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

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ChEMBL ligand: CHEMBL848 (CC-5013, CDC-501, Lenalidomida, Lenalidomide, Lenalidomide accord, Lenalidomide mylan, 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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  • Glyceraldehyde-3-phosphate dehydrogenase, cytosolic in Leishmania mexicana [ChEMBL: CHEMBL4137] [UniProtKB: Q01558]
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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]
Glyceraldehyde-3-phosphate dehydrogenase, cytosolic in Leishmania mexicana (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4137] [UniProtKB: Q01558]
ChEMBL cytomteric bead array (CBA) assay: The Fix buffer I was warmed up to 37° C. in an incubator or water bath prior to use. The Perm Buffer III was chilled in a â¿¿20° C. freezer prior to use. The cells were collected at the end of treatment with testing compounds. One volume of the pre-warmed Fix Buffer I was mixed with one volume of cell suspension. If the volume of the cell suspension is greater than 100 uL, the cells were spun and resuspended in 100 uL medium or PBS. The buffer and the cell suspension were mixed well and incubated in a 37° C. water bath for 10 min. The cells were spun down at 250ÿg for 10 min and the supernatant was aspirated. The cells were washed once with BD Stain Buffer. The pellet was spun and the supernatant was removed. The cells were vortexed to be loosened, and permeabilized by slowly adding cold Perm Buffer III while vortexing or mixing. Subsequently, the cells were incubated on ice for 30 min. The cells were then spun down and washed twice with Stain Buffer. The supernatant was spun and aspirated. The cells were resuspended in a small volume of Stain buffer (50 or 100 uL containing from 200,000 to 1 million cells). Anti-IKFZ3 antibody was added to the cell suspension at 1:1000 dilution and incubated for 45 min at 4° C. The cells were then spun down and washed once with stain buffer. Secondary antibody was added to the cells at 1:5000 dilution and incubated at room temperature for 20 min in the dark. The cells were washed once with stain buffer prior to analysis by FACS. B 5 pIC50 >10000 nM IC50 US-9694015-B2. Methods for the treatment of locally advanced breast cancer (2017)
Interleukin-1 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1909490] [UniProtKB: P01584]
ChEMBL cytomteric bead array (CBA) assay: The Fix buffer I was warmed up to 37° C. in an incubator or water bath prior to use. The Perm Buffer III was chilled in a â¿¿20° C. freezer prior to use. The cells were collected at the end of treatment with testing compounds. One volume of the pre-warmed Fix Buffer I was mixed with one volume of cell suspension. If the volume of the cell suspension is greater than 100 uL, the cells were spun and resuspended in 100 uL medium or PBS. The buffer and the cell suspension were mixed well and incubated in a 37° C. water bath for 10 min. The cells were spun down at 250ÿg for 10 min and the supernatant was aspirated. The cells were washed once with BD Stain Buffer. The pellet was spun and the supernatant was removed. The cells were vortexed to be loosened, and permeabilized by slowly adding cold Perm Buffer III while vortexing or mixing. Subsequently, the cells were incubated on ice for 30 min. The cells were then spun down and washed twice with Stain Buffer. The supernatant was spun and aspirated. The cells were resuspended in a small volume of Stain buffer (50 or 100 uL containing from 200,000 to 1 million cells). Anti-IKFZ3 antibody was added to the cell suspension at 1:1000 dilution and incubated for 45 min at 4° C. The cells were then spun down and washed once with stain buffer. Secondary antibody was added to the cells at 1:5000 dilution and incubated at room temperature for 20 min in the dark. The cells were washed once with stain buffer prior to analysis by FACS. B 6.41 pIC50 390 nM IC50 US-9694015-B2. Methods for the treatment of locally advanced breast cancer (2017)
cereblon/Protein cereblon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3763008] [GtoPdb: 3086] [UniProtKB: Q96SW2]
ChEMBL Binding affinity to CRBN (unknown origin) assessed as dissociation constant by TR-FRET assay B 6.75 pKd 178 nM Kd Eur J Med Chem (2024) 263: 115950-115950 [PMID:37984298]
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 human CRBN TBD assessed as inhibition constant using BODIPY-uracil as substrate by MST assay B 5.19 pKi 6400 nM Ki J Med Chem (2023) 66: 14513-14543 [PMID:37902300]
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 TBD: TBD B 5.83 pKi 1490 nM Ki US-11530219-B2. Ligands to cereblon (CRBN) (2022)
ChEMBL Binding affinity to GST-tagged wild-type human CRBN incubated for 3 hrs by TR-FRET assay B 6.1 pKi 800 nM Ki J Med Chem (2024) 67: 14125-14154 [PMID:39132814]
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]
ChEMBL Binding affinity to human CRBN TBD using BODIPY-uracil as substrate by MST assay B 4.72 pIC50 19000 nM IC50 J Med Chem (2023) 66: 14513-14543 [PMID:37902300]
ChEMBL TBD: TBD B 5.28 pIC50 5190 nM IC50 US-11530219-B2. Ligands to cereblon (CRBN) (2022)
ChEMBL Binding affinity to GST-tagged wild type human CRBN incubated for 3 hrs by TR-FRET assay B 5.44 pIC50 3600 nM IC50 J Med Chem (2023) 66: 12559-12585 [PMID:37647546]
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 Displacement of fluorescent tracer from NanoLuc-tagged CRBN (unknown origin) by NanoBRET assay B 6.41 pIC50 390 nM IC50 RSC Med Chem (2023) 14: 501-506 [PMID:36970148]
ChEMBL Inhibition of CRBN (unknown origin) measured after 60 mins incubation by BMG reader B 7.05 pIC50 88.99 nM IC50 J Med Chem (2024) 67: 2438-2465 [PMID:38321747]
Tumor necrosis factor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1825] [UniProtKB: P01375]
ChEMBL cytomteric bead array (CBA) assay: The Fix buffer I was warmed up to 37° C. in an incubator or water bath prior to use. The Perm Buffer III was chilled in a â¿¿20° C. freezer prior to use. The cells were collected at the end of treatment with testing compounds. One volume of the pre-warmed Fix Buffer I was mixed with one volume of cell suspension. If the volume of the cell suspension is greater than 100 uL, the cells were spun and resuspended in 100 uL medium or PBS. The buffer and the cell suspension were mixed well and incubated in a 37° C. water bath for 10 min. The cells were spun down at 250ÿg for 10 min and the supernatant was aspirated. The cells were washed once with BD Stain Buffer. The pellet was spun and the supernatant was removed. The cells were vortexed to be loosened, and permeabilized by slowly adding cold Perm Buffer III while vortexing or mixing. Subsequently, the cells were incubated on ice for 30 min. The cells were then spun down and washed twice with Stain Buffer. The supernatant was spun and aspirated. The cells were resuspended in a small volume of Stain buffer (50 or 100 uL containing from 200,000 to 1 million cells). Anti-IKFZ3 antibody was added to the cell suspension at 1:1000 dilution and incubated for 45 min at 4° C. The cells were then spun down and washed once with stain buffer. Secondary antibody was added to the cells at 1:5000 dilution and incubated at room temperature for 20 min in the dark. The cells were washed once with stain buffer prior to analysis by FACS. B 6.66 pIC50 220 nM IC50 US-9694015-B2. Methods for the treatment of locally advanced breast cancer (2017)
Zinc finger protein Aiolos in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4739707] [UniProtKB: Q9UKT9]
ChEMBL Induction of ePL tagged Aiolos degradation in human DF15 cells incubated for 4 hrs by luminescence based assay B 7.15 pEC50 70 nM EC50 J Med Chem (2023) 66: 16388-16409 [PMID:37991844]

ChEMBL data shown on this page come from version 36:

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]