Target
Lysine-specific demethylase 4A
Ligand
BDBM50149924
Substrate
n/a
Meas. Tech.
ChEMBL_1558372 (CHEMBL3772964)
IC50
1585±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:
BDBM50149924
Synonyms:
CHEMBL3769511
Type:
Small organic molecule
Emp. Form.:
C15H14N4O2
Mol. Mass.:
282.2973
SMILES:
CC(C)c1ccc(Oc2nc3cnccc3c(=O)[nH]2)cn1
Structure:
Search PDB for entries with ligand similarity: