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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

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]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • Cereblon isoform 4 in Magnetospirillum gryphiswaldense [ChEMBL: CHEMBL3763007] [UniProtKB: A4TVL0]
There should be some charts here, you may need to enable JavaScript!
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
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 32:

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]