Reaction Details |
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Target | Histone lysine demethylase PHF8 |
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Ligand | BDBM223320 |
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Substrate/Competitor | n/a |
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Meas. Tech. | AlphaScreen Assay |
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IC50 | 1e+4±1.3e+3 nM |
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Citation | Tumber, A; Nuzzi, A; Hookway, ES; Hatch, SB; Velupillai, S; Johansson, C; Kawamura, A; Savitsky, P; Yapp, C; Szykowska, A; Wu, N; Bountra, C; Strain-Damerell, C; Burgess-Brown, NA; Ruda, GF; Fedorov, O; Munro, S; England, KS; Nowak, RP; Schofield, CJ; La Thangue, NB; Pawlyn, C; Davies, F; Morgan, G; Athanasou, N; Müller, S; Oppermann, U; Brennan, PE Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells. Cell Chem Biol24:371-380 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Histone lysine demethylase PHF8 |
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Name: | Histone lysine demethylase PHF8 |
Synonyms: | Histone lysine demethylase PHF8 | Histone lysine demethylase PHF8 (PHF8) | KIAA1111 | Lysine-specific demethylase 7A/7B | PHD finger protein 8 | PHF8 | PHF8_HUMAN | ZNF422 |
Type: | Protein |
Mol. Mass.: | 117889.91 |
Organism: | Homo sapiens (Human) |
Description: | Q9UPP1 |
Residue: | 1060 |
Sequence: | MNRSRAIVQRGRVLPPPAPLDTTNLAGRRTLQGRAKMASVPVYCLCRLPYDVTRFMIECD
MCQDWFHGSCVGVEEEKAADIDLYHCPNCEVLHGPSIMKKRRGSSKGHDTHKGKPVKTGS
PTFVRELRSRTFDSSDEVILKPTGNQLTVEFLEENSFSVPILVLKKDGLGMTLPSPSFTV
RDVEHYVGSDKEIDVIDVTRQADCKMKLGDFVKYYYSGKREKVLNVISLEFSDTRLSNLV
ETPKIVRKLSWVENLWPEECVFERPNVQKYCLMSVRDSYTDFHIDFGGTSVWYHVLKGEK
IFYLIRPTNANLTLFECWSSSSNQNEMFFGDQVDKCYKCSVKQGQTLFIPTGWIHAVLTP
VDCLAFGGNFLHSLNIEMQLKAYEIEKRLSTADLFRFPNFETICWYVGKHILDIFRGLRE
NRRHPASYLVHGGKALNLAFRAWTRKEALPDHEDEIPETVRTVQLIKDLAREIRLVEDIF
QQNVGKTSNIFGLQRIFPAGSIPLTRPAHSTSVSMSRLSLPSKNGSKKKGLKPKELFKKA
ERKGKESSALGPAGQLSYNLMDTYSHQALKTGSFQKAKFNITGACLNDSDDDSPDLDLDG
NESPLALLMSNGSTKRVKSLSKSRRTKIAKKVDKARLMAEQVMEDEFDLDSDDELQIDER
LGKEKATLIIRPKFPRKLPRAKPCSDPNRVREPGEVEFDIEEDYTTDEDMVEGVEGKLGN
GSGAGGILDLLKASRQVGGPDYAALTEAPASPSTQEAIQGMLCMANLQSSSSSPATSSLQ
AWWTGGQDRSSGSSSSGLGTVSNSPASQRTPGKRPIKRPAYWRTESEEEEENASLDEQDS
LGACFKDAEYIYPSLESDDDDPALKSRPKKKKNSDDAPWSPKARVTPTLPKQDRPVREGT
RVASIETGLAAAAAKLAQQELQKAQKKKYIKKKPLLKEVEQPRPQDSNLSLTVPAPTVAA
TPQLVTSSSPLPPPEPKQEALSGSLADHEYTARPNAFGMAQANRSTTPMAPGVFLTQRRP
SVGSQSNQAGQGKRPKKGLATAKQRLGRILKIHRNGKLLL
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BDBM223320 |
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n/a |
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Name | BDBM223320 |
Synonyms: | KDOAM-25 |
Type | Small organic molecule |
Emp. Form. | C15H25N5O2 |
Mol. Mass. | 307.3913 |
SMILES | CCN(CCN(C)C)C(=O)CNCc1cc(ccn1)C(N)=O |
Structure |
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