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Target
DNA damage-binding protein 1/Protein cereblon
Ligand
BDBM65454
Substrate
n/a
Meas. Tech.
Fluorescence thermal melt assay
pH
8±n/a
Temperature
343.15±n/a K
IC50
3000±0 nM
Comments
extracted
Citation
 Lopez-Girona, A; Mendy, D; Ito, T; Miller, K; Gandhi, AK; Kang, J; Karasawa, S; Carmel, G; Jackson, P; Abbasian, M; Mahmoudi, A; Cathers, B; Rychak, E; Gaidarova, S; Chen, R; Schafer, PH; Handa, H; Daniel, TO; Evans, JF; Chopra, R Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide. Leukemia 26:2326-35 (2012) [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:
BDBM65454
Synonyms:
191732-72-6 | CC-5013 | Lenalidomide | Revimid | Revlimid | US11530219, Compound Lenalidomide | US9694015, 6.1
Type:
Small organic molecule
Emp. Form.:
C13H13N3O3
Mol. Mass.:
259.2606
SMILES:
Nc1cccc2C(=O)N(Cc12)C1CCC(=O)NC1=O
Structure:
Search PDB for entries with ligand similarity: