thalidomide [Ligand Id: 7327] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL468 (NSC-527179, Thalidomide, Thalidomide, NSC-66847, Thalomid, Talidex, K-17)
  • Cereblon isoform 4 in Magnetospirillum gryphiswaldense [ChEMBL: CHEMBL3763007] [UniProtKB: A4TVL0]
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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 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 data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]