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, Imnovid (previously pomalidomide celgene), Pomalidomida, 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 TBD assessed as inhibition constant using BODIPY-uracil as substrate by MST assay | B | 5.48 | pKi | 3300 | nM | Ki | J Med Chem (2023) 66: 14513-14543 [PMID:37902300] |
| 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] |
| ChEMBL | Binding affinity to human CRBN TBD using BODIPY-uracil as substrate by MST assay | B | 4.89 | pIC50 | 13000 | nM | IC50 | J Med Chem (2023) 66: 14513-14543 [PMID:37902300] |
| 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 | Displacement of fluorescent tracer from NanoLuc-tagged CRBN (unknown origin) by NanoBRET assay | B | 6.13 | pIC50 | 739 | nM | IC50 | RSC Med Chem (2023) 14: 501-506 [PMID:36970148] |
| ChEMBL | Inhibition of CRBN in HEK293 cells using NanoGlo substrate incubated for 2 hrs by NanoBRET assay | B | 7.08 | pIC50 | 83 | nM | IC50 | J Med Chem (2023) 66: 7454-7474 [PMID:37195170] |
| 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 | 7.7 | pEC50 | 20 | nM | EC50 | J Med Chem (2023) 66: 16388-16409 [PMID:37991844] |
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]
