FFAR2

Summary

FFAR2 (free fatty acid receptor 2, HGNC:4501) is a protein-coding gene on chromosome 19q13.12, encoding Free fatty acid receptor 2 (O15552). G protein-coupled receptor that is activated by a major product of dietary fiber digestion, the short chain fatty acids (SCFAs), and that plays a role in the regulation of whole-body energy homeostasis and in intestinal immunity.

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 short chain free fatty acids and may be involved in the inflammatory response and in regulating lipid plasma levels.

Source: NCBI Gene 2867 — RefSeq curated summary.

At a glance

• GWAS associations: 6
• Clinical variants (ClinVar): 79 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001370087

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:4501
Approved symbol	FFAR2
Name	free fatty acid receptor 2
Location	19q13.12
Locus type	gene with protein product
Status	Approved
Aliases	FFA2R
Ensembl gene	ENSG00000126262
Ensembl biotype	protein_coding
OMIM	603823
Entrez	2867

Gene structure

Transcript identifiers

Ensembl transcripts: 3 — 2 protein_coding, 1 protein_coding_CDS_not_defined

ENST00000246549, ENST00000599180, ENST00000601590

RefSeq mRNA: 2 — MANE Select: NM_001370087 NM_001370087, NM_005306

CCDS: CCDS12461

Canonical transcript exons

ENST00000599180 — 2 exons

Exon	Start	End
ENSE00002989529	35449714	35451767
ENSE00003000328	35448257	35448379

Expression profiles

Bgee: expression breadth ubiquitous, 162 present calls, max score 93.79.

FANTOM5 (CAGE): breadth broad, TPM avg 3.8144 / max 642.0280, expressed in 228 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
175335	3.7725	222
175336	0.0419	9

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
blood	UBERON:0000178	93.79	gold quality
granulocyte	CL:0000094	89.11	gold quality
periodontal ligament	UBERON:0008266	85.47	gold quality
leukocyte	CL:0000738	84.51	gold quality
monocyte	CL:0000576	84.48	gold quality
mononuclear cell	CL:0000842	83.76	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	81.52	gold quality
spleen	UBERON:0002106	80.75	gold quality
vermiform appendix	UBERON:0001154	75.76	gold quality
bone marrow	UBERON:0002371	75.66	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	75.03	gold quality
sural nerve	UBERON:0015488	74.69	gold quality
bone marrow cell	CL:0002092	73.88	gold quality
gall bladder	UBERON:0002110	73.87	gold quality
omental fat pad	UBERON:0010414	71.68	gold quality
peritoneum	UBERON:0002358	71.59	gold quality
upper lobe of left lung	UBERON:0008952	71.49	gold quality
adipose tissue of abdominal region	UBERON:0007808	70.98	gold quality
caecum	UBERON:0001153	69.97	gold quality
lower esophagus mucosa	UBERON:0035834	68.80	gold quality
upper lobe of lung	UBERON:0008948	68.77	gold quality
mucosa of transverse colon	UBERON:0004991	68.68	gold quality
lymph node	UBERON:0000029	65.77	gold quality
islet of Langerhans	UBERON:0000006	65.54	gold quality
stromal cell of endometrium	CL:0002255	65.49	gold quality
Brodmann (1909) area 9	UBERON:0013540	63.48	gold quality
smooth muscle tissue	UBERON:0001135	63.25	gold quality
apex of heart	UBERON:0002098	61.64	gold quality
right lobe of liver	UBERON:0001114	61.63	gold quality
left uterine tube	UBERON:0001303	61.63	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	4.46
E-MTAB-6142	no	0.81

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

32 targeting FFAR2, 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-7110-3P	100.00	73.18	2486
HSA-MIR-4476	100.00	68.18	2030
HSA-MIR-6876-5P	100.00	67.68	2126
HSA-MIR-548AN	99.97	70.91	2817
HSA-MIR-6778-3P	99.96	67.29	2693
HSA-MIR-570-3P	99.96	72.41	4910
HSA-MIR-4778-3P	99.93	70.40	1818
HSA-MIR-6715A-3P	99.83	68.05	1473
HSA-MIR-6817-3P	99.79	68.35	2126
HSA-MIR-4643	99.49	67.63	1791
HSA-MIR-766-5P	99.47	67.91	2225
HSA-MIR-766-3P	99.47	65.24	1811
HSA-MIR-6722-3P	99.45	67.62	1919
HSA-MIR-103A-1-5P	99.39	67.78	1545
HSA-MIR-103A-2-5P	99.39	67.72	1577
HSA-MIR-504-3P	99.30	67.18	1745
HSA-MIR-146A-3P	99.13	68.99	1881
HSA-MIR-6506-5P	99.04	65.66	1386
HSA-MIR-1909-3P	99.03	66.56	1662
HSA-MIR-939-3P	98.97	65.07	2347
HSA-MIR-619-5P	98.57	64.97	1988
HSA-MIR-6827-5P	98.46	64.88	1256
HSA-MIR-138-5P	98.43	70.49	1292
HSA-MIR-541-5P	98.24	67.77	1181
HSA-MIR-4457	98.09	67.12	1274
HSA-MIR-4521	97.73	67.64	684
HSA-MIR-4314	97.50	67.30	1369
HSA-MIR-4448	97.04	66.22	752
HSA-MIR-6772-3P	97.04	65.89	784
HSA-MIR-301A-5P	96.88	68.07	931

Literature-anchored findings (GeneRIF, showing 40)

• might play pivotal role in differentiation and immune response of monocytes and granulocytes (PMID:12393494)
• FFA2R is expressed on leukocytes and activated by short-chain fatty acids. (PMID:12684041)
• the highly selective expression of GPR43 in leukocytes, particularly polymorphonuclear cells, suggests a role in the recruitment of these cell populations toward sites of bacterial infection (PMID:12711604)
• GPR41 and 43 mediate SCFA signaling in mammary epithelial cells and thereby play an important role in their stress management. (PMID:16887331)
• Results indicate that the short chain fatty acid receptor, GPR43 is expressed by enteroendocrine L cells containing peptide YY in the human large intestine. (PMID:17899402)
• analysis of conserved polar residues in transmembrane domains V, VI, and VII of free fatty acid receptor 2 and free fatty acid receptor 3 are required for the binding and function of short chain fatty acids (PMID:18801738)
• 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)
• upregulation of FFAR2 expression may contribute to malignant transformation. (PMID:19780758)
• Mutational analysis revealed several important residues located in transmembrane domains 3, 4, 5, 6, and 7 for acetate binding. (PMID:20837008)
• Reduction of GPR43 expression is associated with colon cancers. (PMID:20979106)
• Collaboration among C-reactive protein, M-ficolin, and GPR43 under acidosis curtails interleukin (IL)-8 production, thus preventing immune overactivation during bacterial infection. (PMID:21037097)
• They report the results of mutagenesis studies on the receptor, and the identification of previous unknown residues that may affect receptor activation as well as residues important for allosteric interactions on FFA2. (PMID:21216233)
• Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3. (PMID:21220428)
• 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)
• Data indicate that a single mutation in human FFA2 of C4.57G resulted in a human FFA2 receptor with ligand selectivity similar to the bovine receptor. (PMID:22919070)
• Extracellular ionic locks determine variation in constitutive activity and ligand potency between species orthologs of the free fatty acid receptors FFA2 and FFA3 (PMID:23066016)
• GPR43 modulates NF-kappaB activity via beta-arrestin 2. (PMID:23985900)
• [review] In vivo and in vitro studies suggest that short-chain fatty acid receptors (SCFAs) stimulate gut hormone secretion; therefore, the SCFA-FFA signal is likely to be important for gut physiological functions. (PMID:24458110)
• FFAR2 is a potential therapeutic target of T1 diabetes, representing a link between immune response and glucose homeostasis. (PMID:25298143)
• FFAR2 is expressed in pancreatic beta cells and mediates an inhibition of insulin secretion by coupling to Gi-type G proteins. (PMID:25581519)
• GPR43 expression is reduced in monocytes upon siRNA-knockdown of XBP1, while A549 cells overexpressing XBP1 displayed elevated GPR43 levels. (PMID:25633224)
• GPR3 agonism potentiates insulin secretion in isolated islets. (PMID:26023106)
• FFAR2 signaling occurs by divergent G protein pathways. (PMID:26075576)
• Although both agonist and antagonist ligands contain negatively charged carboxylates that interact with two key positively charged arginine residues in transmembrane domains V and VII of FFA2, there are clear differences in how these interactions occur. (PMID:26518871)
• the results of mutagenesis studies based on the crystal structure of hFFA1 bound to TAK-875 at 2.3 A resolution to identify important residues for orthosteric agonist 6e inducing FFA2 activation. (PMID:26808470)
• Compared with the control group, the densitometric quantification and mean density of GPR43 and ChAT proteins, and expression of GPR43 and CHAT genes, were significantly decreased in the patients with mixed refractory constipation. (PMID:26921846)
• FFA2 processes mediated by Gi signaling, whereas, in concert with blockade by the Gq/G11 inhibitor FR900359, the inability of AZ1729 to mimic or regulate propionate-mediated release of GLP-1 from mouse colonic preparations defined this physiological response as an end point transduced via activation of Gq/G11. (PMID:27385588)
• a single dose of soluble fibre was able to significantly reduce airway inflammation in stable asthma by downregulating GPR43 and GPR41 (PMID:28075383)
• Short-chain fatty acids lowered TNF-alpha-induced MCP-1 expression by reducing phosphorylation of p38 MAPK and JNK in a GPR41/GRP43-dependent manner in renal cortical epithelial cells. (PMID:28322790)
• FFAR2 and FFAR3 interact to form a heteromer in primary monocytes and macrophages via proximity ligation assay, and during heterologous expression in HEK293 cells via bimolecular fluorescence complementation and fluorescence resonance energy transfer. FFAR2 and FFAR3 may interact to form a receptor heteromer with signaling that is distinct from the parent homomers. (PMID:28883043)
• single extracellular amino acid in Free Fatty Acid Receptor 2 defines antagonist species selectivity and G protein selection bias (PMID:29061999)
• Data suggest that the free fatty acid receptor 2 (FFA2/GPR43 receptor) plays an integral role in survival during and after sepsis. (PMID:29338778)
• we show functional similarities but also some important differences between GPR84 and FFA2R in human phagocytes, thus providing some mechanistic insights into GPR84 regulation in blood neutrophils and cells recruited to an aseptic inflammatory site in vivo. (PMID:29477577)
• FFAR2 directly mediates both the stimulatory effects of Sodium acetate and Sodium propionate on insulin secretion and their protection against islet apoptosis. We have also shown that Short chain fatty acids coupling in islets occurs via Gq-coupled intracellular signaling. (PMID:30203438)
• This study characterises enantiomers of functionally selective ligands for FFA2 in cells stably expressing hFFA2. It highlights the novel roles of selective FFA2 enantiomers 4CMTB and 2CTAP on Ca(2+), pERK1/2 and cAMP and their roles as allosteric modulators which, may assist in efforts to design novel therapeutic agents for FFA2-driven inflammatory diseases. (PMID:30546040)
• Increased expression of FFAR2 is associated with uterine cervical neoplasia. (PMID:30836015)
• Metabolic and physiological role of FFAR1 (GPR40), FFAR4 (GPR120), FFAR3 (GPR41) and FFAR2 (GPR43) is REVIEWED. (PMID:31487233)
• Our findings suggest that Ffar2 regulates colonic ILC3 proliferation and function, and they identify an ILC3-receptor signaling pathway modulating gut homeostasis and pathogen defense. (PMID:31628054)
• findings demonstrate that the FFAR2 signaling cascade is important for the efficient endocytosis of IAV into host cells. (PMID:31694949)
• C. butyricum decreased the fecal secondary BA contents, increased the cecal SCFA quantities, and activated G-protein coupled receptors (GPRs), such as GPR43 and GPR109A. The analysis of clinical specimens revealed that the expression of GPR43 and GPR109A gradually decreased from human normal colonic tissue to adenoma to carcinoma (PMID:31734354)

Cross-species orthologs

6 orthologs

Organism	Symbol	Gene ID
danio_rerio	si:dkey-211g8.7	ENSDARG00000058535
danio_rerio	si:dkey-211g8.6	ENSDARG00000063088
danio_rerio		ENSDARG00000079661
danio_rerio	si:ch73-90p23.1	ENSDARG00000097901
mus_musculus	Ffar2	ENSMUSG00000051314
rattus_norvegicus	Ffar2	ENSRNOG00000021021

Paralogs (15): GPR31 (ENSG00000120436), GPR42 (ENSG00000126251), FFAR1 (ENSG00000126266), 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 2 — O15552 (reviewed: O15552)

Alternative names: G-protein coupled receptor 43

All UniProt accessions (2): O15552, C6KYL4

UniProt curated annotations — full annotation on UniProt →

Function. G protein-coupled receptor that is activated by a major product of dietary fiber digestion, the short chain fatty acids (SCFAs), and that plays a role in the regulation of whole-body energy homeostasis and in intestinal immunity. In omnivorous mammals, the short chain fatty acids acetate, propionate and butyrate are produced primarily by the gut microbiome that metabolizes dietary fibers. SCFAs serve as a source of energy but also act as signaling molecules. That G protein-coupled receptor is probably coupled to the pertussis toxin-sensitive, G(i/o)-alpha family of G proteins but also to the Gq family. Its activation results in the formation of inositol 1,4,5-trisphosphate, the mobilization of intracellular calcium, the phosphorylation of the MAPK3/ERK1 and MAPK1/ERK2 kinases and the inhibition of intracellular cAMP accumulation. May play a role in glucose homeostasis by regulating the secretion of GLP-1, in response to short-chain fatty acids accumulating in the intestine. May also regulate the production of LEP/Leptin, a hormone acting on the central nervous system to inhibit food intake. Finally, may also regulate whole-body energy homeostasis through adipogenesis regulating both differentiation and lipid storage of adipocytes. In parallel to its role in energy homeostasis, may also mediate the activation of the inflammatory and immune responses by SCFA in the intestine, regulating the rapid production of chemokines and cytokines. May also play a role in the resolution of the inflammatory response and control chemotaxis in neutrophils. In addition to SCFAs, may also be activated by the extracellular lectin FCN1 in a process leading to activation of monocytes and inducing the secretion of interleukin-8/IL-8 in response to the presence of microbes. Among SCFAs, the fatty acids containing less than 6 carbons, the most potent activators are probably acetate, propionate and butyrate. Exhibits a SCFA-independent constitutive G protein-coupled receptor activity.

Subunit / interactions. Interacts with FCN1 (via Fibrinogen C-terminal domain).

Subcellular location. Cell membrane.

Tissue specificity. Expressed at relatively high levels in peripheral blood leukocytes and, to lesser extent, in spleen.

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

RefSeq proteins (2): NP_001357016, NP_005297 (=MANE)

Domains & families (InterPro)

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

Pfam: PF00001

UniProt features (51 total): mutagenesis site 14, helix 11, topological domain 8, transmembrane region 7, glycosylation site 2, strand 2, turn 2, chain 1, region of interest 1, compositionally biased region 1, sequence variant 1, sequence conflict 1

Structure

Experimental structures (PDB)

11 structures.

PDB	Method	Resolution (Å)
8J24	ELECTRON MICROSCOPY	2.6
9CM3	ELECTRON MICROSCOPY	3.06
8T3S	ELECTRON MICROSCOPY	3.07
8Y6W	ELECTRON MICROSCOPY	3.19
9CLW	ELECTRON MICROSCOPY	3.19
8J22	ELECTRON MICROSCOPY	3.2
8J23	ELECTRON MICROSCOPY	3.2
9CM7	ELECTRON MICROSCOPY	3.29
9NS9	ELECTRON MICROSCOPY	3.3
9K1D	ELECTRON MICROSCOPY	3.34
8Y6Y	ELECTRON MICROSCOPY	3.36

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-O15552-F1	88.46	0.70

Antibody-complex structures (SAbDab): 4 — 8J22, 8J23, 8J24, 8T3S

Functional residue map

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

Glycosylation sites (2): 151, 167

Mutagenesis-validated functional residues (14):

Position	Phenotype
90	partial loss of propionate-induced g protein-coupled receptor activity.
90	complete loss of acetate-induced g protein-coupled receptor activity.
106	partial loss of scfa-induced g protein-coupled receptor activity.
108	complete loss of scfa-induced g protein-coupled receptor activity.
140	partial loss of scfa-induced g protein-coupled receptor activity.
148	no effect on scfa-induced g protein-coupled receptor activity.
148	partial loss of scfa-induced g protein-coupled receptor activity.
159	partial loss of scfa-independent constitutive g protein-coupled receptor activity.
165	partial loss of propionate-induced g protein-coupled receptor activity.
180	complete loss of scfa-induced g protein-coupled receptor activity.
238	partial loss of propionate-induced g protein-coupled receptor activity.
239	complete loss of acetate-induced g protein-coupled receptor activity.
242	complete loss of scfa-induced g protein-coupled receptor activity.
255	complete loss of scfa-induced g protein-coupled receptor activity.

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

ID	Pathway
R-HSA-416476	G alpha (q) signalling events
R-HSA-444209	Free fatty acid receptors

MSigDB gene sets: 220 (showing top): GOBP_CELL_CHEMOTAXIS, GOBP_INFLAMMATORY_RESPONSE, GOBP_POSITIVE_REGULATION_OF_INTERLEUKIN_8_PRODUCTION, GOBP_CELLULAR_RESPONSE_TO_LIPID, GOBP_POSITIVE_REGULATION_OF_CYTOKINE_PRODUCTION_INVOLVED_IN_IMMUNE_RESPONSE, GOBP_REGULATION_OF_HORMONE_LEVELS, GOBP_HORMONE_TRANSPORT, GOBP_POSITIVE_REGULATION_OF_CYTOKINE_PRODUCTION, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, GOBP_POSITIVE_REGULATION_OF_ACUTE_INFLAMMATORY_RESPONSE, GOBP_ORGAN_OR_TISSUE_SPECIFIC_IMMUNE_RESPONSE, GOBP_CELL_CELL_SIGNALING, GOBP_LEUKOCYTE_CHEMOTAXIS, GOBP_REGULATION_OF_ACUTE_INFLAMMATORY_RESPONSE, GOBP_POSITIVE_REGULATION_OF_RESPONSE_TO_EXTERNAL_STIMULUS

GO Biological Process (21): leukocyte chemotaxis involved in inflammatory response (GO:0002232), mucosal immune response (GO:0002385), regulation of acute inflammatory response (GO:0002673), positive regulation of cytokine production involved in immune response (GO:0002720), cell surface pattern recognition receptor signaling pathway (GO:0002752), positive regulation of acute inflammatory response to non-antigenic stimulus (GO:0002879), G protein-coupled receptor signaling pathway (GO:0007186), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), lipid storage (GO:0019915), positive regulation of insulin secretion (GO:0032024), positive regulation of chemokine production (GO:0032722), positive regulation of interleukin-8 production (GO:0032757), glucose homeostasis (GO:0042593), fat cell differentiation (GO:0045444), negative regulation of insulin secretion (GO:0046676), cellular response to fatty acid (GO:0071398), regulation of peptide hormone secretion (GO:0090276), ligand-gated ion channel signaling pathway (GO:1990806), immune system process (GO:0002376), inflammatory response (GO:0006954), signal transduction (GO:0007165)

GO Molecular Function (3): G protein-coupled receptor activity (GO:0004930), lipid binding (GO:0008289), protein binding (GO:0005515)

GO Cellular Component (3): plasma membrane (GO:0005886), cell projection (GO:0042995), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
GPCR downstream signalling	1
Class A/1 (Rhodopsin-like receptors)	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
positive regulation of cytokine production	3
signal transduction	2
G protein-coupled receptor signaling pathway	2
insulin secretion	2
regulation of insulin secretion	2
binding	2
cellular anatomical structure	2
leukocyte migration involved in inflammatory response	1
inflammatory response	1
leukocyte chemotaxis	1
organ or tissue specific immune response	1
acute inflammatory response	1
regulation of inflammatory response	1
cytokine production involved in immune response	1
positive regulation of production of molecular mediator of immune response	1
regulation of cytokine production involved in immune response	1
innate immune response activating cell surface receptor signaling pathway	1
pattern recognition receptor signaling pathway	1
acute inflammatory response to non-antigenic stimulus	1
positive regulation of acute inflammatory response	1
regulation of acute inflammatory response to non-antigenic stimulus	1
G protein-coupled receptor activity	1
phospholipase C activator activity	1
nutrient storage	1
positive regulation of protein secretion	1
positive regulation of peptide hormone secretion	1
chemokine production	1
regulation of chemokine production	1
interleukin-8 production	1
regulation of interleukin-8 production	1
carbohydrate homeostasis	1
cell differentiation	1
negative regulation of protein secretion	1
negative regulation of peptide hormone secretion	1
response to fatty acid	1
cellular response to lipid	1
cellular response to oxygen-containing compound	1
regulation of peptide secretion	1
peptide hormone secretion	1
regulation of hormone secretion	1

Protein interactions and networks

STRING

1382 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
FFAR2	FFAR4	Q5NUL3	867
FFAR2	GCG	P01275	853
FFAR2	PYY	P10082	836
FFAR2	GPR84	Q9NQS5	823
FFAR2	CD22	P20273	777
FFAR2	GAL	P22466	774
FFAR2	ALDH18A1	P54886	755
FFAR2	GPR119	Q8TDV5	718
FFAR2	HCAR2	Q8TDS4	714
FFAR2	GPBAR1	Q8TDU6	701
FFAR2	SLC52A2	Q9HAB3	701
FFAR2	SLC5A8	Q8N695	667
FFAR2	GNAQ	P50148	660
FFAR2	ARRB2	P32121	621
FFAR2	FFAR3	O14843	620

IntAct

341 interactions, top by confidence:

A	B	Type	Score
FIS1	FFAR2	psi-mi:“MI:0915”(physical association)	0.560
PLP1	FFAR2	psi-mi:“MI:0915”(physical association)	0.560
CXCL16	FFAR2	psi-mi:“MI:0915”(physical association)	0.560
SELENOK	FFAR2	psi-mi:“MI:0915”(physical association)	0.560
CCDC167	FFAR2	psi-mi:“MI:0915”(physical association)	0.560
SLC35B4	FFAR2	psi-mi:“MI:0915”(physical association)	0.560
FXYD6	FFAR2	psi-mi:“MI:0915”(physical association)	0.560
BTN2A2	FFAR2	psi-mi:“MI:0915”(physical association)	0.560
LHFPL5	FFAR2	psi-mi:“MI:0915”(physical association)	0.560
LEPROTL1	FFAR2	psi-mi:“MI:0915”(physical association)	0.560
SMCO4	FFAR2	psi-mi:“MI:0915”(physical association)	0.560
CXCL9	FFAR2	psi-mi:“MI:0915”(physical association)	0.560
ERG28	FFAR2	psi-mi:“MI:0915”(physical association)	0.560
CFHR5	FFAR2	psi-mi:“MI:0915”(physical association)	0.560
NKG7	FFAR2	psi-mi:“MI:0915”(physical association)	0.560
TTMP	FFAR2	psi-mi:“MI:0915”(physical association)	0.560
AGTRAP	FFAR2	psi-mi:“MI:0915”(physical association)	0.560
LAT	FFAR2	psi-mi:“MI:0915”(physical association)	0.560
ATP13A1	FFAR2	psi-mi:“MI:0915”(physical association)	0.560
GPR37L1	FFAR2	psi-mi:“MI:0915”(physical association)	0.560
YIF1A	FFAR2	psi-mi:“MI:0915”(physical association)	0.560
PEX16	FFAR2	psi-mi:“MI:0915”(physical association)	0.560
BNIP3	FFAR2	psi-mi:“MI:0915”(physical association)	0.560

BioGRID (120): FFAR2 (Two-hybrid), FFAR2 (Two-hybrid), FFAR2 (Two-hybrid), FFAR2 (Two-hybrid), FFAR2 (Two-hybrid), FFAR2 (Two-hybrid), FFAR2 (Two-hybrid), FFAR2 (Two-hybrid), FFAR2 (Two-hybrid), FFAR2 (Two-hybrid), FFAR2 (Two-hybrid), FFAR2 (Two-hybrid), FFAR2 (Two-hybrid), FFAR2 (Two-hybrid), FFAR2 (Two-hybrid)

ESM2 similar proteins: A7YY44, B0UXR0, B5X337, E7FEL0, O00254, O08675, O14843, O15529, O15552, O46685, P25116, P26824, P30558, P34996, P46093, P47749, P47900, P48042, P49650, P49651, P49652, P50132, P55085, P55086, P56488, P59902, Q00991, Q09QM4, Q13304, Q15743, Q1JQB3, Q2HJA4, Q3UFD7, Q4KLH9, Q58D85, Q63645, Q76EI6, Q86VZ1, Q8BFQ3, Q8BLG2

Diamond homologs: A0A6I8PUB9, A7YY44, B2GV46, F1MV99, O14842, O14843, O15529, O15552, P25116, P55085, P56488, Q00991, Q149R9, Q2HJA4, Q3T181, Q3UFD7, Q3ZC80, Q63645, Q63931, Q76EI6, Q76JU8, Q76JU9, Q76JV1, Q8K3T4, Q8VCK6, Q99678, Q9H1C0, E9QJ73, O09047, O42179, O43193, O55197, O88634, O88680, P30938, P46092, P46093, P47749, P50132, P58826

SIGNOR signaling

8 interactions.

A	Effect	B	Mechanism
FFAR2	“up-regulates activity”	GNAS	binding
FFAR2	“up-regulates activity”	GNAL	binding
FFAR2	“up-regulates activity”	GNAO1	binding
FFAR2	“up-regulates activity”	GNAQ	binding
FFAR2	“up-regulates activity”	GNA15	binding
FFAR2	“up-regulates activity”	GNA12	binding
FFAR2	“up-regulates activity”	GNA13	binding
“propionic acid”	“up-regulates activity”	FFAR2	“chemical activation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	75
Likely benign	2
Benign	2

Top pathogenic / likely-pathogenic (0)

SpliceAI

321 predictions. Top by Δscore:

Variant	Effect	Δscore
19:35449701:T:TA	acceptor_gain	1.0000
19:35449710:CCAG:C	acceptor_loss	1.0000
19:35449712:A:AG	acceptor_gain	1.0000
19:35449712:AG:A	acceptor_gain	1.0000
19:35449712:AGGAT:A	acceptor_gain	1.0000
19:35449713:G:GA	acceptor_gain	1.0000
19:35449713:GG:G	acceptor_gain	1.0000
19:35449713:GGA:G	acceptor_gain	1.0000
19:35449713:GGAT:G	acceptor_gain	1.0000
19:35449713:GGATG:G	acceptor_gain	1.0000
19:35448385:GCAGC:G	donor_gain	0.9800
19:35448353:G:GT	donor_gain	0.9700
19:35448386:C:T	donor_gain	0.9500
19:35448395:T:TA	donor_gain	0.9500
19:35448396:A:AA	donor_gain	0.9500
19:35448375:ACAAG:A	donor_loss	0.9300
19:35448376:CAAGG:C	donor_loss	0.9300
19:35448377:AAG:A	donor_loss	0.9300
19:35448378:AG:A	donor_loss	0.9300
19:35448379:GG:G	donor_loss	0.9300
19:35448380:GC:G	donor_loss	0.9300
19:35448387:AGCT:A	donor_gain	0.9200
19:35448389:C:G	donor_gain	0.9200
19:35448381:C:CC	donor_loss	0.9100
19:35448382:AAG:A	donor_loss	0.9000
19:35449198:G:GT	donor_gain	0.9000
19:35448368:G:GT	donor_gain	0.8900
19:35448394:GT:G	donor_gain	0.8900
19:35448899:TTC:T	donor_gain	0.8500
19:35448412:G:T	donor_gain	0.8100

AlphaMissense

2113 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
19:35449985:A:C	S91R	0.996
19:35449987:C:A	S91R	0.996
19:35449987:C:G	S91R	0.996
19:35450024:A:C	S104R	0.996
19:35450026:C:A	S104R	0.996
19:35450026:C:G	S104R	0.996
19:35450217:T:G	F168C	0.994
19:35450474:T:A	W254R	0.994
19:35450474:T:C	W254R	0.994
19:35449988:A:C	S92R	0.993
19:35449990:C:A	S92R	0.993
19:35449990:C:G	S92R	0.993
19:35450431:C:A	N239K	0.993
19:35450431:C:G	N239K	0.993
19:35450476:G:C	W254C	0.993
19:35450476:G:T	W254C	0.993
19:35450498:A:C	S262R	0.993
19:35450500:T:A	S262R	0.993
19:35450500:T:G	S262R	0.993
19:35450417:T:C	F235L	0.992
19:35450419:C:A	F235L	0.992
19:35450419:C:G	F235L	0.992
19:35449862:A:C	S50R	0.990
19:35449864:C:A	S50R	0.990
19:35449864:C:G	S50R	0.990
19:35450216:T:C	F168L	0.990
19:35450218:C:A	F168L	0.990
19:35450218:C:G	F168L	0.990
19:35450286:C:A	P191H	0.990
19:35450000:A:C	S96R	0.989

dbSNP variants (sampled 300 via entrez): RS1000252712 (19:35448122 A>G,T), RS1000579386 (19:35451568 CTGTT>C), RS1000789099 (19:35447825 C>G,T), RS1001351260 (19:35452090 G>A), RS1001489637 (19:35451895 G>A), RS1001657867 (19:35446988 G>A), RS1002088927 (19:35451217 AT>A), RS1002571039 (19:35448806 T>C), RS1003831170 (19:35449643 C>G), RS1003894029 (19:35450966 A>G), RS1004567939 (19:35446754 G>A,C), RS1006394028 (19:35449101 G>T), RS1006436785 (19:35449615 G>C,T), RS1006791867 (19:35449788 A>G), RS1007395005 (19:35447740 A>C)

Disease associations

OMIM: gene MIM:603823 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

6 associations (top):

Study	Trait	p-value
GCST009391_670	Metabolite levels	4.000000e-06
GCST011366_4	Iron status biomarkers (transferrin saturation)	6.000000e-11
GCST011367_13	Iron status biomarkers (iron levels)	2.000000e-11
GCST90002384_450	Hemoglobin	9.000000e-10
GCST90002394_556	Monocyte percentage of white cells	1.000000e-13
GCST90002398_86	Neutrophil count	9.000000e-10

EFO canonical traits (5, from GWAS)

EFO ID	Trait name
EFO:0009770	leucine measurement
EFO:0006333	transferrin saturation measurement
EFO:0004509	hemoglobin measurement
EFO:0007989	monocyte percentage of leukocytes
EFO:0004833	neutrophil count

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5493 (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: 264 (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
CHEMBL3353541	GLPG-0974	2	264

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 (15 total), top 15:

Ligand	Action	Affinity	Parameter
TUG-2304	Antagonist	8.35	pIC50
GLPG0974	Antagonist	8.05	pIC50
compound 1 [PMID: 23589301]	Agonist	7.1	pEC50
TUG-1375	Agonist	6.69	pKi
CATPB	Antagonist	6.5	pIC50
(S)-4-CMTB	Full agonist	6.4	pEC50
AMG7703	Positive	6.35	pEC50
CPTB	Agonist	6.15	pIC50
propanoic acid	Full agonist	4.9	pEC50
acetic acid	Full agonist	4.6	pEC50
butyric acid	Full agonist	4.6	pEC50
isobutyric acid	Full agonist	3.8	pEC50
trans-2-methylcrotonic acid	Full agonist	3.8	pEC50
pentanoic acid	Full agonist	3.0	pEC50
1-methylcyclopropanecarboxylic acid	Agonist	2.6	pEC50

Binding affinities (BindingDB)

399 measured of 591 human assays (591 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
7-(2,3-difluorobenzenesulfonyl)-4-(2,2-dimethylmorpholin-4-yl)-2-methyl-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	1 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2-fluoro-4-methoxybenzenesulfonyl)-2-methyl-4-[(2S)-2-(trifluoromethyl)morpholin-4-yl]-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	1 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(4-chloro-2-fluorobenzenesulfonyl)-2-methyl-4-[(2S)-2-(trifluoromethyl)morpholin-4-yl]-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	1 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2-fluorobenzenesulfonyl)-2-methyl-4-[(2R)-2-(trifluoromethyl)morpholin-4-yl]-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	1 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2-fluorobenzenesulfonyl)-N2-methyl-4-(2-methylmorpholin-4-yl)-5H-pyrrolo[3,2-d]pyrimidine-2,6-diamine	EC50	1 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(benzenesulfonyl)-4-[(2R,5R)-2,5-dimethylmorpholin-4-yl]-2-methyl-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	2 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2-fluorobenzenesulfonyl)-2-methyl-4-[2-(trifluoromethyl)morpholin-4-yl]-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	2 nM	US-10059713: 3-substituted 2-amino-indole derivatives
4-(2-methylmorpholin-4-yl)-7-(phenylsulfanyl)-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	2 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(benzenesulfonyl)-4-(2-methylmorpholin-4-yl)-2-(methylsulfanyl)-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	2 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(benzenesulfonyl)-2-methyl-4-(propan-2-yloxy)-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	2 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2,4-difluorobenzenesulfonyl)-2-methyl-4-[(2S)-2-(trifluoromethyl)morpholin-4-yl]-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	2 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2,3-difluorobenzenesulfonyl)-2-methyl-4-[(2S)-2-(trifluoromethyl)morpholin-4-yl]-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	2 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2-fluorobenzenesulfonyl)-2-methyl-4-[(2R)-2-(trifluoromethyl)morpholin-4-yl]-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	2 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2,5-difluorobenzenesulfonyl)-2-methyl-4-[(2S)-2-(trifluoromethyl)morpholin-4-yl]-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	2 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(4-chloro-2-fluorobenzenesulfonyl)-2-methyl-4-[(2R)-2-(trifluoromethyl)morpholin-4-yl]-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	2 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2-fluorobenzenesulfonyl)-2-(methylsulfanyl)-4-[2-(trifluoromethyl)morpholin-4-yl]-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	2 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(benzenesulfonyl)-4-(piperidin-1-yl)-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	3 nM	US-10059713: 3-substituted 2-amino-indole derivatives
4-cyclopentyl-7-(3-fluorobenzenesulfonyl)-2-methyl-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	3 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2-fluoro-4-methoxybenzenesulfonyl)-2-methyl-4-[(2S)-2-methylmorpholin-4-yl]-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	3 nM	US-10059713: 3-substituted 2-amino-indole derivatives
4-[(2R,5R)-2,5-dimethylmorpholin-4-yl]-7-(2-fluorobenzenesulfonyl)-2-methyl-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	3 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(3-fluorobenzenesulfonyl)-4-(2-methylmorpholin-4-yl)-2-(trifluoromethyl)-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	3 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2-fluorobenzenesulfonyl)-2-methyl-4-[(2S)-2-(trifluoromethyl)morpholin-4-yl]-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	3 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2,6-difluorobenzenesulfonyl)-4-(2,2-dimethylmorpholin-4-yl)-2-methyl-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	3 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2-fluorobenzenesulfonyl)-2-methyl-4-[(2R)-2-(trifluoromethyl)morpholin-4-yl]-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	3 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2-fluoro-4-methoxybenzenesulfonyl)-2-methyl-4-[(2R)-2-(trifluoromethyl)morpholin-4-yl]-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	3 nM	US-10059713: 3-substituted 2-amino-indole derivatives
4-[(2,2-dimethyloxan-3-yl)oxy]-7-(2-fluorobenzenesulfonyl)-2-methyl-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	3 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2-fluorobenzenesulfonyl)-2-methyl-4-[2-methyl-2-(trifluoromethyl)morpholin-4-yl]-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	3 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(benzenesulfonyl)-4-(2-ethylthiomorpholin-4-yl)-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	4 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2-fluoro-5-methoxybenzenesulfonyl)-2-methyl-4-(2-methylmorpholin-4-yl)-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	4 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(4-chloro-2-fluorobenzenesulfonyl)-4-(2,2-dimethylmorpholin-4-yl)-2-methyl-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	4 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2,6-Difluorobenzenesulfonyl)-2-methyl-4-[(2S)-2-(trifluoromethyl)morpholin-4-yl]-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	4 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(benzenesulfonyl)-4-N-ethyl-4-N-(oxan-4-ylmethyl)-5H-pyrrolo[3,2-d]pyrimidine-4,6-diamine	EC50	5 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2,6-difluorobenzenesulfonyl)-2-methyl-4-(2-methylmorpholin-4-yl)-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	5 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2-fluorobenzenesulfonyl)-2-methyl-4-[(1,1,1-trifluoropropan-2-yl)oxy]-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	5 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2-fluorobenzenesulfonyl)-4-[(2R)-2-(fluoromethyl)morpholin-4-yl]-2-methyl-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	5 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(benzenesulfonyl)-4-[(2R,6S)-2,6-dimethylmorpholin-4-yl]-2-methyl-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	6 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2-fluorobenzenesulfonyl)-2-methyl-4-{6-oxa-9-azaspiro[4.5]decan-9-yl}-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	6 nM	US-10059713: 3-substituted 2-amino-indole derivatives
4-(4,4-difluoropiperidin-1-yl)-7-(3-fluorobenzenesulfonyl)-2-methyl-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	6 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(benzenesulfonyl)-4-[2-(propan-2-yl)morpholin-4-yl]-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	6 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2-fluorobenzenesulfonyl)-2-methyl-4-[(2S)-2-methylmorpholin-4-yl]-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	6 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2,4-difluorobenzenesulfonyl)-2-methyl-4-(2-methylmorpholin-4-yl)-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	6 nM	US-10059713: 3-substituted 2-amino-indole derivatives
3-(benzenesulfonyl)-7-(2,2-dimethylmorpholin-4-yl)-H-pyrrolo[3,2-b]pyridin-2-amine	EC50	6 nM	US-10059713: 3-substituted 2-amino-indole derivatives
benzyl 4-[[6-amino-4-(2-methylmorpholin-4-yl)-5H-pyrrolo[3,2-d]pyrimidin-7-yl]sulfonyl]piperidine-1-carboxylate	EC50	7 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2-fluorobenzenesulfonyl)-2-methyl-4-(prop-1-en-2-yl)-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	7 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(benzenesulfonyl)-4-(1-cyclopropylethoxy)-2-methyl-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	7 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(benzenesulfonyl)-4-[(2,2-difluorocyclopropyl)methoxy]-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	8 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(benzenesulfonyl)-4-(2-methylthiomorpholin-4-yl)-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	8 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2-fluorobenzenesulfonyl)-2-methyl-4-{5-oxa-8-azaspiro[3.5]nonan-8-yl}-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	8 nM	US-10059713: 3-substituted 2-amino-indole derivatives
7-(2-fluorobenzenesulfonyl)-2-methyl-4-(propan-2-yloxy)-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	8 nM	US-10059713: 3-substituted 2-amino-indole derivatives
4-[(RS,SR)-2,3-dimethylmorpholin-4-yl]-7-(2-fluorobenzenesulfonyl)-2-methyl-5H-pyrrolo[3,2-d]pyrimidin-6-amine	EC50	8 nM	US-10059713: 3-substituted 2-amino-indole derivatives

ChEMBL bioactivities

946 potent at pChembl≥5 of 978 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.00	EC50	1	nM	CHEMBL5838437
9.00	EC50	1	nM	CHEMBL5838011
9.00	EC50	1	nM	CHEMBL5885845
9.00	EC50	1	nM	CHEMBL5896488
9.00	EC50	1	nM	CHEMBL5748267
8.70	EC50	2	nM	CHEMBL6013757
8.70	EC50	2	nM	CHEMBL5777334
8.70	EC50	2	nM	CHEMBL5964737
8.70	EC50	2	nM	CHEMBL5828279
8.70	EC50	2	nM	CHEMBL5808688
8.70	EC50	2	nM	CHEMBL5856367
8.70	EC50	2	nM	CHEMBL6003960
8.70	EC50	2	nM	CHEMBL6038222
8.70	EC50	2	nM	CHEMBL5876605
8.70	EC50	2	nM	CHEMBL6018732
8.70	EC50	2	nM	CHEMBL5756440
8.53	IC50	2.951	nM	CHEMBL5415936
8.52	EC50	3	nM	CHEMBL6032982
8.52	EC50	3	nM	CHEMBL6026700
8.52	EC50	3	nM	CHEMBL5919385
8.52	EC50	3	nM	CHEMBL6039935
8.52	EC50	3	nM	CHEMBL5752871
8.52	EC50	3	nM	CHEMBL6039687
8.52	EC50	3	nM	CHEMBL5911933
8.52	EC50	3	nM	CHEMBL5801035
8.52	EC50	3	nM	CHEMBL5780572
8.52	EC50	3	nM	CHEMBL5867859
8.52	EC50	3	nM	CHEMBL5977980
8.46	IC50	3.467	nM	CHEMBL5408510
8.40	IC50	4	nM	CHEMBL5408510
8.40	EC50	4	nM	CHEMBL6031452
8.40	EC50	4	nM	CHEMBL5945896
8.40	EC50	4	nM	CHEMBL5906668
8.40	EC50	4	nM	CHEMBL5975535
8.38	IC50	4.169	nM	CHEMBL5431210
8.36	IC50	4.365	nM	CHEMBL5433180
8.35	IC50	4.467	nM	CHEMBL5408510
8.30	IC50	5.012	nM	CHEMBL5408560
8.30	IC50	5.012	nM	CHEMBL5401041
8.30	EC50	5	nM	CHEMBL5742066
8.30	EC50	5	nM	CHEMBL5782093
8.30	EC50	5	nM	CHEMBL5959343
8.30	EC50	5	nM	CHEMBL5770698
8.26	IC50	5.495	nM	CHEMBL5426494
8.26	IC50	5.495	nM	CHEMBL5431210
8.22	EC50	6	nM	CHEMBL5778231
8.22	EC50	6	nM	CHEMBL5853823
8.22	EC50	6	nM	CHEMBL5771728
8.22	EC50	6	nM	CHEMBL5887491
8.22	EC50	6	nM	CHEMBL5767556

PubChem BioAssay actives

250 with measured affinity, of 634 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
2-(3-chlorophenyl)-N-[(2S)-1-(2H-tetrazol-5-yl)-3-[4-(trifluoromethyl)phenyl]propan-2-yl]acetamide	2031396: Antagonist activity at human FFA2 expressed in Flp-In-T-REx-293 cells co-expressing eYFP assessed as inhibition of propionate-induced cAMP accumulation preincubated with compound for 20 mins followed by propionate addition and measured after 25 mins in the presence of forskolin by TR-FRET analysis	ic50	0.0030	uM
2-(3-methoxyphenyl)-N-[(2S)-1-(2H-tetrazol-5-yl)-3-[4-(trifluoromethyl)phenyl]propan-2-yl]acetamide	2031396: Antagonist activity at human FFA2 expressed in Flp-In-T-REx-293 cells co-expressing eYFP assessed as inhibition of propionate-induced cAMP accumulation preincubated with compound for 20 mins followed by propionate addition and measured after 25 mins in the presence of forskolin by TR-FRET analysis	ic50	0.0035	uM
2-(3-iodophenyl)-N-[(2S)-1-(2H-tetrazol-5-yl)-3-[4-(trifluoromethyl)phenyl]propan-2-yl]acetamide	2031396: Antagonist activity at human FFA2 expressed in Flp-In-T-REx-293 cells co-expressing eYFP assessed as inhibition of propionate-induced cAMP accumulation preincubated with compound for 20 mins followed by propionate addition and measured after 25 mins in the presence of forskolin by TR-FRET analysis	ic50	0.0042	uM
2-phenyl-N-[(2S)-1-(2H-tetrazol-5-yl)-3-[4-(trifluoromethyl)phenyl]propan-2-yl]acetamide	2031396: Antagonist activity at human FFA2 expressed in Flp-In-T-REx-293 cells co-expressing eYFP assessed as inhibition of propionate-induced cAMP accumulation preincubated with compound for 20 mins followed by propionate addition and measured after 25 mins in the presence of forskolin by TR-FRET analysis	ic50	0.0044	uM
2-(3-bromophenyl)-N-[(2S)-1-(2H-tetrazol-5-yl)-3-[4-(trifluoromethyl)phenyl]propan-2-yl]acetamide	2031396: Antagonist activity at human FFA2 expressed in Flp-In-T-REx-293 cells co-expressing eYFP assessed as inhibition of propionate-induced cAMP accumulation preincubated with compound for 20 mins followed by propionate addition and measured after 25 mins in the presence of forskolin by TR-FRET analysis	ic50	0.0050	uM
2-(3-methylphenyl)-N-[(2S)-1-(2H-tetrazol-5-yl)-3-[4-(trifluoromethyl)phenyl]propan-2-yl]acetamide	2031395: Antagonist activity at human FFA2 expressed in Flp-In-T-REx-293 cells co-expressing eYFP assessed as inhibition of [35S]GTPgammaS incorporation preincubated for 15 mins followed by [35S]GTPgammaS addition and measured after 60 min by liquid scintillation spectroscopic analysis	ic50	0.0050	uM
2-(3-fluorophenyl)-N-[(2S)-1-(2H-tetrazol-5-yl)-3-[4-(trifluoromethyl)phenyl]propan-2-yl]acetamide	2031395: Antagonist activity at human FFA2 expressed in Flp-In-T-REx-293 cells co-expressing eYFP assessed as inhibition of [35S]GTPgammaS incorporation preincubated for 15 mins followed by [35S]GTPgammaS addition and measured after 60 min by liquid scintillation spectroscopic analysis	ic50	0.0055	uM
2-(5-bromo-3-pyridinyl)-N-[(2S)-1-(2H-tetrazol-5-yl)-3-[4-(trifluoromethyl)phenyl]propan-2-yl]acetamide	2031396: Antagonist activity at human FFA2 expressed in Flp-In-T-REx-293 cells co-expressing eYFP assessed as inhibition of propionate-induced cAMP accumulation preincubated with compound for 20 mins followed by propionate addition and measured after 25 mins in the presence of forskolin by TR-FRET analysis	ic50	0.0062	uM
2-(4-chlorophenyl)-N-[(2S)-1-(2H-tetrazol-5-yl)-3-[4-(trifluoromethyl)phenyl]propan-2-yl]acetamide	2031395: Antagonist activity at human FFA2 expressed in Flp-In-T-REx-293 cells co-expressing eYFP assessed as inhibition of [35S]GTPgammaS incorporation preincubated for 15 mins followed by [35S]GTPgammaS addition and measured after 60 min by liquid scintillation spectroscopic analysis	ic50	0.0083	uM
N-[(2S)-1-(2H-tetrazol-5-yl)-3-[4-(trifluoromethyl)phenyl]propan-2-yl]bicyclo[4.2.0]octa-1,3,5-triene-7-carboxamide	2031396: Antagonist activity at human FFA2 expressed in Flp-In-T-REx-293 cells co-expressing eYFP assessed as inhibition of propionate-induced cAMP accumulation preincubated with compound for 20 mins followed by propionate addition and measured after 25 mins in the presence of forskolin by TR-FRET analysis	ic50	0.0087	uM
2-(3-ethoxyphenyl)-N-[(2S)-1-(2H-tetrazol-5-yl)-3-[4-(trifluoromethyl)phenyl]propan-2-yl]acetamide	2031396: Antagonist activity at human FFA2 expressed in Flp-In-T-REx-293 cells co-expressing eYFP assessed as inhibition of propionate-induced cAMP accumulation preincubated with compound for 20 mins followed by propionate addition and measured after 25 mins in the presence of forskolin by TR-FRET analysis	ic50	0.0089	uM
N-[(2S)-1-(2H-tetrazol-5-yl)-3-[4-(trifluoromethyl)phenyl]propan-2-yl]-2-[3-(trifluoromethyl)phenyl]acetamide	2031396: Antagonist activity at human FFA2 expressed in Flp-In-T-REx-293 cells co-expressing eYFP assessed as inhibition of propionate-induced cAMP accumulation preincubated with compound for 20 mins followed by propionate addition and measured after 25 mins in the presence of forskolin by TR-FRET analysis	ic50	0.0089	uM
4-[[(2R)-1-(1-benzothiophene-3-carbonyl)-2-methylazetidine-2-carbonyl]-[(3-chlorophenyl)methyl]amino]butanoic acid	1170751: Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization	ic50	0.0090	uM
(3R)-4-[[4-[5-chloro-2-(6-methoxy-3-pyridinyl)phenyl]-1,3-thiazol-2-yl]-cyclopropylamino]-3-(furan-2-ylmethyl)-4-oxobutanoic acid	1363149: Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method	ec50	0.0126	uM
(3R)-3-benzyl-4-[cyclopropyl-[4-(2,5-dichlorophenyl)-1,3-thiazol-2-yl]amino]-4-oxobutanoic acid	1363149: Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method	ec50	0.0126	uM
2-(3-chlorophenyl)-N-[(2R)-4-(2H-tetrazol-5-yl)-1-[4-(trifluoromethyl)phenyl]butan-2-yl]acetamide	2031396: Antagonist activity at human FFA2 expressed in Flp-In-T-REx-293 cells co-expressing eYFP assessed as inhibition of propionate-induced cAMP accumulation preincubated with compound for 20 mins followed by propionate addition and measured after 25 mins in the presence of forskolin by TR-FRET analysis	ic50	0.0191	uM
4-[[1-(1-benzothiophene-3-carbonyl)-2-methylazetidine-2-carbonyl]-[(3-chlorophenyl)methyl]amino]butanoic acid	1170751: Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization	ic50	0.0250	uM
(3R)-3-[cyclopropyl-[4-[2-(6-methoxy-3-pyridinyl)phenyl]-1,3-thiazol-2-yl]carbamoyl]-5-methylhexanoic acid	1363149: Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method	ec50	0.0251	uM
(3R)-3-[cyclopropyl-[4-[2-(6-pyrazol-1-yl-3-pyridinyl)phenyl]-1,3-thiazol-2-yl]carbamoyl]-5-methylhexanoic acid	1363149: Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method	ec50	0.0251	uM
(3R)-3-(cyclopentylmethyl)-4-[cyclopropyl-[4-[2-(6-pyrazol-1-yl-3-pyridinyl)phenyl]-1,3-thiazol-2-yl]amino]-4-oxobutanoic acid	1363149: Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method	ec50	0.0251	uM
(3R)-3-(cyclopentylmethyl)-4-[cyclopropyl-[4-[2-(6-methoxy-3-pyridinyl)phenyl]-1,3-thiazol-2-yl]amino]-4-oxobutanoic acid	1363149: Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method	ec50	0.0251	uM
N-[(2S)-1-(2H-tetrazol-5-yl)-3-[4-(trifluoromethyl)phenyl]propan-2-yl]-2-[3-(trifluoromethoxy)phenyl]acetamide	2031396: Antagonist activity at human FFA2 expressed in Flp-In-T-REx-293 cells co-expressing eYFP assessed as inhibition of propionate-induced cAMP accumulation preincubated with compound for 20 mins followed by propionate addition and measured after 25 mins in the presence of forskolin by TR-FRET analysis	ic50	0.0316	uM
(3R)-4-[[4-(2-chlorophenyl)-1,3-thiazol-2-yl]-methylamino]-3-(cyclopentylmethyl)-4-oxobutanoic acid	1363149: Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method	ec50	0.0316	uM
(3R)-3-benzyl-4-[[4-(2-chlorophenyl)-1,3-thiazol-2-yl]-cyclopropylamino]-4-oxobutanoic acid	1363149: Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method	ec50	0.0316	uM
2-(3-fluorophenyl)-N-[(2S)-1-phenyl-3-(2H-tetrazol-5-yl)propan-2-yl]acetamide	2031396: Antagonist activity at human FFA2 expressed in Flp-In-T-REx-293 cells co-expressing eYFP assessed as inhibition of propionate-induced cAMP accumulation preincubated with compound for 20 mins followed by propionate addition and measured after 25 mins in the presence of forskolin by TR-FRET analysis	ic50	0.0339	uM
2-[[1-[2-(1-benzothiophen-3-yl)acetyl]-2-methylazetidine-2-carbonyl]-[(4-chlorophenyl)methyl]amino]acetic acid	1170751: Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization	ic50	0.0360	uM
4-[1-benzofuran-6-ylmethyl-[1-[2-(1-benzothiophen-3-yl)acetyl]-2-methylazetidine-2-carbonyl]amino]butanoic acid	1170751: Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization	ic50	0.0360	uM
4-[[1-[2-(1-benzothiophen-3-yl)acetyl]-2-methylazetidine-2-carbonyl]-(1H-indazol-6-ylmethyl)amino]butanoic acid	1170751: Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization	ic50	0.0400	uM
4-[[1-[2-(1-benzothiophen-3-yl)acetyl]-2-methylazetidine-2-carbonyl]-[(4-chlorophenyl)methyl]amino]butanoic acid	1170751: Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization	ic50	0.0420	uM
1-[2-(1-benzothiophen-3-yl)acetyl]-N-[(4-chlorophenyl)methyl]-2-methyl-N-[3-(methylsulfamoyl)propyl]azetidine-2-carboxamide	1170751: Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization	ic50	0.0440	uM
4-[[1-[2-(1-benzothiophen-3-yl)acetyl]-2-methylazetidine-2-carbonyl]-(1H-indol-6-ylmethyl)amino]butanoic acid	1170751: Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization	ic50	0.0480	uM
2-pyridin-3-yl-N-[(2S)-1-(2H-tetrazol-5-yl)-3-[4-(trifluoromethyl)phenyl]propan-2-yl]acetamide	2031396: Antagonist activity at human FFA2 expressed in Flp-In-T-REx-293 cells co-expressing eYFP assessed as inhibition of propionate-induced cAMP accumulation preincubated with compound for 20 mins followed by propionate addition and measured after 25 mins in the presence of forskolin by TR-FRET analysis	ic50	0.0513	uM
4-[[1-[2-(1-benzothiophen-3-yl)acetyl]-2-methylazetidine-2-carbonyl]-[[4-(trifluoromethyl)phenyl]methyl]amino]butanoic acid	1170751: Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization	ic50	0.0570	uM
4-(N-[1-(1-benzothiophene-3-carbonyl)-2-methylazetidine-2-carbonyl]-4-chloroanilino)butanoic acid	1170751: Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization	ic50	0.0630	uM
4-[[1-(1-benzothiophene-3-carbonyl)-2-methylazetidine-2-carbonyl]-(1H-indol-6-ylmethyl)amino]butanoic acid	1170751: Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization	ic50	0.0630	uM
2-(6-chloro-3-pyridinyl)-N-[(2S)-1-(2H-tetrazol-5-yl)-3-[4-(trifluoromethyl)phenyl]propan-2-yl]acetamide	2031396: Antagonist activity at human FFA2 expressed in Flp-In-T-REx-293 cells co-expressing eYFP assessed as inhibition of propionate-induced cAMP accumulation preincubated with compound for 20 mins followed by propionate addition and measured after 25 mins in the presence of forskolin by TR-FRET analysis	ic50	0.0631	uM
3-phenyl-N-[(2S)-1-(2H-tetrazol-5-yl)-3-[4-(trifluoromethyl)phenyl]propan-2-yl]propanamide	2031396: Antagonist activity at human FFA2 expressed in Flp-In-T-REx-293 cells co-expressing eYFP assessed as inhibition of propionate-induced cAMP accumulation preincubated with compound for 20 mins followed by propionate addition and measured after 25 mins in the presence of forskolin by TR-FRET analysis	ic50	0.0646	uM
1-[2-(1-benzothiophen-3-yl)acetyl]-N-[(4-chlorophenyl)methyl]-2-methyl-N-(4-morpholin-4-yl-4-oxobutyl)azetidine-2-carboxamide	1170751: Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization	ic50	0.0760	uM
1-[2-(1-benzothiophen-3-yl)acetyl]-N-[(4-chlorophenyl)methyl]-2-methyl-N-(3-sulfamoylpropyl)azetidine-2-carboxamide	1170751: Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization	ic50	0.0760	uM
(2R,4R)-2-(2-chlorophenyl)-3-[4-(3,5-dimethyl-1,2-oxazol-4-yl)benzoyl]-1,3-thiazolidine-4-carboxylic acid	1363031: Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay	ec50	0.0776	uM
4-[[1-[2-(3,5-dimethylphenyl)acetyl]-2-methylazetidine-2-carbonyl]-(1H-indol-6-ylmethyl)amino]butanoic acid	1170751: Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization	ic50	0.0850	uM
4-[[1-[2-(1-benzofuran-3-yl)acetyl]-2-methylazetidine-2-carbonyl]-(1H-indol-6-ylmethyl)amino]butanoic acid	1170751: Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization	ic50	0.0900	uM
4-[1,3-benzothiazol-5-ylmethyl-[1-[2-(1-benzothiophen-3-yl)acetyl]-2-methylazetidine-2-carbonyl]amino]butanoic acid	1170751: Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization	ic50	0.0950	uM
(3R)-3-benzyl-4-[[4-(2-chlorophenyl)-1,3-thiazol-2-yl]-methylamino]-4-oxobutanoic acid	1363149: Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method	ec50	0.1000	uM
(2S)-2-(4-chlorophenyl)-3-methyl-N-(1,3-thiazol-2-yl)butanamide	1363149: Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method	ec50	0.1000	uM
(3S)-3-[[2-(3-chlorophenyl)acetyl]amino]-4-[4-(trifluoromethyl)phenyl]butanoic acid	2031395: Antagonist activity at human FFA2 expressed in Flp-In-T-REx-293 cells co-expressing eYFP assessed as inhibition of [35S]GTPgammaS incorporation preincubated for 15 mins followed by [35S]GTPgammaS addition and measured after 60 min by liquid scintillation spectroscopic analysis	ic50	0.1096	uM
4-[1-benzofuran-6-ylmethyl-[1-(1-benzothiophene-3-carbonyl)-2-methylazetidine-2-carbonyl]amino]butanoic acid	1170751: Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization	ic50	0.1150	uM
4-[[1-[2-(1-benzofuran-3-yl)acetyl]-2-methylazetidine-2-carbonyl]-(1-benzofuran-6-ylmethyl)amino]butanoic acid	1170751: Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization	ic50	0.1160	uM
4-[[1-(1-benzothiophene-3-carbonyl)-2-methylazetidine-2-carbonyl]-[(4-chlorophenyl)methyl]amino]butanoic acid	1170751: Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization	ic50	0.1180	uM
N-(2-amino-2-oxoethyl)-N-[(4-chlorophenyl)methyl]-1-[2-(3,5-dimethylphenyl)acetyl]-2-methylazetidine-2-carboxamide	1170751: Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization	ic50	0.1230	uM

CTD chemical–gene interactions

18 total (human), top 18 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Asian ginseng	affects cotreatment, decreases expression	1
triphenyl phosphate	affects expression	1
propionaldehyde	decreases expression	1
sulforaphane	increases expression	1
di-n-butylphosphoric acid	affects expression	1
CGP 52608	increases reaction, affects binding	1
2,2’,4,4’-tetrabromodiphenyl ether	increases expression	1
gardiquimod	increases expression, decreases reaction	1
Benzo(a)pyrene	affects methylation	1
Diethylhexyl Phthalate	affects cotreatment, decreases expression	1
Ethyl Methanesulfonate	decreases expression	1
Formaldehyde	decreases expression	1
Methyl Methanesulfonate	decreases expression	1
Selenium	increases expression	1
Tretinoin	increases expression	1
Valproic Acid	increases methylation	1
Vincristine	decreases expression	1
Protein Kinase Inhibitors	decreases reaction, increases expression	1

ChEMBL screening assays

68 unique, capped per target: 43 functional, 25 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1069216	Functional	Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production	The first synthetic agonists of FFA2: Discovery and SAR of phenylacetamides as allosteric modulators. — Bioorg Med Chem Lett
CHEMBL2320491	Binding	Agonist activity at human FFA2 in expressed in HEK293 cells assessed as cellular mass movement by dynamic mass redistribution assay	Discovery of a potent and selective free fatty acid receptor 1 agonist with low lipophilicity and high oral bioavailability. — J Med Chem

Cellosaurus cell lines

5 cell lines: 4 spontaneously immortalized cell line, 1 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_D7PU	Ubigene A-549 FFAR2 KO	Cancer cell line	Male
CVCL_H430	CHO-K1/FFA2/Galpha15	Spontaneously immortalized cell line	Female
CVCL_KU57	CHO-K1 FFAR2 Gq	Spontaneously immortalized cell line	Female
CVCL_KX04	PathHunter CHO-K1 FFAR2 beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_U005	CHO-FFAR2	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

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