FFAR1

Summary

FFAR1 (free fatty acid receptor 1, HGNC:4498) is a protein-coding gene on chromosome 19q13.12, encoding Free fatty acid receptor 1 (O14842). G-protein coupled receptor for medium and long chain saturated and unsaturated fatty acids that plays an important role in glucose homeostasis.

This gene encodes a member of the GP40 family of G protein-coupled receptors that are clustered together on chromosome 19. The encoded protein is a receptor for medium and long chain free fatty acids and may be involved in the metabolic regulation of insulin secretion. Polymorphisms in this gene may be associated with type 2 diabetes.

Source: NCBI Gene 2864 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 50 total — 2 pathogenic
• Druggable target: yes — 8 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_005303

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:4498
Approved symbol	FFAR1
Name	free fatty acid receptor 1
Location	19q13.12
Locus type	gene with protein product
Status	Approved
Aliases	FFA1R
Ensembl gene	ENSG00000126266
Ensembl biotype	protein_coding
OMIM	603820
Entrez	2864

Gene structure

Transcript identifiers

Ensembl transcripts: 2 — 2 protein_coding

ENST00000246553, ENST00000950226

RefSeq mRNA: 1 — MANE Select: NM_005303 NM_005303

CCDS: CCDS12458

Canonical transcript exons

ENST00000246553 — 2 exons

Exon	Start	End
ENSE00000862788	35351205	35353864
ENSE00003964439	35347902	35350838

Expression profiles

Bgee: expression breadth broad, 70 present calls, max score 81.57.

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
islet of Langerhans	UBERON:0000006	81.57	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	72.70	gold quality
pancreas	UBERON:0001264	68.82	gold quality
tendon of biceps brachii	UBERON:0008188	65.74	silver quality
buccal mucosa cell	CL:0002336	65.21	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	64.84	gold quality
body of pancreas	UBERON:0001150	63.68	gold quality
spinal cord	UBERON:0002240	63.65	gold quality
sperm	CL:0000019	62.50	gold quality
left ovary	UBERON:0002119	61.89	gold quality
bone marrow	UBERON:0002371	61.15	gold quality
parotid gland	UBERON:0001831	60.67	gold quality
right ovary	UBERON:0002118	60.52	gold quality
endothelial cell	CL:0000115	59.78	gold quality
cerebellar vermis	UBERON:0004720	58.46	gold quality
ovary	UBERON:0000992	58.43	gold quality
granulocyte	CL:0000094	58.24	gold quality
amniotic fluid	UBERON:0000173	58.15	gold quality
medial globus pallidus	UBERON:0002477	57.72	gold quality
trabecular bone tissue	UBERON:0002483	56.51	gold quality
oviduct epithelium	UBERON:0004804	56.42	silver quality
globus pallidus	UBERON:0001875	56.38	gold quality
decidua	UBERON:0002450	55.33	gold quality
nasal cavity epithelium	UBERON:0005384	55.06	gold quality
superficial temporal artery	UBERON:0001614	54.86	gold quality
substantia nigra	UBERON:0002038	54.79	gold quality
midbrain	UBERON:0001891	54.31	gold quality
putamen	UBERON:0001874	54.30	gold quality
skin of hip	UBERON:0001554	53.88	silver quality
vena cava	UBERON:0004087	53.44	gold quality

Single-cell (SCXA)

Detected in 3 experiment(s), a significant marker in 3.

Experiment	Marker?	Max mean expression
E-HCAD-31	yes	20.37
E-MTAB-5061	yes	17.34
E-ANND-3	yes	4.57

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): HR, PAX6, PDX1, ZGLP1

Literature-anchored findings (GeneRIF, showing 40)

• Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40 (PMID:12629551)
• Results suggest that GPR40 is implicated in the control of breast cancer cell growth by fatty acids and that GPR40 may provide a link between fat and cancer. (PMID:15695516)
• results suggest that the Arg211His polymorphism in the GPR40 protein gene may contribute to the variation of insulin secretory capacity in Japanese men (PMID:15736105)
• study provides evidence for GPR40 gene expression in pancreatic beta cells and implicates GPR40 in insulin secretion in humans. (PMID:16525841)
• GPR40 responded to fatty acids with different on-rates, and could be occupied by endogenous agonists before assay, masking the pharmacology of the receptor (PMID:17200419)
• This paper predicts the 5’ structure of the human GP40 gene based on alignments between mouse and human genomic DNA. (PMID:17525159)
• cell-specific expression of the GPR40 gene involves a characteristic chromatin organization of the locus and is controlled at the transcriptional level through HR2, a potent beta cell-specific enhancer (PMID:17525159)
• analysis of residues important for agonist recognition and activation in GPR40 (PMID:17699519)
• Variation in the FFAR1 gene may contribute to impaired beta cell function in type 2 diabetes (PMID:17987108)
• This newly identified GPR40 variant results in a loss of function that prevents the beta-cell ability to adequately sense lipids as an insulin secretory stimulus because of impaired intracellular Ca2+ concentration increase. (PMID:18583466)
• A flow cytometry-based binding assay for FFAR1 is reported. (PMID:18927207)
• In this review, the mechanism of receptor activation, pharmacology, and the physiological functions of the fatty acid binding receptors GPR40, GPR41, GPR43, and GPR119 are discussed. (PMID:19009545)
• Two arginine-glutamate ionic locks near the extracellular surface of FFAR1 gate receptor activation. (PMID:19068482)
• Transfection of GPR40 into mice may provide a novel insulin secretagogue beneficial for the treatment of type 2 diabetes. (PMID:19401434)
• results show expression of GPR40 in pancreatic islets which are regulated by FFA; finding that T2DM islets have lower GPR40 expression & correlation with insulin secretion raises possibility of involvement of GPR40 in diabetes beta-cell dysfunction (PMID:19758793)
• Results describe agonist-receptor interactions of GPR40 using molecular dynamics simulations. (PMID:20227312)
• differences in body composition and lipids associated with common SNPs in the FFAR1 gene (PMID:21552566)
• Phytanic acid and pristanic acid activate the free fatty acid receptor GPR40, a G-protein-coupled receptor which is involved in the Ca2+ signaling of fatty acids. (PMID:21570468)
• GPR40/FFA1 influences both insulin and glucagon secretion in rat islets, but only insulin secretion in human islets. (PMID:22106100)
• GPR41 gene expression is mediated by internal ribosome entry site (IRES)-dependent translation of bicistronic mRNA encoding GPR40 and GPR41 proteins (PMID:22493486)
• Propionate-stimulated GPR41 strongly coupled to ERK1/2 activation, while the coupling of linoleic acid-activated GPR40 and acetate-activated GPR43 was weaker. (PMID:22712802)
• A review of the physiological role of GPR40 and potential antidiabetic drugs targeting GPR40. [Review] (PMID:23023155)
• FFAR1 agonists support beta-cell function, but variation in FFAR1 influences NEFA effects on insulin secretion and therefore could affect therapeutic efficacy of FFAR1 agonists. (PMID:23378609)
• Potent free fatty acid 1 receptor agonist TUG-469 may be promising candidate for the treatment of type 2 diabetes mellitus. (PMID:23861168)
• It was concluded that FFAR1 in the pancreatic beta-cell plays a substantial role not only in acute potentiation of insulin secretion by palmitate but also in the negative long-term effects of palmitate on insulin metabolism. (PMID:24035997)
• In a neuroblastoma cell line, GPR40 was activated by docosahexaenoic acid and selective agonists, yet not by palmitic acid. Its activation provoked the phosphorylation of CREB. (PMID:24550142)
• arrestin-3 and GRK2 play an essential role in the regulation of agonist-mediated GPR40 internalization, but are not involved in the regulation of constitutive GPR40 internalization. (PMID:25038452)
• the crystal structure of hGPR40 receptor bound to TAK-875 at 2.3 A resolution (PMID:25043059)
• the activation of GPR40 attenuates cisplatin-induced apoptosis. (PMID:25092426)
• Characterizing pharmacological ligands to study the long-chain fatty acid receptors GPR40/FFA1 and GPR120/FFA4 (PMID:25131623)
• upregulation of GPR40 expression enhances the mitogenic response to epoxyeicosatrienoic acids (PMID:25679385)
• Palmitic acid boosted inflammatory response of microvascular endothelial cells to LPS via GPR40 and nSMase. (PMID:25795558)
• It regulates insulin secretion in pancreatic beta-cells. (review) (PMID:26028412)
• GPR40 and PPARgamma can function as an integrated two-receptor signal transduction pathway, a finding with implications for rational antidiabetic drug development. (PMID:26105050)
• GPR40 functions via both G protein-mediated and beta-arrestin-mediated mechanisms; endogenous and synthetic ligands differentially engage these pathways to promote insulin secretion. (PMID:26157145)
• These results suggest that distinct effects of GPR120 and GPR40 are involved in the acquisition of malignant property in pancreatic cancer cells. (PMID:26282200)
• Results show that GPR40 negatively regulated the cell motile and invasive activities of HT1080 cells suggesting that GPR40 negatively regulates the tumor progression of fibrosarcoma cells. (PMID:26331585)
• results suggest that FFAR1 is the functionally dominant free fatty acid receptor in both human and guinea pig airway smooth muscle. (PMID:26342087)
• knocking down the expression of the regulatory subunit PKAR1alpha, thereby reproducing the effects of IL-1beta and PGE on VSMCs, we demonstrated the contribution of PKA activity to the observed behavior of VSMCs (PMID:26408932)
• These data demonstrate that R104 in GPR40 is critically involved in the normal receptor functions. Interestingly, R104P is a registered single-nucleotide polymorphism of GPR40. (PMID:26505901)

Cross-species orthologs

2 orthologs

Organism	Symbol	Gene ID
mus_musculus	Ffar1	ENSMUSG00000044453
rattus_norvegicus	Ffar1	ENSRNOG00000024009

Paralogs (15): GPR31 (ENSG00000120436), GPR42 (ENSG00000126251), FFAR2 (ENSG00000126262), OXER1 (ENSG00000162881), OXGR1 (ENSG00000165621), P2RY1 (ENSG00000169860), P2RY6 (ENSG00000171631), GPR82 (ENSG00000171657), P2RY2 (ENSG00000175591), HCAR2 (ENSG00000182782), FFAR3 (ENSG00000185897), P2RY4 (ENSG00000186912), HCAR1 (ENSG00000196917), SUCNR1 (ENSG00000198829), HCAR3 (ENSG00000255398)

Protein

Protein identifiers

Free fatty acid receptor 1 — O14842 (reviewed: O14842)

Alternative names: G-protein coupled receptor 40

All UniProt accessions (1): O14842

UniProt curated annotations — full annotation on UniProt →

Function. G-protein coupled receptor for medium and long chain saturated and unsaturated fatty acids that plays an important role in glucose homeostasis. Fatty acid binding increases glucose-stimulated insulin secretion, and may also enhance the secretion of glucagon-like peptide 1 (GLP-1). May also play a role in bone homeostasis; receptor signaling activates pathways that inhibit osteoclast differentiation. Ligand binding leads to a conformation change that triggers signaling via G-proteins that activate phospholipase C, leading to an increase of the intracellular calcium concentration. Seems to act through a G(q) and G(i)-mediated pathway. Mediates the anti-inflammatory effects of omega-3 polyunsaturated fatty acids (PUFAs) via inhibition of NLRP3 inflammasome activation.

Subcellular location. Cell membrane.

Tissue specificity. Detected in brain and pancreas. Detected in pancreatic beta cells.

Activity regulation. The receptor is strongly activated by gamma-linolenic acid, while myristate gives a lower response. It is also activated by phytanic acid and pristanic acid. Is also activated by synthetic agonists, such as TAK-875 (fasiglifam); this compound is a partial agonist and potentiates the activity of the endogenous ligand gamma-linolenic acid.

Similarity. Belongs to the G-protein coupled receptor 1 family.

RefSeq proteins (1): NP_005294* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR013312	GPR40-rel_orph	Family
IPR013313	GPR40_recept_FA	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (51 total): mutagenesis site 13, helix 12, topological domain 8, transmembrane region 7, strand 3, site 2, chain 1, glycosylation site 1, disulfide bond 1, sequence variant 1, sequence conflict 1, turn 1

Structure

Experimental structures (PDB)

9 structures.

PDB	Method	Resolution (Å)
5TZR	X-RAY DIFFRACTION	2.2
4PHU	X-RAY DIFFRACTION	2.33
5KW2	X-RAY DIFFRACTION	2.76
8EIT	ELECTRON MICROSCOPY	2.8
8EJC	ELECTRON MICROSCOPY	3
9K1C	ELECTRON MICROSCOPY	3.2
5TZY	X-RAY DIFFRACTION	3.22
8T3V	ELECTRON MICROSCOPY	3.39
8EJK	ELECTRON MICROSCOPY	3.4

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-O14842-F1	89.85	0.79

Antibody-complex structures (SAbDab): 4 — 8EIT, 8EJC, 8EJK, 8T3V

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): 145 (important for receptor activation); 172 (important for receptor activation)

Disulfide bonds (1): 79–170

Glycosylation sites (1): 155

Mutagenesis-validated functional residues (13):

Position	Phenotype
12	reduces cell surface expression and response to linolenic acid and synthetic agonists.
44	reduces response to synthetic agonists.
91	reduces response to linolenic acid. reduces response to synthetic agonists.
114	reduces response to synthetic agonists.
123	reduces response to synthetic agonists.
137	reduces response to linolenic acid. reduces response to synthetic agonists.
145	constitutive receptor signaling.
172	constitutive receptor signaling.
183	reduces response to linolenic acid. strongly reduces response to synthetic agonists.
240	reduces response to linolenic acid. reduces response to synthetic agonists.
244	reduces response to linolenic acid. reduces response to synthetic agonists.
258	strongly reduces response to linolenic acid. strongly reduces response to synthetic agonists.
258	reduces response to linolenic acid. strongly reduces response to synthetic agonists.

Function

Pathways and Gene Ontology

Reactome pathways

5 pathways

ID	Pathway
R-HSA-381771	Synthesis, secretion, and inactivation of Glucagon-like Peptide-1 (GLP-1)
R-HSA-400511	Synthesis, secretion, and inactivation of Glucose-dependent Insulinotropic Polypeptide (GIP)
R-HSA-416476	G alpha (q) signalling events
R-HSA-434316	Fatty Acids bound to GPR40 (FFAR1) regulate insulin secretion
R-HSA-444209	Free fatty acid receptors

MSigDB gene sets: 87 (showing top): GSE45365_HEALTHY_VS_MCMV_INFECTION_CD8_TCELL_IFNAR_KO_UP, GOBP_POSITIVE_REGULATION_OF_CALCIUM_ION_TRANSPORT, GOBP_NEGATIVE_REGULATION_OF_INTERLEUKIN_1_PRODUCTION, GOBP_INSULIN_SECRETION, GOBP_POSITIVE_REGULATION_OF_PROTEIN_LOCALIZATION, GOBP_REGULATION_OF_HORMONE_LEVELS, GOBP_HORMONE_TRANSPORT, GOBP_INTERLEUKIN_1_PRODUCTION, GOBP_MONOATOMIC_CATION_TRANSPORT, GOBP_CELL_CELL_SIGNALING, GOBP_POSITIVE_REGULATION_OF_INSULIN_SECRETION, GOBP_REGULATION_OF_PROTEIN_SECRETION, GOBP_NEGATIVE_REGULATION_OF_MULTICELLULAR_ORGANISMAL_PROCESS, GOBP_POSITIVE_REGULATION_OF_MONOATOMIC_ION_TRANSPORT, GOBP_CYTOKINE_PRODUCTION

GO Biological Process (11): G protein-coupled receptor signaling pathway (GO:0007186), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), positive regulation of cytosolic calcium ion concentration (GO:0007204), insulin secretion (GO:0030073), positive regulation of insulin secretion (GO:0032024), negative regulation of interleukin-1 beta production (GO:0032691), glucose homeostasis (GO:0042593), positive regulation of calcium ion transport (GO:0051928), response to fatty acid (GO:0070542), ligand-gated ion channel signaling pathway (GO:1990806), signal transduction (GO:0007165)

GO Molecular Function (3): G protein-coupled receptor activity (GO:0004930), lipid binding (GO:0008289), bioactive lipid receptor activity (GO:0045125)

GO Cellular Component (2): plasma membrane (GO:0005886), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-4 pathways:

Category	Pathways
Incretin synthesis, secretion, and inactivation	2
GPCR downstream signalling	1
Free fatty acids regulate insulin secretion	1
Class A/1 (Rhodopsin-like receptors)	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
G protein-coupled receptor activity	2
signal transduction	2
G protein-coupled receptor signaling pathway	2
phospholipase C activator activity	1
regulation of biological quality	1
protein secretion	1
peptide hormone secretion	1
insulin secretion	1
positive regulation of protein secretion	1
regulation of insulin secretion	1
positive regulation of peptide hormone secretion	1
interleukin-1 beta production	1
regulation of interleukin-1 beta production	1
negative regulation of interleukin-1 production	1
carbohydrate homeostasis	1
calcium ion transport	1
positive regulation of monoatomic ion transport	1
regulation of calcium ion transport	1
response to lipid	1
response to oxygen-containing compound	1
ligand-gated monoatomic ion channel activity	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
transmembrane signaling receptor activity	1
binding	1
membrane	1
cell periphery	1
cellular anatomical structure	1

Protein interactions and networks

STRING

940 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
FFAR1	FFAR4	Q5NUL3	938
FFAR1	GNAQ	P50148	898
FFAR1	GCG	P01275	867
FFAR1	GPR84	Q9NQS5	831
FFAR1	GALR2	O43603	829
FFAR1	GALR1	P47211	818
FFAR1	GPR119	Q8TDV5	814
FFAR1	GAL	P22466	800
FFAR1	CD22	P20273	791
FFAR1	GIP	P09681	718
FFAR1	GLP1R	P43220	713
FFAR1	PPARG	P37231	702
FFAR1	ARRB2	P32121	700
FFAR1	GPR142	Q7Z601	689
FFAR1	INS	P01308	661

IntAct

2 interactions, top by confidence:

A	B	Type	Score
FFAR1	SLC12A8	psi-mi:“MI:0914”(association)	0.350

BioGRID (236): TNPO3 (Affinity Capture-MS), TOMM22 (Affinity Capture-MS), NTSR1 (Affinity Capture-MS), VKORC1L1 (Affinity Capture-MS), RAB18 (Affinity Capture-MS), RMND1 (Affinity Capture-MS), TMCO3 (Affinity Capture-MS), COX6C (Affinity Capture-MS), ABHD17B (Affinity Capture-MS), FBXO2 (Affinity Capture-MS), COX6A1 (Affinity Capture-MS), ND4 (Affinity Capture-MS), DECR2 (Affinity Capture-MS), RAB14 (Affinity Capture-MS), ERGIC2 (Affinity Capture-MS)

ESM2 similar proteins: A0A6I8PUB9, O00155, O00270, O14842, O14843, O15529, O43603, O46685, O60755, O88626, O88634, O88853, O88854, O88855, P0C5I1, P46092, P46093, P50132, Q149R9, Q15722, Q15743, Q1JQB3, Q3T181, Q3UFD7, Q3ZC80, Q4KLH9, Q6XKD3, Q76JU8, Q76JU9, Q76JV1, Q86VZ1, Q8BUD0, Q8BYC4, Q8HYC3, Q8K3T4, Q8TDS5, Q8TDU9, Q920E0, Q924U0, Q96G91

Diamond homologs: A0A4W3GG95, A0A6I8PUB9, B2GV46, B5X337, D4A7K7, E7FEL0, E9QJ73, F8VQN3, O00270, O08726, O08858, O14842, O14843, O15529, O42179, O43603, O46685, O60755, O77408, O88410, O88626, O88634, O88853, P21109, P23944, P25024, P25025, P35344, P35383, P35414, P41231, P41232, P46092, P46093, P49652, P49682, P49683, P50132, P51675, P51679

SIGNOR signaling

8 interactions.

A	Effect	B	Mechanism
TAK-875	up-regulates	FFAR1	“chemical activation”
FFAR1	“up-regulates activity”	GNAS	binding
FFAR1	“up-regulates activity”	GNAL	binding
FFAR1	“up-regulates activity”	GNAI1	binding
FFAR1	“up-regulates activity”	GNAO1	binding
FFAR1	“up-regulates activity”	GNAQ	binding
FFAR1	“up-regulates activity”	GNA12	binding
“hexadecanoic acid”	“up-regulates activity”	FFAR1	“chemical activation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	2
Likely pathogenic	0
Uncertain significance	46
Likely benign	2
Benign	0

Top pathogenic / likely-pathogenic (2)

Variant ID	HGVS	Classification
394109	GRCh37/hg19 19q12-13.12(chr19:30735448-36120396)x3	Pathogenic
4070957	NM_005303.3(FFAR1):c.69_70insTTT (p.Asn23_Val24insPhe)	Pathogenic

SpliceAI

63 predictions. Top by Δscore:

Variant	Effect	Δscore
19:35352725:C:G	acceptor_gain	0.7200
19:35352657:G:C	donor_loss	0.4600
19:35352658:T:A	donor_loss	0.4600
19:35352749:G:A	acceptor_gain	0.4600
19:35352652:GGGAG:G	donor_gain	0.4100
19:35352653:GGAGG:G	donor_gain	0.4100
19:35352724:A:AG	acceptor_gain	0.3600
19:35352312:G:GT	donor_gain	0.3500
19:35352721:T:TA	acceptor_gain	0.3400
19:35352748:T:TA	acceptor_gain	0.3400
19:35352943:AAG:A	acceptor_gain	0.3300
19:35352653:GGAG:G	donor_gain	0.3200
19:35352654:GAGG:G	donor_gain	0.3200
19:35352659:AAGT:A	donor_loss	0.3100
19:35352135:T:TA	acceptor_gain	0.3000
19:35352655:AG:A	donor_gain	0.3000
19:35352656:GG:G	donor_gain	0.3000
19:35352943:AAGG:A	acceptor_gain	0.3000
19:35352448:G:GT	donor_gain	0.2800
19:35352661:G:C	donor_loss	0.2800
19:35352944:A:G	acceptor_gain	0.2700
19:35353772:T:A	acceptor_gain	0.2700
19:35352646:G:GA	donor_gain	0.2600
19:35352654:GAG:G	donor_gain	0.2500
19:35352657:G:GG	donor_gain	0.2500
19:35352696:T:TA	donor_gain	0.2400
19:35352325:G:GT	donor_gain	0.2300
19:35352724:AC:A	acceptor_gain	0.2300
19:35352942:CA:C	acceptor_gain	0.2300
19:35352943:AA:A	acceptor_gain	0.2300

AlphaMissense

1862 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
19:35352350:T:A	W267R	0.987
19:35352350:T:C	W267R	0.987
19:35351767:G:C	W72C	0.986
19:35351767:G:T	W72C	0.986
19:35351852:A:C	S101R	0.984
19:35351854:T:A	S101R	0.984
19:35351854:T:G	S101R	0.984
19:35351737:G:C	K62N	0.983
19:35351737:G:T	K62N	0.983
19:35351606:G:C	G19R	0.975
19:35352274:C:A	N241K	0.975
19:35352274:C:G	N241K	0.975
19:35352353:A:C	S268R	0.973
19:35352355:T:A	S268R	0.973
19:35352355:T:G	S268R	0.973
19:35352073:G:C	W174C	0.972
19:35352073:G:T	W174C	0.972
19:35352122:T:C	F191L	0.970
19:35352124:T:A	F191L	0.970
19:35352124:T:G	F191L	0.970
19:35351931:G:A	C127Y	0.969
19:35351864:T:G	Y105D	0.968
19:35352104:A:C	S185R	0.968
19:35352106:C:A	S185R	0.968
19:35352106:C:G	S185R	0.968
19:35351932:C:G	C127W	0.966
19:35351607:G:A	G19D	0.965
19:35352152:T:C	C201R	0.963
19:35352263:G:A	G238R	0.963
19:35352263:G:C	G238R	0.963

dbSNP variants (sampled 300 via entrez): RS1000167582 (19:35351730 C>T), RS1000902013 (19:35354162 T>TTTTTG), RS1001174421 (19:35348539 C>T), RS1001789199 (19:35348784 C>A,G), RS1002232282 (19:35347301 G>A,T), RS1002373980 (19:35353505 C>T), RS1002424595 (19:35353184 G>A), RS1003048896 (19:35351122 G>A), RS1003238790 (19:35346285 G>A,T), RS1003438044 (19:35352122 T>C), RS1003512240 (19:35350977 G>A,T), RS1003765756 (19:35353350 G>A,C,T), RS1004220590 (19:35346473 C>A,G,T), RS1004309946 (19:35347357 A>G), RS1004377720 (19:35353180 T>A,C)

Disease associations

OMIM: gene MIM:603820 | disease phenotypes: MIM:143890

GenCC curated gene-disease

Mondo (1): hypercholesterolemia, familial, 1 (MONDO:0007750)

Orphanet (1): Homozygous familial hypercholesterolemia (Orphanet:391665)

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 (2): CHEMBL4422 (SINGLE PROTEIN), CHEMBL5482994 (PROTEIN COMPLEX)

Molecules with ChEMBL bioactivity

8 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 503,719 (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
CHEMBL121	ROSIGLITAZONE	4	58,849
CHEMBL1829174	FASIGLIFAM	3	815
CHEMBL367149	DOCONEXENT	3	63,817
CHEMBL464982	GAMOLENIC ACID	3	26,552
CHEMBL267476	LINOLEIC ACID	2	323,195
CHEMBL277522	FENBUFEN	2	30,447
CHEMBL3915620	LY2881835	1	10
CHEMBL4297471	MK-8666	1	34

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

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: gpcr — Free fatty acid receptors

Most potent curated ligand interactions (20 total), top 20:

Ligand	Action	Affinity	Parameter
AMG-837	Agonist	8.5	pEC50
compound 4 [PMID: 27074625]	Agonist	8.4	pKd
TUG-770	Full agonist	8.2	pEC50
TUG-905	Agonist	8.05	pEC50
HWL-088	Agonist	7.72	pEC50
TUG-424	Full agonist	7.5	pEC50
ZYDG2	Agonist	7.39	pEC50
GW9508	Partial agonist	7.3	pEC50
fasiglifam	Agonist	7.1	pEC50
compound B [PMID:18477808]	Full agonist	6.1	pEC50
docosahexaenoic acid	Full agonist	6.0	pEC50
GW1100	Antagonist	6.0	pIC50
medica 16	Full agonist	5.9	pEC50
α-linolenic acid	Full agonist	5.7	pEC50
linoleic acid	Full agonist	5.7	pEC50
oleic acid	Full agonist	5.7	pEC50
rosiglitazone	Full agonist	5.6	pEC50
palmitic acid	Full agonist	5.3	pEC50
myristic acid	Full agonist	5.1	pEC50
setogepram	Agonist	2.98	pEC50

Binding affinities (BindingDB)

577 measured of 639 human assays (639 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
(2S,3R)-3-[3-[[1-[1-[2,5-bis(trifluoromethyl)phenyl]ethyl]azetidin-3-yl]methoxy]phenyl]-3-cyclopropyl-2-methylpropanoic acid	EC50	0.3 nM	US-10059667: Antidiabetic compounds
(3S)-3-[3-[[1-[1-[2,5-bis(trifluoromethyl)phenyl]ethyl]azetidin-3-yl]methoxy]phenyl]-3-cyclopropylpropanoic acid	EC50	0.6 nM	US-10059667: Antidiabetic compounds
(2S,3R)-3-[3-[[1-[[2,5-bis(trifluoromethyl)phenyl]methyl]-3-fluoroazetidin-3-yl]methoxy]phenyl]-3-cyclopropyl-2-methylpropanoic acid	EC50	0.9 nM	US-10059667: Antidiabetic compounds
(2S,3R)-3-[3-[[1-[[2,5-bis(trifluoromethyl)phenyl]methyl]piperidin-4-yl]methoxy]phenyl]-3-cyclopropyl-2-methylpropanoic acid	EC50	1 nM	US-10059667: Antidiabetic compounds
3-(4-methoxy-2-methylphenyl)-5-[[4-[(2S)-1-(2H-tetrazol-5-yl)pent-3-yn-2-yl]phenoxy]methyl]thieno[2,3-c]pyridine	EC50	1 nM	US-10106553: Substituted benzothiophenyl derivatives as GPR40 agonists for the treatment of type II diabetes
(2S,3R)-3-[3-[[1-[[2,5-bis(trifluoromethyl)phenyl]methyl]azetidin-3-yl]methoxy]phenyl]-3-cyclopropyl-2-methylpropanoic acid	EC50	1.4 nM	US-10059667: Antidiabetic compounds
(2S,3R)-3-[3-[[(3R)-1-[[2,5-bis(trifluoromethyl)phenyl]methyl]pyrrolidin-3-yl]methoxy]phenyl]-3-cyclopropyl-2-methylpropanoic acid	EC50	1.5 nM	US-10059667: Antidiabetic compounds
(2S,3R)-3-(3-(((S)-1-(2,5-bis(trifluoromethyl)benzyl)piperidin-3-yl)oxy)phenyl)-3-cyclopropyl-2-methylpropanoic acid	EC50	1.9 nM	US-10059667: Antidiabetic compounds
(3S)-3-[3-[[6-butan-2-yl-5-(2-fluoro-5-methoxyphenyl)pyrazin-2-yl]methoxy]phenyl]-3-cyclopropylpropanoic acid	EC50	2 nM	US-9688642: Substituted pyrazines as GPR40 agonists
(3S)-3-[3-[[6-butyl-5-(2-fluoro-5-methoxyphenyl)pyrazin-2-yl]methoxy]phenyl]-3-cyclopropylpropanoic acid	EC50	2 nM	US-9688642: Substituted pyrazines as GPR40 agonists
(3S)-3-cyclopropyl-3-[3-[[6-(2,2-dimethylpropyl)-5-(2-fluoro-5-methoxyphenyl)pyrazin-2-yl]methoxy]phenyl]propanoic acid	EC50	2 nM	US-9688642: Substituted pyrazines as GPR40 agonists
(3S)-3-cyclopropyl-3-[3-[[5-(5-fluoro-2-methoxy-4-pyridinyl)-6-(2-methylpropyl)pyrazin-2-yl]methoxy]phenyl]propanoic acid	EC50	2 nM	US-9688642: Substituted pyrazines as GPR40 agonists
(2S,3R)-3-[3-[(3R)-1-[[2,5-bis(trifluoromethyl)phenyl]methyl]piperidin-3-yl]oxyphenyl]-3-cyclopropyl-2-methylpropanoic acid	EC50	2 nM	US-10059667: Antidiabetic compounds
5-[(2S)-2-[4-[[3-(2-methylphenyl)-1-benzothiophen-5-yl]methoxy]phenyl]pent-3-ynyl]-2H-tetrazole	EC50	2 nM	US-10106553: Substituted benzothiophenyl derivatives as GPR40 agonists for the treatment of type II diabetes
(3S)-3-(4-((3-(2-Methyl-4- ((tetrahydro-2H-pyran-4- yl)oxy)phenyl)benzo[b]thiophen- 5-yl)methoxy)phenyl) hex-4-ynoic acid	EC50	2 nM	US-10131648: Substituted benzothiophenyl derivatives as GPR40 agonists for the treatment of type II diabetes
3-(4-((3-(2- Methylphenyl)benzo[b]thiophen- 5-yl)methoxy)phenyl) hex-4-ynoic acid	EC50	2 nM	US-10131648: Substituted benzothiophenyl derivatives as GPR40 agonists for the treatment of type II diabetes
trans-(1S,2S)-2-[5-[[(1R)-4-[2,6-dimethyl-4-(2-methyltetrazol-5-yl)phenyl]-7-fluoro-2,3-dihydro-1H-inden-1-yl]amino]pyrazin-2-yl]cyclopropane-1-carboxylic acid	EC50	2 nM	US-10253004: Indanylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
(3S)-3-cyclopropyl-3-[3-[[6-(2,2-dimethylpropoxy)-5-(5-fluoro-2-methoxy-4-pyridinyl)pyrazin-2-yl]methoxy]phenyl]propanoic acid	EC50	3 nM	US-9688642: Substituted pyrazines as GPR40 agonists
3-(2-methylphenyl)-5-[[4-[(2S)-1-(2H-tetrazol-5-yl)pent-3-yn-2-yl]phenoxy]methyl]thieno[2,3-c]pyridine	EC50	3 nM	US-10106553: Substituted benzothiophenyl derivatives as GPR40 agonists for the treatment of type II diabetes
(3S)-3-[4-[[3-[2-Methyl-4-(3- methylsulfonylpropoxy)phenyl] benzo[b]thiophen-5- yl]methoxy]phenyl] hex-4-ynoic acid	EC50	3 nM	US-10131648: Substituted benzothiophenyl derivatives as GPR40 agonists for the treatment of type II diabetes
[(S)-6-{(R)-7-Fluoro-4-[4-(2-methyl-2H-tetrazol-5-yl)-phenoxy]-indan-1-yloxy}-2,3-dihydro-benzofuran-3-yl]-acetic acid	EC50	3 nM	US-9597310: Indanyloxydihydrobenzofuranylacetic acids
(1S,2S)-2-(5-{(R)-4-[2,6-Dimethyl-4-(2-methyl-2H-tetrazol-5-yl)-phenyl]-indan-1-ylamino}-pyrazin-2-yl)-cyclopropanecarboxylic acid	EC50	3 nM	US-10253004: Indanylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
trans-(1S,2S)-2-[5-[[(1R)-7-fluoro-4-[4-[1-(2-hydroxy-2-methylpropyl)tetrazol-5-yl]-2,6-dimethylphenyl]-2,3-dihydro-1H-inden-1-yl]amino]pyrazin-2-yl]cyclopropane-1-carboxylic acid	EC50	3 nM	US-10253004: Indanylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
(2S,3R)-3-cyclopropyl-3-[2-[4-(5-fluoro-2-methoxy-4-pyridinyl)phenyl]-2,3,4,5-tetrahydro-1-benzoxepin-8-yl]-2-methylpropanoic acid	EC50	3.1 nM	US-10131651: [7,6]-fused bicyclic antidiabetic compounds
(3S)-3-(4-((3-(2-Methyl-4- (piperidin-4- ylmethyl)phenyl)benzo[b]thiophen- 5-yl)methoxy)phenyl)hex-4- ynoic acid	EC50	4 nM	US-10131648: Substituted benzothiophenyl derivatives as GPR40 agonists for the treatment of type II diabetes
((S)-6-{(R)-7-Fluoro-4-[2-fluoro-4-(tetrahydro-2H-pyran-4-yloxy)phenoxy]-indan-1-yloxy}-2,3-dihydrobenzofuran-3-yl)-acetic acid	EC50	4 nM	US-9597310: Indanyloxydihydrobenzofuranylacetic acids
((S)-6-{(R)-7-Fluoro-4-[4-(2-methylthiazol-4-yl)phenoxy]-indan-1-yloxy}-2,3-dihydrobenzofuran-3-yl)-acetic acid methyl ester	EC50	4 nM	US-9597310: Indanyloxydihydrobenzofuranylacetic acids
(1S,2S)-2-(5-{(R)-7-Fluoro-4-[4-(3-hydroxy-3-methyl-butoxy)-2,6-dimethyl-phenyl]-indan-1-ylamino}-pyrazin-2-yl)-cyclopropanecarboxylic acid	EC50	4 nM	US-10253004: Indanylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
(1S,2S)-2-(5-{(R)-4-[4-(3-Hydroxy-3-methyl-butoxy)-2,6-dimethyl-phenyl]-indan-1-ylamino}-pyrazin-2-yl)-cyclopropanecarboxylic acid	EC50	4 nM	US-10253004: Indanylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
trans-(1S,2S)-2-[5-[[(1R)-4-[2,6-dimethyl-4-(oxan-4-ylmethoxy)phenyl]-7-fluoro-2,3-dihydro-1H-inden-1-yl]amino]pyrazin-2-yl]cyclopropane-1-carboxylic acid	EC50	4 nM	US-10253004: Indanylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
trans-(1S,2S)-2-[5-[[(1R)-4-(2,6-dichloro-3-methylphenyl)-7-fluoro-2,3-dihydro-1H-inden-1-yl]amino]pyrazin-2-yl]cyclopropane-1-carboxylic acid	EC50	4 nM	US-10253004: Indanylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
trans-(1S,2S)-2-[5-[[(1R)-4-[2,6-dimethyl-4-(5-methylpyrimidin-2-yl)phenyl]-7-fluoro-2,3-dihydro-1H-inden-1-yl]amino]pyrazin-2-yl]cyclopropane-1-carboxylic acid	EC50	4 nM	US-10253004: Indanylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
trans-(1S,2S)-2-[5-[[(1R)-4-(2,6-diethylphenyl)-7-fluoro-2,3-dihydro-1H-inden-1-yl]amino]pyrazin-2-yl]cyclopropane-1-carboxylic acid	EC50	4 nM	US-10253004: Indanylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
trans-(1S,2S)-2-[5-[[(1R)-4-(2,6-dimethyl-4-pyrazin-2-ylphenyl)-7-fluoro-2,3-dihydro-1H-inden-1-yl]amino]pyrazin-2-yl]cyclopropane-1-carboxylic acid	EC50	4 nM	US-10253004: Indanylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
sodium (2S,3R)-3-cyclobutyl-3-[2-[4-(2-fluoro-5-methoxyphenyl)phenyl]-2,3,4,5-tetrahydro-1-benzoxepin-8-yl]-2-methylpropanoate	EC50	4.6 nM	US-10131651: [7,6]-fused bicyclic antidiabetic compounds
(3S)-3-[3-[[6-(2-azaspiro[3.3]heptan-2-yl)-5-(2-fluoro-5-methoxyphenyl)pyrazin-2-yl]methoxy]phenyl]-3-cyclopropylpropanoic acid	EC50	5 nM	US-9688642: Substituted pyrazines as GPR40 agonists
(3S)-3-cyclopropyl-3-[3-[[6-(2,2-dimethylpropoxy)-5-(2-fluoro-5-methoxyphenyl)pyrazin-2-yl]methoxy]phenyl]propanoic acid	EC50	5 nM	US-9688642: Substituted pyrazines as GPR40 agonists
(3S)-3-[4-[[3-(2- Methylphenyl)benzo[b]thiophen- 5-yl]methoxy]phenyl] hex-4-ynoic acid	EC50	5 nM	US-10195178: GPR40 agonists in anti-diabetic drug combinations
(3S)-3-[4-[[3-[4-[(4-Hydroxy- 1,1-dioxo-thian-4-yl)methoxy]- 2-methyl-phenyl]benzo[b] thiophen-5-yl]methoxy]phenyl] hex-4-ynoic acid	EC50	5 nM	US-10131648: Substituted benzothiophenyl derivatives as GPR40 agonists for the treatment of type II diabetes
(3S)-3-(4-((3-(4-(2- Methoxyethoxy)-2- methylphenyl)benzo[b]thiophen- 5-yl)methoxy)phenyl) hex-4-ynoic acid	EC50	5 nM	US-10131648: Substituted benzothiophenyl derivatives as GPR40 agonists for the treatment of type II diabetes
(3S)-3-(4-((3-(2- Bromophenyl)benzo[b]thiophen- 5-yl)methoxy)phenyl) hex-4-ynoic acid	EC50	5 nM	US-10131648: Substituted benzothiophenyl derivatives as GPR40 agonists for the treatment of type II diabetes
[(S)-6-{(R)-7-Fluoro-4-[4-(3-hydroxy-3-methyl-butoxy)-phenoxy]-indan-1-yloxy}-2,3-dihydro-benzofuran-3-yl]-acetic acid	EC50	5 nM	US-9597310: Indanyloxydihydrobenzofuranylacetic acids
[(S)-6-{(R)-7-Fluoro-4-[4-(2-methyl-thiazol-5-yl)-phenoxy]-indan-1-yloxy}-2,3-dihydro-benzofuran-3-yl]-acetic acid	EC50	5 nM	US-9597310: Indanyloxydihydrobenzofuranylacetic acids
[(S)-6-((R)-7-Fluoro-4-{4-[(tetrahydro-2H-pyran-4-yl)methyl]phenoxy}-indan-1-yloxy)-2,3-dihydrobenzofuran-3-yl]-acetic acid	EC50	5 nM	US-9597310: Indanyloxydihydrobenzofuranylacetic acids
trans-(1S,2S)-2-[5-[[(1R)-4-(2,6-dichloro-3,5-dimethoxyphenyl)-7-fluoro-2,3-dihydro-1H-inden-1-yl]amino]pyrazin-2-yl]cyclopropane-1-carboxylic acid	EC50	5 nM	US-10253004: Indanylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
trans-(1S,2S)-2-[5-[[(1R)-7-fluoro-4-[4-(2-methoxy-4-pyridinyl)-2,6-dimethylphenyl]-2,3-dihydro-1H-inden-1-yl]amino]pyrazin-2-yl]cyclopropane-1-carboxylic acid	EC50	5 nM	US-10253004: Indanylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
(3S)-3-(4-((3-(4-((1,1- Dioxidotetrahydro-2H- thiopyran-4-yl)methoxy)-2- methylphenyl)benzo[b]thiophen- 5-yl)methoxy)phenyl) hex-4-ynoic acid	EC50	6 nM	US-10131648: Substituted benzothiophenyl derivatives as GPR40 agonists for the treatment of type II diabetes
2-(3-Oxo-1-(4-((3-(2- methylphenyl) benzo[b]thiophen-5- yl)methoxy)phenyl)cyclobutyl) acetic acid	EC50	6 nM	US-10131648: Substituted benzothiophenyl derivatives as GPR40 agonists for the treatment of type II diabetes
(3S)-3-(4-((3-(6-(2- Methoxyethoxy)-4- methylpyridin-3- yl)benzo[b]thiophen-5- yl)methoxy)phenyl) hex-4-ynoic acid	EC50	6 nM	US-10131648: Substituted benzothiophenyl derivatives as GPR40 agonists for the treatment of type II diabetes
{(S)-6-[(R)-4-(2,3-Dihydro-benzofuran-5-yloxy)-7-fluoro-indan-1-yloxy]-2,3-dihydro-benzofuran-3-yl}-acetic acid	EC50	6 nM	US-9597310: Indanyloxydihydrobenzofuranylacetic acids

ChEMBL bioactivities

3247 potent at pChembl≥5 of 3394 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.40	EC50	0.04	nM	CHEMBL4859651
10.00	EC50	0.1	nM	CHEMBL475027
9.96	EC50	0.11	nM	CHEMBL4541658
9.70	EC50	0.2	nM	CHEMBL4463571
9.70	EC50	0.2	nM	CHEMBL6063201
9.60	EC50	0.25	nM	CHEMBL4457303
9.60	EC50	0.25	nM	CHEMBL4854804
9.52	EC50	0.3	nM	CHEMBL3944424
9.46	EC50	0.35	nM	FASIGLIFAM
9.42	EC50	0.38	nM	CHEMBL4848974
9.39	EC50	0.41	nM	CHEMBL4859407
9.38	EC50	0.417	nM	CHEMBL4847662
9.22	EC50	0.6	nM	CHEMBL3265149
9.22	EC50	0.6	nM	CHEMBL4782004
9.22	EC50	0.6	nM	CHEMBL5808987
9.14	EC50	0.73	nM	CHEMBL4857550
9.14	EC50	0.729	nM	CHEMBL4872298
9.10	EC50	0.8	nM	CHEMBL3922381
9.10	EC50	0.8	nM	CHEMBL4165147
9.10	EC50	0.79	nM	CHEMBL6063201
9.10	EC50	0.8	nM	CHEMBL5948561
9.10	EC50	0.8	nM	CHEMBL5873005
9.05	EC50	0.9	nM	CHEMBL4163182
9.05	EC50	0.9	nM	CHEMBL6041065
9.03	EC50	0.94	nM	CHEMBL4591657
9.01	EC50	0.98	nM	CHEMBL4797124
9.00	EC50	1	nM	CHEMBL4097527
9.00	EC50	1	nM	CHEMBL5847542
9.00	EC50	1	nM	CHEMBL5829303
9.00	EC50	1	nM	CHEMBL5998605
8.96	EC50	1.1	nM	CHEMBL3884803
8.96	EC50	1.1	nM	CHEMBL4159416
8.96	EC50	1.1	nM	CHEMBL4534836
8.96	Ki	1.1	nM	CHEMBL4787010
8.96	EC50	1.1	nM	CHEMBL4787010
8.96	EC50	1.11	nM	CHEMBL4794409
8.92	EC50	1.2	nM	CHEMBL4160527
8.92	EC50	1.2	nM	LY2881835
8.89	EC50	1.3	nM	CHEMBL3287571
8.89	Ki	1.3	nM	CHEMBL4793371
8.89	EC50	1.3	nM	CHEMBL1829173
8.89	EC50	1.3	nM	CHEMBL2385460
8.85	EC50	1.4	nM	CHEMBL3904378
8.85	EC50	1.4	nM	CHEMBL5944756
8.82	Ki	1.5	nM	CHEMBL4798993
8.82	Ki	1.5	nM	CHEMBL4797858
8.82	EC50	1.5	nM	CHEMBL4797858
8.82	EC50	1.5	nM	CHEMBL5802483
8.80	EC50	1.6	nM	CHEMBL4165008
8.80	EC50	1.6	nM	CHEMBL4166625

PubChem BioAssay actives

2335 with measured affinity, of 5005 total; 50 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
3-[2-(4-fluoro-2-methylphenyl)-1H-indol-5-yl]propanoic acid	1750089: Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay	ec50	<0.0001	uM
(3S)-3-cyclopropyl-3-[3-[[4-(2-fluoro-5-methoxyphenyl)cyclohexyl]methoxy]phenyl]-2,2-dimethylpropanoic acid	1586862: Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay	ec50	0.0001	uM
(1R,1aR,6bS)-4-[2-chloro-4-(trifluoromethyl)phenoxy]-1a,6b-dihydro-1H-cyclopropa[b][1]benzofuran-1-carboxylic acid	371568: Agonist activity at GPR40 expressed in CHO cells by FLIPR assay	ec50	0.0001	uM
(2S,3R)-3-cyclopropyl-3-[3-[[4-(2-fluoro-5-methoxyphenyl)cyclohexyl]methoxy]phenyl]-2-methylpropanoic acid	1586862: Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay	ec50	0.0002	uM
sodium (2S,3R)-3-cyclopropyl-3-[2-[5-(5-fluoro-2-methoxy-4-pyridinyl)-2-pyridinyl]-3,4-dihydro-2H-chromen-7-yl]-2-methylpropanoate	1356361: Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay	ec50	0.0002	uM
sodium (2S,3R)-3-cyclopropyl-3-[2-[2-fluoro-4-(5-fluoro-2-methoxy-4-pyridinyl)phenyl]-3,4-dihydro-2H-chromen-7-yl]-2-methylpropanoate	1356361: Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay	ec50	0.0002	uM
sodium (2S,3R)-3-cyclopropyl-3-[2-[4-(5-fluoro-2-methoxy-4-pyridinyl)phenyl]-3,4-dihydro-2H-chromen-7-yl]-2-methylpropanoate	1356361: Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay	ec50	0.0002	uM
(2R,3S)-3-cyclopropyl-2-fluoro-3-[3-[[4-(2-fluoro-5-methoxyphenyl)cyclohexyl]methoxy]phenyl]-2-methylpropanoic acid	1586862: Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay	ec50	0.0003	uM
3-[2-(4-chloro-2-methylphenyl)-1H-indol-5-yl]propanoic acid	1750089: Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay	ec50	0.0003	uM
2-[(3S)-6-[[3-[2,6-dimethyl-4-(3-methylsulfonylpropoxy)phenyl]phenyl]methoxy]-2,3-dihydro-1-benzofuran-3-yl]acetic acid	1734879: Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay	ec50	0.0003	uM
(2S,3R)-3-[3-[[1-[1-[2,5-bis(trifluoromethyl)phenyl]ethyl]azetidin-3-yl]methoxy]phenyl]-3-cyclopropyl-2-methylpropanoic acid	1328824: Agonist activity at human GPR40 expressed in CHO cells coexpressing NFAT BLA assessed as increase in intracellular Ca2+ flux by fluo-4-AM dye based FLIPR assay	ec50	0.0003	uM
3-[2-(2,5-dimethylphenyl)-1H-indol-5-yl]propanoic acid	1750089: Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay	ec50	0.0004	uM
3-[2-(3-chloro-2-methylphenyl)-1H-indol-5-yl]propanoic acid	1750089: Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay	ec50	0.0004	uM
3-[2-(2,4-dimethylphenyl)-1H-indol-5-yl]propanoic acid	1750089: Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay	ec50	0.0004	uM
(3S)-3-[4-[[5-(spiro[indene-1,4’-piperidine]-1’-ylmethyl)thiophen-2-yl]methoxy]phenyl]hex-4-ynoic acid	1734879: Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay	ec50	0.0006	uM
(3S)-3-cyclopropyl-3-[2-[[4-(5-fluoro-2-methoxy-4-pyridinyl)-3-[(1R)-1-methoxy-2,2-dimethylpropyl]phenyl]methoxy]-4-pyridinyl]propanoic acid	1137750: Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin	ec50	0.0006	uM
3-[2-(4-bromo-2-methylphenyl)-1H-indol-5-yl]propanoic acid	1750089: Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay	ec50	0.0007	uM
3-[2-(2,6-dimethylphenyl)-1H-indol-5-yl]propanoic acid	1750089: Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay	ec50	0.0007	uM
(3S)-3-[4-[[3-[[thiophen-3-ylmethyl(2,2,2-trifluoroethyl)amino]methyl]phenyl]methoxy]phenyl]hex-4-ynoic acid	1326120: Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay	ec50	0.0008	uM
sodium (2S,3R)-3-cyclopropyl-3-[(2S)-2-[2-fluoro-4-(2-methoxy-4-pyridinyl)phenyl]-3,4-dihydro-2H-chromen-7-yl]-2-methylpropanoate	1356361: Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay	ec50	0.0008	uM
(3S)-3-cyclopropyl-3-[3-[[4-(2-fluoro-5-methoxyphenyl)cyclohexyl]methoxy]phenyl]propanoic acid	1586862: Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay	ec50	0.0009	uM
(3S)-3-[4-[[2-[4-(difluoromethoxy)phenyl]-[1,2,4]triazolo[1,5-a]pyridin-6-yl]methoxy]phenyl]hex-4-ynoic acid	1472502: Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay	ec50	0.0010	uM
(3S)-3-[4-[[4-methyl-5-(spiro[indene-1,4’-piperidine]-1’-ylmethyl)thiophen-2-yl]methoxy]phenyl]hex-4-ynoic acid	1734879: Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay	ec50	0.0010	uM
sodium (2S,3R)-3-cyclopropyl-3-[2-[4-(2-fluoro-5-methoxyphenyl)phenyl]-3,4-dihydro-2H-chromen-7-yl]-2-methylpropanoate	1356361: Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay	ec50	0.0011	uM
(2R,3S)-3-cyclopropyl-2-fluoro-3-[3-[[4-(2-fluoro-5-methoxyphenyl)cyclohexyl]methoxy]phenyl]propanoic acid	1586862: Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay	ec50	0.0011	uM
(3S)-3-[4-[[4-(spiro[indene-1,4’-piperidine]-1’-ylmethyl)-3-(trifluoromethyl)phenyl]methoxy]phenyl]hex-4-ynoic acid	1734870: Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method	ki	0.0011	uM
(2S,3R)-3-cyclopropyl-3-[(2S)-2-[4-(2-fluoro-5-methoxyphenyl)phenyl]-3,4-dihydro-2H-chromen-7-yl]-2-methylpropanoic acid	1337107: Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay	ec50	0.0011	uM
(3S)-3-[4-[[4-(spiro[indene-1,4’-piperidine]-1’-ylmethyl)phenyl]methoxy]phenyl]hex-4-ynoic acid	1734879: Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay	ec50	0.0012	uM
(3S)-3-[4-[[3-(4-chloro-2-methylphenyl)phenyl]methoxy]phenyl]-3-(1-methyltetrazol-5-yl)propanoic acid	1154882: Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay	ec50	0.0013	uM
(3S)-3-[4-[[3-methyl-4-(spiro[indene-1,4’-piperidine]-1’-ylmethyl)phenyl]methoxy]phenyl]hex-4-ynoic acid	1734870: Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method	ki	0.0013	uM
(1’R,3R)-5-[[3-[(1R)-2,2-dimethylcyclopentyl]-4-(2-fluoro-5-methoxyphenyl)phenyl]methoxy]spiro[1,2-dihydroindene-3,2’-cyclopropane]-1’-carboxylic acid	1936902: Agonist activity at FFAR1 (unknown origin)	ec50	0.0013	uM
(3S)-3-[4-[[3-[4-(trifluoromethyl)phenyl]phenyl]methoxy]phenyl]hex-4-ynoic acid	1734879: Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay	ec50	0.0013	uM
(3S)-3-[4-[[3-[[2-methylpropyl(thiophen-3-ylmethyl)amino]methyl]phenyl]methoxy]phenyl]hex-4-ynoic acid	1326120: Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay	ec50	0.0014	uM
(3S)-3-[4-[[3-chloro-4-(spiro[indene-1,4’-piperidine]-1’-ylmethyl)phenyl]methoxy]phenyl]hex-4-ynoic acid	1734870: Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method	ki	0.0015	uM
(3S)-3-[4-[[4-[(1-phenylspiro[2H-indole-3,4’-piperidine]-1’-yl)methyl]phenyl]methoxy]phenyl]hex-4-ynoic acid	1734870: Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method	ki	0.0015	uM
sodium (2S,3R)-3-cyclopropyl-3-[2-[4-(2-methoxy-4-pyridinyl)phenyl]-3,4-dihydro-2H-chromen-7-yl]-2-methylpropanoate	1356361: Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay	ec50	0.0016	uM
sodium (2S,3R)-3-cyclopropyl-3-[2-[3-fluoro-5-(5-fluoro-2-methoxy-4-pyridinyl)-2-pyridinyl]-3,4-dihydro-2H-chromen-7-yl]-2-methylpropanoate	1356361: Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay	ec50	0.0016	uM
(3S)-3-[4-[[5-(spiro[indene-1,4’-piperidine]-1’-ylmethyl)furan-2-yl]methoxy]phenyl]hex-4-ynoic acid	1734871: Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay	ec50	0.0016	uM
(2S,3R)-3-cyclopropyl-3-[2-[5-(2-fluoro-5-methoxyphenyl)-2-pyridinyl]-3,4-dihydro-2H-chromen-7-yl]-2-methylpropanoic acid	1337107: Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay	ec50	0.0017	uM
sodium (2S,3R)-3-cyclopropyl-3-[2-[5-(2-fluoro-5-methoxyphenyl)-2-pyridinyl]-3,4-dihydro-2H-chromen-7-yl]-2-methylpropanoate	1356361: Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay	ec50	0.0017	uM
(3S)-3-cyclopropyl-3-[2-[[3-[(1R)-2,2-dimethylcyclopentyl]-4-(5-fluoro-2-methoxy-4-pyridinyl)phenyl]methoxy]-4-pyridinyl]propanoic acid	1137750: Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin	ec50	0.0017	uM
(3S)-3-[4-[[3-[[pyridin-4-ylmethyl(thiophen-3-ylmethyl)amino]methyl]phenyl]methoxy]phenyl]hex-4-ynoic acid	1326120: Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay	ec50	0.0019	uM
(3S)-3-[4-[[3-[[cyclopropyl(thiophen-3-ylmethyl)amino]methyl]phenyl]methoxy]phenyl]hex-4-ynoic acid	1326120: Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay	ec50	0.0019	uM
sodium (2S,3R)-3-cyclopropyl-3-[2-[5-(2-methoxy-4-pyridinyl)-2-pyridinyl]-3,4-dihydro-2H-chromen-7-yl]-2-methylpropanoate	1356361: Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay	ec50	0.0019	uM
(3S)-3-[4-[[2-(4-propan-2-ylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-6-yl]methoxy]phenyl]hex-4-ynoic acid	1472502: Agonist activity at human GPR40 receptor expressed in HEK293 cells assessed as increase in intracellular calcium flux after 2.5 hrs measured over 3 mins by calcium 4 dye-based FLIPR assay	ec50	0.0020	uM
(3S)-3-cyclopropyl-3-[3-[[6-(2,2-dimethylpropyl)-5-(2-fluoro-5-methoxyphenyl)pyrazin-2-yl]methoxy]phenyl]propanoic acid	1679417: Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis	ec50	0.0020	uM
(3S)-3-cyclopropyl-3-[3-[[5-(5-fluoro-2-methoxy-4-pyridinyl)-6-(2-methylpropyl)pyrazin-2-yl]methoxy]phenyl]propanoic acid	1679417: Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis	ec50	0.0020	uM
(3S)-3-[4-[[3-[[cyclohexyl(thiophen-3-ylmethyl)amino]methyl]phenyl]methoxy]phenyl]hex-4-ynoic acid	1326120: Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay	ec50	0.0020	uM
trans-(1S,2S)-2-[5-[[(1R)-7-fluoro-4-[4-[2-(2-hydroxy-2-methylpropyl)tetrazol-5-yl]-2,6-dimethylphenyl]-2,3-dihydro-1H-inden-1-yl]amino]-2-pyridinyl]cyclopropane-1-carboxylic acid	1387535: Agonist activity at human GPR40 expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay	ec50	0.0020	uM
(2S,3R)-3-cyclopropyl-3-[2-fluoro-3-[[(1R)-5-(5-fluoro-2-methoxy-4-pyridinyl)-2,3-dihydro-1H-inden-1-yl]oxy]phenyl]-2-methylpropanoic acid	1590251: Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method	ec50	0.0020	uM

CTD chemical–gene interactions

11 total (human), top 11 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	affects methylation	2
fluorene-9-bisphenol	decreases expression	1
abrine	increases expression	1
TAK-875	affects binding, increases activity	1
3-(4-((2,6-dichloropyridin-4-yl)ethynyl)phenyl)propanoic acid	increases response to substance, affects binding, increases activity	1
Resveratrol	affects cotreatment, decreases expression	1
Cadmium	increases abundance, increases expression	1
Plant Extracts	affects cotreatment, decreases expression	1
Valproic Acid	increases methylation	1
Antirheumatic Agents	decreases expression	1
Cadmium Chloride	increases abundance, increases expression	1

ChEMBL screening assays

444 unique, capped per target: 320 functional, 124 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1069231	Functional	Agonist activity at FFA1 receptor up to 30 uM	The first synthetic agonists of FFA2: Discovery and SAR of phenylacetamides as allosteric modulators. — Bioorg Med Chem Lett
CHEMBL1780444	Binding	Inhibition of human GPR40 expressed in CHO cells by SPA based binding assay	3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists. — Bioorg Med Chem Lett

Cellosaurus cell lines

6 cell lines: 3 spontaneously immortalized cell line, 2 cancer cell line, 1 transformed cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_H429	CHO-K1/FFA1/Galpha15	Spontaneously immortalized cell line	Female
CVCL_KT02	1321N1/FFAR1	Cancer cell line	Male
CVCL_KU56	CHO-K1 FFAR1 Gq	Spontaneously immortalized cell line	Female
CVCL_KZ27	PathHunter DLD1 FFAR1 beta-arrestin	Cancer cell line	Male
CVCL_KZ48	PathHunter HEK 293 FFAR1 beta-arrestin-1	Transformed cell line	Female
CVCL_RQ12	CHO-K1 AequoScreen FFAR1	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT06231459	PHASE4	COMPLETED	Expression of Pro- and Anti-inflammatory Cytokines During Anti-PCSK9 in Familial Hypercholesterolemia
NCT00000594	PHASE3	COMPLETED	NHLBI Type II Coronary Intervention Study
NCT00092833	PHASE3	TERMINATED	Investigational Drug in Patients With Hypercholesterolemia or in Patients With Sitosterolemia (0653-026)(COMPLETED)
NCT00134485	PHASE3	COMPLETED	Study To Evaluate The Safety And Efficacy Of Torcetrapib/Atorvastatin In Subjects With Familial Hypercholerolemia
NCT00134511	PHASE3	COMPLETED	Study To Evaluate The Effect Of Torcetrapib/Atorvastatin In Patients With Genetic High Cholesterol Disorder
NCT00136981	PHASE3	COMPLETED	Carotid B-Mode Ultrasound Study to Compare Anti-Atherosclerotic Effect of Torcetrpib/Atorvastatin to Atorvastatin Alone.
NCT00384293	PHASE3	TERMINATED	Carotid IMT (Intima Media Thickening) Study (0524A-041)(TERMINATED)
NCT01524289	PHASE3	COMPLETED	Study to Assess the Tolerability and Efficacy of Anacetrapib (MK-0859) Co-Administered With Statin in Participants With Heterozygous Familial Hypercholesterolemia (MK-0859-020)
NCT00280995	PHASE2	COMPLETED	Dose-escalating Safety Study of ISIS 301012 in Homozygous Familial Hypercholesterolemia Subjects on Lipid Lowering Therapy
NCT00281008	PHASE2	COMPLETED	Study of ISIS 301012 (Mipomersen) in Heterozygous Familial Hypercholesterolemia Subjects on Lipid Lowering Therapy
NCT01375751	PHASE2	COMPLETED	Reduction of Low-Density Lipoprotein Cholesterol (LDL-C) With PCSK9 Inhibition in Heterozygous Familial Hypercholesterolemia Disorder Study
NCT00515307	PHASE1	COMPLETED	Bone Marrow Stem Cells as a Source of Allogenic Hepatocyte Transplantation in Homozygous Familial Hypercholesterolemia
NCT01583647	PHASE1	TERMINATED	A Study of Extended-release (ER) Niacin/Laropiprant in Adolescents With Heterozygous Familial Hypercholesterolemia (MK-0524A-158)
NCT00005168	Not specified	COMPLETED	Hyperapo B and Coronary Heart Disease
NCT01753232	Not specified	COMPLETED	Safety and Efficacy of the DALI LDL-adsorber and MONET Lipoprotein Filter
NCT03018678	Not specified	COMPLETED	Screening Protocol for a Gene Therapy Trial in Subjects With Homozygous Familial Hypercholesterolemia
NCT03110432	Not specified	COMPLETED	Prospective German Very High Cardiovascular Risk Patients Dyslipidemia Treatment Indication Registry
NCT03795038	Not specified	COMPLETED	Comparison of the Plasma Lipoprotein Apheresis Systems DIAMED and MONET vs. the Whole Blood Apheresis System DALI
NCT03989167	Not specified	RECRUITING	Clinical Decision Support for Familial Hypercholesterolemia
NCT04073797	Not specified	RECRUITING	PET Imaging of Inflammation and Lipid Lowering Study
NCT04118348	Not specified	COMPLETED	Evaluating the Efficacy of Pediatric Lipid Screening Alerts
NCT04313270	Not specified	UNKNOWN	Subclinical Atherosclerosis in Patients With Familial Hypercholesterolemia Treated With Evolocumab®
NCT04526457	Not specified	COMPLETED	Is Family Screening Improved by Genetic Testing of Familial Hypercholesterolemia
NCT04656028	Not specified	ACTIVE_NOT_RECRUITING	Genetic Testing and Motivational Counseling for FH
NCT04722068	Not specified	COMPLETED	Regeneron 1331 Kinetics Sub-Study HoFH
NCT04837638	Not specified	UNKNOWN	Diet Quality and Coronary Artery Calcification in Adults With Heterozygous Familial Hypercholesterolemia
NCT06555120	Not specified	RECRUITING	Screening for Familial Hypercholesterolemia in Children
NCT07543731	Not specified	NOT_YET_RECRUITING	A Real-World Study of Long-Term Adherence and Persistence to Inclisiran, Evolocumab, and Alirocumab