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Target
Histone lysine demethylase PHF8
Ligand
BDBM195608
Substrate
n/a
Meas. Tech.
KDM TR-FRET Assay
IC50
7.7e+3±n/a nM
Citation
 Vinogradova, M; Gehling, VS; Gustafson, A; Arora, S; Tindell, CA; Wilson, C; Williamson, KE; Guler, GD; Gangurde, P; Manieri, W; Busby, J; Flynn, EM; Lan, F; Kim, HJ; Odate, S; Cochran, AG; Liu, Y; Wongchenko, M; Yang, Y; Cheung, TK; Maile, TM; Lau, T; Costa, M; Hegde, GV; Jackson, E; Pitti, R; Arnott, D; Bailey, C; Bellon, S; Cummings, RT; Albrecht, BK; Harmange, JC; Kiefer, JR; Trojer, P; Classon, M An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells. Nat Chem Biol 12:531-8 (2016) [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:
BDBM195608
Synonyms:
CPI-455
Type:
Small organic molecule
Emp. Form.:
C16H14N4O
Mol. Mass.:
278.3086
SMILES:
CC(C)c1c([nH]c2c(cnn2c1=O)C#N)-c1ccccc1
Structure:
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