Reaction Details |
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Target | Bromodomain-containing protein 4 [49-170]/DNA damage-binding protein 1/Protein cereblon |
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Ligand | BDBM511634 |
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Substrate/Competitor | n/a |
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Meas. Tech. | CRBN-DDB1/BRD4 Dimerization Assay |
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IC50 | 24.5±n/a nM |
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Citation | Bradner, J; Buckley, D; Winter, G Methods to induce targeted protein degradation through bifunctional molecules US Patent US11059801 Publication Date 7/13/2021 |
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More Info.: | Get all data from this article, Assay Method |
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Bromodomain-containing protein 4 [49-170]/DNA damage-binding protein 1/Protein cereblon |
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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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BDBM511634 |
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n/a |
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Name | BDBM511634 |
Synonyms: | US11059801, Compound dBET43 |
Type | Small organic molecule |
Emp. Form. | C39H41ClN8O5S |
Mol. Mass. | 769.311 |
SMILES | Cc1sc-2c(c1C)C(=N[C@@H](CC(=O)NCCCCCCC(=O)Nc1cccc3C(=O)N(Cc13)C1CCC(=O)NC1=O)c1nnc(C)n-21)c1ccc(Cl)cc1 |r,c:8| |
Structure |
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