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: CHEMBL468 (.alpha.-phthalimidoglutarimide, Celgene, Contergan, Distaval, K-17, Myrin, Neurosedyn, N-phthalylglutamic acid imide, NSC-527179, NSC-66847, Pantosediv, Pharmion, Softenon, Talidex, Thaled, Thalidomide, Thalidomide, Thalomid) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 |
---|---|---|---|---|---|---|---|---|
Cereblon isoform 4 in Magnetospirillum gryphiswaldense (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3763007] [UniProtKB: A4TVL0] | ||||||||
ChEMBL | Inhibition of MANT-uracil binding to Magnetospirillum gryphiswaldense cereblon isoform 4 Y101F mutant by Cheng-Prusoff equation analysis | B | 5.02 | pKi | 9600 | nM | Ki | J Med Chem (2016) 59: 770-774 [PMID:26730808] |
ChEMBL | Inhibition of MANT-uracil binding to wild type Magnetospirillum gryphiswaldense cereblon isoform 4 by Cheng-Prusoff equation analysis | B | 5.36 | pKi | 4400 | nM | Ki | J Med Chem (2016) 59: 770-774 [PMID:26730808] |
ChEMBL | Inhibition of MANT-uracil binding to wild-type Magnetospirillum gryphiswaldense CRBN isoform 4 by FRET assay | B | 5.36 | pKi | 4400 | nM | Ki | J Med Chem (2019) 62: 6615-6629 [PMID:31251063] |
ChEMBL | Inhibition of MANT-uracil binding to Magnetospirillum gryphiswaldense cereblon isoform 4 Y101F mutant by FRET assay | B | 4.97 | pIC50 | 10700 | nM | IC50 | J Med Chem (2016) 59: 770-774 [PMID:26730808] |
ChEMBL | Inhibition of MANT-uracil binding to wild type Magnetospirillum gryphiswaldense cereblon isoform 4 by FRET assay | B | 5.11 | pIC50 | 7800 | nM | IC50 | J Med Chem (2016) 59: 770-774 [PMID:26730808] |
Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979] | ||||||||
ChEMBL | Inhibitory activity (RA1) against Prostaglandin G/H synthase 1 was calculated relative to aspirin | B | 6.43 | pIC50 | 370 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1043-1046 [PMID:11909713] |
Cyclooxygenase-2 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4102] [UniProtKB: P79208] | ||||||||
ChEMBL | Inhibitory activity (RA2) against Prostaglandin G/H synthase 2 was calculated relative to aspirin | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1043-1046 [PMID:11909713] |
cereblon/Protein cereblon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3763008] [GtoPdb: 3086] [UniProtKB: Q96SW2] | ||||||||
GtoPdb | Determined in a BiaCore assay using immobilised thalidomide and recombinant cereblon protein. | - | 8.07 | pKd | 8.5 | nM | Kd | Science (2010) 327: 1345-50 [PMID:20223979] |
ChEMBL | Inhibition of MANT-uracil binding to human CRBN (delta 1 to 315) by Cheng-Prusoff equation analysis | B | 4.64 | pKi | 22700 | nM | Ki | J Med Chem (2016) 59: 770-774 [PMID:26730808] |
ChEMBL | Binding affinity to human CRBN-thalidomide binding domain expressed in Escherichia coli by measuring baseline corrected normalized fluorescence in presence of 0.5% DMSO by MST based assay | B | 5.07 | pKi | 8510 | nM | Ki | ACS Med Chem Lett (2021) 12: 74-81 [PMID:33488967] |
ChEMBL | Inhibition of MANT-uracil binding to human CRBN (delta 1 to 315) by FRET assay | B | 4.52 | pIC50 | 29900 | nM | IC50 | J Med Chem (2016) 59: 770-774 [PMID:26730808] |
ChEMBL | Binding affinity to human CRBN-thalidomide binding domain expressed in Escherichia coli by measuring baseline corrected normalized fluorescence in presence of 0.5% DMSO by MST based assay | B | 4.64 | pIC50 | 22900 | nM | IC50 | ACS Med Chem Lett (2021) 12: 74-81 [PMID:33488967] |
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]