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ChEMBL ligand: CHEMBL3109212 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | Inhibition of human N-terminal His-GST-TEV-fused RIP1 kinase domain (1 to 375) autophosphorylation expressed in baculovirus infected insect Sf9 cells after 4 hrs by ADP-Glo luminescence assay | B | 7.49 | pIC50 | 32 | nM | IC50 | ACS Med Chem Lett (2013) 4: 1238-1243 [PMID:24900635] |
ChEMBL | Inhibition of RIP1 (unknown origin) in ADP-glo assay | B | 7.49 | pIC50 | 32 | nM | IC50 | J Med Chem (2022) 65: 14971-14999 [PMID:36346971] |
ChEMBL | Inhibition of RIP1 in human U937 cells assessed as prevention of TNFalpha/zVAD.fmk-induced necrotic cell death preincubated for 30 to 60 mins followed by TNF-alpha induction measured after overnight incubation by Cell Titer-Glo luminescence assay | B | 7.8 | pIC50 | 16 | nM | IC50 | ACS Med Chem Lett (2013) 4: 1238-1243 [PMID:24900635] |
ChEMBL | Displacement of (14-(2-{[3-({2-{[4-(cyanomethyl)phenyl]amino}-6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-4-pyrimidinyl}amino)propyl]amino}-2-oxoethyl)-16,16,18,18-tetramethyl-6,7,7a,8a,9,10,16,18-octahydrobenzo[2'',3'']indolizino[8'',7'':5',6']pyrano[3',2':3,4]pyrido[1,2-a]indol-5-ium-2-sulfonate from human N-terminal His-GST-TEV-fused RIP1 kinase domain (1 to 375) expressed in baculovirus infected insect Sf9 cells preincubated for 10 mins followed by fluorescent ligand addition measured after 15 mins by fluorescence polarization assay | B | 8.89 | pIC50 | 1.3 | nM | IC50 | ACS Med Chem Lett (2013) 4: 1238-1243 [PMID:24900635] |
ChEMBL | Inhibition of RIP1 (unknown origin) by fluorescence polarization assay | B | 8.89 | pIC50 | 1.3 | nM | IC50 | J Med Chem (2022) 65: 14971-14999 [PMID:36346971] |
GtoPdb | - | - | 8.89 | pIC50 | 1.3 | nM | IC50 | ACS Med Chem Lett (2013) 4: 1238-43 [PMID:24900635] |
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]