Reaction Details |
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Target | Lysine-specific demethylase 4A |
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Ligand | BDBM195612 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1558372 (CHEMBL3772964) |
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IC50 | 631±n/a nM |
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Citation | Westaway, SM; Preston, AG; Barker, MD; Brown, F; Brown, JA; Campbell, M; Chung, CW; Drewes, G; Eagle, R; Garton, N; Gordon, L; Haslam, C; Hayhow, TG; Humphreys, PG; Joberty, G; Katso, R; Kruidenier, L; Leveridge, M; Pemberton, M; Rioja, I; Seal, GA; Shipley, T; Singh, O; Suckling, CJ; Taylor, J; Thomas, P; Wilson, DM; Lee, K; Prinjha, 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 Chem59:1370-87 (2016) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Lysine-specific demethylase 4A |
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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: | MASESETLNPSARIMTFYPTMEEFRNFSRYIAYIESQGAHRAGLAKVVPPKEWKPRASYD
DIDDLVIPAPIQQLVTGQSGLFTQYNIQKKAMTVREFRKIANSDKYCTPRYSEFEELERK
YWKNLTFNPPIYGADVNGTLYEKHVDEWNIGRLRTILDLVEKESGITIEGVNTPYLYFGM
WKTSFAWHTEDMDLYSINYLHFGEPKSWYSVPPEHGKRLERLAKGFFPGSAQSCEAFLRH
KMTLISPLMLKKYGIPFDKVTQEAGEFMITFPYGYHAGFNHGFNCAESTNFATRRWIEYG
KQAVLCSCRKDMVKISMDVFVRKFQPERYKLWKAGKDNTVIDHTLPTPEAAEFLKESELP
PRAGNEEECPEEDMEGVEDGEEGDLKTSLAKHRIGTKRHRVCLEIPQEVSQSELFPKEDL
SSEQYEMTECPAALAPVRPTHSSVRQVEDGLTFPDYSDSTEVKFEELKNVKLEEEDEEEE
QAAAALDLSVNPASVGGRLVFSGSKKKSSSSLGSGSSRDSISSDSETSEPLSCRAQGQTG
VLTVHSYAKGDGRVTVGEPCTRKKGSAARSFSERELAEVADEYMFSLEENKKSKGRRQPL
SKLPRHHPLVLQECVSDDETSEQLTPEEEAEETEAWAKPLSQLWQNRPPNFEAEKEFNET
MAQQAPHCAVCMIFQTYHQVEFGGFNQNCGNASDLAPQKQRTKPLIPEMCFTSTGCSTDI
NLSTPYLEEDGTSILVSCKKCSVRVHASCYGVPPAKASEDWMCSRCSANALEEDCCLCSL
RGGALQRANDDRWVHVSCAVAILEARFVNIAERSPVDVSKIPLPRFKLKCIFCKKRRKRT
AGCCVQCSHGRCPTAFHVSCAQAAGVMMQPDDWPFVVFITCFRHKIPNLERAKGALQSIT
AGQKVISKHKNGRFYQCEVVRLTTETFYEVNFDDGSFSDNLYPEDIVSQDCLQFGPPAEG
EVVQVRWTDGQVYGAKFVASHPIQMYQVEFEDGSQLVVKRDDVYTLDEELPKRVKSRLSV
ASDMRFNEIFTEKEVKQEKKRQRVINSRYREDYIEPALYRAIME
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BDBM195612 |
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n/a |
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Name | BDBM195612 |
Synonyms: | GSK467 |
Type | Small organic molecule |
Emp. Form. | C17H13N5O2 |
Mol. Mass. | 319.3174 |
SMILES | O=c1[nH]c(Oc2cnn(Cc3ccccc3)c2)nc2cnccc12 |
Structure |
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