Target
Ghrelin O-acyltransferase
Ligand
BDBM217381
Substrate
n/a
Meas. Tech.
GOAT Activity Assay
pH
7±n/a
Temperature
298.15±n/a K
IC50
4.4e+4± 2.1e+4 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:
BDBM217381
Synonyms:
CDDO-TFEA, 4
Type:
Small organic molecule
Emp. Form.:
C33H43F3N2O3
Mol. Mass.:
572.7013
SMILES:
CC1(C)CC[C@@]2(CC[C@]3(C)[C@@H]([C@@H]2C1)C(=O)C=C1[C@@]3(C)CC[C@H]2C(C)(C)C(=O)C(=C[C@]12C)C#N)C(=O)NCC(F)(F)F |r,c:17,30|
Structure:
Search PDB for entries with ligand similarity: