Reaction Details |
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Target | Bromodomain-containing protein 2 |
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Ligand | BDBM297163 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2212777 (CHEMBL5125726) |
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IC50 | 0.200000±n/a nM |
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Citation | Hill, MD; Fang, H; Norris, D; Delucca, GV; Huang, H; DeBenedetto, M; Quesnelle, C; Schmitz, WD; Tokarski, JS; Sheriff, S; Yan, C; Fanslau, C; Haarhoff, Z; Huang, C; Kramer, M; Madari, S; Menard, K; Monereau, L; Morrison, J; Raghavan, N; Shields, EE; Simmermacher-Mayer, J; Sinz, M; Tye, CK; Westhouse, R; Xie, C; Zhang, H; Zhang, L; Zvyaga, T; Lee, F; Gavai, AV; Degnan, AP Development of BET Inhibitors as Potential Treatments for Cancer: Optimization of Pharmacokinetic Properties. ACS Med Chem Lett13:1165-1171 (2022) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Bromodomain-containing protein 2 |
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Name: | Bromodomain-containing protein 2 |
Synonyms: | BRD2 | BRD2_HUMAN | Bromodomain and extra-terminal motif (BET) | Bromodomain-containing protein 2 | Bromodomain-containing protein 2 (BRD2) | KIAA9001 | RING3 |
Type: | Protein |
Mol. Mass.: | 88085.95 |
Organism: | Homo sapiens (Human) |
Description: | P25440 |
Residue: | 801 |
Sequence: | MLQNVTPHNKLPGEGNAGLLGLGPEAAAPGKRIRKPSLLYEGFESPTMASVPALQLTPAN
PPPPEVSNPKKPGRVTNQLQYLHKVVMKALWKHQFAWPFRQPVDAVKLGLPDYHKIIKQP
MDMGTIKRRLENNYYWAASECMQDFNTMFTNCYIYNKPTDDIVLMAQTLEKIFLQKVASM
PQEEQELVVTIPKNSHKKGAKLAALQGSVTSAHQVPAVSSVSHTALYTPPPEIPTTVLNI
PHPSVISSPLLKSLHSAGPPLLAVTAAPPAQPLAKKKGVKRKADTTTPTPTAILAPGSPA
SPPGSLEPKAARLPPMRRESGRPIKPPRKDLPDSQQQHQSSKKGKLSEQLKHCNGILKEL
LSKKHAAYAWPFYKPVDASALGLHDYHDIIKHPMDLSTVKRKMENRDYRDAQEFAADVRL
MFSNCYKYNPPDHDVVAMARKLQDVFEFRYAKMPDEPLEPGPLPVSTAMPPGLAKSSSES
SSEESSSESSSEEEEEEDEEDEEEEESESSDSEEERAHRLAELQEQLRAVHEQLAALSQG
PISKPKRKREKKEKKKKRKAEKHRGRAGADEDDKGPRAPRPPQPKKSKKASGSGGGSAAL
GPSGFGPSGGSGTKLPKKATKTAPPALPTGYDSEEEEESRPMSYDEKRQLSLDINKLPGE
KLGRVVHIIQAREPSLRDSNPEEIEIDFETLKPSTLRELERYVLSCLRKKPRKPYTIKKP
VGKTKEELALEKKRELEKRLQDVSGQLNSTKKPPKKANEKTESSSAQQVAVSRLSASSSS
SDSSSSSSSSSSSDTSDSDSG
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BDBM297163 |
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n/a |
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Name | BDBM297163 |
Synonyms: | 2-{8-Fluoro-3-[4-(2H3)methyl-1-methyl-1H-1,2,3-triazol-5-yl]-5-[(S)-oxan-4-yl(phenyl)methyl]-5H-pyrido[3,2-b]indol-7-yl}propan-2-ol | US10112941, Example 279 |
Type | Small organic molecule |
Emp. Form. | C30H32FN5O2 |
Mol. Mass. | 513.6058 |
SMILES | Cc1nnn(C)c1-c1cnc2c(c1)n([C@@H](C1CCOCC1)c1ccccc1)c1cc(c(F)cc21)C(C)(C)O |r| |
Structure |
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