HTR2C

Summary

HTR2C (5-hydroxytryptamine receptor 2C, HGNC:5295) is a protein-coding gene on chromosome Xq23, encoding 5-hydroxytryptamine receptor 2C (P28335). G-protein coupled receptor for 5-hydroxytryptamine (serotonin).

This gene encodes a seven-transmembrane G-protein-coupled receptor. The encoded protein responds to signaling through the neurotransmitter serotonin. The mRNA of this gene is subject to multiple RNA editing events, where adenosine residues encoded by the genome are converted to inosines. RNA editing is predicted to alter the structure of the second intracellular loop, thereby generating alternate protein forms with decreased ability to interact with G proteins. Abnormalities in RNA editing of this gene have been detected in victims of suicide that suffer from depression. In addition, naturally-occuring variation in the promoter and 5’ non-coding and coding regions of this gene may show statistically-significant association with mental illness and behavioral disorders. Alternative splicing results in multiple different transcript variants.

Source: NCBI Gene 3358 — RefSeq curated summary.

At a glance

• Gene–disease (curated): obesity disorder (Strong, GenCC)
• Clinical variants (ClinVar): 147 total
• Druggable target: yes — 276 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_000868

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:5295
Approved symbol	HTR2C
Name	5-hydroxytryptamine receptor 2C
Location	Xq23
Locus type	gene with protein product
Status	Approved
Aliases	5-HT2C, 5HTR2C
Ensembl gene	ENSG00000147246
Ensembl biotype	protein_coding
OMIM	312861
Entrez	3358

Gene structure

Transcript identifiers

Ensembl transcripts: 4 — 4 protein_coding

ENST00000276198, ENST00000371950, ENST00000371951, ENST00000894573

RefSeq mRNA: 3 — MANE Select: NM_000868 NM_000868, NM_001256760, NM_001256761

CCDS: CCDS14564, CCDS59174

Canonical transcript exons

ENST00000276198 — 6 exons

Exon	Start	End
ENSE00000979310	114731294	114731607
ENSE00001095186	114848003	114848203
ENSE00001307811	114613815	114613881
ENSE00001319431	114726858	114726971
ENSE00003617968	114906589	114910061
ENSE00003844018	114584086	114584659

Expression profiles

Bgee: expression breadth broad, 79 present calls, max score 99.77.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.8535 / max 140.2218, expressed in 151 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
197318	0.8078	150
209788	0.0457	23

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
choroid plexus epithelium	UBERON:0003911	99.77	gold quality
lateral globus pallidus	UBERON:0002476	88.92	gold quality
superior vestibular nucleus	UBERON:0007227	88.82	gold quality
nucleus accumbens	UBERON:0001882	88.46	gold quality
caudate nucleus	UBERON:0001873	82.47	gold quality
middle frontal gyrus	UBERON:0002702	81.69	gold quality
hypothalamus	UBERON:0001898	81.27	gold quality
putamen	UBERON:0001874	80.59	gold quality
CA1 field of hippocampus	UBERON:0003881	78.46	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	77.83	gold quality
endothelial cell	CL:0000115	76.73	silver quality
substantia nigra pars compacta	UBERON:0001965	75.07	gold quality
medulla oblongata	UBERON:0001896	72.95	gold quality
dorsal motor nucleus of vagus nerve	UBERON:0002870	72.06	gold quality
entorhinal cortex	UBERON:0002728	71.21	gold quality
inferior olivary complex	UBERON:0002127	68.77	gold quality
Ammon’s horn	UBERON:0001954	68.72	gold quality
temporal lobe	UBERON:0001871	68.16	gold quality
amygdala	UBERON:0001876	67.88	gold quality
telencephalon	UBERON:0001893	67.25	gold quality
substantia nigra	UBERON:0002038	65.85	gold quality
prefrontal cortex	UBERON:0000451	65.46	gold quality
forebrain	UBERON:0001890	65.18	gold quality
midbrain	UBERON:0001891	65.00	gold quality
ventral tegmental area	UBERON:0002691	64.90	gold quality
cerebellar vermis	UBERON:0004720	64.77	gold quality
Brodmann (1909) area 46	UBERON:0006483	63.79	silver quality
orbitofrontal cortex	UBERON:0004167	63.63	silver quality
cingulate cortex	UBERON:0003027	62.81	gold quality
substantia nigra pars reticulata	UBERON:0001966	62.69	gold quality

Single-cell (SCXA)

Detected in 5 experiment(s), a significant marker in 5.

Experiment	Marker?	Max mean expression
E-HCAD-30	yes	1624.59
E-HCAD-35	yes	1504.53
E-HCAD-5	yes	571.27
E-HCAD-25	yes	9.92
E-ANND-3	yes	3.26

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): MBD1, RUNX1, SPI1, TBXT, ZNF699

miRNA regulators (miRDB)

204 targeting HTR2C, 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-4476	100.00	68.18	2030
HSA-MIR-6876-5P	100.00	67.68	2126
HSA-MIR-4533	100.00	69.48	2758
HSA-MIR-1252-5P	100.00	69.80	2774
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-4668-3P	100.00	68.74	2635
HSA-MIR-6758-5P	100.00	66.21	1470
HSA-MIR-5692B	100.00	71.32	2622
HSA-MIR-5692C	100.00	71.32	2622
HSA-MIR-513B-5P	99.99	69.96	2150
HSA-MIR-34A-5P	99.99	71.21	1784
HSA-MIR-449A	99.99	71.05	1776
HSA-MIR-548AW	99.99	72.57	3559
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-4715-3P	99.98	66.03	670
HSA-MIR-302C-5P	99.97	72.56	3642
HSA-MIR-34C-5P	99.97	70.45	1577
HSA-MIR-449B-5P	99.97	70.26	1580
HSA-MIR-3688-3P	99.97	72.02	2834
HSA-MIR-570-3P	99.96	72.41	4910
HSA-MIR-5688	99.96	73.23	4504
HSA-MIR-3658	99.96	73.87	4379
HSA-MIR-495-3P	99.96	72.81	4197
HSA-MIR-23A-3P	99.95	74.24	3163
HSA-MIR-23B-3P	99.95	74.24	3163
HSA-MIR-23C	99.95	73.92	3192
HSA-MIR-559	99.95	72.28	3609
HSA-MIR-548AB	99.95	71.31	3488
HSA-MIR-651-3P	99.94	73.48	5177
HSA-MIR-548A-5P	99.94	71.27	3482

Literature-anchored findings (GeneRIF, showing 40)

• results indicate significantly different 5-HT2C pre-mRNA editing site preferences in brains of suicide victims (PMID:11988167)
• The 5-HT2C receptor subtype polymorphism Cys23Ser is involved in the regulation of food intake in teen-aged women. (PMID:12007749)
• Evolutionary conserved microsatellites in the promoter region of the 5-hydroxytryptamine receptor 2C gene (HTR2C) are not associated with bipolar disorder in females. (PMID:12111480)
• role of helix 7 tyrosine in 5HT2c conformation (PMID:12145300)
• the 5-HT(2C) receptor polymorphism contributes little to the variation of neuroendocrinological responses elicited by activation of the hypothalamic-pituitary axis (PMID:12518270)
• An association was found between the presence of major depressive illness in Alzheimer’s disease and both the 5-HT2A and 5-HT2C polymorphisms. (PMID:12707936)
• Expression in cultured skin cells. (PMID:12767050)
• The findings are consistent a role for the Ser23 allele of 5-HT2c in mediating susceptibility to and increasing severity of anorexia nervosa. (PMID:12858032)
• Study results do not support a significant contribution of the 5-HT2c Cys23Ser polymorphism and 5-HTT promoter genotype to a putative common genetic predisposition of attention-deficit hyperactivity disorder and alcohol dependence. (PMID:14574222)
• the constitutively active 5-HT2cR isoforms are spontaneously internalized in an agonist-independent manner, directly correlated with the constitutive activity status of the RNA edited receptor variants (PMID:14602721)
• 5-HT(2C) receptor displayed considerable constitutive activity, with the Ser23 allele being significantly higher in this regard than the Cys23 form. (PMID:14699441)
• RNA editing represents a novel mechanism for regulating 5-HT2C receptor signaling to pathways linked to actin cytoskeletal organization and regulated exocytosis. (PMID:14722258)
• 5-HT2C receptor promoter polymorphism is associated with obesity (PMID:15048662)
• 5HTR2c Cys23Ser polymorphism may be associated with migraine with aura in a Japanese population. (PMID:15147464)
• Higher distribution of the -759T allele of the 5HT2C receptor in normal controls compared with in patients with schizophrenia. (PMID:15167695)
• Involvement of the -759C/T polymorphism of the 5-HT2CR in clozapine-induced weight gain in German patients with schizophrenia. (PMID:15318026)
• Mutations in 5HT2c are unlikely to be a common cause of severe early-onset human obesity. (PMID:15381968)
• 5-HT2C receptors exist as constitutive homodimers expressed on the plasma membrane of live HEK293 cells. (PMID:15518545)
• (+/-)-1-(2,5-Dimethoxy-4-iodophenyl)-2-aminopropane hydrochloride (DOI), significantly increased arachidonic acid incorporation in widespread brain areas containing 5-HT2A/2C receptors. (PMID:15562295)
• coupling of the 5-HT(2C)R to the extracellular signal-regulated kinases (ERKs) (PMID:15935077)
• The genetic polymorphisms of 5-HT2c receptor at which many of the newer antipsychotic drugs act, are prime candidates for pharmacogenetic analysis of the effects of these drugs in the treatment of schizophrenia. (PMID:15953671)
• Our results complement previous studies of HTR2C in both mice and humans, and suggest the importance of genetic variation and elucidating the fine LD structure in uncovering the genetic factors of obesity. (PMID:16021472)
• dimerization is essential for 5-HT receptor function (PMID:16195233)
• Genotypes and allele frequencies of 102T/C polymorphism of the HTR2A and 796G/C polymorphism of the HTR2C did not differ between controls and patients with obstructive sleep apnea. (PMID:16258205)
• Paradoxical actions of 5-HT2C antagonists and agonists can be reconciled and discusses both established and innovative strategies for the exploitation of 5-HT2C receptors in the improved management of depressed and anxious states. (PMID:16433010)
• analysis of serotonin 5-HT2C receptor homodimer biogenesis in the endoplasmic reticulum (PMID:16857671)
• This indicates that, overall, interaction of 5-HT(2C) receptors with PDZ proteins inhibits receptor desensitization in cortical neurons. (PMID:16914526)
• HTR2C polymorphisms were significantly associated with an increased of obesity as a result of antipsychotic use. (PMID:17016522)
• Significant differences in 5HT2CA1 allele and genotype frequencies were found between Amerindian and European populations in South America. (PMID:17039480)
• This study detected significant evidence of association between the -995A/-759T/-697C/Cys23 haplotype of the 5HT2C gene in anxious, depression and bulimia nervosa. (PMID:17055531)
• This review and extension of previous data presents support for the role of 5HT(2c) in the development of certain symptoms, although the effect size may be small. (PMID:17098333)
• HTR2C and HTR1A gene variants are not major contributors to suicide-, anger-, or aggression-related behaviors. (PMID:17192951)
• These results support the involvement of the -759C/T polymorphism of the 5-HT2C receptor gene in antipsychotics-induced weight gain in the Korean population. (PMID:17275977)
• meta-analysis provides support for the association of HTR2C in weight gain but indicates that firmly establishing the role of pharmacogenetics in clinical psychiatry requires much larger sample sizes that have been hitherto reported. (PMID:17291373)
• Flexible molecular docking, and long-time molecular dynamics (MD) simulations, was employed to construct the structure of the human 5-HT(2C) receptor and determine the characteristics of binding modes of 5-HT(2C) receptor agonists (PMID:17558446)
• Human serum albumin-advanced glycation end products stimulate phosphatidylserine externalization in platelets via 5-HT 2A/2C receptors. (PMID:17625040)
• findings suggest that HTR2C genotypes are associated with antincreased risk of metabolic syndrome in psychiatric patients taking antipsychotics (PMID:17632216)
• The association between polymorphisms in serotonergic genes (SERT and 5-HT2A, 5-HT2C) suggests that these genetic factors can modulate vulnerability to puerperal psychosis in female bipolar participants (PMID:17728663)
• HTR2C (cys23ser) polymorphism influences early onset in bipolar patients in European. (PMID:17767148)
• Patients with Schizophrenia or bipolar disorder , overexpression of the Val156-Ser158-Val160 isoform in the prefrontal cortex may represent an additional risk factor for suicidal behavior. (PMID:17848916)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	htr2cl2	ENSDARG00000013210
danio_rerio	htr2cl1	ENSDARG00000018228
mus_musculus	Htr2c	ENSMUSG00000041380
drosophila_melanogaster	5-HT2A	FBGN0087012
caenorhabditis_elegans		WBGENE00021897

Paralogs (8): HTR2A (ENSG00000102468), HTR1B (ENSG00000135312), HTR2B (ENSG00000135914), HTR7 (ENSG00000148680), HTR5A (ENSG00000157219), HTR6 (ENSG00000158748), HTR1E (ENSG00000168830), HTR1F (ENSG00000179097)

Protein

Protein identifiers

5-hydroxytryptamine receptor 2C — P28335 (reviewed: P28335)

Alternative names: 5-hydroxytryptamine receptor 1C, Serotonin receptor 2C

All UniProt accessions (1): P28335

UniProt curated annotations — full annotation on UniProt →

Function. G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors. HTR2C 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 that modulate the activity of phosphatidylinositol 3-kinase and promote the release of Ca(2+) ions from intracellular stores, respectively. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Regulates neuronal activity via the activation of short transient receptor potential calcium channels in the brain, and thereby modulates the activation of pro-opiomelanocortin neurons and the release of CRH that then regulates the release of corticosterone. Plays a role in the regulation of appetite and eating behavior, responses to anxiogenic stimuli and stress. Plays a role in insulin sensitivity and glucose homeostasis.

Subunit / interactions. Interacts with MPDZ. Interacts with ARRB2. Interacts with MPP3; this interaction stabilizes the receptor at the plasma membrane and prevents the desensitization of the HTR2C receptor-mediated calcium response.

Subcellular location. Cell membrane.

Tissue specificity. Detected in brain.

Post-translational modifications. N-glycosylated.

Activity regulation. Inhibited by inverse agonist ritanserin.

Domain organisation. The PDZ domain-binding motif is involved in the interaction with MPDZ.

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

Isoforms (2)

UniProt ID	Names	Canonical?
P28335-1	1	yes
P28335-2	2

RefSeq proteins (3): NP_000859, NP_001243689, NP_001243690 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000377	5HT2C_rcpt	Family
IPR002231	5HT_rcpt	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (63 total): helix 15, mutagenesis site 10, topological domain 8, transmembrane region 7, sequence variant 4, short sequence motif 3, turn 3, binding site 2, glycosylation site 2, disulfide bond 2, strand 2, signal peptide 1, chain 1, region of interest 1, compositionally biased region 1, splice variant 1

Structure

Experimental structures (PDB)

8 structures.

PDB	Method	Resolution (Å)
9UGL	ELECTRON MICROSCOPY	2.65
6BQH	X-RAY DIFFRACTION	2.7
8DPF	ELECTRON MICROSCOPY	2.84
6BQG	X-RAY DIFFRACTION	3
8DPH	ELECTRON MICROSCOPY	3.2
8DPI	ELECTRON MICROSCOPY	3.4
8DPG	ELECTRON MICROSCOPY	3.6
8ZMF	X-RAY DIFFRACTION	3.6

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P28335-F1	73.71	0.47

Antibody-complex structures (SAbDab): 4 — 8DPF, 8DPG, 8DPH, 8DPI

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 (2): 139; 209

Disulfide bonds (2): 127–207, 337–341

Glycosylation sites (2): 39, 204

Mutagenesis-validated functional residues (10):

Position	Phenotype
159	decreases interaction with arrb2.
218	decreased binding to inverse agonist ritanserin.
223	decreased binding to inverse agonist ritanserin.
320	decreased binding to inverse agonist ritanserin.
324	decreased binding to inverse agonist ritanserin.
354	decreased binding to inverse agonist ritanserin.
456	loss of interaction with mpdz.
456	no effect on interaction with mpdz.
457	no effect on interaction with mpdz.
458	loss of interaction with mpdz.

Function

Pathways and Gene Ontology

Reactome pathways

8 pathways

ID	Pathway
R-HSA-390666	Serotonin receptors
R-HSA-416476	G alpha (q) signalling events
R-HSA-162582	Signal Transduction
R-HSA-372790	Signaling by GPCR
R-HSA-373076	Class A/1 (Rhodopsin-like receptors)
R-HSA-375280	Amine ligand-binding receptors
R-HSA-388396	GPCR downstream signalling
R-HSA-500792	GPCR ligand binding

MSigDB gene sets: 338 (showing top): GOBP_RESPONSE_TO_NITROGEN_COMPOUND, LEE_NEURAL_CREST_STEM_CELL_DN, GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, GOBP_REGULATION_OF_FAT_CELL_DIFFERENTIATION, GOMF_G_PROTEIN_COUPLED_SEROTONIN_RECEPTOR_ACTIVITY, BENPORATH_ES_WITH_H3K27ME3, GOBP_PHOSPHATIDYLINOSITOL_METABOLIC_PROCESS, GOBP_BEHAVIOR, GOBP_REGULATION_OF_CALCIUM_MEDIATED_SIGNALING, TGCTGCT_MIR15A_MIR16_MIR15B_MIR195_MIR424_MIR497, NKX25_02, GCANCTGNY_MYOD_Q6, GOBP_POSITIVE_REGULATION_OF_FAT_CELL_DIFFERENTIATION, GTCTACC_MIR379, GOBP_POSITIVE_REGULATION_OF_MAPK_CASCADE

GO Biological Process (21): behavioral fear response (GO:0001662), intracellular calcium ion homeostasis (GO:0006874), G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger (GO:0007187), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), phospholipase C-activating serotonin receptor signaling pathway (GO:0007208), serotonin receptor signaling pathway (GO:0007210), chemical synaptic transmission (GO:0007268), locomotory behavior (GO:0007626), feeding behavior (GO:0007631), positive regulation of phosphatidylinositol biosynthetic process (GO:0010513), obsolete cGMP-mediated signaling (GO:0019934), regulation of nervous system process (GO:0031644), regulation of appetite (GO:0032098), regulation of corticotropin-releasing hormone secretion (GO:0043397), positive regulation of fat cell differentiation (GO:0045600), positive regulation of calcium-mediated signaling (GO:0050850), release of sequestered calcium ion into cytosol (GO:0051209), positive regulation of ERK1 and ERK2 cascade (GO:0070374), G protein-coupled serotonin receptor signaling pathway (GO:0098664), signal transduction (GO:0007165), G protein-coupled receptor signaling pathway (GO:0007186)

GO Molecular Function (9): Gq/11-coupled serotonin receptor activity (GO:0001587), G protein-coupled serotonin receptor activity (GO:0004993), neurotransmitter receptor activity (GO:0030594), identical protein binding (GO:0042802), serotonin binding (GO:0051378), 1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding (GO:0071886), serotonin receptor activity (GO:0099589), G protein-coupled receptor activity (GO:0004930), protein binding (GO:0005515)

GO Cellular Component (5): plasma membrane (GO:0005886), dendrite (GO:0030425), synapse (GO:0045202), G protein-coupled serotonin receptor complex (GO:0098666), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-6 pathways:

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

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
G protein-coupled receptor signaling pathway	4
G protein-coupled serotonin receptor signaling pathway	2
behavior	2
G protein-coupled serotonin receptor activity	2
amine binding	2
transmembrane signaling receptor activity	2
behavioral defense response	1
fear response	1
intracellular monoatomic cation homeostasis	1
calcium ion homeostasis	1
phospholipase C activator activity	1
Gq/11-coupled serotonin receptor activity	1
phospholipase C-activating G protein-coupled receptor signaling pathway	1
signal transduction	1
serotonin receptor activity	1
cellular response to dopamine	1
anterograde trans-synaptic signaling	1
phosphatidylinositol biosynthetic process	1
positive regulation of biosynthetic process	1
regulation of phosphatidylinositol biosynthetic process	1
positive regulation of phosphorus metabolic process	1
regulation of system process	1
nervous system process	1
response to nutrient levels	1
regulation of biological quality	1
corticotropin-releasing hormone secretion	1
regulation of peptide hormone secretion	1
fat cell differentiation	1
positive regulation of cell differentiation	1
regulation of fat cell differentiation	1
calcium-mediated signaling	1
regulation of calcium-mediated signaling	1
positive regulation of intracellular signal transduction	1
intercellular transport	1
calcium ion transmembrane import into cytosol	1
positive regulation of MAPK cascade	1
ERK1 and ERK2 cascade	1
regulation of ERK1 and ERK2 cascade	1
cell communication	1
cellular process	1

Protein interactions and networks

STRING

1888 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
HTR2C	GNAQ	P50148	952
HTR2C	SLC6A4	P31645	915
HTR2C	TPH1	P17752	844
HTR2C	HTR2A	P28223	817
HTR2C	MAOB	P27338	796
HTR2C	HTR3A	P46098	796
HTR2C	TPH2	Q8IWU9	752
HTR2C	POMC	P01189	731
HTR2C	HTR2B	P41595	700
HTR2C	MAOA	P21397	684
HTR2C	ARRB1	P49407	655
HTR2C	ARRB2	P32121	648
HTR2C	SLC6A2	P23975	625
HTR2C	SLC6A3	Q01959	622
HTR2C	HTR3B	O95264	619

IntAct

207 interactions, top by confidence:

A	B	Type	Score
HTR2C	HTR2C	psi-mi:“MI:2364”(proximity)	0.820
HTR2C	HTR2C	psi-mi:“MI:0915”(physical association)	0.820
HTR2C	HTR2C	psi-mi:“MI:0403”(colocalization)	0.820
HTR2C	TMEM147	psi-mi:“MI:0915”(physical association)	0.740
HTR2C	MPDZ	psi-mi:“MI:0407”(direct interaction)	0.650
SCRIB	HTR2C	psi-mi:“MI:0407”(direct interaction)	0.620
DLG1	HTR2C	psi-mi:“MI:0407”(direct interaction)	0.620
HTR2C	DLG1	psi-mi:“MI:0407”(direct interaction)	0.620
HTR2C	SCRIB	psi-mi:“MI:0407”(direct interaction)	0.620
HTR2C	HTR2A	psi-mi:“MI:2364”(proximity)	0.610
HTR2A	HTR2C	psi-mi:“MI:2364”(proximity)	0.610
HTR2A	HTR2C	psi-mi:“MI:0915”(physical association)	0.610
LIN7C	HTR2C	psi-mi:“MI:0915”(physical association)	0.590
HTR2C	LIN7C	psi-mi:“MI:0407”(direct interaction)	0.590
HTR2C	TMBIM6	psi-mi:“MI:0915”(physical association)	0.560
CNIH1	HTR2C	psi-mi:“MI:0915”(physical association)	0.560
HTR2C	SLC39A9	psi-mi:“MI:0915”(physical association)	0.560

BioGRID (199): MPDZ (Two-hybrid), MPDZ (Two-hybrid), TAPBP (Affinity Capture-MS), FAM134A (Affinity Capture-MS), KLRG2 (Affinity Capture-MS), CERS5 (Affinity Capture-MS), SLC35F1 (Affinity Capture-MS), FAM210B (Affinity Capture-MS), UBE2Q1 (Affinity Capture-MS), C6orf47 (Affinity Capture-MS), HMOX2 (Affinity Capture-MS), ITPRIPL1 (Affinity Capture-MS), FAM134C (Affinity Capture-MS), GPR50 (Affinity Capture-MS), LPCAT3 (Affinity Capture-MS)

ESM2 similar proteins: A0A2R9YJI3, B2ZHY2, B3DM66, B4XF06, D4A3U0, O02777, O43194, O46635, P08909, P08911, P0C0W8, P14842, P18599, P20272, P21554, P28223, P28335, P32240, P34311, P34968, P35363, P47746, P50128, P50129, P56971, P70259, Q09502, Q333S9, Q5IS53, Q5IS66, Q5IS73, Q5IS98, Q5R4Q6, Q5U431, Q60F97, Q6DWJ6, Q71SP5, Q75Z89, Q801M1, Q80UC8

Diamond homologs: E7EM37, G3M4F8, O02213, O08890, O18935, O19014, O19025, O42384, O42385, O73810, O77715, O77723, O77830, P08908, P08909, P08913, P11614, P14416, P18825, P18871, P19020, P20288, P21917, P22086, P22270, P22909, P24628, P28221, P28222, P28334, P28335, P28564, P28566, P30545, P30728, P30729, P30939, P32304, P32305, P34968

SIGNOR signaling

11 interactions.

A	Effect	B	Mechanism
agomelatine	down-regulates	HTR2C	“chemical inhibition”
HTR2C	“up-regulates activity”	GNAI1	binding
HTR2C	“up-regulates activity”	GNAI3	binding
HTR2C	“up-regulates activity”	GNAO1	binding
HTR2C	“up-regulates activity”	GNAZ	binding
HTR2C	“up-regulates activity”	GNAQ	binding
HTR2C	“up-regulates activity”	GNA14	binding
HTR2C	“up-regulates activity”	GNA15	binding
HTR2C	“up-regulates activity”	GNA12	binding
serotonin(1+)	“up-regulates activity”	HTR2C	“chemical activation”
serotonin	“up-regulates activity”	HTR2C	“chemical activation”

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 116 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
Ras activation upon Ca2+ influx through NMDA receptor	5	39.1×	1e-05
Unblocking of NMDA receptors, glutamate binding and activation	5	37.2×	1e-05
Negative regulation of NMDA receptor-mediated neuronal transmission	5	37.2×	1e-05
Long-term potentiation	5	32.6×	2e-05
Assembly and cell surface presentation of NMDA receptors	8	27.8×	5e-08
Neurexins and neuroligins	9	24.3×	3e-08
Protein-protein interactions at synapses	5	18.2×	3e-04
RHOQ GTPase cycle	5	12.4×	1e-03

GO biological processes:

GO term	Partners	Fold	FDR
establishment or maintenance of epithelial cell apical/basal polarity	10	52.8×	1e-12
protein localization to synapse	6	41.8×	1e-06
receptor clustering	7	39.7×	1e-07
regulation of postsynaptic membrane neurotransmitter receptor levels	6	27.0×	1e-05
bicellular tight junction assembly	6	18.0×	7e-05
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	5	14.2×	1e-03
cell-cell adhesion	10	9.2×	1e-05
protein-containing complex assembly	8	8.3×	4e-04

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	74
Likely benign	38
Benign	5

Top pathogenic / likely-pathogenic (0)

SpliceAI

2717 predictions. Top by Δscore:

Variant	Effect	Δscore
X:114586462:GC:G	acceptor_gain	1.0000
X:114612861:A:T	donor_gain	1.0000
X:114613877:CAACT:C	donor_gain	1.0000
X:114613878:AACT:A	donor_gain	1.0000
X:114613879:ACT:A	donor_gain	1.0000
X:114613880:CT:C	donor_gain	1.0000
X:114613882:G:GG	donor_gain	1.0000
X:114715375:TTATA:T	donor_gain	1.0000
X:114726856:A:AG	acceptor_gain	1.0000
X:114726857:G:GG	acceptor_gain	1.0000
X:114726857:GAAA:G	acceptor_gain	1.0000
X:114726967:TTCCT:T	donor_gain	1.0000
X:114726972:G:GG	donor_gain	1.0000
X:114726977:G:GT	donor_gain	1.0000
X:114731293:GT:G	acceptor_gain	1.0000
X:114731606:TG:T	donor_gain	1.0000
X:114731606:TGG:T	donor_loss	1.0000
X:114731607:GG:G	donor_gain	1.0000
X:114731607:GGT:G	donor_loss	1.0000
X:114731608:GTAA:G	donor_loss	1.0000
X:114906584:TTTA:T	acceptor_loss	1.0000
X:114906585:TTA:T	acceptor_loss	1.0000
X:114906587:A:AG	acceptor_gain	1.0000
X:114906587:AG:A	acceptor_gain	1.0000
X:114906587:AGGT:A	acceptor_gain	1.0000
X:114906588:G:GT	acceptor_gain	1.0000
X:114906588:GG:G	acceptor_gain	1.0000
X:114906588:GGT:G	acceptor_gain	1.0000
X:114906588:GGTG:G	acceptor_gain	1.0000
X:114906588:GGTGT:G	acceptor_gain	1.0000

AlphaMissense

3017 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
X:114731471:C:A	N71K	1.000
X:114731471:C:G	N71K	1.000
X:114731533:T:C	L92S	1.000
X:114731542:T:C	L95P	1.000
X:114731545:C:A	A96D	1.000
X:114731553:G:C	D99H	1.000
X:114731554:A:C	D99A	1.000
X:114731554:A:G	D99G	1.000
X:114731554:A:T	D99V	1.000
X:114731555:T:A	D99E	1.000
X:114731555:T:G	D99E	1.000
X:114848084:A:G	H144R	1.000
X:114848087:T:C	L145P	1.000
X:114848096:T:A	I148K	1.000
X:114848108:G:C	R152P	1.000
X:114848188:T:A	W179R	1.000
X:114848188:T:C	W179R	1.000
X:114906657:T:A	C207S	1.000
X:114906658:G:A	C207Y	1.000
X:114906658:G:C	C207S	1.000
X:114906659:C:G	C207W	1.000
X:114906705:T:C	F223L	1.000
X:114906707:C:A	F223L	1.000
X:114906707:C:G	F223L	1.000
X:114906715:C:A	P226Q	1.000
X:114906715:C:G	P226R	1.000
X:114906996:T:C	F320L	1.000
X:114906998:T:A	F320L	1.000
X:114906998:T:G	F320L	1.000
X:114907008:T:A	W324R	1.000

dbSNP variants (sampled 300 via entrez): RS1000035645 (X:114838940 A>G), RS1000051736 (X:114880607 C>A,T), RS1000062868 (X:114676615 G>A), RS1000074196 (X:114677054 T>A), RS1000104056 (X:114612351 G>A), RS1000111329 (X:114711935 G>T), RS1000111624 (X:114804637 G>A), RS1000112725 (X:114588463 A>G), RS1000148008 (X:114742411 C>A,T), RS1000148768 (X:114848309 G>A,T), RS1000189239 (X:114648443 C>T), RS1000214653 (X:114583010 C>T), RS1000215745 (X:114717405 T>C), RS1000228538 (X:114777019 G>A), RS1000248957 (X:114842854 C>A)

Disease associations

OMIM: gene MIM:312861 | disease phenotypes:

GenCC curated gene-disease

Disease	Classification	Inheritance
obesity disorder	Strong	Autosomal dominant

Mondo (2): prostate cancer (MONDO:0008315), obesity disorder (MONDO:0011122)

Orphanet (1): Familial prostate cancer (Orphanet:1331)

HPO phenotypes

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

GWAS associations

0 associations (top):

MeSH disease descriptors (1)

Descriptor	Name	Tree numbers
D011471	Prostatic Neoplasms	C04.588.945.440.770; C12.100.500.260.750; C12.100.500.565.625; C12.200.294.260.750; C12.200.294.565.625; C12.200.758.409.750; C12.900.619.750

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (5): CHEMBL2095200 (PROTEIN FAMILY), CHEMBL2096662 (SELECTIVITY GROUP), CHEMBL2096904 (PROTEIN FAMILY), CHEMBL2111466 (SELECTIVITY GROUP), CHEMBL225 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

276 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 649,680 (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
CHEMBL1423	PIMOZIDE	4	17,310
CHEMBL1729	CISAPRIDE	4	14,365
CHEMBL42	CLOZAPINE	4	37,581
CHEMBL54	HALOPERIDOL	4	60,883
CHEMBL715	OLANZAPINE	4	40,057
CHEMBL716	QUETIAPINE	4	26,465
CHEMBL360328	LORCASERIN	4	2,132
CHEMBL11	IMIPRAMINE	4	48,893
CHEMBL104	CLOTRIMAZOLE	4	56,325
CHEMBL1065	METHYSERGIDE	4	8,455
CHEMBL1071	OXAPROZIN	4	51,044
CHEMBL1078261	PROPIVERINE	4	4,890
CHEMBL10878	AGOMELATINE	4	4,528
CHEMBL109	VALPROIC ACID	4	65,937
CHEMBL1095777	INDACATEROL	4	2,735
CHEMBL1108	DROPERIDOL	4	16,888
CHEMBL1110	ALOSETRON	4	10,794
CHEMBL1112	ARIPIPRAZOLE	4	24,205
CHEMBL1113	AMOXAPINE	4	20,128
CHEMBL1117	IDARUBICIN	4	136,065
CHEMBL1123	DICYCLOMINE	4
CHEMBL1171837	PONATINIB	4
CHEMBL1172	DESLORATADINE	4
CHEMBL1175	DULOXETINE	4
CHEMBL1179047	CHLOROPROCAINE	4
CHEMBL1200406	DIMENHYDRINATE	4
CHEMBL1200492	NEFAZODONE HYDROCHLORIDE	4
CHEMBL1200517	DIHYDROERGOTAMINE MESYLATE	4
CHEMBL1200776	CINACALCET HYDROCHLORIDE	4
CHEMBL1200938	METHYSERGIDE MALEATE	4

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

PharmGKB clinical annotations

12 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs1414334	Toxicity	3	olanzapine	Mental Disorders
rs1414334	Toxicity	3	clozapine	Metabolic Syndrome;Schizophrenia
rs1414334	Toxicity	3	risperidone	Metabolic Syndrome
rs2497538	Toxicity	3	olanzapine	Weight gain
rs3813928	Efficacy	3	risperidone	Autism
rs3813929	Toxicity	3	antipsychotics	Mental Disorders
rs3813929	Toxicity	3	olanzapine	Mental Disorders;Schizophrenia
rs3813929	Toxicity	3	risperidone	Mental Disorders;Schizophrenia
rs3813929	Toxicity	3	clozapine	Mental Disorders;Schizophrenia
rs518147	Toxicity	3	olanzapine	Schizophrenia;Weight gain
rs6318	Toxicity	3	risperidone	Schizophrenia;Weight gain
rs6318	Efficacy	3	escitalopram	Neuropathic pain

PharmGKB variants

11 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs6318	HTR2C	3	1.50	2	escitalopram;risperidone
rs518147	HTR2C	3	3.25	1	olanzapine
rs539748	HTR2C		0.00	0
rs1414334	HTR2C	3	6.88	3	risperidone;olanzapine;clozapine
rs2497538	HTR2C	3	2.25	1	olanzapine
rs3813928	HTR2C	3	1.50	1	risperidone
rs3813929	HTR2C	3	4.00	4	antipsychotics;olanzapine;risperidone;clozapine
rs1023574	HTR2C		0.00	0
rs9698290	HTR2C, MIR764		0.00	0
rs498207	HTR2C		0.00	0
rs12836771	HTR2C, MIR1264, MIR1912		0.00	0

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — 5-Hydroxytryptamine receptors

Most potent curated ligand interactions (102 total), top 25:

Ligand	Action	Affinity	Parameter
ritanserin	Antagonist	9.6	pKi
mesulergine	Inverse agonist	9.3	pKi
[3H]mesulergine	Inverse agonist	9.3	pKd
mianserin	Inverse agonist	9.2	pKi
sertindole	Inverse agonist	9.2	pKi
methysergide	Antagonist	9.1	pKi
SB 228357	Antagonist	9.1	pKi
ziprasidone	Inverse agonist	9.01	pKi
(+)-LSD	Full agonist	9.0	pKi
[125I]DOI	Full agonist	9.0	pKd
SB 242084	Antagonist	9.0	pKi
SB 243213	Antagonist	9.0	pEC50
YM348	Full agonist	9.0	pKi
FR260010	Antagonist	9.0	pKi
brolamfetamine	Full agonist	8.9	pKi
metergoline	Inverse agonist	8.8	pKi
ergotamine	Partial agonist	8.7	pKi
SB 221284	Antagonist	8.7	pKi
amoxapine	Antagonist	8.7	pKi
clozapine	Inverse agonist	8.7	pKi
DOI	Full agonist	8.6	pKi
zotepine	Inverse agonist	8.6	pKi
α-methyl-5-HT	Full agonist	8.6	pKi
Lysergide	Full agonist	8.6	pKi
5-hydroxytryptamine	Full agonist	8.6	pKi

Binding affinities (BindingDB)

368 measured of 401 human assays (457 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
(R)-2-(4-Bromo-2,5-dimethoxy-phenyl)-1-methyl-ethylamine	EC50	0.018 nM
2-(8-Bromo-2,3,6,7-tetrahydro-benzo[1,2-b;4,5-b’]difuran-4-yl)-ethylamine	EC50	0.029 nM
DOHx	KI	0.1 nM
roxindole	KI	0.11 nM
3,3-diethyl-1-[(4R,7R)-6-methyl-6,11-diazatetracyclo[7.6.1.0^{2,7}.0^{12,16}]hexadeca-1(15),2,9,12(16),13-pentaen-4-yl]urea	KI	0.15 nM
4-methyl-2-[4-(4-phenylpiperazin-1-yl)butyl]-1,2,4-triazine-3,5-dione	KI	0.15 nM	US-9290463: Radiolabeled compounds and uses thereof
CHEMBL1434583	EC50	0.181 nM
1-(2-Chloro-3,4-dimethoxybenzyl)-6-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole	KI	0.2 nM
(S,S)-reboxetine	KI	0.3 nM
NSC_8226	KI	0.35 nM
2C-T-2	EC50	0.354 nM
DOBz	KI	0.4 nM
CAS_82830-44-2	EC50	0.418 nM
LSD,2-Bromo	KI	0.48 nM
2-(4-Ethylsulfanyl-2,5-dimethoxy-phenyl)-1-methyl-ethylamine	EC50	0.489 nM
2-Chlor-11-(2-dimethylaminoaethoxy)-dibenzo(b,f)-thiepin	KI	0.5 nM
3-(10,11-dihydro-5H-dibenzo[b,f]azepin-5-yl)-N-methylpropan-1-amine	KI	0.6 nM
(S)-1-(4-bromo-2,5-dimethoxyphenyl)propan-2-amine	EC50	0.66 nM
NSC_3981	KI	0.76 nM
2-(2,5-Dimethoxy-4-propyl-phenyl)-1-methyl-ethylamine(DOPR)	KI	0.9 nM
LY-193525	KI	0.9 nM
S-(-)-DOET	EC50	0.965 nM
5,6-difluoroindol-methylethylamine	KI	0.98 nM
CAS_113-15-5	KI	0.98 nM
eplivanserin	IC50	1 nM
METHIOTHEPIN	KI	1 nM
3-{2-[4-(4-Fluoro-benzoyl)-piperidin-1-yl]-ethyl}-2-methyl-pyrido[1,2-a]pyrimidin-4-one	KI	1.08 nM
(4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[7.6.1.0^{2,7}.0^{12,16}]hexadeca-1(16),2,9,12,14-pentaene-4-carboxamide	KI	1.09 nM
14C-5-hydroxy tryptamine creatinine disulfate	KI	1.2 nM
(1S,2R,10S,11S,14S,15S)-14-(2-hydroxyacetyl)-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-5-one	KI	1.4 nM
SB 215505	KI	1.48 nM
CAS_62865	KI	1.5 nM
2-(4-Bromo-2,5-dimethoxy-phenyl)-ethylamine	EC50	1.89 nM
ACP-103	IC50	1.9 nM
1-{5-[(5-chloro-2-fluorobenzyl)oxy]-1-(cyclopentylmethyl)-1H-pyrazol-3-yl}-N-methylmethanamine	KI	1.9 nM	US-10183913: Pyrazole compound
5-[2-(4-Benzo[d]isothiazol-3-yl-piperazin-1-yl)-ethyl]-6-chloro-1,3-dihydro-indol-2-one	KI	1.9 nM
Permax	KI	1.91 nM
1-{1-(cyclopentylmethyl)-5-[(2,4-difluorobenzyl)oxy]-1H-pyrazol-3-yl}-N-methylmethanamine	KI	2.2 nM	US-10183913: Pyrazole compound
CAS_17692-51-2	KI	2.29 nM
(-)-1-{1-(2-cyclopentylethyl)-5-[(2,5-difluorobenzyl)-oxy]-1H-pyrazol-3-yl}-N-methylethanamine	KI	2.3 nM	US-10183913: Pyrazole compound
1-(4-ethyl-2,5-dimethoxyphenyl)propan-2-amine	EC50	2.4 nM
2-(2,5-dimethoxy-4-ethylphenyl)ethylamine	EC50	2.5 nM
2-[2,5-dimethoxy-4-(trifluoromethylsulfanyl)phenyl]ethanamine	KI	2.5 nM	US-20250236589: THERAPEUTIC PHENETHYLAMINE COMPOSITIONS AND METHODS OF USE
1-{5-[(5-Chloro-2-fluorobenzyl)oxy]-1-(3-fluoro-3-methylbutyl)-1H-pyrazol-3-yl}-N-methylmethanamine hydrochloride	KI	2.6 nM	US-10183913: Pyrazole compound
(R)-2-(4-iodo-2,5-dimethoxyphenyl)-1-methylethylamine	EC50	2.85 nM
1-{1-(cyclohexylmethyl)-5-[(2,5-difluorobenzyl)oxy]-1H-pyrazol-3-yl}-N-methylmethanamine	KI	2.9 nM	US-10183913: Pyrazole compound
N-(4-Methylbenzyl)-N-(1-methyl-4-piperidinyl)-4-methoxybenzeneacetamide	KI	2.9 nM
4-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-1-(4-fluoro-phenyl)-butan-1-one;propionate(HCl)	KI	2.92 nM
8-[4-(4-fluorophenyl)-4-keto-butyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one	KI	2.94 nM	US-9359372: Hexahydrodibenzo[a,g]quinolizine compound, preparation method thereof, pharmaceutical composition and use thereof
(S)-mianserin	KI	3 nM

ChEMBL bioactivities

5891 potent at pChembl≥5 of 6011 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.70	Ki	0.02	nM	CHEMBL149024
10.48	Ki	0.033	nM	CHEMBL1172812
10.39	Ki	0.041	nM	APLYSINOPSIN
10.20	EC50	0.0631	nM	CHEMBL4765074
10.10	Ki	0.079	nM	CHEMBL1173408
10.05	EC50	0.09	nM	SEROTONIN
10.00	EC50	0.1	nM	CHEMBL4213447
10.00	EC50	0.1	nM	CHEMBL595195
10.00	EC50	0.1	nM	CHEMBL609306
9.97	EC50	0.108	nM	CHEMBL4213447
9.96	EC50	0.11	nM	CHEMBL494947
9.96	Ki	0.11	nM	CHEMBL1173820
9.94	EC50	0.116	nM	CHEMBL4213379
9.92	IC50	0.12	nM	CHEMBL5078731
9.92	EC50	0.12	nM	SEROTONIN
9.90	EC50	0.1259	nM	CHEMBL4213379
9.90	EC50	0.1259	nM	SEROTONIN
9.87	EC50	0.1349	nM	SEROTONIN
9.85	EC50	0.14	nM	SEROTONIN
9.80	Ki	0.1585	nM	CHEMBL4765074
9.80	Kd	0.1585	nM	CHEMBL323208
9.78	EC50	0.166	nM	SEROTONIN
9.77	EC50	0.17	nM	SEROTONIN
9.74	EC50	0.18	nM	OXITRIPTAN
9.74	EC50	0.182	nM	SEROTONIN
9.72	EC50	0.19	nM	CHEMBL4208452
9.72	EC50	0.1905	nM	SEROTONIN
9.72	EC50	0.19	nM	SEROTONIN
9.70	Ki	0.1995	nM	CHEMBL93862
9.70	EC50	0.1995	nM	CHEMBL3947276
9.70	Ki	0.2	nM	CHEMBL408579
9.70	Ki	0.2	nM	CHEMBL261476
9.70	EC50	0.1995	nM	CHEMBL4776557
9.70	Ki	0.2	nM	SERTINDOLE
9.70	EC50	0.2	nM	CHEMBL171774
9.68	Ki	0.21	nM	CHEMBL193639
9.68	EC50	0.21	nM	SEROTONIN
9.66	EC50	0.2188	nM	OXITRIPTAN
9.64	EC50	0.23	nM	CHEMBL172159
9.60	Ki	0.2512	nM	CHEMBL91221
9.60	Ki	0.2512	nM	CHEMBL4213379
9.52	Ki	0.3	nM	CHEMBL190699
9.52	Ki	0.3	nM	CHEMBL101008
9.52	Ki	0.3	nM	CHEMBL305275
9.50	EC50	0.3162	nM	CHEMBL3979806
9.50	Ki	0.3162	nM	CHEMBL3959570
9.50	Ki	0.3162	nM	CHEMBL377174
9.50	Ki	0.3162	nM	CHEMBL4776557
9.50	Ki	0.3162	nM	CHEMBL14111
9.49	EC50	0.32	nM	SEROTONIN HYDROCHLORIDE

PubChem BioAssay actives

2969 with measured affinity, of 6100 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-ethylsulfanyl-2,5-dimethoxyphenyl)ethanamine	2060762: Ray2010 Assay 75 from Article : “Psychedelics and the human receptorome.”	ec50	<0.0001	uM
(2R)-1-(4-bromo-2,5-dimethoxyphenyl)propan-2-amine	2060762: Ray2010 Assay 75 from Article : “Psychedelics and the human receptorome.”	ec50	<0.0001	uM
1-(4-ethylsulfanyl-2,5-dimethoxyphenyl)propan-2-amine	2060762: Ray2010 Assay 75 from Article : “Psychedelics and the human receptorome.”	ec50	0.0001	uM
2-(4-bromo-2,3,6,7-tetrahydrofuro[2,3-f][1]benzofuran-8-yl)ethanamine	2060762: Ray2010 Assay 75 from Article : “Psychedelics and the human receptorome.”	ec50	0.0001	uM
(7S)-7-(2-chlorophenoxy)-2-piperazin-1-yl-6,7-dihydro-5H-cyclopenta[b]pyridine	455197: Agonist activity against human 5HT2C receptor by FLIPR assay	ec50	0.0001	uM
(6aR)-4-(cyclobutylmethyl)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine	1387524: Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method	ec50	0.0001	uM
(6aR)-4-benzyl-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine	1387524: Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method	ec50	0.0001	uM
(6aR)-4-propyl-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine	1709163: Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay	ec50	0.0001	uM
1-(cyclopropylmethyl)-3-[2-(dimethylamino)ethyl]indol-4-ol	1834410: Modulation of human 5HT2C expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assay	ic50	0.0001	uM
(2S)-1-(4-bromo-2,5-dimethoxyphenyl)propan-2-amine	2060762: Ray2010 Assay 75 from Article : “Psychedelics and the human receptorome.”	ec50	0.0001	uM
2-(6-chloro-9-thia-1-azatricyclo[6.3.1.04,12]dodeca-2,4(12),5,7-tetraen-3-yl)ethanamine	5843: Functional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2c receptor cell line	ec50	0.0002	uM
7-propyl-2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinoline	1332010: Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting	ec50	0.0002	uM
(6aR)-4-[(3-fluorophenyl)methyl]-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine	1387524: Agonist activity at recombinant 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method	ec50	0.0002	uM
(4aR)-7-propyl-2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinoline	1709163: Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay	ec50	0.0002	uM
2-(1-azatricyclo[6.3.1.04,12]dodeca-2,4,6,8(12)-tetraen-3-yl)ethanamine	5843: Functional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2c receptor cell line	ec50	0.0002	uM
2-(4-ethyl-2,5-dimethoxyphenyl)ethanamine	2060762: Ray2010 Assay 75 from Article : “Psychedelics and the human receptorome.”	ec50	0.0002	uM
1-(4-bromo-2,3,6,7-tetrahydrofuro[2,3-f][1]benzofuran-8-yl)propan-2-amine	5858: Agonistic activity at cloned human 5-hydroxytryptamine 2C receptor using [125I]DOI as radioligand	ki	0.0003	uM
(2R)-1-(4-bromo-2,3,6,7-tetrahydrofuro[2,3-f][1]benzofuran-8-yl)propan-2-amine	5863: Binding ability of compound at cloned human 5-hydroxytryptamine 2C receptor using [125 I]DOI as radioligand	ki	0.0003	uM
5-methoxy-N-[4-methyl-3-(4-methyl-3-pyridinyl)phenyl]-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide	5656: Binding affinity towards human cloned 5-hydroxytryptamine receptor 2C in HEK293 cells, using [3H]mesulergine as radioligand.	ki	0.0003	uM
7-ethylsulfanyl-2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinoline	1332010: Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting	ec50	0.0003	uM
7-(thiophen-2-ylmethyl)-2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinoline	1332014: Displacement of [125I]DOI from recombinant human 5-HT2C receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting	ki	0.0003	uM
Serotonin Hydrochloride	1880144: Agonist activity at human 5HT2C receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay	ec50	0.0003	uM
1-benzhydryl-6-chloro-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole;hydrochloride	1880144: Agonist activity at human 5HT2C receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay	ec50	0.0003	uM
1-[4-methoxy-3-(2-piperidin-1-ylethoxy)phenyl]-4-(4-methylphenyl)-2H-pyrrol-5-one	269243: Binding affinity to human 5HT2C receptor	ki	0.0003	uM
(4R,10aR)-7-chloro-4,6-dimethyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indole	238993: Binding affinity toward 5-HT2C receptor evaluated by displacement of [3H]5-HT radioligand	ki	0.0003	uM
6-chloro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-2,3-dihydroindole-1-carboxamide	1664657: Antagonist activity at recombinant human 5-HT2C expressed in human U2OS cells by pathhunter beta-arrestin assay	ic50	0.0003	uM
5-methoxy-N-[5-(4-methyl-3-pyridinyl)-3-pyridinyl]-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide	5656: Binding affinity towards human cloned 5-hydroxytryptamine receptor 2C in HEK293 cells, using [3H]mesulergine as radioligand.	ki	0.0004	uM
5-fluoro-2-[4-methoxy-3-[2-(4-methylpiperidin-1-yl)ethoxy]phenyl]-7-(trifluoromethyl)-3H-isoindol-1-one	292745: Displacement of [3H]mesulergine from 5HT2C receptor expressed in HEK293 cells	ki	0.0004	uM
7-benzyl-8-fluoro-2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinoline	1332014: Displacement of [125I]DOI from recombinant human 5-HT2C receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting	ki	0.0004	uM
(6aR)-4-(2-methylpropyl)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine	1709163: Agonist activity at 5-HT2CR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay	ec50	0.0004	uM
1-[(5-fluoro-2-pyridinyl)methyl]-1-[(8S)-5-methyl-5-azaspiro[2.5]octan-8-yl]-3-[[4-(2-methylpropoxy)phenyl]methyl]urea	2111506: Displacement of [3H]ketanserin from human 5-HT2C receptor transfected in Jump-In GripTite HEK293 cell membrane measured after 3 hrs incubation by scintillation proximity assay (SPA)	ki	0.0004	uM
N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-5-methylsulfanyl-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide	5659: Binding affinity towards human cloned 5-hydroxytryptamine 2C receptor of HEK293 cells by displacement of [3H]mesulergine	ki	0.0004	uM
5-methyl-N-[5-methyl-6-(pyridin-2-ylmethoxy)-3-pyridinyl]-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide	5660: In vitro binding affinity at human cloned 5-hydroxytryptamine 2C receptor of HEK293 cells by [3H]mesulergine displacement.	ki	0.0004	uM
1-(7-methoxy-4,4-dimethylindeno[1,2-b]pyrrol-1-yl)propan-2-amine	5645: Binding affinity against human 5-hydroxytryptamine 2C receptor using displacement of [3H]DOB	ki	0.0004	uM
1-methyl-4-(3-methylsulfanyl-5,6-dihydrobenzo[b][1]benzothiepin-5-yl)piperazine	752105: Antagonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay	ec50	0.0004	uM
5-methoxy-N-(4-methoxy-3-pyridin-3-ylphenyl)-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide	5656: Binding affinity towards human cloned 5-hydroxytryptamine receptor 2C in HEK293 cells, using [3H]mesulergine as radioligand.	ki	0.0005	uM
5-methoxy-N-(7-pyridin-3-yl-2,3-dihydro-1-benzofuran-5-yl)-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide	5656: Binding affinity towards human cloned 5-hydroxytryptamine receptor 2C in HEK293 cells, using [3H]mesulergine as radioligand.	ki	0.0005	uM
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine	2104596: Binding affinity to human [125I]DOI-labeled 5-HT2C receptor expressed in HEK293 cell membrane incubated for 60 mins	ki	0.0005	uM
(6aR)-4-benzyl-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,7]naphthyridine	1709164: Displacement of [125I]-DOI from recombinant human 5HT2CR transfected in human HEK293 cells incubated for 45 mins by radioligand binding assay	ki	0.0005	uM
6-chloro-1-(2,4,5-trimethoxyphenyl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole;hydrochloride	1880144: Agonist activity at human 5HT2C receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay	ec50	0.0005	uM
(9R)-5-bromo-N,N-diethyl-7-methyl-4-(111C)methyl-6,6a,8,9-tetrahydroindolo[4,3-fg]quinoline-9-carboxamide	1855061: Binding affinity to cerebrum 5-HT2 receptor (unknown origin)	ki	0.0005	uM
2-[2,5-dimethoxy-4-(trifluoromethylsulfanyl)phenyl]ethanamine;hydrochloride	2104577: Displacement of [3H]DOI from human 5-HT2C receptor expressed in HEK293 cell membrane incubated for 90 mins by microbeta liquid scintillation counting method	ki	0.0005	uM
N-[6-[(2-chloro-3-pyridinyl)oxy]-3-pyridinyl]-1H-indole-3-carboxamide	340645: Displacement of [3H]mesulergine at human cloned 5HT2C receptor expressed in CHOK1 cell	ic50	0.0005	uM
benzyl N-[[(6aR,9S,10aR)-4,7-dimethyl-6,6a,8,9,10,10a-hexahydroindolo[4,3-fg]quinolin-9-yl]methyl]carbamate	4747: Evaluated for the binding affinity to porcine choroid plexus at 5-hydroxytryptamine 2C receptor binding site by using [3H]-MES as a radioligand.	ki	0.0005	uM
N-(3-fluoro-4-methyl-5-pyridin-3-ylphenyl)-5-methoxy-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide	5656: Binding affinity towards human cloned 5-hydroxytryptamine receptor 2C in HEK293 cells, using [3H]mesulergine as radioligand.	ki	0.0006	uM
5-methoxy-N-[3-(4-methyl-3-pyridinyl)phenyl]-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide	5656: Binding affinity towards human cloned 5-hydroxytryptamine receptor 2C in HEK293 cells, using [3H]mesulergine as radioligand.	ki	0.0006	uM
N-(3-ethyl-5-pyridin-3-ylphenyl)-5-methoxy-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide	5656: Binding affinity towards human cloned 5-hydroxytryptamine receptor 2C in HEK293 cells, using [3H]mesulergine as radioligand.	ki	0.0006	uM
5-methoxy-N-(5-pyridin-4-yl-3-pyridinyl)-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide	5656: Binding affinity towards human cloned 5-hydroxytryptamine receptor 2C in HEK293 cells, using [3H]mesulergine as radioligand.	ki	0.0006	uM
N-[4-chloro-3-(4-methyl-3-pyridinyl)phenyl]-5-methoxy-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide	5656: Binding affinity towards human cloned 5-hydroxytryptamine receptor 2C in HEK293 cells, using [3H]mesulergine as radioligand.	ki	0.0006	uM
5-methoxy-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide	5656: Binding affinity towards human cloned 5-hydroxytryptamine receptor 2C in HEK293 cells, using [3H]mesulergine as radioligand.	ki	0.0006	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Clozapine	affects binding, affects response to substance	5
Olanzapine	affects response to substance, increases response to substance, affects binding	4
Valproic Acid	affects expression, decreases expression, increases expression	4
Aflatoxin B1	increases methylation, affects expression, decreases methylation	3
mesulergine	affects binding, decreases reaction	2
Calcitriol	increases expression, affects cotreatment	2
Phenylmercuric Acetate	affects cotreatment, decreases expression	2
Risperidone	affects reaction, increases expression, affects response to substance, increases response to substance	2
bisphenol A	increases methylation	1
trichostatin A	increases expression	1
arsenite	increases methylation	1
4-iodo-2,5-dimethoxyphenylisopropylamine	affects binding, decreases reaction	1
norfluoxetine	affects binding	1
nefazodone	affects binding	1
sarpogrelate	affects binding	1
agomelatine	affects binding	1
SB 206553	increases expression	1
6-chloro-5-methyl-1-((2-(2-methylpyrid-3-yloxy)pyrid-5-yl)carbamoyl)indoline	decreases reaction, increases expression	1
entinostat	increases expression	1
SB 243213	affects binding, decreases activity	1
7-methyl-6,7,8,9,14,15-hexahydro-5H-benz(d)indolo(2,3-g)azecine	affects binding	1
bardoxolone methyl	decreases activity	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, decreases expression	1
dorsomorphin	affects cotreatment, decreases expression	1
1-(8-bromobenzo(1,2-b;4,5-b’)difuran-4-yl)-2-aminopropane	affects binding, decreases reaction	1
Aripiprazole	affects activity, affects binding	1
Vorinostat	decreases expression	1
Mirtazapine	affects binding, decreases reaction, increases expression, affects activity	1
Amitriptyline	affects binding	1
Benzo(a)pyrene	affects methylation	1

ChEMBL screening assays

1235 unique, capped per target: 928 binding, 290 functional, 14 admet, 2 unclassified, 1 toxicity

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL5109939	Binding	Binding affinity to cerebrum 5-HT2 receptor (unknown origin)	Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors. — J Med Chem
CHEMBL859802	Functional	Lowering of intraocular pressure in lasered cynomolgus monkey after 1 hr at 250 ug	1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. — J Med Chem
CHEMBL4013769	Unclassified	Selectivity ratio of EC50 for human 5HT2A receptor to EC50 for human 5HT2C-INI receptor	Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications. — J Med Chem

Cellosaurus cell lines

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

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

Cellosaurus	Name	Category	Sex
CVCL_H381	CHO-K1/5-HT2C	Spontaneously immortalized cell line	Female
CVCL_H513	HEK293/5-HT2C	Transformed cell line	Female
CVCL_LA57	PathHunter U2OS HTR2C Activated GPCR Internalization	Cancer cell line	Female
CVCL_LA58	PathHunter U2OS HTR2C beta-arrestin	Cancer cell line	Female
CVCL_LA59	PathHunter U2OS HTR2C(VGV) beta-arrestin	Cancer cell line	Female
CVCL_LA60	PathHunter U2OS HTR2C(VNV) beta-arrestin	Cancer cell line	Female
CVCL_LA61	PathHunter U2OS HTR2C(VSV) beta-arrestin	Cancer cell line	Female
CVCL_RQ11	CHO-K1 (+Galpha16) AequoScreen HTR2C (ne)	Spontaneously immortalized cell line	Female
CVCL_YK51	U2OS HTR2C HiTSeeker	Cancer cell line	Female
CVCL_ZJ76	GeneBLAzer HTR2C-NFAT-bla CHO-K1	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT00076362	PHASE4	COMPLETED	Pediatric Hypothalamic Obesity
NCT00079547	PHASE4	COMPLETED	The Safety and Effectiveness of Low and High Carbohydrate Diets
NCT00115063	PHASE4	TERMINATED	LOSS- Louisiana Obese Subjects Study
NCT00134303	PHASE4	COMPLETED	Trial Comparing Metformin Versus Placebo in Non Alcoholic Steatohepatitis (NASH) Patients Receiving Bariatric Surgery for Obesity
NCT00143936	PHASE4	COMPLETED	The Safety and Efficacy of Low and High Carbohydrate Diets
NCT00143962	PHASE4	COMPLETED	Comparison of Two Approaches to Weight Loss Follow-Up Study
NCT00152360	PHASE4	COMPLETED	The Effect of Xenical on Weight and Risk Factors
NCT00176306	PHASE4	COMPLETED	Levofloxacin Pharmacokinetics (PK) in the Severely Obese
NCT00203450	PHASE4	COMPLETED	Zonegran for the Treatment of Weight Gain Associated With Psychotropic Medication Use: A Placebo-Controlled Trial
NCT00205504	PHASE4	COMPLETED	Oral Contraceptives in the Metabolic Syndrome
NCT00229229	PHASE4	TERMINATED	Comparison of 4 Diets in the Management of Overweight Patients With Vascular Disease
NCT00234988	PHASE4	COMPLETED	A Phase IV, Multi-Center, Open-Label Trial of Sibutramine in Combination With a Hypocaloric Diet in Obese and Overweight Thai Subjects.
NCT00264589	PHASE4	COMPLETED	Exercise Training and Cardiovascular Function in Obesity and in Type 2 Diabetes
NCT00288873	PHASE4	COMPLETED	Characterization of Hyperparathyroidism and Vitamin D Deficiency in Obesity
NCT00298857	PHASE4	TERMINATED	A Pharmacokinetic Study to Compare the Dosing of Valproic Acid in Subjects With Different Body Weights
NCT00315146	PHASE4	COMPLETED	Optimizing Body Composition for Function in Older Adults
NCT00319202	PHASE4	TERMINATED	Clinical Trial to Assess the Effects of Candesartan on the Carbohydrate Metabolism of Obese Subjects
NCT00327912	PHASE4	UNKNOWN	Laparoscopic Roux-en-Y Gastric Bypass Versus Laparoscopic Biliopancreatic Diversion (BPD)- Duodenal Switch for Superobesity
NCT00352287	PHASE4	COMPLETED	Study to Determine the Effects of Human Growth Hormone and Pioglitazone in Overweight, Prediabetic Adults
NCT00353054	PHASE4	COMPLETED	Effect of Calcium/Vitamin D Supplementation on Body Weight and Fat Loss.
NCT00390637	PHASE4	COMPLETED	Diet, Obesity and Genes (DiOGenes)
NCT00415688	PHASE4	COMPLETED	Lifestyle Modification for Obesity-Related Type 2 Diabetes
NCT00433641	PHASE4	COMPLETED	Weight Loss in Response to Sibutramine (MERIDIA) is Influenced by the Inherited Genes
NCT00440375	PHASE4	COMPLETED	Effects of Rosiglitazone on Bone in Postmenopausal Diabetic Women
NCT00453557	PHASE4	COMPLETED	Mechanism of Growth Hormone Effects on Adipose Tissue
NCT00456885	PHASE4	COMPLETED	The Effect of Exenatide on Weight and Hunger in Obese, Healthy Women
NCT00463112	PHASE4	COMPLETED	Effect of Diet Plus Sibutramine on Hormonal and Metabolic Features in Overweight and Obese Women With PCOS
NCT00512187	PHASE4	COMPLETED	Moderate Weight Loss Makes Obese Patients With Severe Chronic Plaque Psoriasis Responsive to Sub-Optimal Dose of Cyclosporine: an Investigator Blinded, Controlled, Randomized Clinical Trial
NCT00516919	PHASE4	COMPLETED	Study of Behavioral Weight Loss Therapy for Obesity and Binge Eating in Monolingual Hispanic Persons
NCT00522470	PHASE4	COMPLETED	Effects of Rosiglitazone on Serum Ghrelin and Peptide YY Levels
NCT00537810	PHASE4	COMPLETED	Treatment of Binge Eating in Obese Patients in Primary Care
NCT00538486	PHASE4	COMPLETED	A Randomized, Double-Blind, Active Control Trial Comparing Effects of Telmisartan, Candesartan and Amlodipine, Alone or Plus Metformin, on Non-Diabetic, Obese Hypertensive Patients
NCT00584389	PHASE4	TERMINATED	The Effect of Rimonabant on Energy Expenditure, Fat Metabolism and Body Composition
NCT00585182	PHASE4	COMPLETED	Study to Evaluate Weight-based Enoxaparin Dosing in Obese Medical Patients at Risk for DVT
NCT00632840	PHASE4	COMPLETED	Pharmacological Regulation of Fat Transport in Metabolic Syndrome
NCT00636142	PHASE4	COMPLETED	Effects of Infliximab on Insulin Sensitivity and Beta Cell Function in Insulin Resistant Human Obesity
NCT00675987	PHASE4	COMPLETED	A Randomized Clinical Trial To Study Losartan On Endothelial Dysfunction and Insulin Resistance In Obese Patients
NCT00694811	PHASE4	COMPLETED	Effects of Re-Feeding Duration on Weight Maintenance After Weight Loss With Very-Low-Energy Diets (VLEDs)
NCT00699413	PHASE4	TERMINATED	Supplements for Controlling Resistance to Insulin
NCT00729963	PHASE4	COMPLETED	Sibutramine Versus Continuous Positive Airway Pressure (CPAP)in Obstructive Sleep Apnea (OSA) Patients