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TargetHistone lysine demethylase PHF8
LigandBDBM60875
Substrate/Competitorn/a
Meas. Tech.KDM TR-FRET Assay
IC50>25000±n/a nM
Citation Vinogradova, MGehling, VSGustafson, AArora, STindell, CAWilson, CWilliamson, KEGuler, GDGangurde, PManieri, WBusby, JFlynn, EMLan, FKim, HJOdate, SCochran, AGLiu, YWongchenko, MYang, YCheung, TKMaile, TMLau, TCosta, MHegde, GVJackson, EPitti, RArnott, DBailey, CBellon, SCummings, RTAlbrecht, BKHarmange, JCKiefer, JRTrojer, PClasson, M An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells. Nat Chem Biol12:531-8 (2016) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Histone lysine demethylase PHF8
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM60875
n/a
NameBDBM60875
Synonyms:3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoic acid | 3-{[2-(pyridin-2-yl)-6-(2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl)pyrimidin-4-yl]amino}propanoic acid | GSK J1 | GSK-J1 | GSKJ1
Typen/a
Emp. Form.C22H23N5O2
Mol. Mass.389.4503
SMILESOC(=O)CCNc1cc(nc(n1)-c1ccccn1)N1CCc2ccccc2CC1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: