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TargetLysine-specific demethylase 4A
LigandBDBM50153072
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1561969
IC50 600±n/a nM
Citation Bavetsias VLanigan RMRuda GFAtrash BMcLaughlin MGTumber AMok NYLe Bihan YVDempster SBoxall KJJeganathan FHatch SBSavitsky PVelupillai SKrojer TEngland KSSejberg JThai CDonovan APal AScozzafava GBennett JMKawamura AJohansson CSzykowska AGileadi CBurgess-Brown NAvon Delft FOppermann UWalters ZShipley JRaynaud FIWestaway SMPrinjha RKFedorov OBurke RSchofield CJWestwood IMBountra CMüller Svan Montfort RLBrennan PEBlagg J 8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors. J Med Chem 59:1388-409 (2016) [PubMed]
More Info.:Get all data from this article,  Assay Method
 
Lysine-specific demethylase 4A
Name:Lysine-specific demethylase 4A
Synonyms:JmjC domain-containing histone demethylation protein 3A | Jumonji domain-containing protein 2A | Lysine-specific demethylase 4A
Type:Enzyme
Mol. Mass.:120647.83
Organism:Homo sapiens (Human)
Description:O75164
Residue:1064
Sequence:
MASESETLNPSARIMTFYPTMEEFRNFSRYIAYIESQGAHRAGLAKVVPPKEWKPRASYD
DIDDLVIPAPIQQLVTGQSGLFTQYNIQKKAMTVREFRKIANSDKYCTPRYSEFEELERK
YWKNLTFNPPIYGADVNGTLYEKHVDEWNIGRLRTILDLVEKESGITIEGVNTPYLYFGM
WKTSFAWHTEDMDLYSINYLHFGEPKSWYSVPPEHGKRLERLAKGFFPGSAQSCEAFLRH
KMTLISPLMLKKYGIPFDKVTQEAGEFMITFPYGYHAGFNHGFNCAESTNFATRRWIEYG
KQAVLCSCRKDMVKISMDVFVRKFQPERYKLWKAGKDNTVIDHTLPTPEAAEFLKESELP
PRAGNEEECPEEDMEGVEDGEEGDLKTSLAKHRIGTKRHRVCLEIPQEVSQSELFPKEDL
SSEQYEMTECPAALAPVRPTHSSVRQVEDGLTFPDYSDSTEVKFEELKNVKLEEEDEEEE
QAAAALDLSVNPASVGGRLVFSGSKKKSSSSLGSGSSRDSISSDSETSEPLSCRAQGQTG
VLTVHSYAKGDGRVTVGEPCTRKKGSAARSFSERELAEVADEYMFSLEENKKSKGRRQPL
SKLPRHHPLVLQECVSDDETSEQLTPEEEAEETEAWAKPLSQLWQNRPPNFEAEKEFNET
MAQQAPHCAVCMIFQTYHQVEFGGFNQNCGNASDLAPQKQRTKPLIPEMCFTSTGCSTDI
NLSTPYLEEDGTSILVSCKKCSVRVHASCYGVPPAKASEDWMCSRCSANALEEDCCLCSL
RGGALQRANDDRWVHVSCAVAILEARFVNIAERSPVDVSKIPLPRFKLKCIFCKKRRKRT
AGCCVQCSHGRCPTAFHVSCAQAAGVMMQPDDWPFVVFITCFRHKIPNLERAKGALQSIT
AGQKVISKHKNGRFYQCEVVRLTTETFYEVNFDDGSFSDNLYPEDIVSQDCLQFGPPAEG
EVVQVRWTDGQVYGAKFVASHPIQMYQVEFEDGSQLVVKRDDVYTLDEELPKRVKSRLSV
ASDMRFNEIFTEKEVKQEKKRQRVINSRYREDYIEPALYRAIME
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  Blast E-value cutoff:
BDBM50153072
n/a
NameBDBM50153072
Synonyms:CHEMBL3775956
TypeSmall organic molecule
Emp. Form.C23H25N7O
Mol. Mass.415.4909
SMILESO=c1[nH]cnc2c(nccc12)-n1cc(CCN2CCC(Cc3cccnc3)CC2)cn1
Structure
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