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

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ChEMBL ligand: CHEMBL848 (CC-5013, CDC-501, Lenalidomide, NSC-747972, Revlimid, SYP-1512)
  • bromodomain containing 4/Bromodomain-containing protein 4 in Human [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
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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
bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
ChEMBL Inhibition of BRD4 bromodomain 2 (unknown origin) in HEK293 cells cotransfected with eGFP by flow cytometry based mCherry reporter gene analysis B 5.28 pIC50 5190 nM IC50 ACS Med Chem Lett (2020) 11: 1088-1089 [PMID:32550984]
cereblon/Cereblon/Ikaros in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4296103] [GtoPdb: 3086] [UniProtKB: Q13422, 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 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]
ChEMBL Binding affinity to human CRBN-thalidomide binding domain expressed in Escherichia coli by measuring baseline corrected normalized fluorescence by MST based assay B 4.79 pKi 16300 nM Ki ACS Med Chem Lett (2021) 12: 74-81 [PMID:33488967]
ChEMBL Binding affinity to CBRN (unknown origin) incubated for 60 mins by lenalidomide displacement assay B 5.83 pKi 1490 nM Ki ACS Med Chem Lett (2020) 11: 1088-1089 [PMID:32550984]
ChEMBL Binding affinity to human CRBN-thalidomide binding domain expressed in Escherichia coli by measuring baseline corrected normalized fluorescence by MST based assay B 4.42 pIC50 37800 nM IC50 ACS Med Chem Lett (2021) 12: 74-81 [PMID:33488967]
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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]