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Target
DNA (cytosine-5)-methyltransferase 1 [621-1600]
Ligand
BDBM50430056
Substrate
n/a
Meas. Tech.
DNA Methylation Assay
pH
7.5±n/a
IC50
1.6e+3± 2e+2 nM
Comments
extracted
Citation
 Fagan, RL; Cryderman, DE; Kopelovich, L; Wallrath, LL; Brenner, C Laccaic acid A is a direct, DNA-competitive inhibitor of DNA methyltransferase 1. J Biol Chem 288:23858-67 (2013) [PubMed]  Article 
Target
Name:
DNA (cytosine-5)-methyltransferase 1 [621-1600]
Synonyms:
AIM | CXXC9 | DNA methyltransferase 1 (RFTS-lacking Dnmt1) | DNMT | DNMT1 | DNMT1_HUMAN
Type:
Protein
Mol. Mass.:
110932.40
Organism:
Homo sapiens (Human)
Description:
Human Dnmt 1 truncation (621-1600 aa)
Residue:
980
Sequence:
TKLVYQIFDTFFAEQIEKDDREDKENAFKRRRCGVCEVCQQPECGKCKACKDMVKFGGSGRSKQACQERRCPNMAMKEADDDEEVDDNIPEMPSPKKMHQGKKKKQNKNRISWVGEAVKTDGKKSYYKKVCIDAETLEVGDCVSVIPDDSSKPLYLARVTALWEDSSNGQMFHAHWFCAGTDTVLGATSDPLELFLVDECEDMQLSYIHSKVKVIYKAPSENWAMEGGMDPESLLEGDDGKTYFYQLWYDQDYARFESPPKTQPTEDNKFKFCVSCARLAEMRQKEIPRVLEQLEDLDSRVLYYSATKNGILYRVGDGVYLPPEAFTFNIKLSSPVKRPRKEPVDEDLYPEHYRKYSDYIKGSNLDAPEPYRIGRIKEIFCPKKSNGRPNETDIKIRVNKFYRPENTHKSTPASYHADINLLYWSDEEAVVDFKAVQGRCTVEYGEDLPECVQVYSMGGPNRFYFLEAYNAKSKSFEDPPNHARSPGNKGKGKGKGKGKPKSQACEPSEPEIEIKLPKLRTLDVFSGCGGLSEGFHQAGISDTLWAIEMWDPAAQAFRLNNPGSTVFTEDCNILLKLVMAGETTNSRGQRLPQKGDVEMLCGGPPCQGFSGMNRFNSRTYSKFKNSLVVSFLSYCDYYRPRFFLLENVRNFVSFKRSMVLKLTLRCLVRMGYQCTFGVLQAGQYGVAQTRRRAIILAAAPGEKLPLFPEPLHVFAPRACQLSVVVDDKKFVSNITRLSSGPFRTITVRDTMSDLPEVRNGASALEISYNGEPQSWFQRQLRGAQYQPILRDHICKDMSALVAARMRHIPLAPGSDWRDLPNIEVRLSDGTMARKLRYTHHDRKNGRSSSGALRGVCSCVEAGKACDPAARQFNTLIPWCLPHTGNRHNHWAGLYGRLEWDGFFSTTVTNPEPMGKQGRVLHPEQHRVVSVRECARSQGFPDTYRLFGNILDKHRQVGNAVPPPLAKAIGLEIKLCMLAKA
  
Inhibitor
Name:
BDBM50430056
Synonyms:
CHEMBL2336409 | SGI-1027
Type:
Small organic molecule
Emp. Form.:
C27H23N7O
Mol. Mass.:
461.5178
SMILES:
Cc1cc(Nc2ccc(NC(=O)c3ccc(Nc4ccnc5ccccc45)cc3)cc2)nc(N)n1
Structure:
Search PDB for entries with ligand similarity: