Target
Glycylpeptide N-tetradecanoyltransferase 1
Ligand
BDBM50033414
Substrate
n/a
Meas. Tech.
ChEMBL_1435039 (CHEMBL3387685)
IC50
9.0±n/a nM
Citation
 Brand, SNorcross, NRThompson, SHarrison, JRSmith, VCRobinson, DATorrie, LSMcElroy, SPHallyburton, INorval, SScullion, PStojanovski, LSimeons, FRvan Aalten, DFrearson, JABrenk, RFairlamb, AHFerguson, MAWyatt, PGGilbert, IHRead, KD Lead optimization of a pyrazole sulfonamide series of Trypanosoma brucei N-myristoyltransferase inhibitors: identification and evaluation of CNS penetrant compounds as potential treatments for stage 2 human African trypanosomiasis. J Med Chem 57:9855-69 (2014) [PubMed]  Article 
Target
Name:
Glycylpeptide N-tetradecanoyltransferase 1
Synonyms:
Myristoyl-CoA:protein N-myristoyltransferase (Nmt) | N-myristoyltransferase (NMT1) | NMT | NMT1 | NMT1_HUMAN | Peptide N-myristoyltransferase | Peptide N-myristoyltransferase 1
Type:
Enzyme
Mol. Mass.:
56814.10
Organism:
Homo sapiens (Human)
Description:
P30419
Residue:
496
Sequence:
MADESETAVKPPAPPLPQMMEGNGNGHEHCSDCENEEDNSYNRGGLSPANDTGAKKKKKKQKKKKEKGSETDSAQDQPVKMNSLPAERIQEIQKAIELFSVGQGPAKTMEEASKRSYQFWDTQPVPKLGEVVNTHGPVEPDKDNIRQEPYTLPQGFTWDALDLGDRGVLKELYTLLNENYVEDDDNMFRFDYSPEFLLWALRPPGWLPQWHCGVRVVSSRKLVGFISAIPANIHIYDTEKKMVEINFLCVHKKLRSKRVAPVLIREITRRVHLEGIFQAVYTAGVVLPKPVGTCRYWHRSLNPRKLIEVKFSHLSRNMTMQRTMKLYRLPETPKTAGLRPMETKDIPVVHQLLTRYLKQFHLTPVMSQEEVEHWFYPQENIIDTFVVENANGEVTDFLSFYTLPSTIMNHPTHKSLKAAYSFYNVHTQTPLLDLMSDALVLAKMKGFDVFNALDLMENKTFLEKLKFGIGDGNLQYYLYNWKCPSMGAEKVGLVLQ
  
Inhibitor
Name:
BDBM50033414
Synonyms:
CHEMBL3357681
Type:
Small organic molecule
Emp. Form.:
C20H22Cl2N6O2S
Mol. Mass.:
481.399
SMILES:
Cc1c(NS(=O)(=O)c2c(Cl)cc(cc2Cl)-c2ccnc(c2)N2CCNCC2)cnn1C
Structure:
Search PDB for entries with ligand similarity: