pomalidomide [Ligand Id: 7348] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL43452 (Actimid, CC-4047, IMID 3, IMID-3, Imnovid, Pomalidomide, Pomalyst) |
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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: Q13422, Q96SW2] | ||||||||
| GtoPdb | Measuring displacement of a Cy5-conjugated cereblon modulating compound from the binding pocket of CRBN by pomalidomide. | - | 5.92 | pIC50 | 1200 | 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 | 7.62 | pEC50 | 24 | 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 | 6.1 | pKi | 800 | nM | Ki | J Med Chem (2019) 62: 6615-6629 [PMID:31251063] |
| programmed cell death 1 (CD279)/Programmed cell death protein 1/Programmed cell death 1 ligand 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4523993] [GtoPdb: 2760] [UniProtKB: Q15116, Q9NZQ7] | ||||||||
| ChEMBL | Inhibition of PD-1/PDL1 protein-protein interaction (unknown origin) by HTRF assay | B | 8 | pIC50 | >10 | nM | IC50 | Eur J Med Chem (2020) 199: 112377-112377 [PMID:32388281] |
| 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 | 5 | pKi | 10000 | nM | Ki | ACS Med Chem Lett (2021) 12: 74-81 [PMID:33488967] |
| ChEMBL | Binding affinity to human CRBN-thalidomide binding domain expressed in Escherichia coli by measuring baseline corrected normalized fluorescence by MST based assay | B | 4.59 | pIC50 | 25800 | 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 pomalidomide. | - | 5.92 | pIC50 | 1200 | 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 | 5.92 | pIC50 | 1200 | 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]
