MBOAT4

gene

On this page

Also known as FKSG89GOAT

Summary

MBOAT4 (membrane bound ghrelin O-acyltransferase MBOAT4, HGNC:32311) is a protein-coding gene on chromosome 8p12, encoding Membrane-bound ghrelin O-acyltransferase MBOAT4 (Q96T53). Catalyzes ghrelin acylation at ‘Ser-3’ using preferentially octanoyl-CoA, hexanoyl-CoA and decanoyl-CoA as acyl-CoA donors leading to ghrelin activity.

Enables acyltransferase activity, transferring groups other than amino-acyl groups. Involved in peptidyl-serine octanoylation. Predicted to be located in endoplasmic reticulum. Predicted to be active in endoplasmic reticulum membrane.

Source: NCBI Gene 619373 — RefSeq curated summary.

At a glance

Clinical variants (ClinVar): 13 total
Druggable target: yes — 1 molecules with ChEMBL bioactivity
MANE Select transcript: NM_001100916

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:32311
Approved symbol	MBOAT4
Name	membrane bound ghrelin O-acyltransferase MBOAT4
Location	8p12
Locus type	gene with protein product
Status	Approved
Aliases	FKSG89, GOAT
Ensembl gene	ENSG00000177669
Ensembl biotype	protein_coding
OMIM	611940
Entrez	619373

Gene structure

Transcript identifiers

Ensembl transcripts: 1 — 1 protein_coding

ENST00000320542

RefSeq mRNA: 1 — MANE Select: NM_001100916 NM_001100916

CCDS: CCDS47835

Canonical transcript exons

ENST00000320542 — 3 exons

Exon	Start	End
ENSE00001280839	30131671	30132906
ENSE00001594172	30144483	30144665
ENSE00001775964	30138532	30138756

Expression profiles

Bgee: expression breadth broad, 86 present calls, max score 87.52.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.0300 / max 9.4064, expressed in 16 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
92608	0.0300	16

Top tissues by expression

98 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
islet of Langerhans	UBERON:0000006	87.52	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	82.12	gold quality
pancreas	UBERON:0001264	67.70	gold quality
granulocyte	CL:0000094	60.20	gold quality
gall bladder	UBERON:0002110	59.89	gold quality
blood	UBERON:0000178	58.67	gold quality
right adrenal gland cortex	UBERON:0035827	58.39	gold quality
right uterine tube	UBERON:0001302	58.25	gold quality
body of pancreas	UBERON:0001150	57.79	gold quality
right adrenal gland	UBERON:0001233	56.75	gold quality
left adrenal gland	UBERON:0001234	55.80	gold quality
lymph node	UBERON:0000029	55.05	gold quality
adrenal gland	UBERON:0002369	55.03	gold quality
left adrenal gland cortex	UBERON:0035825	54.40	gold quality
leukocyte	CL:0000738	54.30	gold quality
duodenum	UBERON:0002114	54.29	gold quality
fallopian tube	UBERON:0003889	53.88	gold quality
monocyte	CL:0000576	53.70	gold quality
stromal cell of endometrium	CL:0002255	53.59	silver quality
body of stomach	UBERON:0001161	53.27	gold quality
stomach	UBERON:0000945	53.17	gold quality
endometrium	UBERON:0001295	52.54	gold quality
fundus of stomach	UBERON:0001160	51.98	gold quality
placenta	UBERON:0001987	51.55	gold quality
bone marrow	UBERON:0002371	51.22	gold quality
vermiform appendix	UBERON:0001154	50.14	gold quality
mucosa of transverse colon	UBERON:0004991	49.71	gold quality
spleen	UBERON:0002106	49.53	gold quality
liver	UBERON:0002107	48.59	gold quality
bone marrow cell	CL:0002092	48.53	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ENAD-27	yes	8.78
E-ANND-3	no	2.90

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

16 targeting MBOAT4, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-4455	100.00	65.48	1587
HSA-MIR-3688-3P	99.97	72.02	2834
HSA-MIR-6783-3P	99.89	67.92	2059
HSA-MIR-1343-3P	99.89	66.78	1815
HSA-MIR-6124	99.87	69.78	3551
HSA-MIR-576-5P	99.84	70.46	2582
HSA-MIR-609	99.82	64.26	505
HSA-MIR-4530	99.69	66.47	1509
HSA-MIR-586	99.65	70.40	2051
HSA-MIR-7151-5P	99.37	67.82	613
HSA-MIR-4263	99.18	69.25	2236
HSA-MIR-6742-3P	97.95	64.50	1490
HSA-MIR-6892-5P	97.27	68.60	847
HSA-MIR-675-3P	95.77	69.27	675
HSA-MIR-4453	95.61	65.84	436
HSA-MIR-4538	95.61	65.34	449

Literature-anchored findings (GeneRIF, showing 22)

The identification and characterization of human GOAT, the ghrelin O-acyl transferase, is reported. (PMID:18443287)
GOAT was expressed in human immortalized chondrocyte cell lines and in human cultured primary chondrocytes. (PMID:19479831)
The presence of PC and GOAT in the cells, as well as n-octanoic acid in the culture medium, was necessary to produce n-octanoyl ghrelin. (PMID:19628676)
Based on the results of tjhis study concluded that genetic variation in GOAT might be implicated in the etiology of anorexia nervosa. (PMID:21035823)
Modulation of GOAT or ghrelin signaling may be a clinically relevant strategy to treat metabolic diseases such as type II diabetes. (PMID:21150588)
Identification of GOAT expression in various tissues support the concept that in addition to the important endocrine effect of acylated ghrelin, the paracrine effects of locally synthetised and acylated ghrelin may be important. (PMID:21646729)
Genetic variation of the ghrelin activator gene ghrelin O-acyltransferase (GOAT) is associated with anorexia nervosa. (Review) (PMID:21930173)
Visceral adipose tissue from obese patients with type 2 diabetes showed higher levels of GOAT. (PMID:22869322)
GOAT is also present in human plasma and GOAT protein levels depend on the metabolic environment with decreased levels in anorexic and increased levels in morbidly obese patients (PMID:23454172)
Data indicate that ghrelin O-acyltransferase (GOAT) mRNA and protein are expressed in the normal prostate and prostate cancer tissue samples. (PMID:23879975)
Architectural organization of the metabolic regulatory enzyme ghrelin O-acyltransferase. (PMID:24045953)
Studies suggest that dysregulation in the components of the ghrelin system including ghrelin, ghrelin receptor (GHSR1a) and ghrelin-O-acyl-transferase can lead to or influence the development and/or progression of highly concerning pathologies. (PMID:24194510)
The GOAT active site was characterized by defining substrate-enzyme interactions used to bind and recognize ghrelin. (PMID:25562443)
GOAT prefers n-hexanoyl-CoA over n-octanoyl-CoA as the acyl donor, although in the stomach the n-octanoyl form is the predominant form of acyl-modified ghrelin. (PMID:27489223)
Plasma GOAT levels exhibit high specificity/sensitivity to predict prostate carcinoma-presence compared with other PCa-biomarkers, especially in non-diabetic individuals. (PMID:27693462)
The role of ghrelin O-acyltransferase cysteine residue in the ghrelin acylation (PMID:28134508)
GOAT is a druggable target, and its inhibitors are promising antiobesity drugs. (PMID:28846466)
GOAT-levels could also represent a novel predictive biomarker of aggressiveness, as its levels are positively associated with Gleason Score and the presence of metastasis at the time of diagnoses. (PMID:30256519)
GOAT was significantly overexpressed in gastroenteropancreatic tumor samples compared to adjacent non-tumor tissue (PMID:30297816)
MBOAT4 expression is significantly increased in Japanese patients with schizophrenia compared to controls. (PMID:30597386)
Unacylated-Ghrelin Impairs Hippocampal Neurogenesis and Memory in Mice and Is Altered in Parkinson’s Dementia in Humans. (PMID:33103129)
Anorexia of ageing is associated with elevated fasted and lower post-prandial ghrelin, independent of ghrelin O-acyltransferase. (PMID:38341037)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	mboat4	ENSDARG00000052110
mus_musculus	Mboat4	ENSMUSG00000071113
rattus_norvegicus	Mboat4	ENSRNOG00000030102

Paralogs (5): PORCN (ENSG00000102312), LPCAT3 (ENSG00000111684), MBOAT7 (ENSG00000125505), MBOAT2 (ENSG00000143797), MBOAT1 (ENSG00000172197)

Protein

Protein identifiers

Membrane-bound ghrelin O-acyltransferase MBOAT4 — Q96T53 (reviewed: Q96T53)

Alternative names: Membrane-bound O-acyltransferase domain-containing protein 4

All UniProt accessions (1): Q96T53

UniProt curated annotations — full annotation on UniProt →

Function. Catalyzes ghrelin acylation at ‘Ser-3’ using preferentially octanoyl-CoA, hexanoyl-CoA and decanoyl-CoA as acyl-CoA donors leading to ghrelin activity. In vitro also uses acyl-CoA donors of different lengths from short-chain (C2) to long-chain fatty acids (C16) knowing that acyl-CoA donors from butanoyl-CoA (C4) to dodecanoyl-CoA (C12) are more efficient compared to longer acyl-CoA donors, such as myristoyl-CoA (C14) and palmitoyl-CoA (C16) that are not efficient.

Subunit / interactions. Monomer.

Subcellular location. Endoplasmic reticulum membrane.

Tissue specificity. Expressed predominantly in stomach with moderate levels in pancreas and relatively low levels in most other tissues.

Post-translational modifications. Not glycosylated.

Activity regulation. Inhibited by c8-acylated ghrelin mimetic peptide with an IC(50) of 22 nM. Inhibited by 1-[2-cyano-3,12-dioxooleana-1,9(11)- dien-28-oyl] (CDDO) derivatives such as CDDO-imidazole (CDDO-Im), CDDO-methyl ester (CDDO-Me), CDDO-ethylamide (CDDO-EA), CDDO-trifluoroethylamide (CDDO-TFEA) with an IC(50) of 38 uM, 6uM, 8 uM and 44 uM respectively. Inhibited by cyclohexenone derivatives such as 2-cyano-2-cyclohexanone and 2-bromo-2-cyclohexanone. Inhibited by steroid derivatives such as alpha-cyanoenone steroid.

Similarity. Belongs to the membrane-bound acyltransferase family.

Isoforms (2)

UniProt ID	Names	Canonical?
Q96T53-1	1	yes
Q96T53-2	2

RefSeq proteins (1): NP_001094386* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR004299	MBOAT_fam	Family
IPR049941	LPLAT_7/PORCN-like	Family

Pfam: PF03062

Catalyzed reactions (Rhea), 11 shown:

L-seryl-[protein] + acetyl-CoA = O-acetyl-L-seryl-[protein] + CoA (RHEA:59392)
octanoyl-CoA + L-seryl-[protein] = O-octanoyl-L-seryl-[protein] + CoA (RHEA:59964)
decanoyl-CoA + L-seryl-[protein] = O-decanoyl-L-seryl-[protein] + CoA (RHEA:59972)
L-seryl-[protein] + a fatty acyl-CoA = O-fatty acyl-L-seryl-[protein] + CoA (RHEA:68272)
L-seryl-[protein] + butanoyl-CoA = O-butanoyl-L-seryl-[protein] + CoA (RHEA:68276)
pentanoyl-CoA + L-seryl-[protein] = O-pentanoyl-L-seryl-[protein] + CoA (RHEA:68280)
hexanoyl-CoA + L-seryl-[protein] = O-hexanoyl-L-seryl-[protein] + CoA (RHEA:68284)
heptanoyl-CoA + L-seryl-[protein] = O-heptanoyl-L-seryl-[protein] + CoA (RHEA:68288)
nonanoyl-CoA + L-seryl-[protein] = O-nonanoyl-L-seryl-[protein] + CoA (RHEA:68292)
L-seryl-[protein] + dodecanoyl-CoA = O-dodecanoyl-L-seryl-[protein] + CoA (RHEA:68296)
L-seryl-[protein] + tetradecanoyl-CoA = O-tetradecanoyl-L-seryl-[protein] + CoA (RHEA:68300)

UniProt features (31 total): topological domain 12, transmembrane region 11, active site 2, splice variant 2, sequence variant 2, chain 1, mutagenesis site 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q96T53-F1	88.73	0.70

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Catalytic / active sites (2): 307; 338

Mutagenesis-validated functional residues (1):

Position	Phenotype
338	abolishes ability to acylate ghrelin.

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

ID	Pathway
R-HSA-422085	Synthesis, secretion, and deacylation of Ghrelin
R-HSA-2980736	Peptide hormone metabolism
R-HSA-392499	Metabolism of proteins

MSigDB gene sets: 49 (showing top): GOBP_LIPID_MODIFICATION, GOBP_LIPOPROTEIN_METABOLIC_PROCESS, GOBP_PEPTIDYL_SERINE_MODIFICATION, GOBP_REGULATION_OF_HORMONE_LEVELS, GOBP_PROTEIN_MATURATION, GOBP_AMIDE_METABOLIC_PROCESS, GOBP_LIPOPROTEIN_BIOSYNTHETIC_PROCESS, GOBP_LIPID_METABOLIC_PROCESS, chr8p12, GOBP_PROTEIN_ACYLATION, GOCC_NUCLEAR_OUTER_MEMBRANE_ENDOPLASMIC_RETICULUM_MEMBRANE_NETWORK, GOBP_PROTEOLYSIS, GOCC_ORGANELLE_SUBCOMPARTMENT, GOMF_ACYLTRANSFERASE_ACTIVITY, GOMF_O_ACYLTRANSFERASE_ACTIVITY

GO Biological Process (3): peptide hormone processing (GO:0016486), peptidyl-serine octanoylation (GO:0018191), lipid modification (GO:0030258)

GO Molecular Function (5): obsolete O-acyltransferase activity (GO:0008374), serine O-acyltransferase activity (GO:0016412), acyltransferase activity, transferring groups other than amino-acyl groups (GO:0016747), transferase activity (GO:0016740), acyltransferase activity (GO:0016746)

GO Cellular Component (3): endoplasmic reticulum (GO:0005783), endoplasmic reticulum membrane (GO:0005789), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
Peptide hormone metabolism	1
Metabolism of proteins	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
hormone metabolic process	1
signaling receptor ligand precursor processing	1
protein octanoylation	1
peptidyl-serine modification	1
lipid metabolic process	1
acyltransferase activity, transferring groups other than amino-acyl groups	1
acyltransferase activity	1
catalytic activity	1
transferase activity	1
cytoplasm	1
endomembrane system	1
intracellular membrane-bounded organelle	1
organelle membrane	1
nuclear outer membrane-endoplasmic reticulum membrane network	1
endoplasmic reticulum subcompartment	1
cellular anatomical structure	1

Protein interactions and networks

STRING

456 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
MBOAT4	GHRL	Q9UBU3	968
MBOAT4	GHSR	Q92847	949
MBOAT4	GPR39	O43194	804
MBOAT4	AGRP	O00253	733
MBOAT4	NPY	P01303	709
MBOAT4	GHRH	P01286	659
MBOAT4	CPT1A	P50416	627
MBOAT4	PTPRN2	Q92932	619
MBOAT4	HHAT	Q5VTY9	611
MBOAT4	MC4R	P32245	610
MBOAT4	MLN	P12872	566
MBOAT4	GAST	P01350	563
MBOAT4	UCP2	P55851	554
MBOAT4	CRH	P06850	548
MBOAT4	LEAP2	Q969E1	524

IntAct

0 interactions, top by confidence:

ESM2 similar proteins: A0A8C2M425, A1A5Z0, A9ULG4, B1Q005, B1Q006, D3ZI76, O75908, O77759, O88908, P0C7A3, Q07175, Q148G2, Q14DK4, Q1XHX8, Q32LM8, Q49LS0, Q5D0E6, Q5KR61, Q5TM67, Q5U2T1, Q5U4T9, Q60850, Q641Y9, Q643R3, Q6AZ83, Q6MG14, Q6NSQ9, Q6NUI2, Q6NVG1, Q6PJN8, Q767L9, Q7SZQ0, Q7TN58, Q7TPN3, Q7TQM4, Q8BPS4, Q8CIP5, Q8IXM6, Q8VC65, Q96T53

Diamond homologs: B1Q005, B1Q006, P0C7A3, Q96T53

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

13 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	11
Likely benign	2
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

368 predictions. Top by Δscore:

Variant	Effect	Δscore
8:30138605:T:C	donor_gain	1.0000
8:30138526:GCTTA:G	donor_loss	0.9900
8:30138527:CTTA:C	donor_loss	0.9900
8:30138528:TTA:T	donor_loss	0.9900
8:30138529:TA:T	donor_loss	0.9900
8:30138753:GTACC:G	acceptor_loss	0.9800
8:30138755:ACCT:A	acceptor_loss	0.9800
8:30138756:CCTG:C	acceptor_loss	0.9800
8:30138758:T:C	acceptor_loss	0.9800
8:30144478:CCTA:C	donor_loss	0.9800
8:30144479:CTA:C	donor_loss	0.9800
8:30144480:TACCT:T	donor_loss	0.9800
8:30144482:C:A	donor_loss	0.9800
8:30138531:CCT:C	donor_gain	0.9700
8:30138531:CCTCA:C	donor_gain	0.9700
8:30138564:A:AC	donor_gain	0.9700
8:30138621:C:CT	donor_gain	0.9700
8:30138622:C:CT	donor_gain	0.9700
8:30144477:GCCTA:G	donor_loss	0.9700
8:30138565:G:C	donor_gain	0.9500
8:30138759:G:C	acceptor_loss	0.9500
8:30138757:C:CC	acceptor_gain	0.9400
8:30144644:A:C	donor_gain	0.9400
8:30138575:G:T	donor_gain	0.9300
8:30138752:GGTAC:G	acceptor_gain	0.9300
8:30138530:A:AC	donor_gain	0.9000
8:30138531:C:CC	donor_gain	0.9000
8:30138760:AAAGA:A	acceptor_loss	0.8900
8:30132720:TCCC:T	acceptor_gain	0.8800
8:30138524:CTGCT:C	donor_loss	0.8800

AlphaMissense

2836 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
8:30132750:G:C	S167R	0.990
8:30132750:G:T	S167R	0.990
8:30132752:T:G	S167R	0.990
8:30132258:A:C	F331L	0.986
8:30132258:A:T	F331L	0.986
8:30132260:A:G	F331L	0.986
8:30132242:A:G	W337R	0.984
8:30132242:A:T	W337R	0.984
8:30132879:C:A	M124I	0.984
8:30132879:C:G	M124I	0.984
8:30132879:C:T	M124I	0.984
8:30132693:A:C	F186L	0.979
8:30132693:A:T	F186L	0.979
8:30132695:A:G	F186L	0.979
8:30132207:G:C	F348L	0.977
8:30132207:G:T	F348L	0.977
8:30132209:A:G	F348L	0.977
8:30132245:A:G	W336R	0.976
8:30132245:A:T	W336R	0.976
8:30132294:G:C	F319L	0.976
8:30132294:G:T	F319L	0.976
8:30132296:A:G	F319L	0.976
8:30132867:C:A	Q128H	0.974
8:30132867:C:G	Q128H	0.974
8:30132240:C:A	W337C	0.973
8:30132240:C:G	W337C	0.973
8:30138599:A:G	W93R	0.972
8:30138599:A:T	W93R	0.972
8:30132314:A:G	W313R	0.970
8:30132314:A:T	W313R	0.970

dbSNP variants (sampled 300 via entrez): RS1000067962 (8:30142283 T>C), RS1000236346 (8:30135319 T>C), RS1000533422 (8:30138158 C>T), RS1000579422 (8:30133400 A>G), RS1000671656 (8:30131472 A>G), RS1000946664 (8:30137887 A>C), RS1000971227 (8:30133786 C>A,T), RS1001616875 (8:30135029 G>A), RS1001639991 (8:30144528 A>G), RS1002256066 (8:30138832 G>A,C), RS1002811046 (8:30144844 A>C,T), RS1002881734 (8:30145230 T>C), RS1003219904 (8:30146289 T>G), RS1003316530 (8:30136136 A>G), RS1003368947 (8:30135908 T>G)

Disease associations

OMIM: gene MIM:611940 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL3588729 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,032 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1762621	BARDOXOLONE METHYL	3	1,032

PharmGKB: 1 entry (VIP=true, CPIC=false)

Binding affinities (BindingDB)

178 measured of 195 human assays (196 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
6-[5-Bromo-6-(2-oxa-6-aza-spiro[3.3]hept-6-yl)-pyridin-2-ylmethyl]-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridine-7-ylamine	IC50	0.02 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-2-cyclopropylamino-nicotinonitrile	IC50	0.02 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(5-Bromo-6-methoxy-pyridin-2-ylmethyl)-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.022 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-2-(3-fluoro-propoxy)-nicotinonitrile	IC50	0.026 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(5-Bromo-6-morpholin-4-yl-pyridin-2-ylmethyl)-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.026 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-2-(3,3-difluoro-azetidin-1-yl)-nicotinonitrile	IC50	0.027 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-2-(3-fluoro-propylamino)-nicotinonitrile	IC50	0.027 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(5,6-Dibromo-pyridin-2-ylmethyl)-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.03 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
1-[6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-3-bromo-pyridin-2-yl]-3-methyl-azetidin-3-ol	IC50	0.033 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-2-morpholin-4-yl-nicotinonitrile	IC50	0.033 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-[5-Bromo-6-(2-fluoro-ethoxy)-pyridin-2-ylmethyl]-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.034 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(6-Bromo-5-difluoromethoxy-pyridin-2-ylmethyl)-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.038 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(5-Bromo-6-cyclopropylamino-pyridin-2-ylmethyl)-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.038 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-{5-Bromo-6-[(3-methyl-oxetan-3-ylmethyl)-amino]-pyridin-2-ylmethyl}-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.045 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-2-(3,3-difluoro-pyrrolidin-1-yl)-nicotinonitrile	IC50	0.046 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(5-Brom32.2-chloro-pyridin-2-ylmethyl)-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.047 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(6-Amino-5-thiazol-5-yl-pyridin-2-ylmethyl)-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.05 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-[5-Bromo-6-(3,3-difluoro-azetidin-1-yl)-pyridin-2-ylmethyl]-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.052 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-2-(2-oxa-6-aza-spiro[3.3]hept-6-yl)-nicotinonitrile	IC50	0.054 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-2-(3,3-difluoro-propylamino)-nicotinonitrile	IC50	0.055 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
3-[6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-3-bromo-pyridin-2-ylamino]-2,2-di methyl-propionamide	IC50	0.056 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-[5-Bromo-6-(2,2-difluoro-ethoxy)-pyridin-2-yl methyl]-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.058 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
1-[6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-3-bromo-pyridin-2-yloxy]-2-methyl-propan-2-ol	IC50	0.058 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(5-Brom32.2-fluoro-pyridin-2-ylmethyl)-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.066 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-[5-Bromo-6-(2,2-difluoro-propoxy)-pyridin-2-ylmethyl]-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.072 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(7-amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-yl methyl)-3-cyclopropylpyridine-2-carbonitrile	IC50	0.073 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-[5-Bromo-6-(3-fluoro-propoxy)-pyridin-2-yl methyl]-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.074 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(5-Bromo-6-methylsulfanyl-pyridin-2-ylmethyl)-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.074 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-2-(3-hydroxy-3-methyl-azetidin-1-yl)-nicotinonitrile	IC50	0.075 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-[5-bromo-4-(trifluoromethyl)pyrimidin-2-yl]methyl-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-amine	IC50	0.077 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-[5-Bromo-6-(2,2,2-trifluoro-ethoxy)-pyridin-2-ylmethyl]-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.079 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(5-Brom32.2-difluoromethoxy-pyridin-2-ylmethyl)-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.082 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-3-difluoromethoxy-pyridine-2-carbonitrile	IC50	0.082 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-[5-Bromo-6-(3-methyl-oxetan-3-ylmethoxy)-pyridin-2-ylmethyl]-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.082 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-3-phenoxy-pyridine-2-carbonitrile	IC50	0.085 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-2-(2,2-difluoro-propoxy)-nicotinonitrile	IC50	0.086 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(6-Amino-5-difluoromethoxy-pyridin-2-ylmethyl)-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.091 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-2-(2,2-difluoro-ethoxy)-nicotinonitrile	IC50	0.093 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-[5-Bromo-6-(3,3-difluoro-cyclobutylamino)-pyridin-2-ylmethyl]-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.096 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
1-[6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-3-bromo-pyridin-2-yl]-[1,4]diazepan-5-one	IC50	0.097 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-[5-Bromo-6-(3,3-difluoro-propylamino)-pyridin-2-ylmethyl]-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.099 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(6-Furan-2-yl-pyridin-2-ylmethyl)-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.1 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
1-[6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-pyridin-2-yl]-cyclopentanecarbonitrile	IC50	0.1 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-2-(3-methyl-oxetan-3-ylmethoxy)-nicotinonitrile	IC50	0.1 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
3-[6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-3-bromo-pyridin-2-ylamino]-2,2-di methyl-propionitrile	IC50	0.1 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-[5-Bromo-6-(3,3-difluoro-pyrrolidin-1-yl)-pyridin-2-ylmethyl]-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.1 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-[6-Amino-5-(2,4-dimethyl-2H-pyrazol-3-yl)-pyridin-2-ylmethyl]-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-ylamine	IC50	0.11 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-2-(2-fluoro-ethoxy)-nicotinonitrile	IC50	0.11 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-2-chloro-nicotinonitrile	IC50	0.12 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
6-(7-Amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-ylmethyl)-2-(2-hydroxy-2-methyl-propoxy)-nicotinonitrile	IC50	0.12 nM	US-10308667: Oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors

ChEMBL bioactivities

281 potent at pChembl≥5 of 286 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.70	IC50	0.02	nM	CHEMBL4793203
10.70	IC50	0.02	nM	CHEMBL6065698
10.66	IC50	0.022	nM	CHEMBL5779713
10.59	IC50	0.026	nM	CHEMBL5961160
10.59	IC50	0.026	nM	CHEMBL6019672
10.57	IC50	0.027	nM	CHEMBL6006052
10.57	IC50	0.027	nM	CHEMBL5776289
10.55	IC50	0.028	nM	CHEMBL4746798
10.52	IC50	0.03	nM	CHEMBL6011632
10.48	IC50	0.033	nM	CHEMBL5995459
10.48	IC50	0.033	nM	CHEMBL5854761
10.47	IC50	0.034	nM	CHEMBL5824003
10.42	IC50	0.038	nM	CHEMBL6014902
10.42	IC50	0.038	nM	CHEMBL6009615
10.35	IC50	0.045	nM	CHEMBL6052908
10.34	IC50	0.046	nM	CHEMBL5840069
10.33	IC50	0.047	nM	CHEMBL5836965
10.30	IC50	0.05	nM	CHEMBL5995222
10.28	IC50	0.052	nM	CHEMBL5779509
10.27	IC50	0.054	nM	CHEMBL6036203
10.26	IC50	0.055	nM	CHEMBL5939271
10.25	IC50	0.056	nM	CHEMBL5831824
10.24	IC50	0.058	nM	CHEMBL5910082
10.24	IC50	0.058	nM	CHEMBL5930205
10.18	IC50	0.066	nM	CHEMBL4754865
10.18	IC50	0.066	nM	CHEMBL5747478
10.14	IC50	0.073	nM	CHEMBL5859399
10.14	IC50	0.072	nM	CHEMBL5993997
10.13	IC50	0.074	nM	CHEMBL6009627
10.13	IC50	0.074	nM	CHEMBL5816590
10.12	IC50	0.075	nM	CHEMBL5925406
10.11	IC50	0.077	nM	CHEMBL5960642
10.10	IC50	0.079	nM	CHEMBL5762142
10.09	IC50	0.082	nM	CHEMBL5971493
10.09	IC50	0.082	nM	CHEMBL5912742
10.09	IC50	0.082	nM	CHEMBL5842474
10.07	IC50	0.086	nM	CHEMBL6043565
10.07	IC50	0.085	nM	CHEMBL5881073
10.04	IC50	0.091	nM	CHEMBL5925045
10.03	IC50	0.093	nM	CHEMBL5770311
10.02	IC50	0.096	nM	CHEMBL5976263
10.01	IC50	0.097	nM	CHEMBL6063436
10.00	IC50	0.1	nM	CHEMBL5875803
10.00	IC50	0.1	nM	CHEMBL5778722
10.00	IC50	0.1	nM	CHEMBL5845203
10.00	IC50	0.1	nM	CHEMBL5848325
10.00	IC50	0.1	nM	CHEMBL5878052
10.00	IC50	0.099	nM	CHEMBL5960841
9.96	IC50	0.11	nM	CHEMBL5996268
9.96	IC50	0.11	nM	CHEMBL5992856

PubChem BioAssay actives

28 with measured affinity, of 45 total; 25 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
6-[(7-amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-6-yl)methyl]-2-(cyclopropylamino)pyridine-3-carbonitrile	1679023: Inhibition of human GOAT expressed in HEK293 cells harboring -preproghrelin in presence of Octanoate-BSA incubated for 5 hr by ELISA	ic50	<0.0001	uM
5-methyl-6-[[3-[6-(trifluoromethyl)-2-pyridinyl]pyrazol-1-yl]methyl]-[1,2,5]oxadiazolo[3,4-b]pyridin-7-amine	1679023: Inhibition of human GOAT expressed in HEK293 cells harboring -preproghrelin in presence of Octanoate-BSA incubated for 5 hr by ELISA	ic50	<0.0001	uM
6-[[5-bromo-6-(difluoromethoxy)-2-pyridinyl]methyl]-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine	1679023: Inhibition of human GOAT expressed in HEK293 cells harboring -preproghrelin in presence of Octanoate-BSA incubated for 5 hr by ELISA	ic50	0.0001	uM
6-[[2-methoxy-4-(trifluoromethyl)phenyl]methyl]-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-7-amine	1679023: Inhibition of human GOAT expressed in HEK293 cells harboring -preproghrelin in presence of Octanoate-BSA incubated for 5 hr by ELISA	ic50	0.0001	uM
5-methyl-6-[[4-(trifluoromethoxy)piperidin-1-yl]methyl]-[1,2,5]oxadiazolo[3,4-b]pyridin-7-amine	1679023: Inhibition of human GOAT expressed in HEK293 cells harboring -preproghrelin in presence of Octanoate-BSA incubated for 5 hr by ELISA	ic50	0.0006	uM
2-[4,7-dichloro-6-[[2-methyl-6-(trifluoromethyl)-3-pyridinyl]methoxy]-1-benzothiophen-2-yl]acetic acid	1679017: Inhibition of human GOAT expressed in baculovirus infected sf9 insect cell microsomes using biotinylated des-acyl ghrelin and octanoyl-CoA as substrate incubated for 15 mins by HTRF assay	ic50	0.0017	uM
(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-3-amino-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-hydroxypropanoyl]amino]propanoyl]amino]-3-naphthalen-1-ylpropanoyl]amino]-3-hydroxypropanoyl]-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]pyrrolidine-2-carboxamide	1679013: Inhibition of GOAT (unknown origin)	ic50	0.0060	uM
2-[(2,4-dichlorophenyl)methylsulfanyl]-1,3-benzoxazole-5-carboxylic acid	1679017: Inhibition of human GOAT expressed in baculovirus infected sf9 insect cell microsomes using biotinylated des-acyl ghrelin and octanoyl-CoA as substrate incubated for 15 mins by HTRF assay	ic50	0.0086	uM
2-[4-chloro-6-[[(5S)-6,7-dihydro-5H-cyclopenta[b]pyridin-5-yl]oxy]-1-benzothiophen-3-yl]acetic acid	1679022: Inhibition of human His-tagged GOAT expressed in baculovirus infected Sf9 cell membrane using biotinylated ghrelin peptide/octanoyl-CoA/palmitoyl CoA as substrate incubated for 80 mins by TR-FRET assay	ic50	0.0500	uM
N-[(2S)-1-[4-[2-(4-amino-2-chloro-6-methylpyrimidin-5-yl)ethyl]piperidin-1-yl]-1-oxopropan-2-yl]-5-methyl-1H-pyrazole-4-carboxamide	1679011: Inhibition of human His-tagged GOAT expressed in baculovirus infected Sf9 cell membrane using desacyl-ghrelin-biotin and octanoyl-CoA as substrate incubated for 1 hr by ELISA	ic50	0.0544	uM
N-[(2S)-1-[4-[2-(4-amino-6-chloro-2-methylpyrimidin-5-yl)ethyl]piperidin-1-yl]-1-oxopropan-2-yl]-2-methylpyrazole-3-carboxamide	2084169: Inhibition of GOAT (unknown origin)	ic50	0.0600	uM
N-[(2S)-1-[4-[2-(2,4-diamino-6-chloropyrimidin-5-yl)ethyl]piperidin-1-yl]-1-oxopropan-2-yl]-1-methylpyrazole-3-carboxamide	1679011: Inhibition of human His-tagged GOAT expressed in baculovirus infected Sf9 cell membrane using desacyl-ghrelin-biotin and octanoyl-CoA as substrate incubated for 1 hr by ELISA	ic50	0.0689	uM
N-[(2S)-1-[4-[2-[4-amino-6-methyl-2-(trifluoromethyl)pyrimidin-5-yl]ethyl]piperidin-1-yl]-1-oxopropan-2-yl]-2-methylpyrazole-3-carboxamide	1679011: Inhibition of human His-tagged GOAT expressed in baculovirus infected Sf9 cell membrane using desacyl-ghrelin-biotin and octanoyl-CoA as substrate incubated for 1 hr by ELISA	ic50	0.0695	uM
N-[(2S)-1-[4-[2-(4-amino-6-chloro-2-methylpyrimidin-5-yl)ethyl]piperidin-1-yl]-1-oxopropan-2-yl]-2-methyl-1,3-thiazole-5-carboxamide	1679011: Inhibition of human His-tagged GOAT expressed in baculovirus infected Sf9 cell membrane using desacyl-ghrelin-biotin and octanoyl-CoA as substrate incubated for 1 hr by ELISA	ic50	0.0964	uM
methyl N-[(2S)-1-[4-[2-(4-amino-6-chloro-2-methylpyrimidin-5-yl)ethyl]piperidin-1-yl]-1-oxopropan-2-yl]carbamate	1679011: Inhibition of human His-tagged GOAT expressed in baculovirus infected Sf9 cell membrane using desacyl-ghrelin-biotin and octanoyl-CoA as substrate incubated for 1 hr by ELISA	ic50	0.1490	uM
4-[2-(4-amino-2-methylfuro[2,3-d]pyrimidin-5-yl)ethyl]benzoic acid	2084169: Inhibition of GOAT (unknown origin)	ic50	0.1700	uM
N-[(2S)-1-[4-[2-(2,4-diamino-6-chloropyrimidin-5-yl)ethyl]piperidin-1-yl]-1-oxopropan-2-yl]cyclopropanecarboxamide	1679011: Inhibition of human His-tagged GOAT expressed in baculovirus infected Sf9 cell membrane using desacyl-ghrelin-biotin and octanoyl-CoA as substrate incubated for 1 hr by ELISA	ic50	0.1920	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-hydroxypropanoyl]amino]-3-[4-(3-phenylpropyl)triazol-1-yl]propanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanamide	1233395: Inhibition of human GOAT octanoylation activity expressed in insect Sf9 cell membranes using GSSFLCAcDan as substrate after 1 hr by reverse phase HPLC with fluorescence detection method	ic50	0.7000	uM
methyl (E,2S)-5-hydroxy-5-methyl-2-(phenylmethoxycarbonylamino)dodec-3-enoate	2084169: Inhibition of GOAT (unknown origin)	ic50	1.5000	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-hydroxypropanoyl]amino]-3-[4-(2-phenylethyl)triazol-1-yl]propanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanamide	1233395: Inhibition of human GOAT octanoylation activity expressed in insect Sf9 cell membranes using GSSFLCAcDan as substrate after 1 hr by reverse phase HPLC with fluorescence detection method	ic50	3.8000	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-hydroxypropanoyl]amino]-3-(4-benzyltriazol-1-yl)propanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanamide	1233395: Inhibition of human GOAT octanoylation activity expressed in insect Sf9 cell membranes using GSSFLCAcDan as substrate after 1 hr by reverse phase HPLC with fluorescence detection method	ic50	6.0000	uM
methyl (4aS,6aR,6bS,8aR,12aS,14aR,14bS)-11-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,3,4,5,6,7,8,8a,14a,14b-decahydropicene-4a-carboxylate	1802486: GOAT Activity Assay from Article 10.1021/acs.biochem.6b01008: “Synthetic Triterpenoid Inhibition of Human Ghrelin O-Acyltransferase: The Involvement of a Functionally Required Cysteine Provides Mechanistic Insight into Ghrelin Acylation.”	ic50	6.0000	uM
(5S,8S,9S,10S,13S,14S)-10,13-dimethyl-3-oxo-4,5,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthrene-2-carbonitrile	1802486: GOAT Activity Assay from Article 10.1021/acs.biochem.6b01008: “Synthetic Triterpenoid Inhibition of Human Ghrelin O-Acyltransferase: The Involvement of a Functionally Required Cysteine Provides Mechanistic Insight into Ghrelin Acylation.”	ic50	8.0000	uM
(5R,8S,9S,10S,13S,14S)-4,4,10,13-tetramethyl-3-oxo-6,7,8,9,11,12,14,15,16,17-decahydro-5H-cyclopenta[a]phenanthrene-2-carbonitrile	1679014: Inhibition of human GOAT expressed in baculovirus infected sf9 insect cell membrane using GSSFLC-acrylodan and octanoyl-CoA as substrate preincubated for 30 mins followed by substrate addition and measured after 3 hrs by HPLC analysis	ic50	8.0000	uM
(4aS,6aR,6bS,8aR,12aS,14aR,14bS)-11-cyano-N-ethyl-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,3,4,5,6,7,8,8a,14a,14b-decahydropicene-4a-carboxamide	1679014: Inhibition of human GOAT expressed in baculovirus infected sf9 insect cell membrane using GSSFLC-acrylodan and octanoyl-CoA as substrate preincubated for 30 mins followed by substrate addition and measured after 3 hrs by HPLC analysis	ic50	8.0000	uM

CTD chemical–gene interactions

14 total (human), top 14 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	increases expression	2
OTX015	decreases expression	1
dicrotophos	decreases expression	1
S-(1,2-dichlorovinyl)cysteine	affects response to substance, increases expression, affects cotreatment	1
arctigenin	decreases reaction, increases expression	1
abrine	decreases expression	1
Benzo(a)pyrene	affects methylation	1
Cadmium	decreases expression, increases abundance	1
Glucose	decreases reaction, increases expression	1
Lipopolysaccharides	affects response to substance, increases expression, affects cotreatment	1
Urethane	decreases expression	1
Aflatoxin B1	increases expression	1
Cadmium Chloride	increases abundance, decreases expression	1
Okadaic Acid	increases expression	1

ChEMBL screening assays

20 unique, capped per target: 20 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL3590857	Binding	Inhibition of human GOAT octanoylation activity expressed in insect Sf9 cell membranes using GSSFLCAcDan as substrate after 1 hr by reverse phase HPLC with fluorescence detection method	A new class of ghrelin O-acyltransferase inhibitors incorporating triazole-linked lipid mimetic groups. — Bioorg Med Chem Lett

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.

No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.