TAAR1

Summary

TAAR1 (trace amine associated receptor 1, HGNC:17734) is a protein-coding gene on chromosome 6q23.2, encoding Trace amine-associated receptor 1 (Q96RJ0). Intracellular G-protein coupled receptor for trace amines, which recognizes endogenous amine-containing metabolites such as beta-phenylethylamine (beta-PEA), 3-iodothyronamine (T1AM), isoamylamine (IAA), cadaverine (CAD), cyclohexylamine (CHA), p-tyramine (p-TYR), trimethylamine….

The protein encoded by this gene is a G-protein coupled receptor activated by trace amines. The encoded protein responds little or not at all to dopamine, serotonin, epinephrine, or histamine, but responds well to beta-phenylethylamine, p-tyramine, octopamine, and tryptamine. While primarily functioning in neurologic systems, there is evidence that this gene is involved in blood cell and immunologic functions as well. This gene is thought to be intronless.

Source: NCBI Gene 134864 — RefSeq curated summary.

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 50 total
• Druggable target: yes — 20 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_138327

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:17734
Approved symbol	TAAR1
Name	trace amine associated receptor 1
Location	6q23.2
Locus type	gene with protein product
Status	Approved
Aliases	TAR1, TA1
Ensembl gene	ENSG00000146399
Ensembl biotype	protein_coding
OMIM	609333
Entrez	134864

Gene structure

Transcript identifiers

Ensembl transcripts: 1 — 1 protein_coding

ENST00000275216

RefSeq mRNA: 1 — MANE Select: NM_138327 NM_138327

CCDS: CCDS5158

Canonical transcript exons

ENST00000275216 — 2 exons

Exon	Start	End
ENSE00000975669	132643312	132646129
ENSE00003920017	132659130	132659182

Expression profiles

Bgee: expression breadth broad, 22 present calls, max score 58.35.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.0728 / max 99.5028, expressed in 5 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
75603	0.0575	4
75604	0.0152	2

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
islet of Langerhans	UBERON:0000006	58.35	gold quality
right uterine tube	UBERON:0001302	54.99	gold quality
duodenum	UBERON:0002114	47.23	gold quality
fallopian tube	UBERON:0003889	44.14	gold quality
endometrium	UBERON:0001295	39.72	silver quality
colonic epithelium	UBERON:0000397	37.20	gold quality
ventricular zone	UBERON:0003053	36.48	gold quality
cortical plate	UBERON:0005343	36.47	gold quality
pancreas	UBERON:0001264	36.22	gold quality
bone marrow cell	CL:0002092	36.16	gold quality
blood	UBERON:0000178	36.01	gold quality
bone marrow	UBERON:0002371	35.80	gold quality
ganglionic eminence	UBERON:0004023	35.49	gold quality
tonsil	UBERON:0002372	34.61	silver quality
skeletal muscle tissue	UBERON:0001134	33.38	gold quality
muscle tissue	UBERON:0002385	33.34	gold quality
smooth muscle tissue	UBERON:0001135	33.03	gold quality
liver	UBERON:0002107	32.73	gold quality
monocyte	CL:0000576	32.21	gold quality
stomach	UBERON:0000945	32.21	gold quality
hindlimb stylopod muscle	UBERON:0004252	32.15	gold quality
urinary bladder	UBERON:0001255	31.98	gold quality
leukocyte	CL:0000738	31.79	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	31.04	silver quality
sural nerve	UBERON:0015488	30.93	gold quality
metanephros cortex	UBERON:0010533	30.72	gold quality
body of stomach	UBERON:0001161	30.62	gold quality
right lobe of liver	UBERON:0001114	30.07	gold quality
stromal cell of endometrium	CL:0002255	29.87	gold quality
cortex of kidney	UBERON:0001225	29.66	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-ANND-3	no	1.00

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): TP53

Literature-anchored findings (GeneRIF, showing 26)

• Previous studies reported TAAR expression in brain. This paper found TAAR expression only in olfactory epithelial cells and that each TAAR detects a unique set of amine ligands. TAARs seem to function as a family of chemosensory receptors for amines. (PMID:16878137)
• Expression of neuronal trace amine-associated receptor (Taar) mRNAs in leukocytes. (PMID:17900709)
• A systematic evaluation of a series of beta-phenethylamines as ligands to TAAR1 is reported. (PMID:18602830)
• Data support that TAAR1 tonically activates inwardly rectifying K(+) channels, which reduces the basal firing frequency of dopamine neurons in the ventral tegmental area. (PMID:19892733)
• Overview focuses on recent studies which reveal a role for TAAR1 in the functional regulation of monoamine transporters and the neuronal regulatory mechanisms that modulate dopaminergic activity. [review] (PMID:21073468)
• data suggest that TAAR1 and D2R have functional and physical interactions that could be critical for the modulation of the dopaminergic system by TAAR1 in vivo (PMID:21670104)
• an increase in TAAR1 receptor expression is concomitant with lymphocyte immune activation, suggesting a possible role for TAAR1 in the generation or regulation of an immune response (PMID:22038157)
• Methamphetamine-but not morphine-induced conditioned place preference was augmented in TAAR1 transgenic mice. (PMID:22079347)
• Trace amine 1 receptors (TA1R) exert an inhibitory influence on both dopaminergic and serotonergic transmission, and MDMA (ecstasy) auto-inhibits its neurochemical and functional actions by recruitment of TA1R. (PMID:22114263)
• biogenic amines potently regulate blood cell functions via TAAR1 and TAAR2 and open the perspective of their specific pharmacological modulation. (PMID:23315425)
• SNPs in human TAAR1 alter its function, resulting in expressed, but functional, sub-functional and non-functional receptors (PMID:27031617)
• This study identified a rare heterozygous variant (c.545G>T; p.Cys182Phe) in Trace amine associated receptor 1 gene (TAAR1 6q23.2) in three affected members in a small SZ family. (PMID:28242106)
• TAAR1 seems to be an independent predictor for breast cancer survival. (PMID:28409272)
• It clearly demonstrate variable expression and sub-cellular localization of TAAR1 across BC cell lines, we find no evidence for association with BC subtype. (PMID:31111198)
• Findings suggest that TAAR1 activation protects against methamphetamine-induced cell apoptosis and TAAR1 may play a role in cell death in neurodegenerative diseases. (PMID:31409621)
• Neuroadaptation to chronic Methamphetamine use may be altered by TAAR1 genotype and result in increased dopamine signaling and craving in individuals with the V288V genotype. (PMID:31600226)
• Cadaverine and Spermine Elicit Ca(2+) Uptake in Human CP Cells via a Trace Amine-Associated Receptor 1 Dependent Pathway. (PMID:32816235)
• Trace Amine-Associated Receptor 1 (TAAR1) Is a Positive Prognosticator for Epithelial Ovarian Cancer. (PMID:34445181)
• Trace amine-associated receptor 1 (TAAR1): Potential application in mood disorders: A systematic review. (PMID:34537265)
• TAAR1 Expression in Human Macrophages and Brain Tissue: A Potential Novel Facet of MS Neuroinflammation. (PMID:34769007)
• Search for Structural Basis of Interactions of Biogenic Amines with Human TAAR1 and TAAR6 Receptors. (PMID:35008636)
• Thymosin alpha1 interacts with Galectin-1 modulating the beta-galactosides affinity and inducing alteration in the biological activity. (PMID:37028279)
• T1AM/TAAR1 System Reduces Inflammatory Response and beta-Amyloid Toxicity in Human Microglial HMC3 Cell Line. (PMID:37511328)
• Ligand recognition and G-protein coupling of trace amine receptor TAAR1. (PMID:37935376)
• Structural and signaling mechanisms of TAAR1 enabled preferential agonist design. (PMID:37963465)
• Molecular basis of human trace amine-associated receptor 1 activation. (PMID:38168118)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	taar1b	ENSDARG00000089000
mus_musculus	Taar1	ENSMUSG00000056379
rattus_norvegicus	Taar1	ENSRNOG00000016073

Paralogs (25): DRD4 (ENSG00000069696), HRH3 (ENSG00000101180), HRH2 (ENSG00000113749), CHRM3 (ENSG00000133019), HRH4 (ENSG00000134489), TAAR5 (ENSG00000135569), GPR84 (ENSG00000139572), GPR161 (ENSG00000143147), TAAR2 (ENSG00000146378), TAAR6 (ENSG00000146383), TAAR8 (ENSG00000146385), DRD3 (ENSG00000151577), HTR4 (ENSG00000164270), CHRM1 (ENSG00000168539), DRD5 (ENSG00000169676), HTR1A (ENSG00000178394), HTR1D (ENSG00000179546), CHRM4 (ENSG00000180720), CHRM2 (ENSG00000181072), DRD1 (ENSG00000184845), CHRM5 (ENSG00000184984), GPR21 (ENSG00000188394), HRH1 (ENSG00000196639), GPR52 (ENSG00000203737), TAAR9 (ENSG00000237110)

Protein

Protein identifiers

Trace amine-associated receptor 1 — Q96RJ0 (reviewed: Q96RJ0)

All UniProt accessions (1): Q96RJ0

UniProt curated annotations — full annotation on UniProt →

Function. Intracellular G-protein coupled receptor for trace amines, which recognizes endogenous amine-containing metabolites such as beta-phenylethylamine (beta-PEA), 3-iodothyronamine (T1AM), isoamylamine (IAA), cadaverine (CAD), cyclohexylamine (CHA), p-tyramine (p-TYR), trimethylamine (TMA), octopamine and tryptamine. Also functions as a receptor for various drugs and psychoactive substances, such as amphetamine and methamphetamine. Unresponsive to classical biogenic amines, such as epinephrine and histamine and only partially activated by dopamine and serotonin. Expressed in both the central and peripheral nervous system: TAAR1 activation regulates the activity of several neurotransmitter signaling pathways by (1) decreasing the basal firing rates of the neurons involved and by (2) lowering the sensitivity of receptors to neurotransmitters. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors. TAAR1 is coupled with different G(i)/G(o)-, G(s)- or G(q)/G(11) classes of G alpha proteins depending on the ligand. CAD-binding is coupled to G(i)/G(o) G alpha proteins and mediates inhibition of adenylate cyclase activity. T1AM- or beta-PEA-binding is coupled to G(s) G alpha proteins and mediates activation of adenylate cyclase activity. CHA- or IAA-binding is coupled to G(q)/G(11) G alpha proteins and activates phospholipase C-beta, releasing diacylglycerol (DAG) and inositol 1,4,5-trisphosphate (IP3) second messengers. TMA-binding is coupled with all three G(i)/G(o)-, G(s)- or G(q)/G(11) G alpha protein subtypes. Amphetamine-binding is coupled with G(s)- or G(12)/G(13) G alpha protein subtypes.

Subcellular location. Endomembrane system. Endoplasmic reticulum membrane. Cell membrane.

Tissue specificity. Expressed at low level in both the central and peripheral nervous system. Moderately expressed in stomach. Low levels in amygdala, kidney, and lung, and small intestine. Trace amounts in cerebellum, dorsal root ganglia, hippocampus, hypothalamus, liver, medulla, pancreas, pituitary, pontine reticular formation, prostate, skeletal muscle and spleen.

Activity regulation. Activated by SEP-363856 small molecule: IHCH-7179 acts both as an agonist activator for HTR1A and TAAR1.

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

RefSeq proteins (1): NP_612200* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR009132	TAAR_fam	Family
IPR009133	TAAR1	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain
IPR050569	TAAR	Family

Pfam: PF00001

UniProt features (80 total): mutagenesis site 33, helix 15, topological domain 8, transmembrane region 7, turn 5, disulfide bond 3, glycosylation site 2, sequence variant 2, strand 2, chain 1, region of interest 1, binding site 1

Structure

Experimental structures (PDB)

17 structures.

PDB	Method	Resolution (Å)
8W88	ELECTRON MICROSCOPY	2.6
9JKQ	ELECTRON MICROSCOPY	2.66
8W87	ELECTRON MICROSCOPY	2.8
8W8A	ELECTRON MICROSCOPY	2.8
8ZSJ	ELECTRON MICROSCOPY	2.8
8JLQ	ELECTRON MICROSCOPY	2.84
8WC8	ELECTRON MICROSCOPY	2.9
8JLR	ELECTRON MICROSCOPY	3
8W89	ELECTRON MICROSCOPY	3
8ZSS	ELECTRON MICROSCOPY	3.07
8ZSP	ELECTRON MICROSCOPY	3.14
8JLP	ELECTRON MICROSCOPY	3.23
8JLN	ELECTRON MICROSCOPY	3.24
8UHB	ELECTRON MICROSCOPY	3.35
8JSO	ELECTRON MICROSCOPY	3.4
8WCA	ELECTRON MICROSCOPY	3.48
8JLO	ELECTRON MICROSCOPY	3.52

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q96RJ0-F1	90.17	0.75

Antibody-complex structures (SAbDab): 15 — 8JLN, 8JLQ, 8JLR, 8JSO, 8UHB, 8W87, 8W88, 8W89, 8W8A, 8WC8, 8WCA, 8ZSJ, 8ZSP, 8ZSS, 9JKQ

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 (1): 103

Disulfide bonds (3): 5–178, 13–88, 96–182

Glycosylation sites (2): 10, 17

Mutagenesis-validated functional residues (33):

Position	Phenotype
55	reduced activation of g(s) g alpha proteins in response to agonist-binding.
83	reduced activation of g(i) g alpha proteins in response to agonist-binding. does not affect activation of g(s) g alpha p
83	abolished activation of g alpha proteins in response to agonist-binding.
88	slightly affects g-protein coupled receptor activity.
96	abolished g-protein coupled receptor activity.
103	abolished activation of g(s) g alpha proteins in response to agonist-binding.
104	reduced activation of g alpha proteins in response to agonist-binding.
107	abolished activation of g(s) g alpha proteins in response to agonist-binding. does not affect activation of g(i) or g(q)
114	reduced activation of g(i) g alpha proteins in response to agonist-binding.
154	abolished activation of g alpha proteins in response to agonist-binding.
178	slightly affects g-protein coupled receptor activity.
183	reduced activation of g(i) g alpha proteins in response to agonist-binding. does not affect activation of g(s) g alpha p
184	abolished activation of g alpha proteins in response to agonist-binding.
184	decreased g-protein coupled receptor activity in response to p-tyramine-binding.
185	abolished activation of g alpha proteins in response to agonist-binding.
186	reduced activation of g(q) g alpha proteins in response to agonist-binding. does not affect activation of g(s) g alpha p
194	abolished activation of g alpha proteins in response to agonist-binding.
195	increased g-protein coupled receptor activity in response to p-tyramine-binding.
220	reduced activation of g(s) g alpha proteins in response to agonist-binding.
224	reduced activation of g(s) g alpha proteins in response to agonist-binding.
253	reduced activation of g(i) g alpha proteins in response to agonist-binding.
260	reduced activation of g(s) g alpha proteins in response to agonist-binding.
264	abolished activation of g alpha proteins in response to 3-iodothyronamine-binding.
264	abolished activation of g alpha proteins in response to agonist-binding.
267	abolished activation of g alpha proteins in response to 3-iodothyronamine-binding. reduced activation of g(q) g alpha pr

Function

Pathways and Gene Ontology

Reactome pathways

7 pathways

ID	Pathway
R-HSA-375280	Amine ligand-binding receptors
R-HSA-418555	G alpha (s) signalling events
R-HSA-162582	Signal Transduction
R-HSA-372790	Signaling by GPCR
R-HSA-373076	Class A/1 (Rhodopsin-like receptors)
R-HSA-388396	GPCR downstream signalling
R-HSA-500792	GPCR ligand binding

MSigDB gene sets: 35 (showing top): GOBP_ADENYLATE_CYCLASE_MODULATING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, GOBP_ADENYLATE_CYCLASE_INHIBITING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, GOBP_PHOSPHOLIPASE_C_ACTIVATING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, GOCC_NUCLEAR_OUTER_MEMBRANE_ENDOPLASMIC_RETICULUM_MEMBRANE_NETWORK, GOBP_ADENYLATE_CYCLASE_ACTIVATING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, GOCC_ORGANELLE_SUBCOMPARTMENT, GOMF_G_PROTEIN_COUPLED_AMINE_RECEPTOR_ACTIVITY, REACTOME_CLASS_A_1_RHODOPSIN_LIKE_RECEPTORS, chr6q23, GOMF_TRANSMEMBRANE_SIGNALING_RECEPTOR_ACTIVITY, GOMF_G_PROTEIN_COUPLED_RECEPTOR_ACTIVITY, BRUINS_UVC_RESPONSE_VIA_TP53_GROUP_A, GOBP_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, GOMF_TRACE_AMINE_RECEPTOR_ACTIVITY

GO Biological Process (5): G protein-coupled receptor signaling pathway (GO:0007186), adenylate cyclase-activating G protein-coupled receptor signaling pathway (GO:0007189), adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway (GO:0007193), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), signal transduction (GO:0007165)

GO Molecular Function (3): trace-amine receptor activity (GO:0001594), G protein-coupled receptor activity (GO:0004930), G protein-coupled amine receptor activity (GO:0008227)

GO Cellular Component (5): endoplasmic reticulum membrane (GO:0005789), plasma membrane (GO:0005886), endomembrane system (GO:0012505), endoplasmic reticulum (GO:0005783), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-5 pathways:

Category	Pathways
Signaling by GPCR	2
Class A/1 (Rhodopsin-like receptors)	1
GPCR downstream signalling	1
Signal Transduction	1
GPCR ligand binding	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
G protein-coupled receptor activity	2
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	2
G protein-coupled receptor signaling pathway	2
cellular anatomical structure	2
signal transduction	1
adenylate cyclase activator activity	1
adenylate cyclase inhibitor activity	1
phospholipase C activator activity	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
G protein-coupled amine receptor activity	1
transmembrane signaling receptor activity	1
organelle membrane	1
nuclear outer membrane-endoplasmic reticulum membrane network	1
endoplasmic reticulum subcompartment	1
membrane	1
cell periphery	1
vacuole	1
plasma membrane	1
cytoplasm	1
endomembrane system	1
intracellular membrane-bounded organelle	1

Protein interactions and networks

STRING

644 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
TAAR1	EPB41L4B	Q9H329	850
TAAR1	EPB41L4A	Q9HCS5	813
TAAR1	PTPN4	P29074	761
TAAR1	SLC18A2	Q05940	604
TAAR1	SLC6A3	Q01959	601
TAAR1	GPR142	Q7Z601	556
TAAR1	PTMA	P06454	543
TAAR1	RHO	P08100	520
TAAR1	SLC6A4	P31645	502
TAAR1	MAOB	P27338	500
TAAR1	EPB41	P11171	493
TAAR1	PPIG	Q13427	479
TAAR1	MAOA	P21397	476
TAAR1	STX7	O15400	462
TAAR1	CFTR	P13569	457

IntAct

11 interactions, top by confidence:

A	B	Type	Score
RAMP1	TAAR1	psi-mi:“MI:0915”(physical association)	0.400
TAAR1	RAMP1	psi-mi:“MI:0915”(physical association)	0.400
TAAR1	RAMP2	psi-mi:“MI:0915”(physical association)	0.400
RAMP2	TAAR1	psi-mi:“MI:0915”(physical association)	0.400
RAMP3	TAAR1	psi-mi:“MI:0915”(physical association)	0.400
TAAR1	RAMP3	psi-mi:“MI:0915”(physical association)	0.400
GRIK1	TAAR1	psi-mi:“MI:0915”(physical association)	0.370
PCMT1	TAAR1	psi-mi:“MI:0915”(physical association)	0.370
RNASEK	TAAR1	psi-mi:“MI:0915”(physical association)	0.370
SVOP	TAAR1	psi-mi:“MI:0915”(physical association)	0.370

BioGRID (6): TAAR1 (Affinity Capture-MS), GRIK1 (Two-hybrid), PCMT1 (Two-hybrid), RNASEK (Two-hybrid), SVOP (Two-hybrid), TAAR1 (Protein-RNA)

ESM2 similar proteins: A6NMU1, B3DH96, O01608, O13076, O17819, O17820, O97504, P32244, P32245, P33032, P34974, P35345, P37289, P41149, P41968, P43118, P52592, P54127, P61793, P61794, P70115, Q01718, Q0Z8I9, Q28031, Q28905, Q5QD16, Q5QD17, Q5QD24, Q5QD25, Q5QD29, Q5QNP2, Q64326, Q6W049, Q8HXX3, Q8HYN8, Q8HZ64, Q8K5E0, Q923Y7, Q92633, Q96RJ0

Diamond homologs: A0A678XMK4, O02662, O02666, O14804, O19091, O42574, O70528, O77680, O77700, P07700, P11617, P17124, P18089, P21728, P23944, P25021, P25100, P25102, P25115, P28221, P28565, P35405, P35406, P42289, P42290, P42291, P43141, P46626, P47747, P47800, P49145, P50406, P53452, P53454, P60021, P61752, P79400, P97288, P97292, P97714

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	45
Likely benign	2
Benign	3

Top pathogenic / likely-pathogenic (0)

SpliceAI

297 predictions. Top by Δscore:

Variant	Effect	Δscore
6:132645464:T:TA	donor_gain	0.9200
6:132645654:A:C	acceptor_gain	0.8000
6:132645367:TT:T	acceptor_gain	0.7800
6:132645654:A:AC	acceptor_gain	0.7500
6:132645365:TATT:T	acceptor_gain	0.7400
6:132645647:A:T	acceptor_gain	0.6800
6:132645346:GTTCT:G	acceptor_gain	0.6600
6:132645347:TTCTT:T	acceptor_gain	0.6600
6:132645348:TCTTT:T	acceptor_gain	0.6600
6:132645460:A:AT	donor_gain	0.6500
6:132645646:CAA:C	acceptor_gain	0.6500
6:132645369:C:CC	acceptor_gain	0.6400
6:132645601:T:C	donor_gain	0.6100
6:132645364:ATATT:A	acceptor_gain	0.6000
6:132645367:TTCT:T	acceptor_loss	0.6000
6:132645368:TC:T	acceptor_loss	0.6000
6:132645369:CTGT:C	acceptor_loss	0.6000
6:132645370:T:C	acceptor_loss	0.6000
6:132645648:A:C	acceptor_gain	0.5900
6:132645374:A:AC	acceptor_gain	0.5800
6:132645648:A:AC	acceptor_gain	0.5800
6:132645643:G:T	acceptor_gain	0.5700
6:132645371:G:C	acceptor_loss	0.5500
6:132645429:ACC:A	donor_gain	0.5500
6:132645430:CCC:C	donor_gain	0.5500
6:132645535:CAAA:C	acceptor_gain	0.5400
6:132645076:A:T	acceptor_gain	0.5300
6:132645366:ATT:A	acceptor_gain	0.5200
6:132645372:TAA:T	acceptor_gain	0.5200
6:132645534:CCAAA:C	acceptor_gain	0.5200

AlphaMissense

2277 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
6:132645642:C:G	R121P	0.981
6:132645224:G:C	F260L	0.980
6:132645224:G:T	F260L	0.980
6:132645226:A:G	F260L	0.980
6:132645701:G:C	S101R	0.979
6:132645701:G:T	S101R	0.979
6:132645703:T:G	S101R	0.979
6:132645562:A:G	W148R	0.974
6:132645562:A:T	W148R	0.974
6:132645563:A:C	S147R	0.971
6:132645563:A:T	S147R	0.971
6:132645565:T:G	S147R	0.971
6:132645717:C:G	C96S	0.968
6:132645718:A:T	C96S	0.968
6:132645851:G:C	F51L	0.967
6:132645851:G:T	F51L	0.967
6:132645853:A:G	F51L	0.967
6:132645737:C:A	W89C	0.962
6:132645737:C:G	W89C	0.962
6:132645402:A:T	I201K	0.956
6:132645211:A:G	C265R	0.955
6:132645739:A:G	W89R	0.954
6:132645739:A:T	W89R	0.954
6:132645407:A:C	F199L	0.952
6:132645407:A:T	F199L	0.952
6:132645409:A:G	F199L	0.952
6:132645071:A:C	F311L	0.951
6:132645071:A:T	F311L	0.951
6:132645073:A:G	F311L	0.951
6:132645634:C:G	A124P	0.951

dbSNP variants (sampled 300 via entrez): RS1000128587 (6:132654716 C>T), RS1000285386 (6:132651044 C>T), RS1000398616 (6:132644197 G>A), RS1000422347 (6:132650754 C>G,T), RS1000500904 (6:132654937 G>A), RS1000698297 (6:132656152 A>G), RS1000951954 (6:132646433 G>A), RS1000953930 (6:132648205 T>C), RS1001365851 (6:132642998 G>T), RS1001487058 (6:132660823 C>T), RS1001516737 (6:132661076 A>G), RS1001538435 (6:132653629 T>C), RS1001903959 (6:132647058 G>A), RS1002013030 (6:132657884 T>A), RS1002051856 (6:132652545 T>C)

Disease associations

OMIM: gene MIM:609333 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

1 associations (top):

Study	Trait	p-value
GCST009819_2	Compulsion score in obsessive compulsive disorder	4.000000e-06

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0007802	obsessive-compulsive symptom measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5857 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

20 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 611,266 (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
CHEMBL1026	FENOLDOPAM MESYLATE	4	2,560
CHEMBL1200413	TETRAHYDROZOLINE HYDROCHLORIDE	4	4,907
CHEMBL1200705	HYDROXYAMPHETAMINE HYDROBROMIDE	4	330
CHEMBL1201201	METHAMPHETAMINE	4	28,681
CHEMBL1574	PHENTERMINE	4	25,781
CHEMBL1689	TOLAZOLINE HYDROCHLORIDE	4	1,330
CHEMBL1706	NAPHAZOLINE HYDROCHLORIDE	4	3,736
CHEMBL19393	LEVAMFETAMINE	4	2,668
CHEMBL420	GUANABENZ	4	16,459
CHEMBL59	DOPAMINE	4	217,028
CHEMBL612	DEXTROAMPHETAMINE	4	72,138
CHEMBL770	TOLAZOLINE	4	10,239
CHEMBL11608	TYRAMINE	3	38,171
CHEMBL1256819	ANTAZOLINE HYDROCHLORIDE	3	71
CHEMBL39	SEROTONIN	3	186,160
CHEMBL4650337	ULOTARONT	3	118
CHEMBL1395071	FORMETOREX	2	92
CHEMBL1927030	LEVMETAMFETAMINE	2	737
CHEMBL2104690	AZAQUINZOLE	2	17
CHEMBL4594376	RALMITARONT	2	43

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Trace amine receptor

Most potent curated ligand interactions (13 total), top 13:

Ligand	Action	Affinity	Parameter
[3H]tyramine	Full agonist	7.7	pKd
RO5166017	Full agonist	7.3	pEC50
ralmitaront	Agonist	7.23	pEC50
β-phenylethylamine	Full agonist	7.0	pEC50
3-iodothyronamine	Full agonist	7.0	pEC50
2-phenyl-propylamine	Agonist	6.98	pEC50
dexamfetamine	Full agonist	6.9	pEC50
ulotaront	Agonist	6.85	pIC50
tyramine	Full agonist	6.7	pEC50
R(-)amphetamine	Full agonist	6.6	pEC50
octopamine	Full agonist	5.8	pEC50
EPPTB	Inverse agonist	5.1	pIC50
ractopamine	Agonist	4.8	pEC50

Binding affinities (BindingDB)

6 measured of 8 human assays (10 total across all organisms); most potent 6 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
1-(8-chloro-10,11-dihydrodibenzo[b,f]thiepin-10-yl)-4-methylpiperazine	KI	1.8 nM
NSC_6054	KI	8 nM
5-ethyl-4-methyl-N-[4-[(2S)-morpholin-2-yl]phenyl]pyrazolidine-3-carboxamide	EC50	58.5 nM	US-10508107
4-methyl-N-[4-[(2S)-morpholin-2-yl]phenyl]-5-phenylpyrazolidine-3-carboxamide	EC50	109 nM	US-10508107
5-ethyl-4-methyl-N-[4-[(2R)-morpholin-2-yl]phenyl]pyrazolidine-3-carboxamide	EC50	263 nM	US-10508107
cid_65340	KI	8250 nM

ChEMBL bioactivities

990 potent at pChembl≥5 of 1145 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.93	EC50	1.17	nM	CHEMBL4301324
8.70	Ki	2	nM	CHEMBL2206385
8.70	Ki	2	nM	CHEMBL2206400
8.46	EC50	3.5	nM	CHEMBL5082760
8.40	Ki	4	nM	CHEMBL2206377
8.40	Ki	4	nM	CHEMBL2206376
8.40	Ki	4	nM	CHEMBL2206890
8.34	EC50	4.6	nM	CHEMBL2206890
8.30	Ki	5	nM	CHEMBL2206381
8.26	EC50	5.5	nM	CHEMBL6189796
8.22	Ki	6	nM	CHEMBL2206375
8.21	EC50	6.1	nM	CHEMBL6190548
8.17	EC50	6.8	nM	CHEMBL2206404
8.11	EC50	7.8	nM	CHEMBL6191655
8.08	EC50	8.3	nM	CHEMBL252803
8.05	EC50	9	nM	CHEMBL3652684
8.02	EC50	9.46	nM	CHEMBL5561710
8.01	EC50	9.85	nM	CHEMBL476516
7.96	Ki	11	nM	CHEMBL2206384
7.96	Ki	11	nM	CHEMBL2206402
7.96	EC50	11	nM	CHEMBL3781675
7.95	EC50	11.3	nM	CHEMBL5561108
7.92	Ki	12	nM	CHEMBL2206388
7.92	Ki	12	nM	CHEMBL2206379
7.92	Ki	12	nM	CHEMBL2206408
7.92	EC50	12	nM	CHEMBL3684915
7.89	Ki	13	nM	CHEMBL2206380
7.85	EC50	14.12	nM	CHEMBL5549988
7.83	EC50	14.8	nM	CHEMBL6190548
7.82	EC50	15	nM	CHEMBL3780993
7.82	EC50	15	nM	PHENETHYLAMINE
7.79	EC50	16.3	nM	ULOTARONT
7.77	EC50	17	nM	CHEMBL3781694
7.75	Ki	18	nM	CHEMBL2206378
7.75	EC50	18	nM	CHEMBL3684834
7.75	EC50	18	nM	CHEMBL3684869
7.70	Ki	20	nM	CHEMBL494421
7.68	EC50	21	nM	CHEMBL3684805
7.68	EC50	21.08	nM	ULOTARONT
7.66	Ki	22	nM	CHEMBL2206404
7.66	EC50	22	nM	CHEMBL6173723
7.64	EC50	23	nM	CHEMBL2206375
7.64	EC50	23	nM	CHEMBL3680116
7.63	EC50	23.4	nM	CHEMBL5564712
7.62	Ki	24	nM	CHEMBL2206397
7.62	EC50	23.95	nM	CHEMBL1732597
7.60	EC50	25	nM	CHEMBL4555465
7.58	EC50	26	nM	CHEMBL3684912
7.57	EC50	27	nM	CHEMBL3680146
7.57	EC50	27	nM	CHEMBL3781589

PubChem BioAssay actives

228 with measured affinity, of 627 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-[4-(3-fluorophenyl)phenyl]ethanamine	2081067: Agonist activity at Gs-mediated TAAR1 activation (unknown origin) expressed in HEK293 cells pretreated with coelenterazine for 30 mins followed by compound addition by BRET assay	ec50	0.0012	uM
5-(2-phenylethyl)-1H-imidazole	714266: Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis	ki	0.0020	uM
3-chloro-N-ethyl-N-(1H-imidazol-5-ylmethyl)aniline	714266: Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis	ki	0.0020	uM
[(7S)-5,7-dihydro-4H-thieno[2,3-c]pyran-7-yl]methanamine	1813802: Agonist activity at recombinant human TAAR1 expressed in CHO-K1 cells assessed as increase in intracellular cAMP incubated for 30 mins by HTRF analysis	ec50	0.0035	uM
3,5-dichloro-N-(1H-imidazol-5-ylmethyl)-N-propan-2-ylaniline	714266: Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis	ki	0.0040	uM
3-chloro-N-(1H-imidazol-5-ylmethyl)-N-propan-2-ylaniline	714266: Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis	ki	0.0040	uM
3,4-dichloro-N-(1H-imidazol-5-ylmethyl)-N-propan-2-ylaniline	714266: Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis	ki	0.0040	uM
N-(1H-imidazol-5-ylmethyl)-3-methoxy-N-propan-2-ylaniline	714266: Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis	ki	0.0050	uM
4-chloro-N-(1H-imidazol-5-ylmethyl)-N-propan-2-ylaniline	714266: Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis	ki	0.0060	uM
N-(1H-imidazol-5-ylmethyl)-N-propan-2-ylaniline	714270: Agonist activity at human TAAR1 receptor expressed in HEK293 cells after 30 mins	ec50	0.0068	uM
2-thiophen-2-ylethanamine	1813802: Agonist activity at recombinant human TAAR1 expressed in CHO-K1 cells assessed as increase in intracellular cAMP incubated for 30 mins by HTRF analysis	ec50	0.0083	uM
(4S)-4-(2-phenoxyethyl)-4,5-dihydro-1,3-oxazol-2-amine	1288302: Agonist activity at human TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer	ec50	0.0090	uM
N,N-dimethyl-1-(4-phenylphenyl)methanamine	2081067: Agonist activity at Gs-mediated TAAR1 activation (unknown origin) expressed in HEK293 cells pretreated with coelenterazine for 30 mins followed by compound addition by BRET assay	ec50	0.0095	uM
2-(4-bromophenyl)ethanamine	2081067: Agonist activity at Gs-mediated TAAR1 activation (unknown origin) expressed in HEK293 cells pretreated with coelenterazine for 30 mins followed by compound addition by BRET assay	ec50	0.0098	uM
(4S)-4-(4-chloro-2-methylphenyl)-4,5-dihydro-1,3-oxazol-2-amine	1288302: Agonist activity at human TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer	ec50	0.0110	uM
N-(1H-imidazol-5-ylmethyl)-N-methylaniline	714266: Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis	ki	0.0110	uM
3-chloro-N-(1H-imidazol-5-ylmethyl)-N-methylaniline	714266: Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis	ki	0.0110	uM
4-(furan-2-yl)aniline	2081068: Agonist activity at Gq-mediated TAAR1 activation (unknown origin) expressed in HEK293 cells pretreated with coelenterazine for 30 mins followed by compound addition by BRET assay	ec50	0.0113	uM
1-(1H-imidazol-5-ylmethyl)-3,4-dihydro-2H-quinoline	714266: Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis	ki	0.0120	uM
(4S)-4-(4-chloro-2-cyclopropylphenyl)-4,5-dihydro-1,3-oxazol-2-amine	1288302: Agonist activity at human TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer	ec50	0.0120	uM
N-(1H-imidazol-5-ylmethyl)-6-methoxy-N-propan-2-ylpyridin-2-amine	714266: Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis	ki	0.0120	uM
3-fluoro-N-(1H-imidazol-5-ylmethyl)-N-propan-2-ylaniline	714266: Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis	ki	0.0120	uM
4-fluoro-N-(1H-imidazol-5-ylmethyl)-N-propan-2-ylaniline	714266: Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis	ki	0.0130	uM
1-[4-(3-chlorophenyl)phenyl]-N,N-dimethylmethanamine	2081068: Agonist activity at Gq-mediated TAAR1 activation (unknown origin) expressed in HEK293 cells pretreated with coelenterazine for 30 mins followed by compound addition by BRET assay	ec50	0.0141	uM
2-phenylethanamine	1813802: Agonist activity at recombinant human TAAR1 expressed in CHO-K1 cells assessed as increase in intracellular cAMP incubated for 30 mins by HTRF analysis	ec50	0.0150	uM
(3S)-5-chlorospiro[2,4-dihydro-1H-naphthalene-3,4’-5H-1,3-oxazole]-2’-amine	1288302: Agonist activity at human TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer	ec50	0.0150	uM
1-[(7S)-5,7-dihydro-4H-thieno[2,3-c]pyran-7-yl]-N-methylmethanamine	2081067: Agonist activity at Gs-mediated TAAR1 activation (unknown origin) expressed in HEK293 cells pretreated with coelenterazine for 30 mins followed by compound addition by BRET assay	ec50	0.0163	uM
(4S)-4-(3-fluoro-2-methylphenyl)-4,5-dihydro-1,3-oxazol-2-amine	1288302: Agonist activity at human TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer	ec50	0.0170	uM
(4S)-4-[2-(3-chlorophenyl)ethyl]-4,5-dihydro-1,3-oxazol-2-amine	1288302: Agonist activity at human TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer	ec50	0.0180	uM
(4S)-4-[(2S)-2-phenylbutyl]-4,5-dihydro-1,3-oxazol-2-amine	1288302: Agonist activity at human TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer	ec50	0.0180	uM
2-fluoro-N-(1H-imidazol-5-ylmethyl)-N-propan-2-ylaniline	714266: Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis	ki	0.0180	uM
5-benzyl-1H-imidazole	714266: Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis	ki	0.0200	uM
(4S)-4-(3-chlorophenyl)-4,5-dihydro-1,3-oxazol-2-amine	1288302: Agonist activity at human TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer	ec50	0.0210	uM
(4S)-4-(2-chlorophenyl)-4,5-dihydro-1,3-oxazol-2-amine	1288302: Agonist activity at human TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer	ec50	0.0230	uM
2-amino-N-[4-(furan-2-yl)phenyl]acetamide	2081067: Agonist activity at Gs-mediated TAAR1 activation (unknown origin) expressed in HEK293 cells pretreated with coelenterazine for 30 mins followed by compound addition by BRET assay	ec50	0.0234	uM
2-[(2,6-diethylphenyl)methyl]-1H-imidazole	714266: Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis	ki	0.0240	uM
2-thiophen-3-ylethanamine	1813802: Agonist activity at recombinant human TAAR1 expressed in CHO-K1 cells assessed as increase in intracellular cAMP incubated for 30 mins by HTRF analysis	ec50	0.0250	uM
(4S)-4-(4-chloro-2-ethylphenyl)-4,5-dihydro-1,3-oxazol-2-amine	1288302: Agonist activity at human TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer	ec50	0.0260	uM
(4S)-4-[(3-chloro-N-methylanilino)methyl]-4,5-dihydro-1,3-oxazol-2-amine	1288302: Agonist activity at human TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer	ec50	0.0270	uM
(4S)-4-(3-phenylpropyl)-4,5-dihydro-1,3-oxazol-2-amine	1288302: Agonist activity at human TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer	ec50	0.0270	uM
(4S)-4-(2-phenylethyl)-4,5-dihydro-1,3-oxazol-2-amine	1288302: Agonist activity at human TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer	ec50	0.0270	uM
4-(3-fluorophenyl)aniline	2081068: Agonist activity at Gq-mediated TAAR1 activation (unknown origin) expressed in HEK293 cells pretreated with coelenterazine for 30 mins followed by compound addition by BRET assay	ec50	0.0289	uM
(4S)-4-[(3-chloro-N-ethylanilino)methyl]-4,5-dihydro-1,3-oxazol-2-amine	1288302: Agonist activity at human TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer	ec50	0.0290	uM
(4S)-4-(3,4-dichlorophenyl)-4,5-dihydro-1,3-oxazol-2-amine	1288302: Agonist activity at human TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer	ec50	0.0310	uM
N-benzyl-N-(1H-imidazol-5-ylmethyl)aniline	714266: Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis	ki	0.0320	uM
N-tert-butyl-3-chloro-N-(1H-imidazol-5-ylmethyl)aniline	714266: Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis	ki	0.0330	uM
1-(1H-imidazol-5-ylmethyl)-2,3-dihydroindole	714266: Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis	ki	0.0350	uM
2-[(2,6-dimethylphenyl)methyl]-1H-imidazole	714266: Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis	ki	0.0360	uM
2-chloro-N-(1H-imidazol-5-ylmethyl)-N-propan-2-ylaniline	714266: Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis	ki	0.0400	uM
(2R)-2-amino-N-[4-(furan-2-yl)phenyl]propanamide	2081068: Agonist activity at Gq-mediated TAAR1 activation (unknown origin) expressed in HEK293 cells pretreated with coelenterazine for 30 mins followed by compound addition by BRET assay	ec50	0.0405	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
phenethylamine	increases activity, increases abundance, increases reaction	2
tryptamine	increases abundance, decreases reaction, increases activity, increases reaction	2
Octopamine	decreases reaction, increases activity, increases reaction, increases abundance	2
Tyramine	decreases reaction, increases activity, increases reaction, increases abundance	2
2-palmitoylglycerol	increases expression	1
indatraline	decreases reaction, increases activity, increases reaction	1
Cyclic AMP	increases abundance, increases activity	1
Desipramine	decreases reaction, increases activity, increases reaction	1
Dopamine	increases reaction, decreases reaction, increases activity	1
Methamphetamine	decreases reaction, increases activity, increases reaction	1
Methylphenidate	increases reaction, decreases reaction, increases activity	1
Norepinephrine	increases activity, increases reaction	1
Serotonin	increases activity, increases reaction	1
Citalopram	decreases reaction, increases activity, increases reaction	1

ChEMBL screening assays

75 unique, capped per target: 49 functional, 26 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1048859	Functional	Activation of human TAAR1 expressed in CHOK1 cells assessed as cAMP accumulation at 0.1 to 1 uM	Amiodarone and its putative metabolites fail to activate wild type hTAAR1. — Bioorg Med Chem Lett
CHEMBL1670082	Binding	Inhibition of human TAAR1	Selective antagonists of mouse trace amine-associated receptor 1 (mTAAR1): discovery of EPPTB (RO5212773). — Bioorg Med Chem Lett

Cellosaurus cell lines

1 cell lines: 1 spontaneously immortalized cell line

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

Cellosaurus	Name	Category	Sex
CVCL_KV85	cAMP Hunter CHO-K1 TAAR1 Gs	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

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