Reaction Details Report a problem with these data
Target
DNA damage-binding protein 1/Protein cereblon
Ligand
BDBM65497
Substrate
n/a
Meas. Tech.
TR-FRET cereblon binding assay
pH
7±n/a
IC50
60±0 nM
Comments
extracted
Citation
 Matyskiela, ME; Zhang, W; Man, HW; Muller, G; Khambatta, G; Baculi, F; Hickman, M; LeBrun, L; Pagarigan, B; Carmel, G; Lu, CC; Lu, G; Riley, M; Satoh, Y; Schafer, P; Daniel, TO; Carmichael, J; Cathers, BE; Chamberlain, PP A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos. J Med Chem 61:535-542 (2017) [PubMed]  Article 
Target
Name:
DNA damage-binding protein 1/Protein cereblon
Synonyms:
CRBN-DDB1 | CRBN-DDB1 complex | Cereblon_DDB1 | Protein cereblon/DNA damage-binding protein 1
Type:
Enzyme
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
DNA damage-binding protein 1
Synonyms:
DDB p127 subunit | DDB1 | DDB1_HUMAN | DDBa | DNA damage-binding protein a | Damage-specific DNA-binding protein 1 | HBV X-associated protein 1 | UV-DDB 1 | UV-damaged DNA-binding factor | UV-damaged DNA-binding protein 1 | XAP-1 | XAP1 | XPCe | XPE-BF | XPE-binding factor | Xeroderma pigmentosum group E-complementing protein
Type:
Protein
Mol. Mass.:
126936.22
Organism:
Homo sapiens (Human)
Description:
Q16531
Residue:
1140
Sequence:
MSYNYVVTAQKPTAVNGCVTGHFTSAEDLNLLIAKNTRLEIYVVTAEGLRPVKEVGMYGKIAVMELFRPKGESKDLLFILTAKYNACILEYKQSGESIDIITRAHGNVQDRIGRPSETGIIGIIDPECRMIGLRLYDGLFKVIPLDRDNKELKAFNIRLEELHVIDVKFLYGCQAPTICFVYQDPQGRHVKTYEVSLREKEFNKGPWKQENVEAEASMVIAVPEPFGGAIIIGQESITYHNGDKYLAIAPPIIKQSTIVCHNRVDPNGSRYLLGDMEGRLFMLLLEKEEQMDGTVTLKDLRVELLGETSIAECLTYLDNGVVFVGSRLGDSQLVKLNVDSNEQGSYVVAMETFTNLGPIVDMCVVDLERQGQGQLVTCSGAFKEGSLRIIRNGIGIHEHASIDLPGIKGLWPLRSDPNRETDDTLVLSFVGQTRVLMLNGEEVEETELMGFVDDQQTFFCGNVAHQQLIQITSASVRLVSQEPKALVSEWKEPQAKNISVASCNSSQVVVAVGRALYYLQIHPQELRQISHTEMEHEVACLDITPLGDSNGLSPLCAIGLWTDISARILKLPSFELLHKEMLGGEIIPRSILMTTFESSHYLLCALGDGALFYFGLNIETGLLSDRKKVTLGTQPTVLRTFRSLSTTNVFACSDRPTVIYSSNHKLVFSNVNLKEVNYMCPLNSDGYPDSLALANNSTLTIGTIDEIQKLHIRTVPLYESPRKICYQEVSQCFGVLSSRIEVQDTSGGTTALRPSASTQALSSSVSSSKLFSSSTAPHETSFGEEVEVHNLLIIDQHTFEVLHAHQFLQNEYALSLVSCKLGKDPNTYFIVGTAMVYPEEAEPKQGRIVVFQYSDGKLQTVAEKEVKGAVYSMVEFNGKLLASINSTVRLYEWTTEKELRTECNHYNNIMALYLKTKGDFILVGDLMRSVLLLAYKPMEGNFEEIARDFNPNWMSAVEILDDDNFLGAENAFNLFVCQKDSAATTDEERQHLQEVGLFHLGEFVNVFCHGSLVMQNLGETSTPTQGSVLFGTVNGMIGLVTSLSESWYNLLLDMQNRLNKVIKSVGKIEHSFWRSFHTERKTEPATGFIDGDLIESFLDISRPKMQEVVANLQYDDGSGMKREATADDLIKVVEELTRIH
  
Component 2
Name:
Protein cereblon
Synonyms:
CRBN | CRBN_HUMAN | Protein cereblon
Type:
PROTEIN
Mol. Mass.:
50537.73
Organism:
Homo sapiens (Human)
Description:
ChEMBL_116917
Residue:
442
Sequence:
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTSLCCKQCQETEITTKNEIFSLSLCGPMAAYVNPHGYVHETLTVYKACNLNLIGRPSTEHSWFPGYAWTVAQCKICASHIGWKFTATKKDMSPQKFWGLTRSALLPTIPDTEDEISPDKVILCL
  
Inhibitor
Name:
BDBM65497
Synonyms:
CC-220 (Compound 6) | US9694015, 6.4S
Type:
Small organic molecule
Emp. Form.:
C25H27N3O5
Mol. Mass.:
449.499
SMILES:
O=C1N(Cc2c1cccc2OCc1ccc(CN2CCOCC2)cc1)[C@H]1CCC(=O)NC1=O
Structure:
Search PDB for entries with ligand similarity: