Reaction Details |
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Target | Lysine-specific demethylase 4C |
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Ligand | BDBM191599 |
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Substrate/Competitor | n/a |
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Meas. Tech. | AlphaScreen Assay |
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IC50 | 2400±0.0 nM |
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Citation | Tumber, A; Nuzzi, A; Hookway, ES; Hatch, SB; Velupillai, S; Johansson, C; Kawamura, A; Savitsky, P; Yapp, C; Szykowska, A; Wu, N; Bountra, C; Strain-Damerell, C; Burgess-Brown, NA; Ruda, GF; Fedorov, O; Munro, S; England, KS; Nowak, RP; Schofield, CJ; La Thangue, NB; Pawlyn, C; Davies, F; Morgan, G; Athanasou, N; Müller, S; Oppermann, U; Brennan, PE Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells. Cell Chem Biol24:371-380 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Lysine-specific demethylase 4C |
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Name: | Lysine-specific demethylase 4C |
Synonyms: | GASC-1 protein | GASC1 | Gene amplified in squamous cell carcinoma 1 protein | JHDM3C | JMJD2C | JmjC domain-containing histone demethylation protein 3C | Jumonji domain-containing protein 2C | KDM4C | KDM4C_HUMAN | KIAA0780 |
Type: | Protein |
Mol. Mass.: | 119979.01 |
Organism: | Homo sapiens (Human) |
Description: | Q9H3R0 |
Residue: | 1056 |
Sequence: | MEVAEVESPLNPSCKIMTFRPSMEEFREFNKYLAYMESKGAHRAGLAKVIPPKEWKPRQC
YDDIDNLLIPAPIQQMVTGQSGLFTQYNIQKKAMTVKEFRQLANSGKYCTPRYLDYEDLE
RKYWKNLTFVAPIYGADINGSIYDEGVDEWNIARLNTVLDVVEEECGISIEGVNTPYLYF
GMWKTTFAWHTEDMDLYSINYLHFGEPKSWYAIPPEHGKRLERLAQGFFPSSSQGCDAFL
RHKMTLISPSVLKKYGIPFDKITQEAGEFMITFPYGYHAGFNHGFNCAESTNFATVRWID
YGKVAKLCTCRKDMVKISMDIFVRKFQPDRYQLWKQGKDIYTIDHTKPTPASTPEVKAWL
QRRRKVRKASRSFQCARSTSKRPKADEEEEVSDEVDGAEVPNPDSVTDDLKVSEKSEAAV
KLRNTEASSEEESSASRMQVEQNLSDHIKLSGNSCLSTSVTEDIKTEDDKAYAYRSVPSI
SSEADDSIPLSSGYEKPEKSDPSELSWPKSPESCSSVAESNGVLTEGEESDVESHGNGLE
PGEIPAVPSGERNSFKVPSIAEGENKTSKSWRHPLSRPPARSPMTLVKQQAPSDEELPEV
LSIEEEVEETESWAKPLIHLWQTKSPNFAAEQEYNATVARMKPHCAICTLLMPYHKPDSS
NEENDARWETKLDEVVTSEGKTKPLIPEMCFIYSEENIEYSPPNAFLEEDGTSLLISCAK
CCVRVHASCYGIPSHEICDGWLCARCKRNAWTAECCLCNLRGGALKQTKNNKWAHVMCAV
AVPEVRFTNVPERTQIDVGRIPLQRLKLKCIFCRHRVKRVSGACIQCSYGRCPASFHVTC
AHAAGVLMEPDDWPYVVNITCFRHKVNPNVKSKACEKVISVGQTVITKHRNTRYYSCRVM
AVTSQTFYEVMFDDGSFSRDTFPEDIVSRDCLKLGPPAEGEVVQVKWPDGKLYGAKYFGS
NIAHMYQVEFEDGSQIAMKREDIYTLDEELPKRVKARFSTASDMRFEDTFYGADIIQGER
KRQRVLSSRFKNEYVADPVYRTFLKSSFQKKCQKRQ
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BDBM191599 |
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n/a |
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Name | BDBM191599 |
Synonyms: | KDOAM-21 | ethyl 2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinate (KDM5-C70) |
Type | Small organic molecule |
Emp. Form. | C17H28N4O3 |
Mol. Mass. | 336.4292 |
SMILES | CCOC(=O)c1ccnc(CNCC(=O)N(CC)CCN(C)C)c1 |
Structure |
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