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ChEMBL ligand: CHEMBL848 (CC-5013, CDC-501, Lenalidomide, NSC-747972, Revlimid, SYP-1512) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | 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 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]