Reaction Details |
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Target | Peregrin |
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Ligand | BDBM50028142 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1434751 (CHEMBL3383420) |
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IC50 | <4.0±n/a nM |
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Citation | Gosmini, R; Nguyen, VL; Toum, J; Simon, C; Brusq, JM; Krysa, G; Mirguet, O; Riou-Eymard, AM; Boursier, EV; Trottet, L; Bamborough, P; Clark, H; Chung, CW; Cutler, L; Demont, EH; Kaur, R; Lewis, AJ; Schilling, MB; Soden, PE; Taylor, S; Walker, AL; Walker, MD; Prinjha, RK; Nicodème, E The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor. J Med Chem57:8111-31 (2014) [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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BDBM50028142 |
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n/a |
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Name | BDBM50028142 |
Synonyms: | CHEMBL2177300 |
Type | Small organic molecule |
Emp. Form. | C25H23ClN2O3 |
Mol. Mass. | 434.915 |
SMILES | C[C@H]1C[C@@H](Nc2ccc(Cl)cc2)c2cc(ccc2N1C(C)=O)-c1ccc(cc1)C(O)=O |r| |
Structure |
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