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TargetBromodomain-containing protein 4 [49-170]/DNA damage-binding protein 1/Protein cereblon
LigandBDBM511602
Substrate/Competitorn/a
Meas. Tech.CRBN-DDB1/BRD4 Dimerization Assay
IC50 83.0±n/a nM
Citation Bradner, JBuckley, DWinter, G Methods to induce targeted protein degradation through bifunctional molecules US Patent US11059801 Publication Date 7/13/2021
More Info.:Get all data from this article,  Assay Method
 
Bromodomain-containing protein 4 [49-170]/DNA damage-binding protein 1/Protein cereblon
Name:Bromodomain-containing protein 4 [49-170]/DNA damage-binding protein 1/Protein cereblon
Synonyms:CRBN-DDB1/BRD4
Type:Enzyme
Mol. Mass.:n/a
Description:n/a
Components:This complex has 3 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:
MSYNYVVTAQKPTAVNGCVTGHFTSAEDLNLLIAKNTRLEIYVVTAEGLRPVKEVGMYGK
IAVMELFRPKGESKDLLFILTAKYNACILEYKQSGESIDIITRAHGNVQDRIGRPSETGI
IGIIDPECRMIGLRLYDGLFKVIPLDRDNKELKAFNIRLEELHVIDVKFLYGCQAPTICF
VYQDPQGRHVKTYEVSLREKEFNKGPWKQENVEAEASMVIAVPEPFGGAIIIGQESITYH
NGDKYLAIAPPIIKQSTIVCHNRVDPNGSRYLLGDMEGRLFMLLLEKEEQMDGTVTLKDL
RVELLGETSIAECLTYLDNGVVFVGSRLGDSQLVKLNVDSNEQGSYVVAMETFTNLGPIV
DMCVVDLERQGQGQLVTCSGAFKEGSLRIIRNGIGIHEHASIDLPGIKGLWPLRSDPNRE
TDDTLVLSFVGQTRVLMLNGEEVEETELMGFVDDQQTFFCGNVAHQQLIQITSASVRLVS
QEPKALVSEWKEPQAKNISVASCNSSQVVVAVGRALYYLQIHPQELRQISHTEMEHEVAC
LDITPLGDSNGLSPLCAIGLWTDISARILKLPSFELLHKEMLGGEIIPRSILMTTFESSH
YLLCALGDGALFYFGLNIETGLLSDRKKVTLGTQPTVLRTFRSLSTTNVFACSDRPTVIY
SSNHKLVFSNVNLKEVNYMCPLNSDGYPDSLALANNSTLTIGTIDEIQKLHIRTVPLYES
PRKICYQEVSQCFGVLSSRIEVQDTSGGTTALRPSASTQALSSSVSSSKLFSSSTAPHET
SFGEEVEVHNLLIIDQHTFEVLHAHQFLQNEYALSLVSCKLGKDPNTYFIVGTAMVYPEE
AEPKQGRIVVFQYSDGKLQTVAEKEVKGAVYSMVEFNGKLLASINSTVRLYEWTTEKELR
TECNHYNNIMALYLKTKGDFILVGDLMRSVLLLAYKPMEGNFEEIARDFNPNWMSAVEIL
DDDNFLGAENAFNLFVCQKDSAATTDEERQHLQEVGLFHLGEFVNVFCHGSLVMQNLGET
STPTQGSVLFGTVNGMIGLVTSLSESWYNLLLDMQNRLNKVIKSVGKIEHSFWRSFHTER
KTEPATGFIDGDLIESFLDISRPKMQEVVANLQYDDGSGMKREATADDLIKVVEELTRIH
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Component 2
Name:Protein cereblon
Synonyms:CRBN | CRBN_HUMAN
Type:PROTEIN
Mol. Mass.:50537.73
Organism:Homo sapiens (Human)
Description:ChEMBL_116917
Residue:442
Sequence:
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYL
GADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTF
AVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQA
KVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSW
PRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLK
IGSAIQRLRCELDIMNKCTSLCCKQCQETEITTKNEIFSLSLCGPMAAYVNPHGYVHETL
TVYKACNLNLIGRPSTEHSWFPGYAWTVAQCKICASHIGWKFTATKKDMSPQKFWGLTRS
ALLPTIPDTEDEISPDKVILCL
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Component 3
Name:Bromodomain-containing protein 4 [49-170]
Synonyms:BRD4 | BRD4-BD1 | BRD4-BD1 (aa 49-170) | BRD4_HUMAN | Bromodomain containing 4 (aa 49-170) | Bromodomain-containing protein 4 (BRD4) | Bromodomain-containing protein 4 (BRD4)(49-170) | Bromodomain-containing protein 4 (BRD4)(BD1) | HUNK1
Type:Enzyme Catalytic Domain
Mol. Mass.:14593.14
Organism:Homo sapiens (Human)
Description:aa 49-170 (BRD4-BD1)
Residue:122
Sequence:
ETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMG
TIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEE
TE
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BDBM511602
n/a
NameBDBM511602
Synonyms:US11059801, Compound dBET10
TypeSmall organic molecule
Emp. Form.C47H59N9O12
Mol. Mass.942.0245
SMILESCC[C@H]1N(C2CCCC2)c2nc(Nc3ccc(cc3OC)C(=O)NCCCOCCOCCOCCCNC(=O)COc3cccc4C(=O)N(C5CCC(=O)NC5=O)C(=O)c34)ncc2N(C)C1=O |r|
Structure
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