Target
Acyl-protein thioesterase 1 [I75L,S82A]
Ligand
BDBM207992
Substrate
n/a
Meas. Tech.
Steady-State Kinetic Assays
pH
6.5±n/a
Ki
280±20 nM
Comments
extracted
Citation
 Won, SJDavda, DLabby, KJHwang, SYPricer, RMajmudar, JDArmacost, KARodriguez, LARodriguez, CLChong, FSTorossian, KAPalakurthi, JHur, ESMeagher, JLBrooks, CLStuckey, JAMartin, BR Molecular Mechanism for Isoform-Selective Inhibition of Acyl Protein Thioesterases 1 and 2 (APT1 and APT2). ACS Chem Biol 11:3374-3382 (2016) [PubMed]  Article 
Target
Name:
Acyl-protein thioesterase 1 [I75L,S82A]
Synonyms:
APT1 | Acyl-protein thioesterase 1 (APT1 I75L/S82A) | LPL1 | LYPA1_HUMAN | LYPLA1
Type:
Protein
Mol. Mass.:
24654.33
Organism:
Homo sapiens (Human)
Description:
Human APT1 with I75L/S82A mutations
Residue:
230
Sequence:
MCGNNMSTPLPAIVPAARKATAAVIFLHGLGDTGHGWAEAFAGIRSSHIKYICPHAPVRPVTLNMNVAMPSWFDLIGLSPDAQEDESGIKQAAENIKALIDQEVKNGIPSNRIILGGFSQGGALSLYTALTTQQKLAGVTALSCWLPLRASFPQGPIGGANRDISILQCHGDCDPLVPLMFGSLTVEKLKTLVNPANVTFKTYEGMMHSSCQQEMMDVKQFIDKLLPPID
  
Inhibitor
Name:
BDBM207992
Synonyms:
ML349
Type:
Small organic molecule
Emp. Form.:
C23H22N2O4S2
Mol. Mass.:
454.562
SMILES:
COc1ccc(cc1)N1CCN(CC1)C(=O)c1cc2CS(=O)(=O)c3ccccc3-c2s1
Structure:
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