lenalidomide [Ligand Id: 7331] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL848 (Lenalidomide, SYP-1512, CDC-501, CC-5013, Revlimid)
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  • Cereblon isoform 4 in Magnetospirillum gryphiswaldense [ChEMBL: CHEMBL3763007] [UniProtKB: A4TVL0]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
cereblon/Cereblon/Ikaros in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4296103] [GtoPdb: 3086] [UniProtKB: Q13422Q96SW2]
GtoPdb Measuring displacement of a Cy5-conjugated cereblon modulating compound from the binding pocket of CRBN by lenalidomide. - 5.82 pIC50 1500 nM IC50 J Med Chem (2018) 61: 535-542 [PMID:28425720]
ChEMBL Induction of cereblon-mediated ikaros degradation in human DF15 cells expressing ePL-tagged ikaros after 4 hrs by luminometric analysis B 7.17 pEC50 67 nM EC50 J Med Chem (2018) 61: 535-542 [PMID:28425720]
Cereblon isoform 4 in Magnetospirillum gryphiswaldense (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3763007] [UniProtKB: A4TVL0]
ChEMBL Inhibition of MANT-uracil binding to wild-type Magnetospirillum gryphiswaldense CRBN isoform 4 by FRET assay B 5.51 pKi 3100 nM Ki J Med Chem (2019) 62: 6615-6629 [PMID:31251063]
cereblon/Protein cereblon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3763008] [GtoPdb: 3086] [UniProtKB: Q96SW2]
GtoPdb Measuring displacement of a Cy5-conjugated cereblon modulating compound from the binding pocket of CRBN by lenalidomide. - 5.82 pIC50 1500 nM IC50 J Med Chem (2018) 61: 535-542 [PMID:28425720]
ChEMBL Displacement of cy5-conjugated 2-((1E,3E,5Z)-5-(1-(6-((4-(2-((2-(2,6-Dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)oxy)acetamido)butyl)amino)-6-oxohexyl)-3,3-dimethylindolin-2-ylidene)penta-1,3-dien-1-yl)-1,3,3-trimethyl-3H-indol-1-ium from DDB1-fused human full length 6xHis-tagged CRBN expressed in Sf9 insect cells after 10 mins by TR-FRET assay B 5.82 pIC50 1500 nM IC50 J Med Chem (2018) 61: 535-542 [PMID:28425720]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]