Reaction Details |
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Target | Peregrin |
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Ligand | BDBM50269847 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1707378 (CHEMBL4058611) |
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IC50 | 4600±n/a nM |
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Citation | Romero, FA; Murray, J; Lai, KW; Tsui, V; Albrecht, BK; An, L; Beresini, MH; de Leon Boenig, G; Bronner, SM; Chan, EW; Chen, KX; Chen, Z; Choo, EF; Clagg, K; Clark, K; Crawford, TD; Cyr, P; de Almeida Nagata, D; Gascoigne, KE; Grogan, JL; Hatzivassiliou, G; Huang, W; Hunsaker, TL; Kaufman, S; Koenig, SG; Li, R; Li, Y; Liang, X; Liao, J; Liu, W; Ly, J; Maher, J; Masui, C; Merchant, M; Ran, Y; Taylor, AM; Wai, J; Wang, F; Wei, X; Yu, D; Zhu, BY; Zhu, X; Magnuson, S GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP). J Med Chem60:9162-9183 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Peregrin |
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Name: | Peregrin |
Synonyms: | BR140 | BRPF1 | BRPF1_HUMAN | Bromodomain and PHD finger-containing protein 1 | Peregrin | Protein Br140 |
Type: | PROTEIN |
Mol. Mass.: | 137524.47 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_108054 |
Residue: | 1214 |
Sequence: | MGVDFDVKTFCHNLRATKPPYECPVETCRKVYKSYSGIEYHLYHYDHDNPPPPQQTPLRK
HKKKGRQSRPANKQSPSPSEVSQSPGREVMSYAQAQRMVEVDLHGRVHRISIFDNLDVVS
EDEEAPEEAPENGSNKENTETPAATPKSGKHKNKEKRKDSNHHHHHNVSASTTPKLPEVV
YRELEQDTPDAPPRPTSYYRYIEKSAEELDEEVEYDMDEEDYIWLDIMNERRKTEGVSPI
PQEIFEYLMDRLEKESYFESHNKGDPNALVDEDAVCCICNDGECQNSNVILFCDMCNLAV
HQECYGVPYIPEGQWLCRRCLQSPSRAVDCALCPNKGGAFKQTDDGRWAHVVCALWIPEV
CFANTVFLEPIDSIEHIPPARWKLTCYICKQRGSGACIQCHKANCYTAFHVTCAQQAGLY
MKMEPVRETGANGTSFSVRKTAYCDIHTPPGSARRLPALSHSEGEEDEDEEEDEGKGWSS
EKVKKAKAKSRIKMKKARKILAEKRAAAPVVSVPCIPPHRLSKITNRLTIQRKSQFMQRL
HSYWTLKRQSRNGVPLLRRLQTHLQSQRNCDQVGRDSEDKNWALKEQLKSWQRLRHDLER
ARLLVELIRKREKLKRETIKVQQIAMEMQLTPFLILLRKTLEQLQEKDTGNIFSEPVPLS
EVPDYLDHIKKPMDFFTMKQNLEAYRYLNFDDFEEDFNLIVSNCLKYNAKDTIFYRAAVR
LREQGGAVLRQARRQAEKMGIDFETGMHIPHSLAGDEATHHTEDAAEEERLVLLENQKHL
PVEEQLKLLLERLDEVNASKQSVGRSRRAKMIKKEMTALRRKLAHQRETGRDGPERHGPS
SRGSLTPHPAACDKDGQTDSAAEESSSQETSKGLGPNMSSTPAHEVGRRTSVLFSKKNPK
TAGPPKRPGRPPKNRESQMTPSHGGSPVGPPQLPIMSSLRQRKRGRSPRPSSSSDSDSDK
STEDPPMDLPANGFSGGNQPVKKSFLVYRNDCSLPRSSSDSESSSSSSSSAASDRTSTTP
SKQGRGKPSFSRGTFPEDSSEDTSGTENEAYSVGTGRGVGHSMVRKSLGRGAGWLSEDED
SPLDALDLVWAKCRGYPSYPALIIDPKMPREGMFHHGVPIPVPPLEVLKLGEQMTQEARE
HLYLVLFFDNKRTWQWLPRTKLVPLGVNQDLDKEKMLEGRKSNIRKSVQIAYHRALQHRS
KVQGEQSSETSDSD
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BDBM50269847 |
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n/a |
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Name | BDBM50269847 |
Synonyms: | CHEMBL4097025 |
Type | Small organic molecule |
Emp. Form. | C27H33F2N7O2 |
Mol. Mass. | 525.5934 |
SMILES | CNC(=O)N1CCc2c(C1)c(nn2C1CCOCC1)N1CCCc2cc(-c3cnn(C)c3)c(cc12)C(F)F |
Structure |
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