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Target
Lysine-specific histone demethylase 1A
Ligand
BDBM283259
Substrate
n/a
Meas. Tech.
In Vitro Enzyme Inhibition Assay-LSD-1
IC50
5500±n/a nM
Citation
 Xu, J; Cho, R; Nguyen, A Treatment of relapsed and/or refractory solid tumors and non-hodgkin's lymphomas US Patent  US10328077 Publication Date 6/25/2019 
Target
Name:
Lysine-specific histone demethylase 1A
Synonyms:
AOF2 | BRAF35-HDAC complex protein BHC110 | Flavin-containing amine oxidase domain-containing protein 2 | KDM1 | KDM1A | KDM1A_HUMAN | KIAA0601 | LSD1 | Lysine-specific demethylase 1 (LSD1) | Lysine-specific histone demethylase 1 | Lysine-specific histone demethylase 1 (LSD1)
Type:
Enzyme
Mol. Mass.:
92901.01
Organism:
Homo sapiens (Human)
Description:
O60341
Residue:
852
Sequence:
MLSGKKAAAAAAAAAAAATGTEAGPGTAGGSENGSEVAAQPAGLSGPAEVGPGAVGERTPRKKEPPRASPPGGLAEPPGSAGPQAGPTVVPGSATPMETGIAETPEGRRTSRRKRAKVEYREMDESLANLSEDEYYSEEERNAKAEKEKKLPPPPPQAPPEEENESEPEEPSGVEGAAFQSRLPHDRMTSQEAACFPDIISGPQQTQKVFLFIRNRTLQLWLDNPKIQLTFEATLQQLEAPYNSDTVLVHRVHSYLERHGLINFGIYKRIKPLPTKKTGKVIIIGSGVSGLAAARQLQSFGMDVTLLEARDRVGGRVATFRKGNYVADLGAMVVTGLGGNPMAVVSKQVNMELAKIKQKCPLYEANGQAVPKEKDEMVEQEFNRLLEATSYLSHQLDFNVLNNKPVSLGQALEVVIQLQEKHVKDEQIEHWKKIVKTQEELKELLNKMVNLKEKIKELHQQYKEASEVKPPRDITAEFLVKSKHRDLTALCKEYDELAETQGKLEEKLQELEANPPSDVYLSSRDRQILDWHFANLEFANATPLSTLSLKHWDQDDDFEFTGSHLTVRNGYSCVPVALAEGLDIKLNTAVRQVRYTASGCEVIAVNTRSTSQTFIYKCDAVLCTLPLGVLKQQPPAVQFVPPLPEWKTSAVQRMGFGNLNKVVLCFDRVFWDPSVNLFGHVGSTTASRGELFLFWNLYKAPILLALVAGEAAGIMENISDDVIVGRCLAILKGIFGSSAVPQPKETVVSRWRADPWARGSYSYVAAGSSGNDYDLMAQPITPGPSIPGAPQPIPRLFFAGEHTIRNYPATVHGALLSGLREAGRIADQFLGAMYTLPRQATPGVPAQQSPSM
  
Inhibitor
Name:
BDBM283259
Synonyms:
3-[2-(4-amino-piperidin-1-yl)-4- (4-cyano-3-fluoro-phenyl)-1- methyl-6-oxo-1,6-dihydro- pyrimidin-5-yl]-benzoic acid | US10023543, Example 43 | US10207999, Example 43 | US10328077, Example 43 | US10548896, Example 43 | US10849898, Example 43 | US10960005, Example 43 | US11084793, Example 43 | US9573930, Example 43 | US9771329, Example 43 | US9776974, Example 43
Type:
Small organic molecule
Emp. Form.:
C24H22FN5O3
Mol. Mass.:
447.4616
SMILES:
Cn1c(nc(-c2ccc(C#N)c(F)c2)c(-c2cccc(c2)C(O)=O)c1=O)N1CCC(N)CC1
Structure:
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