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Target
Lysine-specific histone demethylase 1A
Ligand
BDBM283279
Substrate
n/a
Meas. Tech.
In Vitro Enzyme Inhibition Assay-LSD-1
IC50
<100±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:
BDBM283279
Synonyms:
4-[2-[1,4]diazepan-1-yl-5-(6- methoxy-pyridin-3-yl)-1-methyl- 6-oxo-1,6-dihydro-pyrimidin-4- yl]-2-fluoro-benzonitrile | US10023543, Example 62 | US10207999, Example 62 | US10328077, Example 62 | US10548896, Example 62 | US10849898, Example 62 | US10960005, Example 62 | US11084793, Example 62 | US9573930, Example 62 | US9771329, Example 62 | US9776974, Example 62
Type:
Small organic molecule
Emp. Form.:
C23H24N6O2
Mol. Mass.:
416.4757
SMILES:
COc1ccc(cn1)-c1c(nc(N2CCCNCC2)n(C)c1=O)-c1ccc(cc1)C#N
Structure:
Search PDB for entries with ligand similarity: