting serine/threonine kinase 1/Receptor-interacting serine/threonine-protein kinase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3784911] [GtoPdb: 2189] [UniProtKB: Q60855]
ChEMBL	Inhibition of RIP1 in mouse L929 cells assessed as reduction in necroptosis incubated for 24 hrs by cell titer-glo luminescent cell viability assay	B	5.89	pIC50	1300	nM	IC50	ACS Med Chem Lett (2019) 10: 857-862 [PMID:31223438]

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]