Reaction Details Report a problem with these data
Target
Histone lysine demethylase PHF8
Ligand
BDBM223320
Substrate
n/a
Meas. Tech.
AlphaScreen Assay
IC50
1e+4±1.3e+3 nM
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 Biol 24:371-380 (2017) [PubMed]  Article 
Target
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:
MNRSRAIVQRGRVLPPPAPLDTTNLAGRRTLQGRAKMASVPVYCLCRLPYDVTRFMIECDMCQDWFHGSCVGVEEEKAADIDLYHCPNCEVLHGPSIMKKRRGSSKGHDTHKGKPVKTGSPTFVRELRSRTFDSSDEVILKPTGNQLTVEFLEENSFSVPILVLKKDGLGMTLPSPSFTVRDVEHYVGSDKEIDVIDVTRQADCKMKLGDFVKYYYSGKREKVLNVISLEFSDTRLSNLVETPKIVRKLSWVENLWPEECVFERPNVQKYCLMSVRDSYTDFHIDFGGTSVWYHVLKGEKIFYLIRPTNANLTLFECWSSSSNQNEMFFGDQVDKCYKCSVKQGQTLFIPTGWIHAVLTPVDCLAFGGNFLHSLNIEMQLKAYEIEKRLSTADLFRFPNFETICWYVGKHILDIFRGLRENRRHPASYLVHGGKALNLAFRAWTRKEALPDHEDEIPETVRTVQLIKDLAREIRLVEDIFQQNVGKTSNIFGLQRIFPAGSIPLTRPAHSTSVSMSRLSLPSKNGSKKKGLKPKELFKKAERKGKESSALGPAGQLSYNLMDTYSHQALKTGSFQKAKFNITGACLNDSDDDSPDLDLDGNESPLALLMSNGSTKRVKSLSKSRRTKIAKKVDKARLMAEQVMEDEFDLDSDDELQIDERLGKEKATLIIRPKFPRKLPRAKPCSDPNRVREPGEVEFDIEEDYTTDEDMVEGVEGKLGNGSGAGGILDLLKASRQVGGPDYAALTEAPASPSTQEAIQGMLCMANLQSSSSSPATSSLQAWWTGGQDRSSGSSSSGLGTVSNSPASQRTPGKRPIKRPAYWRTESEEEEENASLDEQDSLGACFKDAEYIYPSLESDDDDPALKSRPKKKKNSDDAPWSPKARVTPTLPKQDRPVREGTRVASIETGLAAAAAKLAQQELQKAQKKKYIKKKPLLKEVEQPRPQDSNLSLTVPAPTVAATPQLVTSSSPLPPPEPKQEALSGSLADHEYTARPNAFGMAQANRSTTPMAPGVFLTQRRPSVGSQSNQAGQGKRPKKGLATAKQRLGRILKIHRNGKLLL
  
Inhibitor
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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