Target
Lysine-specific histone demethylase 1A
Ligand
BDBM369476
Substrate
n/a
Meas. Tech.
LSD1 enzymatic activity
IC50
4.00±n/a nM
Citation
 Marx, MAVaisburg, AChristensen, JGGalemmo, Jr., RA LSD1 inhibitors US Patent  US10233152 Publication Date 3/19/2019 
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:
BDBM369476
Synonyms:
N-(Methylsulfonyl)-2-(4-(2-(4-(((1R,2S)-2-phenylcyclopropyl)amino)piperidin-1-yl)ethoxy)phenyl)acetamide di-hydrochloride (58) and 2-(4-(2-(4-(((1R,2S)-2-phenylcyclopropyl)amino)piperidin-1-yl)ethoxy)phenyl)-N-(phenyl sulfonyl)acetamide di-hydrochloride (60) | US10233152, Example 16 | US10233152, Example 17
Type:
Small organic molecule
Emp. Form.:
C30H35N3O4S
Mol. Mass.:
533.682
SMILES:
O=C(Cc1ccc(OCCN2CCC(CC2)N[C@@H]2C[C@H]2c2ccccc2)cc1)NS(=O)(=O)c1ccccc1 |r|
Structure:
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