Target
Lysine-specific demethylase 4A
Ligand
BDBM50149925
Substrate
n/a
Meas. Tech.
ChEMBL_1558372 (CHEMBL3772964)
IC50
398±n/a nM
Citation
 Westaway, SMPreston, AGBarker, MDBrown, FBrown, JACampbell, MChung, CWDrewes, GEagle, RGarton, NGordon, LHaslam, CHayhow, TGHumphreys, PGJoberty, GKatso, RKruidenier, LLeveridge, MPemberton, MRioja, ISeal, GAShipley, TSingh, OSuckling, CJTaylor, JThomas, PWilson, DMLee, KPrinjha, RK Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives. J Med Chem 59:1370-87 (2016) [PubMed]  Article 
Target
Name:
Lysine-specific demethylase 4A
Synonyms:
JHDM3A | JMJD2 | JMJD2A | JmjC domain-containing histone demethylation protein 3A | Jumonji domain-containing protein 2A | KDM4A | KDM4A_HUMAN | KIAA0677 | Lysine-specific demethylase 4A | Lysine-specific demethylase 4A (KDM4A)
Type:
Enzyme
Mol. Mass.:
120647.83
Organism:
Homo sapiens (Human)
Description:
O75164
Residue:
1064
Sequence:
MASESETLNPSARIMTFYPTMEEFRNFSRYIAYIESQGAHRAGLAKVVPPKEWKPRASYDDIDDLVIPAPIQQLVTGQSGLFTQYNIQKKAMTVREFRKIANSDKYCTPRYSEFEELERKYWKNLTFNPPIYGADVNGTLYEKHVDEWNIGRLRTILDLVEKESGITIEGVNTPYLYFGMWKTSFAWHTEDMDLYSINYLHFGEPKSWYSVPPEHGKRLERLAKGFFPGSAQSCEAFLRHKMTLISPLMLKKYGIPFDKVTQEAGEFMITFPYGYHAGFNHGFNCAESTNFATRRWIEYGKQAVLCSCRKDMVKISMDVFVRKFQPERYKLWKAGKDNTVIDHTLPTPEAAEFLKESELPPRAGNEEECPEEDMEGVEDGEEGDLKTSLAKHRIGTKRHRVCLEIPQEVSQSELFPKEDLSSEQYEMTECPAALAPVRPTHSSVRQVEDGLTFPDYSDSTEVKFEELKNVKLEEEDEEEEQAAAALDLSVNPASVGGRLVFSGSKKKSSSSLGSGSSRDSISSDSETSEPLSCRAQGQTGVLTVHSYAKGDGRVTVGEPCTRKKGSAARSFSERELAEVADEYMFSLEENKKSKGRRQPLSKLPRHHPLVLQECVSDDETSEQLTPEEEAEETEAWAKPLSQLWQNRPPNFEAEKEFNETMAQQAPHCAVCMIFQTYHQVEFGGFNQNCGNASDLAPQKQRTKPLIPEMCFTSTGCSTDINLSTPYLEEDGTSILVSCKKCSVRVHASCYGVPPAKASEDWMCSRCSANALEEDCCLCSLRGGALQRANDDRWVHVSCAVAILEARFVNIAERSPVDVSKIPLPRFKLKCIFCKKRRKRTAGCCVQCSHGRCPTAFHVSCAQAAGVMMQPDDWPFVVFITCFRHKIPNLERAKGALQSITAGQKVISKHKNGRFYQCEVVRLTTETFYEVNFDDGSFSDNLYPEDIVSQDCLQFGPPAEGEVVQVRWTDGQVYGAKFVASHPIQMYQVEFEDGSQLVVKRDDVYTLDEELPKRVKSRLSVASDMRFNEIFTEKEVKQEKKRQRVINSRYREDYIEPALYRAIME
  
Inhibitor
Name:
BDBM50149925
Synonyms:
CHEMBL3770740
Type:
Small organic molecule
Emp. Form.:
C13H8ClN3O3
Mol. Mass.:
289.674
SMILES:
Oc1cc(Oc2nc3cnccc3c(=O)[nH]2)ccc1Cl
Structure:
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