Target
Ghrelin O-acyltransferase
Ligand
BDBM217379
Substrate
n/a
Meas. Tech.
GOAT Activity Assay
pH
7±n/a
Temperature
298.15±n/a K
IC50
6e+3± 2e+3 nM
Comments
extracted
Citation
 McGovern-Gooch, KRMahajani, NSGaragozzo, ASchramm, AJHannah, LGSieburg, MAChisholm, JDHougland, JL Synthetic Triterpenoid Inhibition of Human Ghrelin O-Acyltransferase: The Involvement of a Functionally Required Cysteine Provides Mechanistic Insight into Ghrelin Acylation. Biochemistry 56:919-931 (2017) [PubMed]  Article 
Target
Name:
Ghrelin O-acyltransferase
Synonyms:
GOAT | Ghrelin O-acyltransferase (GOAT) | MBOA4_HUMAN | MBOAT4 | Membrane-bound O-acyltransferase domain-containing protein 4 | O-acyltransferase domain-containing protein 4 | OACT4
Type:
Enzyme
Mol. Mass.:
49733.10
Organism:
Homo sapiens (Human)
Description:
Q96T53
Residue:
435
Sequence:
MEWLWLFFLHPISFYQGAAFPFALLFNYLCIMDSFSTRARYLFLLTGGGALAVAAMGSYAVLVFTPAVCAVALLCSLAPQQVHRWTFCFQMSWQTLCHLGLHYTEYYLHEPPSVRFCITLSSLMLLTQRVTSLSLDICEGKVKAASGGFRSRSSLSEHVCKALPYFSYLLFFPALLGGSLCSFQRFQARVQGSSALHPRHSFWALSWRGLQILGLECLNVAVSRVVDAGAGLTDCQQFECIYVVWTTAGLFKLTYYSHWILDDSLLHAAGFGPELGQSPGEEGYVPDADIWTLERTHRISVFSRKWNQSTARWLRRLVFQHSRAWPLLQTFAFSAWWHGLHPGQVFGFVCWAVMVEADYLIHSFANEFIRSWPMRLFYRTLTWAHTQLIIAYIMLAVEVRSLSSLWLLCNSYNSVFPMVYCILLLLLAKRKHKCN
  
Inhibitor
Name:
BDBM217379
Synonyms:
CDDO-Me, 2
Type:
Small organic molecule
Emp. Form.:
C32H43NO4
Mol. Mass.:
505.6881
SMILES:
COC(=O)[C@]12CCC(C)(C)C[C@H]1[C@H]1C(=O)C=C3[C@@]4(C)C=C(C#N)C(=O)C(C)(C)[C@@H]4CC[C@@]3(C)[C@]1(C)CC2 |r,t:16,20|
Structure:
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