HTR3B
gene geneOn this page
Also known as 5-HT3B
Summary
HTR3B (5-hydroxytryptamine receptor 3B, HGNC:5298) is a protein-coding gene on chromosome 11q23.2, encoding 5-hydroxytryptamine receptor 3B (O95264). Forms serotonin (5-hydroxytryptamine/5-HT3)-activated cation-selective channel complexes, which when activated cause fast, depolarizing responses in neurons.
The product of this gene belongs to the ligand-gated ion channel receptor superfamily. This gene encodes subunit B of the type 3 receptor for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor causes fast, depolarizing responses in neurons after activation. It is not functional as a homomeric complex, but a pentaheteromeric complex with subunit A (HTR3A) displays the full functional features of this receptor.
Source: NCBI Gene 9177 — RefSeq curated summary.
At a glance
- GWAS associations: 5
- Clinical variants (ClinVar): 84 total
- Druggable target: yes — 20 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_006028
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:5298 |
| Approved symbol | HTR3B |
| Name | 5-hydroxytryptamine receptor 3B |
| Location | 11q23.2 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | 5-HT3B |
| Ensembl gene | ENSG00000149305 |
| Ensembl biotype | protein_coding |
| OMIM | 604654 |
| Entrez | 9177 |
Gene structure
Transcript identifiers
Ensembl transcripts: 3 — 3 protein_coding
ENST00000260191, ENST00000537778, ENST00000543092
RefSeq mRNA: 2 — MANE Select: NM_006028
NM_001363563, NM_006028
CCDS: CCDS8364, CCDS86249
Canonical transcript exons
ENST00000260191 — 9 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000747392 | 113932936 | 113933093 |
| ENSE00000747394 | 113932289 | 113932458 |
| ENSE00000795713 | 113942982 | 113943192 |
| ENSE00000930649 | 113931384 | 113931428 |
| ENSE00000930650 | 113931758 | 113931867 |
| ENSE00001106077 | 113909295 | 113909455 |
| ENSE00001106080 | 113944573 | 113944755 |
| ENSE00001130152 | 113945902 | 113949079 |
| ENSE00001130156 | 113904796 | 113904985 |
Expression profiles
Bgee: expression breadth broad, 59 present calls, max score 72.36.
FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.0277 / max 5.2313, expressed in 19 samples.
FANTOM5 promoters (1 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 116764 | 0.0277 | 19 |
Top tissues by expression
244 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| prefrontal cortex | UBERON:0000451 | 72.36 | gold quality |
| tongue squamous epithelium | UBERON:0006919 | 70.69 | gold quality |
| right frontal lobe | UBERON:0002810 | 69.06 | gold quality |
| diaphragm | UBERON:0001103 | 67.28 | gold quality |
| frontal cortex | UBERON:0001870 | 66.24 | gold quality |
| Brodmann (1909) area 9 | UBERON:0013540 | 66.22 | gold quality |
| dorsolateral prefrontal cortex | UBERON:0009834 | 64.52 | gold quality |
| neocortex | UBERON:0001950 | 64.01 | gold quality |
| hair follicle | UBERON:0002073 | 63.09 | gold quality |
| anterior cingulate cortex | UBERON:0009835 | 61.78 | gold quality |
| cingulate cortex | UBERON:0003027 | 61.77 | gold quality |
| olfactory bulb | UBERON:0002264 | 60.40 | gold quality |
| type B pancreatic cell | CL:0000169 | 60.21 | gold quality |
| lower esophagus mucosa | UBERON:0035834 | 59.44 | gold quality |
| cerebral cortex | UBERON:0000956 | 58.99 | gold quality |
| superficial temporal artery | UBERON:0001614 | 55.92 | gold quality |
| ileal mucosa | UBERON:0000331 | 55.12 | silver quality |
| tibialis anterior | UBERON:0001385 | 52.68 | silver quality |
| quadriceps femoris | UBERON:0001377 | 52.50 | gold quality |
| telencephalon | UBERON:0001893 | 52.06 | gold quality |
| Brodmann (1909) area 46 | UBERON:0006483 | 51.81 | gold quality |
| left ventricle myocardium | UBERON:0006566 | 51.81 | gold quality |
| vastus lateralis | UBERON:0001379 | 51.62 | gold quality |
| primary visual cortex | UBERON:0002436 | 51.55 | gold quality |
| deltoid | UBERON:0001476 | 51.29 | gold quality |
| superior frontal gyrus | UBERON:0002661 | 50.89 | gold quality |
| epithelial cell of pancreas | CL:0000083 | 50.29 | gold quality |
| dorsal motor nucleus of vagus nerve | UBERON:0002870 | 50.07 | gold quality |
| kidney epithelium | UBERON:0004819 | 49.85 | gold quality |
| thymus | UBERON:0002370 | 49.70 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 4.09 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
12 targeting HTR3B, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-7110-3P | 100.00 | 73.18 | 2486 |
| HSA-MIR-6845-3P | 99.94 | 66.88 | 1439 |
| HSA-MIR-552-5P | 99.93 | 68.56 | 1583 |
| HSA-MIR-1343-3P | 99.89 | 66.78 | 1815 |
| HSA-MIR-6783-3P | 99.89 | 67.92 | 2059 |
| HSA-MIR-4437 | 99.52 | 65.29 | 1266 |
| HSA-MIR-939-3P | 98.97 | 65.07 | 2347 |
| HSA-MIR-4451 | 98.82 | 68.17 | 1455 |
| HSA-MIR-5691 | 98.23 | 67.02 | 1335 |
| HSA-MIR-6805-3P | 98.23 | 67.02 | 1334 |
| HSA-MIR-4664-5P | 98.17 | 65.07 | 1020 |
| HSA-MIR-342-5P | 97.25 | 64.10 | 817 |
Literature-anchored findings (GeneRIF, showing 40)
- Cell surface expression of 5-hydroxytryptamine type 3 receptors is controlled by an endoplasmic reticulum retention signal (PMID:12750374)
- Only 1.3% of antiemetic treatment failure with 5-HT3 receptor antagonists is associated with 5-HT3B receptor gene variant (PMID:12775740)
- By constructing chimaeric 5-HT3A and 5-HT3B subunits we identified a region (the ‘HA-stretch’) within the large cytoplasmic loop of the receptor that markedly influences channel conductance (PMID:12867984)
- 5-HT excited human enteric neurons via 5-HT3 receptors, which may comprise both 5-HT3A and 5-HT3B receptor subunits. (PMID:15887114)
- Six sequence variants found in Gilles de la Tourette syndrome. (PMID:16314763)
- Different transcriptional regulation of the HTR3B gene by two alternative promoters in the peripheral and the central nervous system leads to expression of transcripts with variations in the 5’ coding sequence. (PMID:17010535)
- The -100_-102AAG deletion variant of the 5-HT3B receptor gene may affect paroxetine-induced nausea. (PMID:17697394)
- an HTR3B variant associated with major depression dramatically augments the signaling of the human 5-HT3AB receptor (PMID:18184810)
- the incorporation of the 5-HT3B subunit leads to spontaneous channel opening and altered ligand properties (PMID:18187416)
- performed electrophoretic mobility shift and luciferase reporter gene assays to elucidate the effect of this -100_-102delAAG deletion polymorphism on the HTR3B promoter activity in PC-12 and HEK293 cells (PMID:18300944)
- Variants in the HTR3B gene is associated with psychiatric diseases (PMID:18698232)
- The results suggest that HTR3B is involved in the development of TRS in the Japanese population. (PMID:18807291)
- 5-HT3B(I143T)-containing 5-HT3AB receptors display significantly reduced cell surface expression and different signalling properties compared with WT 5-HT3AB receptors. (PMID:19008750)
- 5-HT3R might contribute to the imbalance between excitation and inhibition that characterize the brain of alcoholics (PMID:19185213)
- Genetic variations in the HTR3A and HTR3B gene seem to be associated with the individual risk of developing postoperative vomiting. (PMID:19713259)
- an involvement of serotonin receptor type 3B variants in the aetiopathology of eating disorders in humans. (PMID:19741568)
- Six functional and coding variants of the subunit genes HTR3A, HTR3B as well as the novel HTR3C, HTR3D, and HTR3E subunits in the response to haloperidol or risperidone, were assessed. (PMID:19794330)
- role of the subunits A and B of the HTR3 receptor using 140 schizophrenia patients taking clozapine for 6 months (PMID:20168265)
- The HTR3B rs1176744 gain-of-function Ser129 allele predicted alcohol dependence & was more common in men with alcohol and drug dependence. (PMID:20838391)
- findings indicate that HTR3A and HTR3B polymorphisms may not play a major role in the susceptibility to suicidal behavior in schizophrenia subjects. (PMID:21184810)
- No associations were found with the 5-HT3B receptor haplotypes and the risk of delayed chemotherapy-induced nausea and vomiting in patients treated with ondansetron and metoclopramide. (PMID:21840870)
- HTR3A and HTR3B were detected in all investigated brain tissues with the exception of the cerebellum, and large differences in the A:B subunit ratio were observed. (PMID:22832903)
- Genetic interactions between HTR3B, HTR3A and SLC6A4 play a significant role in nicotine dependence in both European American and African American smokers. (PMID:23290502)
- Five single nucleotide polymorphisms (SNPs) in HTR3A and HTR3B were found. (PMID:23464988)
- Data suggest that HTR3A/HTR3B subunits readily form functionally distinct heteromeric receptors; molecular models have been developed regarding affinities of competitive ligands, non-competitive antagonists, and allosteric modulators. [REVIEW] (PMID:23489111)
- Genetic variability within SLC6A4, HTR3A, and HTR3B contributes to the risk of alcohol dependence and related phenotypes. (PMID:23757001)
- HTR3B gene variants may contribute to variability in severity of and response to antiemetic therapy for nausea and vomiting of pregnancy. (PMID:23786674)
- The ability of 5-HT to gate the homomeric or heteromeric receptor appears to rely on the D loop triplet RQY of the complementary face. (PMID:23810831)
- Polymorphisms in the HTR3B gene are predictors of reduced alcohol drinking in response to ondansetron. (PMID:23897038)
- the stoichiometry of 5-HT3AB receptors on the plasma membrane (PMID:23972841)
- This is the first study to show an association between 5-HTR3B and PCS scores, thus suggesting a role of the serotonin pathway in pain catastrophizing. (PMID:24244382)
- variants in HTR3A, HTR3B, and SLC6A4 interactively contribute to etiology of alcohol, cocaine, and nicotine dependence (PMID:24590108)
- we found an association of the HTR3B with poor concentration in schizophrenia patients.These results suggest that the HTR3B may be involved in the attention problem of schizophrenia in Korean population. (PMID:24880582)
- Study demonstrates that the 5-HT3Br1 transcriptional variant of the 5-HT3B subunit can contribute to the functional properties of heteromeric receptors in a similar manner to the originally characterized 5-HT3B subunit (PMID:25951416)
- The response to ondansetron for PONV was significantly influenced by the -100_-102AAG deletion polymorphisms of the 5-HT3B gene. Thus, the -100_-102AAG deletion variants may be a pharmacogenetic predictor for responsiveness to ondansetron for PONV. (PMID:26256989)
- the -AAG deletion variant of the 5-HT3B receptor gene may contribute to variability in response to antiemetic therapy for chemotherapy-induced nausea and vomiting (PMID:27488933)
- A protective haplotype in HTR3B was also associated with OCD (OR = 0.77, CI = 0.63-0.95, permutated P = 0.0179). These results support that common HTR3 variants are involved in OCD and some of its clinical phenotypes (PMID:27616601)
- Analysis of our small Chinese sample revealed a significant association of HTR3A with bipolar disorder, but yielded no evidence of an association between HTR3B and bipolar disorder. Furthermore, evidence for an association was found for a haplotype of HTR3A. (PMID:27706728)
- the important role of HTR3B polymorphisms in heroin dependence among the Chinese Han population (PMID:27773795)
- The HTR3B rs1176744 polymorphisms do not seem to directly influence experimental muscle pain in healthy individuals. However, women reported higher pain intensity and larger pain area than men, which might partly be attributed to genotype. (PMID:28002447)
Cross-species orthologs
3 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | htr3b | ENSDARG00000061749 |
| mus_musculus | Htr3b | ENSMUSG00000008590 |
| rattus_norvegicus | Htr3b | ENSRNOG00000006920 |
Paralogs (45): GABRA3 (ENSG00000011677), GABRA1 (ENSG00000022355), CHRNA3 (ENSG00000080644), GABRP (ENSG00000094755), CHRNA4 (ENSG00000101204), GLRA2 (ENSG00000101958), GABRE (ENSG00000102287), CHRNE (ENSG00000108556), GABRA4 (ENSG00000109158), GLRB (ENSG00000109738), GABRR2 (ENSG00000111886), GABRG2 (ENSG00000113327), CHRNB4 (ENSG00000117971), CHRNA2 (ENSG00000120903), CHRNA10 (ENSG00000129749), CHRND (ENSG00000135902), CHRNA1 (ENSG00000138435), GLRA3 (ENSG00000145451), GABRA6 (ENSG00000145863), GABRB2 (ENSG00000145864), GLRA1 (ENSG00000145888), GABRR1 (ENSG00000146276), CHRNB3 (ENSG00000147432), CHRNA6 (ENSG00000147434), GABRA2 (ENSG00000151834), CHRNB2 (ENSG00000160716), GABRG1 (ENSG00000163285), GABRB1 (ENSG00000163288), GABRB3 (ENSG00000166206), CHRFAM7A (ENSG00000166664), HTR3A (ENSG00000166736), CHRNA5 (ENSG00000169684), CHRNB1 (ENSG00000170175), CHRNA9 (ENSG00000174343), CHRNA7 (ENSG00000175344), HTR3C (ENSG00000178084), GABRG3 (ENSG00000182256), GABRR3 (ENSG00000183185), HTR3E (ENSG00000186038), HTR3D (ENSG00000186090)
Protein
Protein identifiers
5-hydroxytryptamine receptor 3B — O95264 (reviewed: O95264)
Alternative names: Serotonin receptor 3B
All UniProt accessions (2): O95264, H0YFX8
UniProt curated annotations — full annotation on UniProt →
Function. Forms serotonin (5-hydroxytryptamine/5-HT3)-activated cation-selective channel complexes, which when activated cause fast, depolarizing responses in neurons.
Subunit / interactions. Forms homopentameric as well as heteropentameric serotonin-activated cation-selective channel complexes with HTR3A. The homomeric complex is not functional. Heteropentameric complexes display properties which resemble that of neuronal serotonin-activated channels in vivo.
Subcellular location. Postsynaptic cell membrane. Cell membrane.
Tissue specificity. Expressed in the brain cortex, in the caudate nucleus, the hippocampus, the thalamus and the amygdala. Detected in the kidney and testis as well as in monocytes of the spleen, small and large intestine, uterus, prostate, ovary and placenta.
Post-translational modifications. N-glycosylation required for membrane localization.
Domain organisation. The HA-stretch region of HTR3B seems to confer increased conductance to HTR3A/HTR3B heteromers compared to that of HTR3A homomers.
Similarity. Belongs to the ligand-gated ion channel (TC 1.A.9) family. 5-hydroxytryptamine receptor (TC 1.A.9.2) subfamily. HTR3B sub-subfamily.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| O95264-1 | 1 | yes |
| O95264-2 | 2 |
RefSeq proteins (2): NP_001350492, NP_006019* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR006029 | Neurotrans-gated_channel_TM | Domain |
| IPR006201 | Neur_channel | Family |
| IPR006202 | Neur_chan_lig-bd | Domain |
| IPR008132 | 5HT3_rcpt | Family |
| IPR008134 | 5HT3_rcpt_B | Family |
| IPR036719 | Neuro-gated_channel_TM_sf | Homologous_superfamily |
| IPR036734 | Neur_chan_lig-bd_sf | Homologous_superfamily |
| IPR038050 | Neuro_actylchol_rec | Homologous_superfamily |
| IPR049944 | LGIC_TM_5-HT3 | Domain |
Pfam: PF02931, PF02932
Catalyzed reactions (Rhea), 3 shown:
- K(+)(in) = K(+)(out) (RHEA:29463)
- Ca(2+)(in) = Ca(2+)(out) (RHEA:29671)
- Na(+)(in) = Na(+)(out) (RHEA:34963)
UniProt features (29 total): glycosylation site 6, topological domain 5, mutagenesis site 5, sequence variant 4, transmembrane region 4, signal peptide 1, chain 1, region of interest 1, disulfide bond 1, splice variant 1
Structure
Experimental structures (PDB)
0 structures.
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-O95264-F1 | 82.13 | 0.53 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Disulfide bonds (1): 155–169
Glycosylation sites (6): 52, 96, 138, 168, 203, 287
Mutagenesis-validated functional residues (5):
| Position | Phenotype |
|---|---|
| 52 | reduced molecular weight. very little expression in the cell membrane. |
| 96 | reduced molecular weight. very little expression in the cell membrane. |
| 138 | reduced molecular weight. very little expression in the cell membrane. |
| 168 | reduced molecular weight and cell membrane expression. |
| 203 | reduced molecular weight. very little expression in the cell membrane. |
Function
Pathways and Gene Ontology
Reactome pathways
3 pathways
| ID | Pathway |
|---|---|
| R-HSA-112314 | Neurotransmitter receptors and postsynaptic signal transmission |
| R-HSA-112315 | Transmission across Chemical Synapses |
| R-HSA-112316 | Neuronal System |
MSigDB gene sets: 120 (showing top):
CREL_01, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, NKX25_02, GOCC_CELL_SURFACE, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, GOBP_CELL_CELL_SIGNALING, EVI1_05, GOBP_REGULATION_OF_POSTSYNAPTIC_MEMBRANE_POTENTIAL, IRF1_Q6, WTGAAAT_UNKNOWN, SCHAEFFER_PROSTATE_DEVELOPMENT_12HR_DN, GOBP_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, GOBP_CELLULAR_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_SYNAPTIC_SIGNALING, GOCC_NEURON_PROJECTION
GO Biological Process (9): serotonin receptor signaling pathway (GO:0007210), chemical synaptic transmission (GO:0007268), monoatomic ion transmembrane transport (GO:0034220), regulation of membrane potential (GO:0042391), obsolete inorganic cation transmembrane transport (GO:0098662), serotonin-gated cation-selective signaling pathway (GO:0140227), monoatomic ion transport (GO:0006811), regulation of postsynaptic membrane potential (GO:0060078), excitatory postsynaptic potential (GO:0060079)
GO Molecular Function (7): excitatory extracellular ligand-gated monoatomic ion channel activity (GO:0005231), serotonin-gated monoatomic cation channel activity (GO:0022850), transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential (GO:1904315), transmembrane signaling receptor activity (GO:0004888), monoatomic ion channel activity (GO:0005216), extracellular ligand-gated monoatomic ion channel activity (GO:0005230), ligand-gated monoatomic ion channel activity (GO:0015276)
GO Cellular Component (8): plasma membrane (GO:0005886), cell surface (GO:0009986), neuron projection (GO:0043005), synapse (GO:0045202), postsynaptic membrane (GO:0045211), transmembrane transporter complex (GO:1902495), serotonin-activated cation-selective channel complex (GO:1904602), membrane (GO:0016020)
Reactome top-level categories
Rollup of top-2 pathways:
| Category | Pathways |
|---|---|
| Transmission across Chemical Synapses | 1 |
| Neuronal System | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| serotonin receptor activity | 2 |
| serotonin receptor signaling pathway | 2 |
| regulation of postsynaptic membrane potential | 2 |
| transmitter-gated monoatomic ion channel activity | 2 |
| cellular anatomical structure | 2 |
| signal transduction | 1 |
| cellular response to dopamine | 1 |
| anterograde trans-synaptic signaling | 1 |
| monoatomic ion transport | 1 |
| transmembrane transport | 1 |
| monoatomic ion transmembrane transport | 1 |
| regulation of biological quality | 1 |
| serotonin-gated monoatomic cation channel activity | 1 |
| ligand-gated ion channel signaling pathway | 1 |
| transport | 1 |
| regulation of membrane potential | 1 |
| chemical synaptic transmission, postsynaptic | 1 |
| extracellular ligand-gated monoatomic ion channel activity | 1 |
| excitatory postsynaptic potential | 1 |
| ligand-gated monoatomic cation channel activity | 1 |
| signaling receptor activity | 1 |
| monoatomic ion transmembrane transporter activity | 1 |
| channel activity | 1 |
| ligand-gated monoatomic ion channel activity | 1 |
| monoatomic ion channel activity | 1 |
| ligand-gated channel activity | 1 |
| membrane | 1 |
| cell periphery | 1 |
| plasma membrane bounded cell projection | 1 |
| cell junction | 1 |
| synaptic membrane | 1 |
| postsynapse | 1 |
| membrane protein complex | 1 |
| transporter complex | 1 |
| cation channel complex | 1 |
| serotonin receptor complex | 1 |
| neurotransmitter receptor complex | 1 |
Protein interactions and networks
STRING
700 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| HTR3B | HTR3A | P46098 | 978 |
| HTR3B | HTR3D | Q70Z44 | 874 |
| HTR3B | HTR3C | Q8WXA8 | 831 |
| HTR3B | HTR1E | P28566 | 696 |
| HTR3B | HTR7 | P34969 | 690 |
| HTR3B | HTR1B | P28222 | 676 |
| HTR3B | HTR1F | P30939 | 666 |
| HTR3B | SLC6A4 | P31645 | 664 |
| HTR3B | HTR2A | P28223 | 658 |
| HTR3B | HTR5A | P47898 | 655 |
| HTR3B | HTR2B | P41595 | 621 |
| HTR3B | HTR2C | P28335 | 619 |
| HTR3B | HTR1A | P08908 | 617 |
| HTR3B | HTR3E | A5X5Y0 | 611 |
| HTR3B | HTR1D | P28221 | 602 |
IntAct
4 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| HTR3A | HTR3B | psi-mi:“MI:0407”(direct interaction) | 0.500 |
| HTR3A | HTR3B | psi-mi:“MI:0403”(colocalization) | 0.500 |
| HTR3B | TMEM223 | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (19): LMF2 (Affinity Capture-MS), SCCPDH (Affinity Capture-MS), CYB5R1 (Affinity Capture-MS), NXPE3 (Affinity Capture-MS), GLRB (Affinity Capture-MS), PXYLP1 (Affinity Capture-MS), LRRC24 (Affinity Capture-MS), SLC9A1 (Affinity Capture-MS), RNASE7 (Affinity Capture-MS), ITPRIP (Affinity Capture-MS), BSCL2 (Affinity Capture-MS), POMT2 (Affinity Capture-MS), C3orf33 (Affinity Capture-MS), ABCB9 (Affinity Capture-MS), SLC15A4 (Affinity Capture-MS)
ESM2 similar proteins: A2A259, A5X5Y0, H2Q5A1, O46547, O70212, O95264, O97741, P01906, P01909, P02713, P02715, P02716, P04758, P04759, P04760, P07510, P09660, P09690, P11230, P13536, P18916, P20782, P23979, P25109, P25110, P35563, P37088, P37089, P46098, P55270, P78334, Q04844, Q07001, Q14246, Q5Y4N8, Q60HE8, Q61180, Q61549, Q70Z44, Q7Z418
Diamond homologs: A5X5Y0, O70212, O95264, P04757, P05376, P18845, P19370, P22770, P23979, P26153, P32297, P35563, P36544, P43143, P43679, P46098, P48182, P49581, P49582, P54131, Q05941, Q07263, Q15825, Q494W8, Q5IS76, Q68RJ7, Q70Z44, Q866A2, Q8R4G9, Q8WXA8, Q9I8C7, Q9JHJ5, Q9JJ16, A8WQK3, A8XNX8, O16926, O70174, O76554, P02716, P02717
SIGNOR signaling
2 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| serotonin | “up-regulates activity” | HTR3B | “chemical activation” |
| HTR3B | up-regulates | Excitatory_synaptic_transmission |
Disease & clinical
Clinical variants and AI predictions
ClinVar
84 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 74 |
| Likely benign | 5 |
| Benign | 2 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
1711 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 11:113909453:GTG:G | donor_gain | 1.0000 |
| 11:113931863:GAGTT:G | donor_gain | 1.0000 |
| 11:113931865:GTT:G | donor_gain | 1.0000 |
| 11:113931866:TT:T | donor_gain | 1.0000 |
| 11:113931868:G:GG | donor_gain | 1.0000 |
| 11:113932284:T:G | acceptor_gain | 1.0000 |
| 11:113932287:A:AG | acceptor_gain | 1.0000 |
| 11:113932287:AGTGT:A | acceptor_gain | 1.0000 |
| 11:113932288:G:GG | acceptor_gain | 1.0000 |
| 11:113932288:GT:G | acceptor_gain | 1.0000 |
| 11:113932288:GTGTG:G | acceptor_gain | 1.0000 |
| 11:113932934:A:AG | acceptor_gain | 1.0000 |
| 11:113932935:G:GA | acceptor_gain | 1.0000 |
| 11:113933007:GACA:G | donor_gain | 1.0000 |
| 11:113933011:G:GG | donor_gain | 1.0000 |
| 11:113943049:T:A | acceptor_gain | 1.0000 |
| 11:113944570:CAG:C | acceptor_loss | 1.0000 |
| 11:113944572:G:GA | acceptor_loss | 1.0000 |
| 11:113945901:GA:G | acceptor_gain | 1.0000 |
| 11:113909452:TGTGG:T | donor_loss | 0.9900 |
| 11:113909454:TGGTA:T | donor_loss | 0.9900 |
| 11:113909456:G:C | donor_loss | 0.9900 |
| 11:113909456:G:GG | donor_gain | 0.9900 |
| 11:113909457:T:G | donor_loss | 0.9900 |
| 11:113909458:A:C | donor_loss | 0.9900 |
| 11:113931752:TAACA:T | acceptor_loss | 0.9900 |
| 11:113931754:ACAG:A | acceptor_loss | 0.9900 |
| 11:113931755:CAGGT:C | acceptor_loss | 0.9900 |
| 11:113931756:A:T | acceptor_loss | 0.9900 |
| 11:113931866:TTG:T | donor_loss | 0.9900 |
AlphaMissense
2903 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 11:113943063:A:C | S260R | 0.980 |
| 11:113943065:C:A | S260R | 0.980 |
| 11:113943065:C:G | S260R | 0.980 |
| 11:113943033:A:C | S250R | 0.974 |
| 11:113943035:C:A | S250R | 0.974 |
| 11:113943035:C:G | S250R | 0.974 |
| 11:113932404:T:C | F162L | 0.971 |
| 11:113932406:T:A | F162L | 0.971 |
| 11:113932406:T:G | F162L | 0.971 |
| 11:113944611:A:C | S316R | 0.964 |
| 11:113944613:C:A | S316R | 0.964 |
| 11:113944613:C:G | S316R | 0.964 |
| 11:113931841:G:C | W114C | 0.955 |
| 11:113931841:G:T | W114C | 0.955 |
| 11:113932443:A:C | S175R | 0.955 |
| 11:113932445:C:A | S175R | 0.955 |
| 11:113932445:C:G | S175R | 0.955 |
| 11:113943107:G:C | K274N | 0.953 |
| 11:113943107:G:T | K274N | 0.953 |
| 11:113931761:T:A | W88R | 0.946 |
| 11:113931761:T:C | W88R | 0.946 |
| 11:113932410:T:C | F164L | 0.945 |
| 11:113932412:T:A | F164L | 0.945 |
| 11:113932412:T:G | F164L | 0.945 |
| 11:113931839:T:A | W114R | 0.943 |
| 11:113931839:T:C | W114R | 0.943 |
| 11:113933018:G:C | W207C | 0.943 |
| 11:113933018:G:T | W207C | 0.943 |
| 11:113931763:G:C | W88C | 0.941 |
| 11:113931763:G:T | W88C | 0.941 |
dbSNP variants (sampled 300 via entrez): RS1000086244 (11:113947345 G>A), RS1000149846 (11:113912624 T>G), RS1000188228 (11:113918412 C>T), RS1000272816 (11:113947479 C>T), RS1000292402 (11:113915675 T>C), RS1000351406 (11:113900554 C>T), RS1000358870 (11:113899509 A>T), RS1000414678 (11:113925056 G>A), RS1000427565 (11:113943373 A>G,T), RS1000471718 (11:113899122 G>A), RS1000554874 (11:113905805 A>G), RS1000589849 (11:113931076 A>AT), RS1000676391 (11:113942800 AT>A,ATT), RS1000708426 (11:113942433 T>C), RS1000767681 (11:113938059 C>A,G)
Disease associations
OMIM: gene MIM:604654 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
5 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST002606_17 | Prostate cancer | 3.000000e-08 |
| GCST002606_36 | Prostate cancer | 5.000000e-08 |
| GCST003140_1 | Chronic kidney disease | 5.000000e-06 |
| GCST010397_46 | Gut microbiota (bacterial taxa, rank normal transformation method) | 2.000000e-06 |
| GCST010397_55 | Gut microbiota (bacterial taxa, rank normal transformation method) | 3.000000e-06 |
EFO canonical traits (1, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0007874 | gut microbiome measurement |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (4): CHEMBL2094132 (PROTEIN COMPLEX GROUP), CHEMBL2096904 (PROTEIN FAMILY), CHEMBL2111332 (PROTEIN COMPLEX), CHEMBL3895 (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: 689,583 (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 |
|---|---|---|---|
| CHEMBL1112 | ARIPIPRAZOLE | 4 | 24,205 |
| CHEMBL1729 | CISAPRIDE | 4 | 14,365 |
| CHEMBL289469 | GRANISETRON | 4 | 431 |
| CHEMBL3 | NICOTINE | 4 | 184,969 |
| CHEMBL42 | CLOZAPINE | 4 | 37,581 |
| CHEMBL46 | ONDANSETRON | 4 | 41,386 |
| CHEMBL56564 | TROPISETRON | 4 | 19,312 |
| CHEMBL6437 | MIANSERIN | 4 | 14,778 |
| CHEMBL708 | ZIPRASIDONE | 4 | 21,536 |
| CHEMBL715 | OLANZAPINE | 4 | 40,057 |
| CHEMBL86 | METOCLOPRAMIDE | 4 | 37,825 |
| CHEMBL11 | IMIPRAMINE | 4 | 48,893 |
| CHEMBL1189679 | PALONOSETRON | 4 | 9,399 |
| CHEMBL39 | SEROTONIN | 3 | 186,160 |
| CHEMBL18041 | ZACOPRIDE | 2 | 1,760 |
| CHEMBL18772 | QUIPAZINE | 2 | 1,108 |
| CHEMBL2107804 | BEMESETRON | 2 | 1,019 |
| CHEMBL478 | CHLOROPHENYLPIPERAZINE | 2 | 3,138 |
| CHEMBL7257 | MEBUFOTENIN | 2 | 1,595 |
| CHEMBL214268 | PHA-543613 | 1 | 66 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
PharmGKB clinical annotations
5 annotations.
| Variant | Type | Level | Drugs | Phenotypes |
|---|---|---|---|---|
| rs11606194 | Toxicity | 3 | nicotine | Tobacco Use Disorder |
| rs1176744 | Toxicity | 4 | paroxetine | Mental Disorders |
| rs2276307 | Toxicity | 3 | atorvastatin;pravastatin;simvastatin | Myalgia |
| rs3758987 | Toxicity | 3 | heroin | Heroin Dependence |
| rs3758987 | Toxicity | 3 | nicotine | Tobacco Use Disorder |
PharmGKB variants
13 variants.
| Variant | Genes | Level | Score | #Clin annots | Drugs |
|---|---|---|---|---|---|
| rs1176744 | HTR3B | 4 | -0.25 | 1 | paroxetine |
| rs1176746 | HTR3B | 0.00 | 0 | ||
| rs2276305 | HTR3B | 0.00 | 0 | ||
| rs2276307 | HTR3B | 3 | 2.50 | 1 | atorvastatin;pravastatin;simvastatin |
| rs3758987 | HTR3B | 3 | 3.00 | 2 | heroin;nicotine |
| rs10789970 | HTR3B | 0.00 | 0 | ||
| rs11214763 | HTR3B | 0.00 | 0 | ||
| rs45460698 | HTR3B | 0.00 | 0 | ||
| rs7943062 | HTR3B | 0.00 | 0 | ||
| rs11606194 | HTR3B | 3 | 3.00 | 1 | nicotine |
| rs7103572 | HTR3B | 0.00 | 0 | ||
| rs3782025 | HTR3B | 0.00 | 0 | ||
| rs1672717 | HTR3B | 0.00 | 0 |
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: lgic — 5-HT3 receptors
Binding affinities (BindingDB)
4 measured of 4 human assays (4 total across all organisms); most potent 4 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value |
|---|---|---|
| 5’-phenyl-(2’R)-spiro[4-azabicyclo[2.2.2]octane-2,2’-furo[2,3-b]pyridine] | KI | 73 nM |
| [2,2’]Bithiophenyl-5-carboxylic acid (1-aza-bicyclo[2.2.2]oct-3-yl)-amide | KI | 1040 nM |
| N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]-5-phenylthiophene-2-carboxamide | KI | 2020 nM |
| 5-Phenyl-thiophene-2-carboxylic acid (1-aza-bicyclo[2.2.2]oct-3-yl)-amide | KI | 2020 nM |
ChEMBL bioactivities
334 potent at pChembl≥5 of 340 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 11.00 | Kd | 0.01 | nM | CHEMBL143197 |
| 10.70 | Kd | 0.01995 | nM | GRANISETRON |
| 10.60 | Kd | 0.02512 | nM | TROPISETRON |
| 10.60 | Kd | 0.02512 | nM | CHEMBL143197 |
| 10.20 | Kd | 0.0631 | nM | TROPISETRON |
| 10.15 | Ki | 0.071 | nM | CHEMBL325422 |
| 10.10 | Kd | 0.07943 | nM | ONDANSETRON |
| 10.10 | Kd | 0.07943 | nM | GRANISETRON |
| 10.10 | Kd | 0.07943 | nM | ZACOPRIDE |
| 10.09 | IC50 | 0.08128 | nM | CHEMBL416662 |
| 9.90 | Kd | 0.1259 | nM | GRANISETRON |
| 9.85 | Kd | 0.14 | nM | PALONOSETRON |
| 9.80 | Kd | 0.16 | nM | GRANISETRON |
| 9.80 | Kd | 0.1585 | nM | CHEMBL323208 |
| 9.80 | Kd | 0.1585 | nM | CHEMBL40935 |
| 9.74 | Kd | 0.18 | nM | PALONOSETRON |
| 9.70 | Kd | 0.2 | nM | GRANISETRON |
| 9.66 | Kd | 0.22 | nM | GRANISETRON |
| 9.64 | Ki | 0.23 | nM | CHEMBL43355 |
| 9.64 | Ki | 0.23 | nM | CHEMBL327197 |
| 9.64 | Kd | 0.23 | nM | PALONOSETRON |
| 9.60 | Kd | 0.25 | nM | GRANISETRON |
| 9.54 | IC50 | 0.2884 | nM | CHEMBL299634 |
| 9.49 | Ki | 0.32 | nM | CHEMBL111448 |
| 9.47 | Kd | 0.34 | nM | PALONOSETRON |
| 9.45 | IC50 | 0.3548 | nM | CHEMBL53416 |
| 9.41 | Ki | 0.39 | nM | CHEMBL111059 |
| 9.40 | Kd | 0.3981 | nM | ONDANSETRON |
| 9.36 | Ki | 0.44 | nM | CHEMBL113742 |
| 9.35 | IC50 | 0.4467 | nM | QUIPAZINE |
| 9.35 | Ki | 0.45 | nM | CHEMBL325349 |
| 9.33 | Ki | 0.47 | nM | CHEMBL113519 |
| 9.32 | Kd | 0.48 | nM | PALONOSETRON |
| 9.32 | Ki | 0.48 | nM | CHEMBL320480 |
| 9.30 | Kd | 0.5012 | nM | BEMESETRON |
| 9.29 | Ki | 0.51 | nM | CHEMBL315861 |
| 9.29 | Ki | 0.51 | nM | CHEMBL333371 |
| 9.24 | Ki | 0.58 | nM | CHEMBL112941 |
| 9.20 | Kd | 0.631 | nM | CHEMBL40324 |
| 9.20 | Kd | 0.631 | nM | ONDANSETRON |
| 9.17 | Ki | 0.68 | nM | CHEMBL112237 |
| 9.16 | Ki | 0.69 | nM | CHEMBL109322 |
| 9.15 | Ki | 0.7 | nM | CHEMBL13535 |
| 9.11 | Kd | 0.78 | nM | GRANISETRON |
| 9.10 | IC50 | 0.7943 | nM | CHEMBL49932 |
| 9.10 | IC50 | 0.7943 | nM | CHEMBL334923 |
| 9.08 | Ki | 0.83 | nM | CHEMBL287987 |
| 9.07 | Ki | 0.86 | nM | CHEMBL321477 |
| 9.06 | IC50 | 0.88 | nM | PALONOSETRON |
| 9.06 | Ki | 0.88 | nM | CHEMBL325235 |
PubChem BioAssay actives
297 with measured affinity, of 628 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 |
|---|---|---|---|---|
| 7-(4-prop-2-enylpiperazin-1-yl)-2,8,13-triazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaene | 6355: Binding affinity against 5-hydroxytryptamine 3 receptor was measured using [3H]granisetron as radioligand | ic50 | <0.0001 | uM |
| 1-methyl-N-(9-methyl-9-azabicyclo[3.3.1]nonan-3-yl)indazole-3-carboxamide | 6027: Potency at neuronal 5-hydroxytryptamine 3 receptor in the rabbit heart | kd | <0.0001 | uM |
| 7-(4-benzylpiperazin-1-yl)-2,8,13-triazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaene | 6355: Binding affinity against 5-hydroxytryptamine 3 receptor was measured using [3H]granisetron as radioligand | ic50 | <0.0001 | uM |
| 4-[4-(1,3-benzodioxol-5-ylmethyl)piperazin-1-yl]-7-chloropyrrolo[1,2-a]quinoxaline | 6355: Binding affinity against 5-hydroxytryptamine 3 receptor was measured using [3H]granisetron as radioligand | ic50 | 0.0001 | uM |
| (1-methylindol-3-yl)-(4,5,6,7-tetrahydro-3H-benzimidazol-5-yl)methanone | 5980: Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15 | ki | 0.0001 | uM |
| Ondansetron | 6027: Potency at neuronal 5-hydroxytryptamine 3 receptor in the rabbit heart | kd | 0.0001 | uM |
| Palonosetron | 1056977: Binding affinity to human 5-HT3B receptor H73A mutant after 24 hrs by liquid scintillation counting analysis | kd | 0.0001 | uM |
| [(1R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] 1H-indole-3-carboxylate | 6026: Binding affinity to 5-hydroxytryptamine 3 receptor of neuronal in the afferent rabbit vagus | kd | 0.0001 | uM |
| 4-(4-methylpiperazin-1-yl)pyrrolo[1,2-a]quinoxaline | 6335: Binding affinity towards 5-hydroxytryptamine 3 receptor | ki | 0.0002 | uM |
| 6-(4-methylpiperazin-1-yl)-7,8,9,10-tetrahydrophenanthridine | 6335: Binding affinity towards 5-hydroxytryptamine 3 receptor | ki | 0.0002 | uM |
| (2-methyl-4-oxo-2-azabicyclo[3.3.1]nonan-8-yl) 1H-indole-3-carboxylate | 6028: Potency at neuronal 5-hydroxytryptamine 3 receptors in the rabbit heart | kd | 0.0002 | uM |
| (4-oxo-2-azatricyclo[3.3.1.02,7]nonan-8-yl) 1H-indole-3-carboxylate | 200911: Potency was evaluated on rabbit heart serotonergic receptors | kd | 0.0002 | uM |
| 4-(4-benzylpiperazin-1-yl)-7-chloropyrrolo[1,2-a]quinoxaline | 6355: Binding affinity against 5-hydroxytryptamine 3 receptor was measured using [3H]granisetron as radioligand | ic50 | 0.0003 | uM |
| (8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 2-oxo-1-propan-2-ylquinoline-4-carboxylate | 5980: Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15 | ki | 0.0003 | uM |
| 4-(4-benzylpiperazin-1-yl)pyrrolo[1,2-a]quinoxaline | 6355: Binding affinity against 5-hydroxytryptamine 3 receptor was measured using [3H]granisetron as radioligand | ic50 | 0.0004 | uM |
| (8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 2-butoxyquinoline-4-carboxylate | 5980: Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15 | ki | 0.0004 | uM |
| (8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 2-(2-methylpropoxy)quinoline-4-carboxylate | 5980: Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15 | ki | 0.0004 | uM |
| (8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 2-oxo-1-propylquinoline-4-carboxylate | 5980: Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15 | ki | 0.0004 | uM |
| 2-piperazin-1-ylquinoline | 6355: Binding affinity against 5-hydroxytryptamine 3 receptor was measured using [3H]granisetron as radioligand | ic50 | 0.0004 | uM |
| (8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 1-(2-methylpropyl)-2-oxoquinoline-4-carboxylate | 5980: Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15 | ki | 0.0005 | uM |
| 7-fluoro-4-(4-methylpiperazin-1-yl)pyrrolo[1,2-a]quinoline | 6335: Binding affinity towards 5-hydroxytryptamine 3 receptor | ki | 0.0005 | uM |
| (8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 2-oxo-1-phenylquinoline-4-carboxylate | 5980: Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15 | ki | 0.0005 | uM |
| 1-butyl-4-hydroxy-N-(8-methyl-8-azabicyclo[3.2.1]octan-3-yl)-2-oxoquinoline-3-carboxamide | 5980: Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15 | ki | 0.0005 | uM |
| [(1R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] 3,5-dichlorobenzoate | 6027: Potency at neuronal 5-hydroxytryptamine 3 receptor in the rabbit heart | kd | 0.0005 | uM |
| (1,1-dimethylpiperidin-1-ium-4-yl)-(1H-indol-3-yl)methanone iodide | 6028: Potency at neuronal 5-hydroxytryptamine 3 receptors in the rabbit heart | kd | 0.0006 | uM |
| (8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 2-methoxyquinoline-4-carboxylate | 5980: Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15 | ki | 0.0006 | uM |
| 2-(3,4,5-trichlorophenyl)guanidine | 6339: Binding affinity to 5-HT3 serotonin receptor in NG 108-15 neuroblastoma glioma cells using [3H]GR-65630 radioligand. | ki | 0.0007 | uM |
| (8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 1-butyl-2-oxoquinoline-4-carboxylate | 5980: Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15 | ki | 0.0007 | uM |
| (8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 2-(2-methylpropyl)quinoline-4-carboxylate | 5980: Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15 | ki | 0.0007 | uM |
| 10-(4-methylpiperazin-1-yl)-9-azatetracyclo[11.2.1.02,11.03,8]hexadeca-2(11),3,5,7,9-pentaene | 6335: Binding affinity towards 5-hydroxytryptamine 3 receptor | ki | 0.0008 | uM |
| 7-[4-(1,3-benzodioxol-5-ylmethyl)piperazin-1-yl]-2,8,13-triazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaene | 6355: Binding affinity against 5-hydroxytryptamine 3 receptor was measured using [3H]granisetron as radioligand | ic50 | 0.0008 | uM |
| N,N-dimethyl-2-[(Z)-(3-methylthieno[2,3-b]pyrrolizin-8-ylidene)amino]oxyethanamine | 6316: Compound was tested for binding affinity towards 5-hydroxytryptamine 3 receptor | ic50 | 0.0008 | uM |
| 8-(4-prop-2-enylpiperazin-1-yl)-5-thia-1,7-diazatricyclo[7.3.0.02,6]dodeca-2(6),3,7,9,11-pentaene | 6355: Binding affinity against 5-hydroxytryptamine 3 receptor was measured using [3H]granisetron as radioligand | ic50 | 0.0009 | uM |
| (8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 2-pentoxyquinoline-4-carboxylate | 5980: Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15 | ki | 0.0009 | uM |
| (8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 2-ethoxyquinoline-4-carboxylate | 5980: Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15 | ki | 0.0009 | uM |
| 7-(4-methylpiperazin-1-yl)-2,8,13-triazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaene | 6355: Binding affinity against 5-hydroxytryptamine 3 receptor was measured using [3H]granisetron as radioligand | ic50 | 0.0010 | uM |
| (8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 3,5-dimethylbenzoate | 6027: Potency at neuronal 5-hydroxytryptamine 3 receptor in the rabbit heart | kd | 0.0010 | uM |
| (8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 2-oxo-1-pentylquinoline-4-carboxylate | 5980: Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15 | ki | 0.0010 | uM |
| 8-(4-benzylpiperazin-1-yl)-3-thia-1,7-diazatricyclo[7.3.0.02,6]dodeca-2(6),4,7,9,11-pentaene | 1855131: Binding affinity to 5-HT3 receptor (unknown origin) assessed as inhibition constant | ki | 0.0010 | uM |
| 1-azabicyclo[2.2.2]octan-3-yl 1H-indole-3-carboxylate | 6344: In vitro Binding affinity towards 5-hydroxytryptamine 3 receptor was determined | ki | 0.0011 | uM |
| Imipramine | 2198785: Inhibition of 5HT receptor (unknown origin) | ic50 | 0.0011 | uM |
| (8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 1-ethyl-2-oxoquinoline-4-carboxylate | 5980: Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15 | ki | 0.0011 | uM |
| (8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 1-hexyl-2-oxoquinoline-4-carboxylate | 5980: Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15 | ki | 0.0011 | uM |
| 8-[4-[(4-fluorophenyl)methyl]piperazin-1-yl]-5-thia-1,7-diazatricyclo[7.3.0.02,6]dodeca-2(6),3,7,9,11-pentaene | 6355: Binding affinity against 5-hydroxytryptamine 3 receptor was measured using [3H]granisetron as radioligand | ic50 | 0.0012 | uM |
| (8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 1-benzyl-2-oxoquinoline-4-carboxylate | 5980: Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15 | ki | 0.0013 | uM |
| 4-amino-N-[(4S,5R)-1-azabicyclo[3.3.1]nonan-4-yl]-5-chloro-2-methoxybenzamide | 6028: Potency at neuronal 5-hydroxytryptamine 3 receptors in the rabbit heart | kd | 0.0013 | uM |
| 4-hydroxy-N-(8-methyl-8-azabicyclo[3.2.1]octan-3-yl)-2-oxo-1-phenylquinoline-3-carboxamide | 5980: Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15 | ki | 0.0014 | uM |
| 7-piperazin-1-yl-2,8,13-triazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaene | 6355: Binding affinity against 5-hydroxytryptamine 3 receptor was measured using [3H]granisetron as radioligand | ic50 | 0.0015 | uM |
| N-(8-methyl-8-azabicyclo[3.2.1]octan-3-yl)-4-oxo-1H-quinoline-3-carboxamide | 5980: Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15 | ki | 0.0015 | uM |
| (8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 1-(3-methylbutyl)-2-oxoquinoline-4-carboxylate | 5980: Binding affinity towards [3H]quipazine labeled 5-hydroxytryptamine 3 receptor sites in HG108-15 | ki | 0.0015 | uM |
CTD chemical–gene interactions
18 total (human), top 18 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| bisphenol A | affects cotreatment, increases methylation, increases expression | 2 |
| CGP 52608 | affects binding, increases reaction | 1 |
| Resveratrol | affects cotreatment, decreases expression | 1 |
| Fulvestrant | affects cotreatment, increases methylation | 1 |
| Ethanol | affects binding, increases activity, increases reaction | 1 |
| 1-Propanol | affects binding, increases activity, increases reaction | 1 |
| Pentanols | affects binding, increases activity, increases reaction | 1 |
| Hexanols | affects binding, decreases reaction, increases activity | 1 |
| Octanols | increases activity, affects binding, decreases reaction | 1 |
| Arsenic | affects methylation | 1 |
| Benzo(a)pyrene | affects methylation | 1 |
| Copper | affects cotreatment, decreases expression | 1 |
| Dopamine | affects binding, increases activity | 1 |
| Serotonin | affects binding, increases activity, increases reaction, decreases reaction | 1 |
| Aflatoxin B1 | increases methylation | 1 |
| Hydroxymethylglutaryl-CoA Reductase Inhibitors | increases response to substance | 1 |
| Okadaic Acid | decreases expression | 1 |
| 1-Butanol | affects binding, increases activity, increases reaction | 1 |
ChEMBL screening assays
194 unique, capped per target: 129 binding, 64 functional, 1 admet
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL4368604 | Binding | Displacement of [3H]BRL 43694 from recombinant human 5-HT3 receptor at 10 uM after 120 mins by radiometric scintillation analysis relative to control | Design, synthesis and evaluation of activity and pharmacokinetic profile of new derivatives of xanthone and piperazine in the central nervous system. — Bioorg Med Chem Lett |
| CHEMBL615717 | Functional | Compound was tested for agonistic activity against 5-HT uptake | First tricyclic oximino derivatives as 5-HT3 ligands. — Bioorg Med Chem Lett |
| CHEMBL4413391 | ADMET | Antagonist activity at serotonin receptor in human PBMC assessed as inhibition of PMA-stimulated superoxide anion generation at 10 uM preincubated for 1 hr followed by PMA-stimulation and measured after 30 mins by spectrophotometric method | Identification of a novel DGKα inhibitor for XLP-1 therapy by virtual screening. — Eur J Med Chem |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.