GNA15

Summary

GNA15 (G protein subunit alpha 15, HGNC:4383) is a protein-coding gene on chromosome 19p13.3, encoding Guanine nucleotide-binding protein subunit alpha-15 (P30679). Member of the G-protein alpha subunit family that plays a crucial role in intracellular signaling.

Enables G protein-coupled receptor binding activity. Acts upstream of or within with a positive effect on calcium-mediated signaling. Predicted to be located in plasma membrane. Predicted to be part of heterotrimeric G-protein complex.

Source: NCBI Gene 2769 — RefSeq curated summary.

At a glance

• GWAS associations: 11
• Clinical variants (ClinVar): 64 total
• Druggable target: yes — 2 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_002068

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:4383
Approved symbol	GNA15
Name	G protein subunit alpha 15
Location	19p13.3
Locus type	gene with protein product
Status	Approved
Aliases	GNA16
Ensembl gene	ENSG00000060558
Ensembl biotype	protein_coding
OMIM	139314
Entrez	2769

Gene structure

Transcript identifiers

Ensembl transcripts: 3 — 1 protein_coding, 1 retained_intron, 1 nonsense_mediated_decay

ENST00000262958, ENST00000586082, ENST00000592455

RefSeq mRNA: 1 — MANE Select: NM_002068 NM_002068

CCDS: CCDS12104

Canonical transcript exons

ENST00000262958 — 7 exons

Exon	Start	End
ENSE00000382975	3157728	3157881
ENSE00000663864	3155823	3155952
ENSE00000859540	3136033	3136595
ENSE00000859541	3162793	3163749
ENSE00003518039	3151707	3151835
ENSE00003576971	3148591	3148775
ENSE00003628220	3150131	3150285

Expression profiles

Bgee: expression breadth ubiquitous, 218 present calls, max score 98.14.

FANTOM5 (CAGE): breadth broad, TPM avg 14.8247 / max 834.2004, expressed in 633 samples.

FANTOM5 promoters (9 alternative TSS)

Promoter ID	TPM avg	Samples expressed
173145	6.0390	426
173144	4.5048	395
173142	3.2293	501
173147	0.5609	38
173146	0.1955	31
173143	0.1050	60
208644	0.0804	45
173149	0.0582	28
173148	0.0516	29

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
lower esophagus mucosa	UBERON:0035834	98.14	gold quality
esophagus squamous epithelium	UBERON:0006920	95.29	gold quality
esophagus mucosa	UBERON:0002469	95.24	gold quality
palpebral conjunctiva	UBERON:0001812	94.80	gold quality
squamous epithelium	UBERON:0006914	94.68	gold quality
epithelium of esophagus	UBERON:0001976	94.62	gold quality
cervix squamous epithelium	UBERON:0006922	94.35	gold quality
tongue squamous epithelium	UBERON:0006919	93.48	gold quality
gingival epithelium	UBERON:0001949	92.79	gold quality
gingiva	UBERON:0001828	92.23	gold quality
monocyte	CL:0000576	91.06	gold quality
oral cavity	UBERON:0000167	90.79	gold quality
mononuclear cell	CL:0000842	90.70	gold quality
skin of abdomen	UBERON:0001416	90.50	gold quality
buccal mucosa cell	CL:0002336	90.46	gold quality
leukocyte	CL:0000738	90.35	gold quality
amniotic fluid	UBERON:0000173	90.32	gold quality
skin of leg	UBERON:0001511	89.68	gold quality
cervix epithelium	UBERON:0004801	88.61	gold quality
zone of skin	UBERON:0000014	88.37	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	88.30	gold quality
periodontal ligament	UBERON:0008266	87.59	gold quality
granulocyte	CL:0000094	87.06	gold quality
pharyngeal mucosa	UBERON:0000355	86.34	gold quality
nasal cavity epithelium	UBERON:0005384	85.32	gold quality
blood	UBERON:0000178	85.28	gold quality
eye	UBERON:0000970	84.90	gold quality
pancreatic ductal cell	CL:0002079	84.37	silver quality
vagina	UBERON:0000996	84.03	gold quality
nasal cavity mucosa	UBERON:0001826	82.21	gold quality

Single-cell (SCXA)

Detected in 8 experiment(s), a significant marker in 6.

Experiment	Marker?	Max mean expression
E-HCAD-4	yes	40.83
E-MTAB-8142	yes	18.00
E-ANND-3	yes	15.60
E-CURD-122	yes	13.78
E-MTAB-6701	yes	12.33
E-CURD-112	yes	8.87
E-GEOD-86618	no	31.19
E-GEOD-36552	no	9.89

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

23 targeting GNA15, 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-4283	100.00	66.42	2097
HSA-MIR-4779	99.86	66.50	1583
HSA-MIR-204-5P	99.79	71.62	2439
HSA-MIR-211-5P	99.79	71.65	2440
HSA-MIR-4766-5P	99.75	69.23	2662
HSA-MIR-4306	99.72	70.50	3630
HSA-MIR-6752-3P	99.72	66.71	1587
HSA-MIR-298	99.63	67.56	1916
HSA-MIR-1827	99.63	68.57	3265
HSA-MIR-6832-3P	99.52	70.44	1726
HSA-MIR-185-5P	99.35	68.60	2497
HSA-MIR-4644	99.35	69.12	2514
HSA-MIR-361-3P	99.19	66.45	1381
HSA-MIR-12135	98.99	70.26	1814
HSA-MIR-412-3P	98.86	66.89	712
HSA-MIR-6754-3P	98.84	66.60	889
HSA-MIR-4710	98.61	65.96	1048
HSA-MIR-6887-5P	98.56	68.49	1295
HSA-MIR-6795-5P	98.52	68.51	1277
HSA-MIR-6748-3P	97.20	65.66	836
HSA-MIR-4296	96.35	63.55	1233
HSA-MIR-4265	96.18	64.68	557
HSA-MIR-4322	96.18	64.85	539

Literature-anchored findings (GeneRIF, showing 16)

• Megakaryocytopoiesis was accompanied by down-regulation of the 43 kDa and 46 kDa variants of G16alpha, constant expression of Gsalpha, and up-regulation of Gqalpha and Gialpha1/2. (PMID:11686331)
• role of intracellular loops of cannabinoid CB1 receptor in functional interaction with Galpha16. (PMID:12095632)
• G protein-coupled receptors activate STAT3 via G alpha(16), a G alpha subunit which is primarily expressed in hematopoietic cells. (PMID:12670499)
• Galpha16 stimulates STAT3 via a c-Src/JAK- and ERK-dependent mechanism (PMID:14551213)
• Results suggest that the G(q) class proteins are degraded through the proteasome pathway and that cellular localization and/or other protein interactions determine their stability. (PMID:16218966)
• Co-stimulation of G(s) and G(q) can result in the fine-tuning of STAT3 activation status, and this may provide the basis for cell type-specific responses following activation of hIP. (PMID:18755267)
• The paper describes G alpha 15 resistance to arrestin-desensitization making it differ from other heterotrimeric G proteins (Gq, Gs, Gi, G12/13 class) (PMID:19275934)
• The ability of CCR1 to signal through Galpha(14/16) thus provides a linkage for chemokines to regulate NF-kappaB-dependent responses. (PMID:19687291)
• This review summarizes the specific features that distinguish Galpha15/GNA15 (G15 alpha subunit) from all other alpha subunits of the Gq class. G15 is a heterotrimeric G protein complex that is named after its alpha subunit. (PMID:20150327)
• beta3 region of Galpha16 is essential for interaction with TPR1 and the subsequent activation of Ras (PMID:21486497)
• This paper shows how G alpha 15 and other Gq class members phosphorylate PKD in differing patterns (PMID:22227248)
• G15 ectopic presence could functionally contribute to the transformation process since siRNA-induced depletion of Galpha15 in pancreatic carcinoma cell lines dramatically inhibited anchorage-independent growth and resistance to the lack of nutrients. (PMID:23200847)
• Data indicate the importance of Galpha16 as a downstream effector of the non-canonical Wnt signaling pathway and as a potential therapeutic target for the treatment of non small cell lung cancer. (PMID:24204697)
• GNA15 was not expressed in normal neuroendocrine cells but was overexpressed in gastroenteropancreatic neuroendocrine neoplasia cell lines. (PMID:25701539)
• Exosomal miR-211-5p regulates glucose metabolism, pyroptosis, and immune microenvironment of melanoma through GNA15. (PMID:36642112)
• GNA15 facilitates the malignant development of thyroid carcinoma cells via the BTK-mediated MAPK signaling pathway. (PMID:38333922)

Cross-species orthologs

26 orthologs

Organism	Symbol	Gene ID
danio_rerio	gna15.1	ENSDARG00000016364
danio_rerio	gna15.2	ENSDARG00000056654
danio_rerio	gna15.4	ENSDARG00000071416
danio_rerio	si:ch211-207c7.2	ENSDARG00000092481
danio_rerio	gna15.3	ENSDARG00000092948
danio_rerio		ENSDARG00000116003
mus_musculus	Gna15	ENSMUSG00000034792
rattus_norvegicus	Gna15	ENSRNOG00000005378
drosophila_melanogaster	cta	FBGN0000384
drosophila_melanogaster	Galphai	FBGN0001104
drosophila_melanogaster	Galphaf	FBGN0010223
drosophila_melanogaster	CG17760	FBGN0033756
drosophila_melanogaster	CG30054	FBGN0050054
caenorhabditis_elegans		WBGENE00001664
caenorhabditis_elegans		WBGENE00001665
caenorhabditis_elegans		WBGENE00001666
caenorhabditis_elegans		WBGENE00001667
caenorhabditis_elegans		WBGENE00001668
caenorhabditis_elegans		WBGENE00001670
caenorhabditis_elegans		WBGENE00001671
caenorhabditis_elegans		WBGENE00001673
caenorhabditis_elegans		WBGENE00001674
caenorhabditis_elegans		WBGENE00001675
caenorhabditis_elegans	gpa-14	WBGENE00001676
caenorhabditis_elegans	gpa-16	WBGENE00001678
caenorhabditis_elegans	gsa-1	WBGENE00001745

Paralogs (15): GNAI3 (ENSG00000065135), GNAO1 (ENSG00000087258), GNAS (ENSG00000087460), GNA11 (ENSG00000088256), GNAT1 (ENSG00000114349), GNAI2 (ENSG00000114353), GNA13 (ENSG00000120063), GNAI1 (ENSG00000127955), GNAZ (ENSG00000128266), GNAT2 (ENSG00000134183), GNAL (ENSG00000141404), GNA12 (ENSG00000146535), GNA14 (ENSG00000156049), GNAQ (ENSG00000156052), GNAT3 (ENSG00000214415)

Protein

Protein identifiers

Guanine nucleotide-binding protein subunit alpha-15 — P30679 (reviewed: P30679)

Alternative names: Epididymis tissue protein Li 17E, Guanine nucleotide-binding protein subunit alpha-16

All UniProt accessions (2): P30679, K7EP74

UniProt curated annotations — full annotation on UniProt →

Function. Member of the G-protein alpha subunit family that plays a crucial role in intracellular signaling. Functions as a molecular switch, transducing signals from G protein-coupled receptors (GPCRs) to downstream effectors. In collaboration with the adapter protein TTC1, promotes HRAS activation and ERK1/2 phosphorylation independently of phospholipase Cbeta signaling. Also initiates EMR2-mediated signaling, leading to activation of Akt, MAPK, and NF-kappa-B, which in turn drives macrophage differentiation and inflammatory responses.

Subunit / interactions. G proteins are composed of 3 units; alpha, beta and gamma. The alpha chain contains the guanine nucleotide binding site. Interacts with adapter protein TTC1. Interacts with SOS2.

Tissue specificity. Specifically expressed in hematopoietic cells. Expressed in epididymis (at protein level).

Similarity. Belongs to the G-alpha family. G(q) subfamily.

RefSeq proteins (1): NP_002059* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000654	Gprotein_alpha_Q	Family
IPR001019	Gprotein_alpha_su	Family
IPR011025	GproteinA_insert	Homologous_superfamily
IPR027417	P-loop_NTPase	Homologous_superfamily

Pfam: PF00503

Enzyme classification (BRENDA):

• EC 3.6.5.1 — heterotrimeric G-protein GTPase (BRENDA: 35 organisms, 39 substrates, 15 inhibitors, 17 Km, 24 kcat entries)

Substrate kinetics (BRENDA)

1 substrates with measured Km, best-characterized 1. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
GTP	0.0008–0.85	16

UniProt features (17 total): binding site 7, region of interest 5, chain 1, domain 1, modified residue 1, sequence variant 1, mutagenesis site 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P30679-F1	90.74	0.76

Functional residue map

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

Ligand- & substrate-binding residues (7): 189; 208–212; 277–280; 346; 49–56; 56; 183–189

Post-translational modifications (1): 186

Mutagenesis-validated functional residues (1):

Position	Phenotype
212	gtpase-deficient mutant. no loss of binding to ttc1.

Function

Pathways and Gene Ontology

Reactome pathways

9 pathways

ID	Pathway
R-HSA-112043	PLC beta mediated events
R-HSA-202040	G-protein activation
R-HSA-399997	Acetylcholine regulates insulin secretion
R-HSA-416476	G alpha (q) signalling events
R-HSA-418592	ADP signalling through P2Y purinoceptor 1
R-HSA-428930	Thromboxane signalling through TP receptor
R-HSA-434316	Fatty Acids bound to GPR40 (FFAR1) regulate insulin secretion
R-HSA-456926	Thrombin signalling through proteinase activated receptors (PARs)
R-HSA-6814122	Cooperation of PDCL (PhLP1) and TRiC/CCT in G-protein beta folding

MSigDB gene sets: 307 (showing top): GSE37336_LY6C_POS_VS_NEG_NAIVE_CD4_TCELL_DN, GSE45365_NK_CELL_VS_CD8_TCELL_UP, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, BIOCARTA_FMLP_PATHWAY, YAGI_AML_WITH_INV_16_TRANSLOCATION, JAEGER_METASTASIS_DN, REACTOME_PLATELET_ACTIVATION_SIGNALING_AND_AGGREGATION, MODULE_64, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, MODULE_16, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, GOBP_CELL_CELL_SIGNALING, RICKMAN_METASTASIS_DN, RICKMAN_TUMOR_DIFFERENTIATED_WELL_VS_POORLY_DN, MODULE_289

GO Biological Process (5): phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathway (GO:0007207), calcium-mediated signaling (GO:0019722), signal transduction (GO:0007165), G protein-coupled receptor signaling pathway (GO:0007186), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200)

GO Molecular Function (7): G protein-coupled receptor binding (GO:0001664), GTPase activity (GO:0003924), GTP binding (GO:0005525), G-protein beta/gamma-subunit complex binding (GO:0031683), metal ion binding (GO:0046872), nucleotide binding (GO:0000166), guanyl nucleotide binding (GO:0019001)

GO Cellular Component (3): heterotrimeric G-protein complex (GO:0005834), plasma membrane (GO:0005886), synapse (GO:0045202)

Reactome top-level categories

Rollup of top-8 pathways:

Category	Pathways
Signal amplification	2
G-protein mediated events	1
Opioid Signalling	1
Regulation of insulin secretion	1
GPCR downstream signalling	1
Free fatty acids regulate insulin secretion	1
Platelet activation, signaling and aggregation	1
Chaperonin-mediated protein folding	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
phospholipase C-activating G protein-coupled receptor signaling pathway	1
G protein-coupled acetylcholine receptor signaling pathway	1
intracellular signaling cassette	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
G protein-coupled receptor activity	1
signal transduction	1
G protein-coupled receptor signaling pathway	1
phospholipase C activator activity	1
signaling receptor binding	1
ribonucleoside triphosphate phosphatase activity	1
guanyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
protein-containing complex binding	1
cation binding	1
nucleoside phosphate binding	1
heterocyclic compound binding	1
purine nucleotide binding	1
extrinsic component of cytoplasmic side of plasma membrane	1
plasma membrane protein complex	1
GTPase complex	1
membrane	1
cell periphery	1
cell junction	1

Protein interactions and networks

STRING

1336 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
GNA15	S1PR4	O95977	870
GNA15	NPFFR2	Q9Y5X5	800
GNA15	PLCB2	Q00722	744
GNA15	LPAR2	Q9HBW0	713
GNA15	S1PR3	Q99500	708
GNA15	NPFF	O15130	705
GNA15	ADRB2	P07550	642
GNA15	GRK2	P25098	642
GNA15	GNA14	O95837	641
GNA15	C5AR1	P21730	614
GNA15	NPFFR1	Q9GZQ6	559
GNA15	SUCLG1	P53597	532
GNA15	TAS1R2	Q8TE23	528
GNA15	CXCR2	P25025	517
GNA15	TAS1R3	Q7RTX0	509

IntAct

14 interactions, top by confidence:

A	B	Type	Score
GNA15	HSPA8	psi-mi:“MI:0914”(association)	0.530
KISS1R	GNA15	psi-mi:“MI:0915”(physical association)	0.400
MLF1	GNA15	psi-mi:“MI:0915”(physical association)	0.400
Hacd3	GNA15	psi-mi:“MI:0915”(physical association)	0.400
GNA15	MLF2	psi-mi:“MI:0915”(physical association)	0.400
GNA15		psi-mi:“MI:0915”(physical association)	0.400
PSMD2	GNA15	psi-mi:“MI:0915”(physical association)	0.400
Usp19	GNA15	psi-mi:“MI:0915”(physical association)	0.400
GNA15	FKBPL	psi-mi:“MI:0915”(physical association)	0.400
CACYBP	GNA15	psi-mi:“MI:0915”(physical association)	0.400
GNA15	AARSD1	psi-mi:“MI:0915”(physical association)	0.400
M		psi-mi:“MI:0914”(association)	0.350

BioGRID (20): C2orf44 (Affinity Capture-MS), HSPA8 (Affinity Capture-MS), APPBP2 (Affinity Capture-MS), FECH (Affinity Capture-MS), GNA15 (Reconstituted Complex), GNA15 (Affinity Capture-Western), GNA15 (Reconstituted Complex), TTC1 (Two-hybrid), TTC1 (Affinity Capture-Western), GNA15 (Reconstituted Complex), GNA15 (Affinity Capture-Western), APPBP2 (Affinity Capture-MS), MNAT1 (Affinity Capture-MS), C2orf44 (Affinity Capture-MS), HSPA8 (Affinity Capture-MS)

ESM2 similar proteins: A8MTJ3, O14438, O15975, O70443, O73819, O95837, P04695, P11488, P16051, P16894, P19086, P19627, P21278, P21279, P23625, P29992, P30677, P30678, P30679, P38408, P38409, P38410, P38411, P38412, P41776, P43444, P45645, P50148, P53359, P82471, P87033, P87034, P91907, P91950, Q19572, Q21917, Q28294, Q2PKF4, Q2XSV9, Q4VT35

Diamond homologs: A8MTJ3, B0XRA0, B2RSH2, O13055, O13315, O15975, O15976, O42784, O70443, O73819, O74227, O74259, O88302, O95837, P04695, P04696, P04897, P04899, P08239, P08752, P08753, P08754, P09471, P0C7Q4, P10824, P10825, P11488, P16378, P16894, P18872, P19086, P19087, P19627, P20353, P20612, P21278, P21279, P23625, P27044, P27045

SIGNOR signaling

29 interactions.

A	Effect	B	Mechanism
P2RY2	“up-regulates activity”	GNA15	binding
P2RY13	“up-regulates activity”	GNA15	binding
P2RY4	“up-regulates activity”	GNA15	binding
AGTR1	“up-regulates activity”	GNA15	binding
CHRM3	“up-regulates activity”	GNA15	binding
CYSLTR1	“up-regulates activity”	GNA15	binding
GALR2	“up-regulates activity”	GNA15	binding
FFAR2	“up-regulates activity”	GNA15	binding
P2RY6	“up-regulates activity”	GNA15	binding
BDKRB2	“up-regulates activity”	GNA15	binding
LPAR1	“up-regulates activity”	GNA15	binding
P2RY1	“up-regulates activity”	GNA15	binding
CHRM5	“up-regulates activity”	GNA15	binding
NMUR2	“up-regulates activity”	GNA15	binding
F2R	“up-regulates activity”	GNA15	binding
HCRTR1	“up-regulates activity”	GNA15	binding
HTR2C	“up-regulates activity”	GNA15	binding
MC3R	“up-regulates activity”	GNA15	binding
F2RL2	“up-regulates activity”	GNA15	binding
MCHR2	“up-regulates activity”	GNA15	binding
LPAR3	“up-regulates activity”	GNA15	binding
F2RL1	“up-regulates activity”	GNA15	binding
CCKAR	“up-regulates activity”	GNA15	binding
BDKRB1	“up-regulates activity”	GNA15	binding
CCKBR	“up-regulates activity”	GNA15	binding
GPR132	“up-regulates activity”	GNA15	binding
PMAIP1	“up-regulates activity”	GNA15	phosphorylation
TRHR	“up-regulates activity”	GNA15	binding
GNA15	“up-regulates activity”	PLCB1	binding

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	51
Likely benign	1
Benign	3

Top pathogenic / likely-pathogenic (0)

SpliceAI

950 predictions. Top by Δscore:

Variant	Effect	Δscore
19:3136591:TTTGG:T	donor_gain	1.0000
19:3136592:TTGG:T	donor_gain	1.0000
19:3136593:TGG:T	donor_gain	1.0000
19:3136594:GG:G	donor_gain	1.0000
19:3136594:GGG:G	donor_gain	1.0000
19:3136595:GG:G	donor_gain	1.0000
19:3136596:G:GG	donor_gain	1.0000
19:3148586:CCCA:C	acceptor_loss	1.0000
19:3148589:A:AG	acceptor_gain	1.0000
19:3148589:A:C	acceptor_loss	1.0000
19:3148589:AG:A	acceptor_gain	1.0000
19:3148590:G:GT	acceptor_gain	1.0000
19:3148590:GG:G	acceptor_gain	1.0000
19:3148590:GGC:G	acceptor_gain	1.0000
19:3148771:GCAAG:G	donor_gain	1.0000
19:3148774:AG:A	donor_gain	1.0000
19:3148775:GG:G	donor_gain	1.0000
19:3148776:G:GG	donor_gain	1.0000
19:3148776:GTG:G	donor_loss	1.0000
19:3150128:CA:C	acceptor_loss	1.0000
19:3150129:A:AG	acceptor_gain	1.0000
19:3150130:G:GA	acceptor_gain	1.0000
19:3150130:GC:G	acceptor_gain	1.0000
19:3150130:GCA:G	acceptor_gain	1.0000
19:3150130:GCAC:G	acceptor_gain	1.0000
19:3150130:GCACC:G	acceptor_gain	1.0000
19:3150278:GCCGT:G	donor_gain	1.0000
19:3150281:GTGTA:G	donor_gain	1.0000
19:3150283:GTA:G	donor_gain	1.0000
19:3150286:G:GG	donor_gain	1.0000

AlphaMissense

2465 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
19:3155863:T:A	W219R	1.000
19:3155863:T:C	W219R	1.000
19:3148608:A:C	K55Q	0.999
19:3148609:A:T	K55M	0.999
19:3148610:G:C	K55N	0.999
19:3148610:G:T	K55N	0.999
19:3155865:G:C	W219C	0.999
19:3155865:G:T	W219C	0.999
19:3157816:A:T	K278I	0.999
19:3148605:G:T	G54W	0.998
19:3148606:G:A	G54E	0.998
19:3148611:A:C	S56R	0.998
19:3148613:C:A	S56R	0.998
19:3148613:C:G	S56R	0.998
19:3148628:G:C	Q61H	0.998
19:3148628:G:T	Q61H	0.998
19:3155875:T:C	F223L	0.998
19:3155877:C:A	F223L	0.998
19:3155877:C:G	F223L	0.998
19:3136587:T:C	L46P	0.997
19:3136595:G:C	G49R	0.997
19:3148608:A:G	K55E	0.997
19:3148612:G:T	S56I	0.997
19:3148633:G:C	R63P	0.997
19:3155830:G:C	D208H	0.997
19:3155831:A:G	D208G	0.997
19:3155832:C:A	D208E	0.997
19:3155832:C:G	D208E	0.997
19:3157807:T:C	F275S	0.997
19:3157817:A:C	K278N	0.997

dbSNP variants (sampled 300 via entrez): RS1000111596 (19:3162541 A>G), RS1000121611 (19:3162760 G>A), RS1000204914 (19:3135125 A>C,T), RS1000239405 (19:3137242 A>G), RS1000239753 (19:3140418 G>A), RS1000255629 (19:3135309 C>G,T), RS1000348924 (19:3144731 T>C,G), RS1000371945 (19:3144757 T>C), RS1000456546 (19:3154402 T>C,G), RS1000591831 (19:3140118 CATT>C), RS1000650127 (19:3147480 G>A), RS1000672573 (19:3142708 C>T), RS1000766403 (19:3154035 G>T), RS1000868163 (19:3158275 T>C,G), RS1000945022 (19:3148910 C>A,G)

Disease associations

OMIM: gene MIM:139314 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

11 associations (top):

Study	Trait	p-value
GCST000675_10	Heart failure	6.000000e-06
GCST002726_72	Glucose homeostasis traits	7.000000e-08
GCST009798_49	Asthma	7.000000e-10
GCST009817_4	Clozapine-induced myocarditis in schizophrenia	1.000000e-07
GCST010042_35	Asthma	4.000000e-11
GCST90002392_51	Mean corpuscular volume	2.000000e-09
GCST90002396_8	Mean reticulocyte volume	2.000000e-09
GCST90002397_398	Mean spheric corpuscular volume	3.000000e-10
GCST90002398_100	Neutrophil count	5.000000e-13
GCST90002407_351	White blood cell count	2.000000e-09
GCST90014325_70	Asthma	9.000000e-09

EFO canonical traits (3, from GWAS)

EFO ID	Trait name
EFO:0006830	insulin metabolic clearance rate measurement
EFO:0010701	mean reticulocyte volume
EFO:0004833	neutrophil count

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5482994 (PROTEIN COMPLEX)

Molecules with ChEMBL bioactivity

2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 324,010 (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
CHEMBL1829174	FASIGLIFAM	3	815
CHEMBL267476	LINOLEIC ACID	2	323,195

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

Binding affinities (BindingDB)

566 measured of 568 human assays (568 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
1-[(2R)-4-[4-(1H-benzimidazol-2-yl)-2-(trifluoromethyl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-(4-chloropyrazol-1-yl)ethanone	IC50	0.1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(1H-benzimidazol-2-yl)-2-(trifluoromethyl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-(5-methylpyrazol-1-yl)ethanone	IC50	0.1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-[6-(2-aminoethyl)-1H-benzimidazol-2-yl]-2-(trifluoromethyl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-(3,5-dimethyl-1,2,4-triazol-1-yl)ethanone	IC50	0.1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(6-chloro-1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-pyrrolo[2,3-b]pyridin-1-ylethanone	IC50	0.2 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-pyrrolo[2,3-c]pyridin-1-ylethanone	IC50	0.2 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(1H-benzimidazol-2-yl)-2-(trifluoromethyl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-(3-methylpyrazol-1-yl)ethanone	IC50	0.2 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
2-imidazo[4,5-b]pyridin-3-yl-1-[(2R)-4-[4-(1H-imidazo[4,5-b]pyridin-2-yl)-2-(trifluoromethyl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]ethanone	IC50	0.3 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[2-[(2R)-4-[4-(1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-oxoethyl]-3,3-difluoroindol-2-one	IC50	0.3 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(5,6-difluoro-1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-imidazo[4,5-b]pyridin-3-ylethanone	IC50	0.4 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(1H-benzimidazol-2-yl)-2-(trifluoromethyl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-(6-methyl-3-pyridinyl)ethanone	IC50	0.4 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(5-chloro-4-methyl-1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-imidazo[4,5-b]pyridin-3-ylethanone	IC50	0.5 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(6-fluoro-1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-imidazo[4,5-b]pyridin-3-ylethanone	IC50	0.5 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(1H-benzimidazol-2-yl)-2-(trifluoromethyl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-pyrazol-1-ylethanone	IC50	0.5 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]-2-ethylpiperazin-1-yl]-2-pyrrolo[2,3-b]pyridin-1-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-2-methyl-4-[4-(4-methyl-1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]piperazin-1-yl]-2-pyrrolo[2,3-b]pyridin-1-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(6-tert-butyl-1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-pyrrolo[2,3-b]pyridin-1-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(5-chloro-6-fluoro-1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-pyrrolo[2,3-b]pyridin-1-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(4,5-difluoro-1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-pyrrolo[2,3-b]pyridin-1-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(1H-benzimidazol-2-yl)-2-(trifluoromethyl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-imidazo[4,5-b]pyridin-3-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2S,6R)-4-[4-(6-chloro-1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]-2,6-dimethylpiperazin-1-yl]-2-imidazo[4,5-b]pyridin-3-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(1H-benzimidazol-2-yl)-2-bromo-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-imidazo[4,5-b]pyridin-3-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(6-chloro-1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-imidazo[4,5-b]pyridin-3-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
3-[2-[(2R)-4-[4-(6-chloro-1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-oxoethyl]-1,3-benzoxazol-2-one	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
2-imidazo[4,5-b]pyridin-3-yl-1-[(2R)-2-methyl-4-[4-(6-methyl-1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]piperazin-1-yl]ethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(6-tert-butyl-1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-imidazo[4,5-b]pyridin-3-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(5-chloro-6-methyl-1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-imidazo[4,5-b]pyridin-3-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
2-imidazo[4,5-b]pyridin-3-yl-1-[(2R)-2-methyl-4-[4-(6-propan-2-yl-1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]piperazin-1-yl]ethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(5-chloro-6-fluoro-1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-imidazo[4,5-b]pyridin-3-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
2-imidazo[4,5-b]pyridin-3-yl-1-[(2R)-2-methyl-4-[4-[6-(trifluoromethyl)-1H-benzimidazol-2-yl]-1,3-thiazol-5-yl]piperazin-1-yl]ethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-[5-chloro-6-(trifluoromethyl)-1H-benzimidazol-2-yl]-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-imidazo[4,5-b]pyridin-3-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(6-ethyl-1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-imidazo[4,5-b]pyridin-3-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
2-imidazo[4,5-b]pyridin-3-yl-1-[(2R)-2-methyl-4-[4-(6-phenyl-1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]piperazin-1-yl]ethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[2-[(2R)-4-[4-(1H-benzimidazol-2-yl)-2-(trifluoromethyl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-oxoethyl]-3H-indol-2-one	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
3-[2-[(2R)-4-[4-(1H-benzimidazol-2-yl)-2-(trifluoromethyl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-oxoethyl]-1H-imidazo[4,5-b]pyridin-2-one	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-pyrazolo[5,4-b]pyridin-1-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-(3-chloropyrrolo[2,3-b]pyridin-1-yl)ethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(1H-benzimidazol-2-yl)-2-ethyl-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-imidazo[4,5-b]pyridin-3-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(6-chloro-1H-benzimidazol-2-yl)-2-(trifluoromethyl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-imidazo[4,5-b]pyridin-3-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-[6-(hydroxymethyl)-1H-benzimidazol-2-yl]-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-imidazo[4,5-b]pyridin-3-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(6-cyclopropyl-1H-benzimidazol-2-yl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-imidazo[4,5-b]pyridin-3-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-[6-(2-hydroxyethoxy)-1H-benzimidazol-2-yl]-2-(trifluoromethyl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-imidazo[4,5-b]pyridin-3-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(6-acetyl-1H-benzimidazol-2-yl)-2-(trifluoromethyl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-imidazo[4,5-b]pyridin-3-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-[6-(1-hydroxyethyl)-1H-benzimidazol-2-yl]-2-(trifluoromethyl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-imidazo[4,5-b]pyridin-3-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
methyl 2-[5-[(3R)-4-(2-imidazo[4,5-b]pyridin-3-ylacetyl)-3-methylpiperazin-1-yl]-2-(trifluoromethyl)-1,3-thiazol-4-yl]-3H-benzimidazole-5-carboxylate	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
2-imidazo[4,5-b]pyridin-3-yl-1-[(2R)-2-methyl-4-[4-(7H-purin-8-yl)-2-(trifluoromethyl)-1,3-thiazol-5-yl]piperazin-1-yl]ethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
2-(benzimidazol-1-yl)-1-[(2R)-4-[4-(1H-benzimidazol-2-yl)-2-(trifluoromethyl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]ethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(1H-benzimidazol-2-yl)-2-(trifluoromethyl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-quinolin-8-ylethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(1H-benzimidazol-2-yl)-2-(trifluoromethyl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-(4-methylpyrazol-1-yl)ethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(1H-benzimidazol-2-yl)-2-(trifluoromethyl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-(3,5-dimethylpyrazol-1-yl)ethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
1-[(2R)-4-[4-(1H-benzimidazol-2-yl)-2-(trifluoromethyl)-1,3-thiazol-5-yl]-2-methylpiperazin-1-yl]-2-[3-(trifluoromethyl)pyrazol-1-yl]ethanone	IC50	1 nM	US-9266876: 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives

ChEMBL bioactivities

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

pChembl	Type	Value	Unit	Molecule
7.56	EC50	27.4	nM	CHEMBL5422928
7.45	EC50	35.8	nM	FASIGLIFAM
7.32	EC50	48	nM	GW9508
7.03	EC50	93.3	nM	CHEMBL2151289
5.00	EC50	1.01e+04	nM	LINOLEIC ACID

PubChem BioAssay actives

4 with measured affinity, of 8 total; 4 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-[(S)-[4-[[3-(2,6-dimethylphenyl)phenyl]methoxy]phenyl]sulfinyl]acetic acid	1996572: Agonist activity at human GPR40/Galpha-16 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay	ec50	0.0274	uM
2-[(3S)-6-[[3-[2,6-dimethyl-4-(3-methylsulfonylpropoxy)phenyl]phenyl]methoxy]-2,3-dihydro-1-benzofuran-3-yl]acetic acid	1996572: Agonist activity at human GPR40/Galpha-16 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay	ec50	0.0358	uM
3-[4-[(3-phenoxyphenyl)methylamino]phenyl]propanoic acid	2087777: Agonist activity at human GPR40/Galpha-16 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay	ec50	0.0480	uM
(3R)-3-[4-[[4-(3-methoxyphenyl)phenyl]methoxy]phenyl]hex-4-ynoic acid	1996572: Agonist activity at human GPR40/Galpha-16 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay	ec50	0.0933	uM

CTD chemical–gene interactions

51 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	affects methylation, decreases methylation	2
Nickel	increases expression	2
Tobacco Smoke Pollution	affects expression, increases expression	2
GSK-J4	increases expression	1
citral dimethyl acetal	increases response to substance, increases activity	1
triphenyl phosphate	affects expression	1
bisphenol A	decreases methylation	1
geraniol	increases response to substance, increases activity	1
pelargonic acid	increases response to substance, increases activity	1
azelaic acid	increases activity, increases response to substance	1
pyrogallol 1,3-dimethyl ether	increases expression, affects cotreatment, affects localization	1
alpha-ionone	increases activity, increases response to substance	1
2-heptanone	increases response to substance, decreases activity	1
butyraldehyde	increases expression	1
benzo(e)pyrene	increases methylation	1
aflatoxin B2	increases methylation	1
nickel sulfate	increases expression	1
octanoic acid	increases response to substance, increases activity	1
caprylic aldehyde	increases response to substance, increases activity	1
2,4-decadienal	increases response to substance, increases activity	1
2,6-nonadienal	increases response to substance, increases activity	1
2-palmitoylglycerol	increases expression	1
2,4-nonadienal	increases response to substance, increases activity	1
erucylphospho-N,N,N-trimethylpropylammonium	increases expression	1
bourgeonal	increases response to substance, increases activity	1
abrine	increases expression	1
alpha-methyl-3,4-methylene-dioxyhydrocinnamic aldehyde	increases response to substance, increases activity	1
bisphenol S	increases methylation	1
(+)-JQ1 compound	decreases expression	1
Acetaminophen	decreases expression	1

ChEMBL screening assays

3 unique, capped per target: 2 binding, 1 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL5349699	Binding	Agonist activity at human GPR40/Galpha-16 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay	Discovery of orally effective and safe GPR40 agonists by incorporating a chiral, rigid and polar sulfoxide into β-position to the carboxylic acid. — Eur J Med Chem
CHEMBL5528508	Functional	Agonist activity at human GPR40/Galpha-16 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay	Synthetic GPR40/FFAR1 agonists: An exhaustive survey on the most recent chemical classes and their structure-activity relationships. — Eur J Med Chem

Cellosaurus cell lines

127 cell lines: 116 spontaneously immortalized cell line, 8 transformed cell line, 3 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_5I82	1321N1 (+Galpha16) AequoScreen	Cancer cell line	Male
CVCL_5I89	CHO-K1 (+Galpha16) AequoScreen	Spontaneously immortalized cell line	Female
CVCL_5I97	HEK293 AequoScreen	Transformed cell line	Female
CVCL_B0GV	I3.4.2	Cancer cell line	Male
CVCL_E5JS	CHO-K1/Galpha15/MRGPRX1	Spontaneously immortalized cell line	Female
CVCL_F2AJ	CHO-K1 (+Galpha16) AequoScreen Serotonin 5-HT2A	Spontaneously immortalized cell line	Female
CVCL_F2AK	CHO-K1 (+Galpha16) AequoScreen Cannabinoid CB1	Spontaneously immortalized cell line	Female
CVCL_F2AL	CHO-K1 (+Galpha16) AequoScreen Opioid Mu (OP3)	Spontaneously immortalized cell line	Female
CVCL_H357	1321N1/P2Y12/Galpha15	Cancer cell line	Male
CVCL_H362	293/ADORA1/Galpha15	Transformed cell line	Female

Clinical trials (associated diseases)

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