OXTR

Summary

OXTR (oxytocin receptor, HGNC:8529) is a protein-coding gene on chromosome 3p25.3, encoding Oxytocin receptor (P30559). Receptor for oxytocin.

The protein encoded by this gene belongs to the G-protein coupled receptor family and acts as a receptor for oxytocin. Its activity is mediated by G proteins which activate a phosphatidylinositol-calcium second messenger system. The oxytocin-oxytocin receptor system plays an important role in the uterus during parturition.

Source: NCBI Gene 5021 — RefSeq curated summary.

At a glance

• GWAS associations: 5
• Clinical variants (ClinVar): 104 total — 1 pathogenic, 1 likely-pathogenic
• Druggable target: yes — 15 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_000916

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:8529
Approved symbol	OXTR
Name	oxytocin receptor
Location	3p25.3
Locus type	gene with protein product
Status	Approved
Aliases	OTR
Ensembl gene	ENSG00000180914
Ensembl biotype	protein_coding
OMIM	167055
Entrez	5021

Gene structure

Transcript identifiers

Ensembl transcripts: 8 — 7 protein_coding, 1 retained_intron

ENST00000316793, ENST00000431493, ENST00000449615, ENST00000474615, ENST00000894689, ENST00000894690, ENST00000894691, ENST00000894692

RefSeq mRNA: 5 — MANE Select: NM_000916 NM_000916, NM_001354653, NM_001354654, NM_001354655, NM_001354656

CCDS: CCDS2570

Canonical transcript exons

ENST00000316793 — 4 exons

Exon	Start	End
ENSE00001217148	8750381	8753224
ENSE00001323116	8767266	8768329
ENSE00001337891	8768496	8768591
ENSE00001915371	8769231	8769613

Expression profiles

Bgee: expression breadth ubiquitous, 204 present calls, max score 93.34.

FANTOM5 (CAGE): breadth broad, TPM avg 6.1489 / max 284.3299, expressed in 755 samples.

FANTOM5 promoters (12 alternative TSS)

Promoter ID	TPM avg	Samples expressed
40950	2.1838	338
40947	1.9909	517
40948	0.9430	287
40949	0.3641	95
40945	0.2145	107
40944	0.1041	54
40946	0.0929	46
40941	0.0770	35
40940	0.0679	45
40943	0.0523	22

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
decidua	UBERON:0002450	93.34	gold quality
bronchial epithelial cell	CL:0002328	93.33	gold quality
epithelium of mammary gland	UBERON:0003244	92.66	gold quality
mammary duct	UBERON:0001765	92.56	gold quality
epithelium of bronchus	UBERON:0002031	92.56	gold quality
bronchus	UBERON:0002185	91.68	gold quality
buccal mucosa cell	CL:0002336	90.32	gold quality
stromal cell of endometrium	CL:0002255	90.30	gold quality
mucosa of paranasal sinus	UBERON:0005030	89.06	gold quality
mammary gland	UBERON:0001911	86.21	gold quality
thoracic mammary gland	UBERON:0005200	86.07	gold quality
medial globus pallidus	UBERON:0002477	84.84	gold quality
substantia nigra pars reticulata	UBERON:0001966	83.71	gold quality
globus pallidus	UBERON:0001875	81.79	gold quality
substantia nigra pars compacta	UBERON:0001965	80.77	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	78.39	gold quality
substantia nigra	UBERON:0002038	77.05	gold quality
nasal cavity epithelium	UBERON:0005384	76.03	gold quality
midbrain	UBERON:0001891	75.62	gold quality
cartilage tissue	UBERON:0002418	75.55	gold quality
epithelium of nasopharynx	UBERON:0001951	74.84	gold quality
ganglionic eminence	UBERON:0004023	74.37	gold quality
nucleus accumbens	UBERON:0001882	73.85	gold quality
dorsal motor nucleus of vagus nerve	UBERON:0002870	73.28	gold quality
saphenous vein	UBERON:0007318	72.87	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	72.67	gold quality
hypothalamus	UBERON:0001898	72.51	gold quality
Brodmann (1909) area 23	UBERON:0013554	72.39	gold quality
CA1 field of hippocampus	UBERON:0003881	72.04	silver quality
middle temporal gyrus	UBERON:0002771	71.99	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-GEOD-124858	no	1106.77
E-ANND-3	no	3.40

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): AP1, CEBPA, CEBPB, CEBPG, ESR1, ESR2, FOS, GABPA, GABPB1, JUN, MAFF, NFKB, PGR, RELA, SP1, TBPL1, TBXT, THRA, ZEB1, ZEB2

miRNA regulators (miRDB)

76 targeting OXTR, 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-6867-5P	100.00	82.21	3464
HSA-MIR-9-5P	100.00	72.28	2361
HSA-MIR-3185	99.99	68.12	1959
HSA-MIR-4531	99.99	69.70	3181
HSA-MIR-33A-5P	99.99	68.62	1055
HSA-MIR-33B-5P	99.99	68.58	1062
HSA-MIR-520D-5P	99.98	73.34	4883
HSA-MIR-524-5P	99.98	73.43	4882
HSA-MIR-4789-5P	99.98	70.76	2721
HSA-MIR-507	99.97	70.11	1915
HSA-MIR-557	99.96	70.01	1640
HSA-MIR-548AT-5P	99.96	70.83	2666
HSA-MIR-767-5P	99.95	70.85	993
HSA-MIR-335-3P	99.93	73.36	4958
HSA-MIR-552-5P	99.93	68.56	1583
HSA-MIR-3682-5P	99.93	67.97	1163
HSA-MIR-589-3P	99.91	69.62	2088
HSA-MIR-6809-3P	99.91	71.45	3814
HSA-MIR-627-3P	99.90	71.42	3316
HSA-MIR-153-5P	99.89	73.86	6317
HSA-MIR-629-3P	99.85	67.99	1875
HSA-MIR-576-5P	99.84	70.46	2582
HSA-MIR-5010-3P	99.83	70.60	2357
HSA-MIR-3133	99.81	70.92	3506
HSA-MIR-4694-3P	99.79	69.53	2640
HSA-MIR-3680-3P	99.75	72.51	3095
HSA-MIR-4446-5P	99.72	69.19	2544
HSA-MIR-4755-5P	99.71	70.34	2716
HSA-MIR-5006-3P	99.71	70.26	2728
HSA-MIR-4729	99.69	72.18	4233

Literature-anchored findings (GeneRIF, showing 40)

• The role of the N-terminus of the oxytocin receptor in high-affinity agonist binding has been characterized in detail, revealing that a single residue, Arg34, provides the agonist-specific epitope within this domain. (PMID:11955056)
• oxytocin receptors are present on human osteoblast-like cells; when oxytocin binds, it decreases IL-6 production, which may affect bone metabolism in humans (PMID:12126740)
• identification, localization and functional activity of oxytocin receptors in epididymis (PMID:12161007)
• estradiol and progesterone not only regulate oxytocin receptor expression and binding in normal mammary myoepithelium but also in malignant mammary cell lines (PMID:12166628)
• expressed in osteoclast cell cultures (PMID:12270111)
• oxytocin receptor activation of a Gbetagamma-mediated pathway as a consequence of Galpha(q) activation in myometrium and OTR-COSM6 cells that results in increased ERK1/2-P. (PMID:12810550)
• Oxytocin receptor is spatially regulated, with significantly greater expression in the fundal region of the uterus at term (PMID:12843193)
• depending on their localization, oxytocin receptors transactivate EGFR and activate ERK1/2 using different signalling intermediates. The final outcome is a different temporal pattern of EGFR and ERK1/2 phosphorylation (PMID:12955084)
• Oxytocin receptor forms homodimers and oligomers in the cell model used and that these oligomers are present at the cell surface. (PMID:14664707)
• Oxytocin receptor is expressed in penis ata concentration similar to that present in other portions of male genital tract and mediates corpus cavernosum contractility. (PMID:14691010)
• Oxytocin receptor antagonist reduced peak tension to 43%+/-12% of its original value without affecting peak calcium. (PMID:14749664)
• Three amino acids in the hydrophilic face of helix 8 of OTR are important to its role in preserving the receptor conformation that is necessary for ligand binding and stimulation of G-protein-mediated phospholipase C activation. (PMID:15035619)
• Data demonstrate that the dynamics of oxytocin receptor expression can be modulated by stimulation with estradiol and oxytocin in both the pregnant and non-pregnant uterus. (PMID:15044599)
• the oxytocin receptor localization in lipid rafts enriched in caveolin-1 turns the inhibition of cell growth into a proliferative response, eliciting different epidermal growth factor receptor/mitogen-activated protein kinase activation patterns. (PMID:15089975)
• the human oxytocin receptor forms dimeric and oligomeric complexes in vivo in intact living cells, and that these complexes exist at the cell surface level. (PMID:15089977)
• OT and OT-receptor mRNAs are expressed throughout the GI tract (PMID:15093695)
• Oxytocin receptor is highly expressed in the penis during fetal life and modulates migration and proliferation of its smooth muscle cells. (PMID:15591449)
• atosiban acts as a “biased agonist” of the human oxytocin receptors (PMID:15705593)
• Oxytocin receptor is expressed in smooth muscle cells and epithelial cells of peritoneal endometriotic lesions and ovarian endometriotic cysts (PMID:15831296)
• The oxytocin receptor DRY motif, besides playing a crucial role in receptor activation, may also be implicated in receptor promiscuity (PMID:16042376)
• molecular dynamics analysis of mechanism of desmopressin binding in vasopressin V2 receptor versus vasopressin V1a and oxytocin receptors (PMID:16333859)
• results suggest elevation of IL1 in myometrium at the end of pregnancy initiates process of down-regulation of oxytocin receptors in advanced labour resulting in desensitization of the myometrium to elevated levels of oxytocin in blood during lactation (PMID:16888077)
• increasing cell cholesterol levels is not sufficient per se to affect OTR signaling (PMID:16966388)
• Specific amino acids in the RVSSVKL segment in the COOH-terminal region of the third intracellular domain of oxytocin receptor influence the ability of OTR to activate G protein-mediated actions. (PMID:17148753)
• These findings provide support for association of OXTR with autism in a Caucasian population. (PMID:17383819)
• Changes in prostatic concentrations of oxytocin (OT) that occur with aging and malignant disease may act to facilitate cell proliferation. Localization of oxytocin receptor within the plasma membrane modulates OT’s proliferative response in the prostate. (PMID:17492653)
• Melatonin, like oxytocin, can negatively regulate oxytocin receptor transcription in human myometrial cells via modulation of protein kinase C signaling (PMID:17726073)
• This study showing that SNPs and haplotypes in the OXTR gene confer risk for ASD. (PMID:17893705)
• study is the first to report associations between AVPR1A and OXTR genetic variation with life history traits in humans (PMID:17939166)
• OTR staining occurred in most of these cells in myomas, while controls contained only scattered cells positive for OTR (PMID:17952758)
• A lower oxytocin receptor gene expression at mid-cycle could be involved in the aetiology of primary dysmenorrhoea. (PMID:18082926)
• The resulting pattern of findings confirmed the hypotheses of the significance of the genes involved in the development of affiliative behaviors in the manifestation of ASD, the strongest results were obtained for allelic associations with the OXTR genes. (PMID:18207134)
• Androgen dependent prostate growth in benign prostate hyperplasia may be linked to the interaction of androgen binding protein and oxytocin receptor, associated with caveolin 1 (PMID:18312604)
• Melatonin synergizes with oxytocin to promote myometrial cell contractions in vitro, which in vivo would promote coordinated and forceful contractions of the late term pregnant uterus necessary for parturition. (PMID:19001515)
• Controlling for maternal education, depression and marital discord, OXTR genes were significantly associated with maternal sensitivity. Mothers with OXTR AA or AG genotypes were less sensitive than mothers with the GG genotype. (PMID:19015103)
• OTRs are capable of very efficient and complete resensitization due to receptor recycling via the rab4/rab5 short cycle (PMID:19126785)
• Oxytocin, its receptor and the PGF(2alpha) receptor are involved in the regulation of labour through a paracrine mechanism. (PMID:19347709)
• A role is supported for oxytocin receptor haplotypes in the generation of affectivity, emotional loneliness and intelligence quotient. (PMID:19376182)
• oxytocin receptor responsiveness is regulated by G protein-coupled receptor kinase 6 in human myometrial smooth muscle (PMID:19423652)
• The gene encoding the related oxytocin receptor (OXTR) was tested for association with the Dictator Game and a related paradigm, the Social Values Orientation (SVO) task. (PMID:19461999)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	oxtra	ENSDARG00000033956
danio_rerio	oxtrb	ENSDARG00000044175
mus_musculus	Oxtr	ENSMUSG00000049112
rattus_norvegicus	Oxtr	ENSRNOG00000005806
drosophila_melanogaster	CCAP-R	FBGN0039396

Paralogs (16): NPFFR2 (ENSG00000056291), GNRHR (ENSG00000109163), CCKBR (ENSG00000110148), HCRTR1 (ENSG00000121764), AVPR2 (ENSG00000126895), GALR3 (ENSG00000128310), HCRTR2 (ENSG00000137252), NPFFR1 (ENSG00000148734), CCKAR (ENSG00000163394), AVPR1A (ENSG00000166148), GALR1 (ENSG00000166573), GPR22 (ENSG00000172209), GPR150 (ENSG00000178015), FFAR4 (ENSG00000186188), QRFPR (ENSG00000186867), AVPR1B (ENSG00000198049)

Protein

Protein identifiers

Oxytocin receptor — P30559 (reviewed: P30559)

All UniProt accessions (4): B2R9L7, C9JN09, C9JQC4, P30559

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for oxytocin. The activity of this receptor is mediated by G proteins which activate a phosphatidylinositol-calcium second messenger system.

Subcellular location. Cell membrane.

Similarity. Belongs to the G-protein coupled receptor 1 family. Vasopressin/oxytocin receptor subfamily.

RefSeq proteins (5): NP_000907, NP_001341582, NP_001341583, NP_001341584, NP_001341585 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR001817	Vasoprsn_rcpt	Family
IPR002062	Oxytocn_rcpt	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (49 total): helix 13, topological domain 8, transmembrane region 7, strand 5, glycosylation site 3, turn 3, region of interest 2, modified residue 2, sequence variant 2, chain 1, compositionally biased region 1, disulfide bond 1, sequence conflict 1

Structure

Experimental structures (PDB)

3 structures.

PDB	Method	Resolution (Å)
7RYC	ELECTRON MICROSCOPY	2.9
6TPK	X-RAY DIFFRACTION	3.2
7QVM	ELECTRON MICROSCOPY	3.25

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P30559-F1	79.87	0.54

Antibody-complex structures (SAbDab): 2 — 7QVM, 7RYC

Functional residue map

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

Post-translational modifications (2): 366, 368

Disulfide bonds (1): 112–187

Glycosylation sites (3): 8, 15, 26

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

ID	Pathway
R-HSA-388479	Vasopressin-like receptors
R-HSA-416476	G alpha (q) signalling events

MSigDB gene sets: 157 (showing top): GSE45365_CTRL_VS_MCMV_INFECTION_NK_CELL_UP, TGGTGCT_MIR29A_MIR29B_MIR29C, GOBP_REGULATION_OF_BLOOD_PRESSURE, GOBP_CIRCULATORY_SYSTEM_PROCESS, PEREZ_TP63_TARGETS, MODULE_64, GOBP_REGULATION_OF_SYSTEMIC_ARTERIAL_BLOOD_PRESSURE, GOBP_REGULATION_OF_ANATOMICAL_STRUCTURE_SIZE, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, GOBP_POSITIVE_REGULATION_OF_VASOCONSTRICTION, GOBP_CELLULAR_RESPONSE_TO_HORMONE_STIMULUS, GOBP_MUSCLE_CONTRACTION, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, GOBP_SECRETION, GOBP_PARTURITION

GO Biological Process (14): regulation of systemic arterial blood pressure by vasopressin (GO:0001992), muscle contraction (GO:0006936), cell surface receptor signaling pathway (GO:0007166), G protein-coupled receptor signaling pathway (GO:0007186), female pregnancy (GO:0007565), lactation (GO:0007595), cellular response to hormone stimulus (GO:0032870), positive regulation of blood pressure (GO:0045777), positive regulation of vasoconstriction (GO:0045907), maternal process involved in parturition (GO:0060137), positive regulation of cold-induced thermogenesis (GO:0120162), system process (GO:0003008), signal transduction (GO:0007165), regulation of biological quality (GO:0065008)

GO Molecular Function (3): oxytocin receptor activity (GO:0004990), vasopressin receptor activity (GO:0005000), G protein-coupled receptor activity (GO:0004930)

GO Cellular Component (2): plasma membrane (GO:0005886), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
Peptide ligand-binding receptors	1
GPCR downstream signalling	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
signal transduction	2
positive regulation of multicellular organismal process	2
G protein-coupled peptide receptor activity	2
regulation of systemic arterial blood pressure by hormone	1
muscle system process	1
G protein-coupled receptor activity	1
multi-organism reproductive process	1
multi-multicellular organism process	1
body fluid secretion	1
mammary gland development	1
milk ejection reflex	1
response to hormone	1
cellular response to chemical stimulus	1
cellular response to endogenous stimulus	1
regulation of blood pressure	1
regulation of vasoconstriction	1
vasoconstriction	1
parturition	1
multicellular organismal reproductive process	1
cold-induced thermogenesis	1
regulation of cold-induced thermogenesis	1
multicellular organismal process	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
biological regulation	1
transmembrane signaling receptor activity	1
G protein-coupled receptor signaling pathway	1
membrane	1
cell periphery	1
cellular anatomical structure	1

Protein interactions and networks

STRING

1382 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
OXTR	OXT	P01178	999
OXTR	GNAQ	P50148	953
OXTR	AVP	P01185	830
OXTR	ESR2	Q92731	791
OXTR	DRD2	P14416	744
OXTR	ESR1	P03372	735
OXTR	CD38	P28907	727
OXTR	CRH	P06850	724
OXTR	GJA1	P17302	703
OXTR	SLC6A4	P31645	690
OXTR	MAFF	Q9ULX9	688
OXTR	FKBP5	Q13451	687
OXTR	DRD4	P21917	658
OXTR	AVPR1A	P37288	632
OXTR	ARRB1	P49407	632

IntAct

23 interactions, top by confidence:

A	B	Type	Score
HTR2A	OXTR	psi-mi:“MI:2364”(proximity)	0.380
OXTR	HTR2A	psi-mi:“MI:0403”(colocalization)	0.380
DRD2	OXTR	psi-mi:“MI:0403”(colocalization)	0.380
DRD2	OXTR	psi-mi:“MI:2364”(proximity)	0.380
GHSR	OXTR	psi-mi:“MI:0403”(colocalization)	0.380
GHSR	OXTR	psi-mi:“MI:2364”(proximity)	0.380
ALAS1	OXTR	psi-mi:“MI:0915”(physical association)	0.370
ASH1L	OXTR	psi-mi:“MI:0915”(physical association)	0.370
CD81	OXTR	psi-mi:“MI:0915”(physical association)	0.370
EMC10	OXTR	psi-mi:“MI:0915”(physical association)	0.370
CYFIP2	OXTR	psi-mi:“MI:0915”(physical association)	0.370
MVB12A	OXTR	psi-mi:“MI:0915”(physical association)	0.370
FSCN1	OXTR	psi-mi:“MI:0915”(physical association)	0.370
LCNL1	OXTR	psi-mi:“MI:0915”(physical association)	0.370
PSMA7	OXTR	psi-mi:“MI:0915”(physical association)	0.370
SIRT2	OXTR	psi-mi:“MI:0915”(physical association)	0.370
TSPAN7	OXTR	psi-mi:“MI:0915”(physical association)	0.370
THOC5	OXTR	psi-mi:“MI:0915”(physical association)	0.370
TMEM161A	OXTR	psi-mi:“MI:0915”(physical association)	0.370
YIPF3	OXTR	psi-mi:“MI:0915”(physical association)	0.370
E5	ESYT2	psi-mi:“MI:0914”(association)	0.350
OXTR	OXTR	psi-mi:“MI:2364”(proximity)	0.270

BioGRID (15): ALAS1 (Two-hybrid), ASH1L (Two-hybrid), CD81 (Two-hybrid), EMC10 (Two-hybrid), CYFIP2 (Two-hybrid), MVB12A (Two-hybrid), FSCN1 (Two-hybrid), LCNL1 (Two-hybrid), PSMA7 (Two-hybrid), SIRT2 (Two-hybrid), TSPAN7 (Two-hybrid), THOC5 (Two-hybrid), TMEM161A (Two-hybrid), YIPF3 (Two-hybrid), OXTR (Affinity Capture-MS)

ESM2 similar proteins: O18821, O42329, P05363, P0C0L6, P16610, P21452, P30549, P30559, P30560, P30968, P30969, P32236, P32237, P32306, P37288, P47751, P47901, P48043, P48974, P49922, P51144, P56449, P56494, P70536, P79218, P97926, Q01776, Q19PY9, Q28756, Q56H79, Q5DUB2, Q62463, Q64077, Q6W5P4, Q7T3Q7, Q868T3, Q8BZP8, Q8CH60, Q90252, Q90334

Diamond homologs: O02300, O08858, O42329, O77808, O88721, P0C0L6, P30518, P30559, P30560, P30938, P31391, P32306, P32307, P35346, P37288, P47901, P48043, P48044, P48974, P56449, P56494, P70536, P97926, Q00788, Q28756, Q56H79, Q5WA50, Q62463, Q6TAC8, Q75W84, Q7YW31, Q868T3, Q8BZP8, Q90252, Q90334, Q90352, Q9WTV8, Q9WTV9, Q9WU02, P08588

SIGNOR signaling

15 interactions.

A	Effect	B	Mechanism
Oxytocin	up-regulates	OXTR	binding
OXTR	“up-regulates activity”	GNAS	binding
OXTR	“up-regulates activity”	GNAL	binding
OXTR	“up-regulates activity”	GNAI1	binding
OXTR	“up-regulates activity”	GNAI3	binding
OXTR	“up-regulates activity”	GNAQ	binding
OXTR	“up-regulates activity”	GNA14	binding
oxytocin	“up-regulates activity”	OXTR	“chemical activation”
Oxytocin	“up-regulates activity”	OXTR	binding
PDPK1	“up-regulates activity”	OXTR	phosphorylation
OXTR	“up-regulates activity”	DRD2	binding
GRK2	“down-regulates activity”	OXTR	phosphorylation

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	1
Likely pathogenic	1
Uncertain significance	70
Likely benign	14
Benign	10

Top pathogenic / likely-pathogenic (2)

Variant ID	HGVS	Classification
8294	NM_033337.3(CAV3):c.253G>A (p.Ala85Thr)	Pathogenic
499100	NM_033337.3(CAV3):c.366dup (p.Leu123fs)	Likely pathogenic

SpliceAI

544 predictions. Top by Δscore:

Variant	Effect	Δscore
3:8753220:CGAGG:C	acceptor_gain	1.0000
3:8753222:AGG:A	acceptor_gain	1.0000
3:8753225:C:CC	acceptor_gain	1.0000
3:8753233:G:C	acceptor_gain	1.0000
3:8753233:G:GC	acceptor_gain	1.0000
3:8753240:C:CT	acceptor_gain	1.0000
3:8753241:A:T	acceptor_gain	1.0000
3:8767268:T:TA	donor_gain	1.0000
3:8769378:A:AC	donor_gain	1.0000
3:8769379:C:CC	donor_gain	1.0000
3:8753222:AGGCT:A	acceptor_loss	0.9900
3:8753223:GG:G	acceptor_gain	0.9900
3:8753225:CT:C	acceptor_loss	0.9900
3:8769218:AGCAC:A	donor_gain	0.9900
3:8769266:C:CA	donor_gain	0.9900
3:8769267:C:A	donor_gain	0.9900
3:8769365:G:C	donor_gain	0.9900
3:8753221:GAGG:G	acceptor_gain	0.9800
3:8768497:T:TA	donor_gain	0.9800
3:8768592:C:CC	acceptor_gain	0.9800
3:8768423:T:C	donor_gain	0.9700
3:8769217:TAGC:T	donor_gain	0.9700
3:8769218:AGCA:A	donor_gain	0.9700
3:8769226:GCTAC:G	donor_loss	0.9700
3:8769228:TA:T	donor_loss	0.9700
3:8769229:A:AT	donor_loss	0.9700
3:8768328:CC:C	acceptor_gain	0.9600
3:8768329:CC:C	acceptor_gain	0.9600
3:8769231:C:G	donor_loss	0.9600
3:8767365:TG:T	donor_gain	0.9500

AlphaMissense

2519 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
3:8767663:G:C	F175L	0.998
3:8767663:G:T	F175L	0.998
3:8767665:A:G	F175L	0.998
3:8767853:C:G	C112S	0.998
3:8767854:A:T	C112S	0.998
3:8753168:A:G	W327R	0.997
3:8753168:A:T	W327R	0.997
3:8753181:G:C	S322R	0.997
3:8753181:G:T	S322R	0.997
3:8753183:T:G	S322R	0.997
3:8753190:G:C	S319R	0.997
3:8753190:G:T	S319R	0.997
3:8753192:T:G	S319R	0.997
3:8767627:G:C	C187W	0.997
3:8767628:C:T	C187Y	0.997
3:8767853:C:T	C112Y	0.997
3:8767873:G:C	F105L	0.997
3:8767873:G:T	F105L	0.997
3:8767875:A:G	F105L	0.997
3:8767942:G:C	S82R	0.997
3:8767942:G:T	S82R	0.997
3:8767944:T:G	S82R	0.997
3:8767336:G:C	F284L	0.996
3:8767336:G:T	F284L	0.996
3:8767338:A:G	F284L	0.996
3:8767628:C:G	C187S	0.996
3:8767629:A:T	C187S	0.996
3:8767664:A:C	F175C	0.996
3:8767684:G:C	S168R	0.996
3:8767684:G:T	S168R	0.996

dbSNP variants (sampled 300 via entrez): RS1000018443 (3:8761794 G>A), RS1000111300 (3:8741524 G>A,C), RS1000136584 (3:8767555 C>A), RS1000220271 (3:8746762 T>A,C), RS1000351981 (3:8744012 A>C,G), RS1000454283 (3:8744407 T>C), RS1000584092 (3:8757698 A>C,G,T), RS1000669024 (3:8746621 T>C), RS1000689596 (3:8745260 G>A), RS1000858546 (3:8766317 C>A), RS1000934937 (3:8758016 G>A), RS1000970794 (3:8763141 C>T), RS1000992734 (3:8760869 G>A), RS1001015577 (3:8771495 C>T), RS1001184175 (3:8762291 G>A)

Disease associations

OMIM: gene MIM:167055 | disease phenotypes: MIM:192600, MIM:611818, MIM:614321, MIM:606072, MIM:612285

GenCC curated gene-disease

Mondo (9): long QT syndrome (MONDO:0002442), hypertrophic cardiomyopathy 1 (MONDO:0008647), long QT syndrome 9 (MONDO:0012736), distal myopathy, Tateyama type (MONDO:0013686), rippling muscle disease 2 (MONDO:0019947), cardiomyopathy (MONDO:0004994), caveolinopathy (MONDO:0016146), Joubert syndrome 9 (MONDO:0012849), familial hypertrophic cardiomyopathy (MONDO:0024573)

Orphanet (10): Romano-Ward syndrome (Orphanet:101016), Autosomal dominant limb-girdle muscular dystrophy type 1C (Orphanet:265), Distal myopathy, Tateyama type (Orphanet:488650), Congenital long QT syndrome (Orphanet:768), Rare cardiomyopathy (Orphanet:167848), Qualitative or quantitative defects of caveolin-3 (Orphanet:207078), Joubert syndrome with oculorenal defect (Orphanet:2318), Rare familial disorder with hypertrophic cardiomyopathy (Orphanet:99739), Rippling muscle disease (Orphanet:97238), NON RARE IN EUROPE: Familial isolated hypertrophic cardiomyopathy (Orphanet:155)

HPO phenotypes

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

GWAS associations

5 associations (top):

Study	Trait	p-value
GCST001313_1	Depression and alcohol dependence	2.000000e-06
GCST003606_1	Liver fibrosis severity in HIV/hepatitis C co-infection	1.000000e-09
GCST004970_3	Caudate activity during reward	3.000000e-07
GCST007565_104	Morning person	6.000000e-15
GCST007576_300	Chronotype	6.000000e-15

EFO canonical traits (3, from GWAS)

EFO ID	Trait name
EFO:0008387	caudate nucleus measurement
EFO:0008396	response to reward
EFO:0008328	chronotype measurement

MeSH disease descriptors (5)

Descriptor	Name	Tree numbers
D009202	Cardiomyopathies	C14.280.238
D024741	Cardiomyopathy, Hypertrophic, Familial	C14.280.238.100.500; C14.280.484.048.750.070.160.500; C16.320.160
D008133	Long QT Syndrome	C14.280.067.565; C14.280.123.625; C16.131.240.400.715; C23.550.073.547
C567364	Joubert Syndrome 9 (supp.)
C567515	Long Qt Syndrome 9 (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL2049 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

15 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 61,673 (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
CHEMBL1429	DESMOPRESSIN	4	122
CHEMBL3301668	CARBETOCIN	4	1,721
CHEMBL373742	VASOPRESSIN	4	7,202
CHEMBL382301	ATOSIBAN	4	2,367
CHEMBL395429	OXYTOCIN	4	41,727
CHEMBL420762	MOZAVAPTAN	4	244
CHEMBL1254025	NOLASIBAN	3	100
CHEMBL276711	SEMAXANIB	3	6,180
CHEMBL429736	RETOSIBAN	3	99
CHEMBL49429	LIXIVAPTAN	3	319
CHEMBL1817709	SELEPRESSIN	2	86
CHEMBL1819440	ORNIPRESSIN	2	1,274
CHEMBL2037511	EPELSIBAN	2	83
CHEMBL4594444	PECAVAPTAN	2	48
CHEMBL582857	NELIVAPTAN	2	101

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Vasopressin and oxytocin receptors

Most potent curated ligand interactions (53 total), top 25:

Ligand	Action	Affinity	Parameter
[35S]non-peptide OT antagonist	Antagonist	10.38	pKd
d(CH2)5[Tyr(Me)2,Thr4,Tyr(3125I)-NH29]OVT	Antagonist	10.0	pKd
d(CH2)5[Tyr(Me)2,Thr4,Tyr-NH29]OVT	Antagonist	10.0	pKi
[125I]d(CH2)5[Tyr(Me)2,Thr4,Orn8,Tyr-NH29]OVT	Antagonist	10.0	pKd
oxytocin	Full agonist	9.6	pKi
d(CH2)5[Tyr(Me)2,Thr4,Phe(3125I,4N3)-NH29]OVT	Antagonist	9.6	pKd
[3H]OT (human, mouse, rat)	Full agonist	9.5	pKd
L-366,875	Antagonist	9.5	pKi
arginine vasotocin	Full agonist	9.4	pKi
vasopressin	Partial agonist	9.3	pKi
L023103	Antagonist	9.2	pKi
retosiban	Antagonist	9.19	pKi
SSR126768A	Antagonist	9.05	pKi
d(CH2)5[Tyr(Me)2,Thr4,Phe(3I,4N3)-NH29]OVT	Antagonist	9.0	pKi
[3H]AVP (human, mouse, rat)	Partial agonist	8.9	pKd
compound 37 [PMID: 16250654]	Antagonist	8.9	pKi
[Phe3]OT	Full agonist	8.8	pKi
nelivaptan	Antagonist	8.8	pKi
L-371,257	Antagonist	8.8	pKi
L-366,948	Antagonist	8.6	pKi
L-365,209	Antagonist	8.5	pKi
L-368,930	Antagonist	8.5	pKi
L-369,020	Antagonist	8.5	pKi
desGlyNH2-d(CH2)5[Tyr(Me)2,Thr4,Orn8]OT	Antagonist	8.5	pKi
L-366,682	Antagonist	8.4	pKi

Binding affinities (BindingDB)

10 measured of 21 human assays (21 total across all organisms); most potent 10 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
CAS_50-56-6	KI	0.5 nM
J325.349J	KI	1.3 nM
J440.775J	KI	4.1 nM
NSC_3083084	KI	4.5 nM
NSC_188397	KI	5.1 nM
CAS_196819	KI	9.4 nM
(2S,4Z)-N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino)-1-[(2’-methyl[1,1’-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide	KI	17 nM
J440.774A	KI	21 nM
CAS_90779-69-4	KI	27 nM
L-368112	IC50	68 nM

ChEMBL bioactivities

1256 potent at pChembl≥5 of 1272 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
11.00	EC50	0.01	nM	CHEMBL3354579
11.00	EC50	0.01	nM	CHEMBL3353956
11.00	EC50	0.01	nM	CHEMBL3353948
11.00	EC50	0.01	nM	CHEMBL3353946
11.00	EC50	0.01	nM	CHEMBL3353940
11.00	EC50	0.01	nM	CHEMBL3353939
11.00	EC50	0.01	nM	CHEMBL3353932
11.00	EC50	0.01	nM	CHEMBL3353930
11.00	EC50	0.01	nM	CHEMBL4102192
11.00	EC50	0.01	nM	OXYTOCIN
10.96	EC50	0.011	nM	CHEMBL4567752
10.93	EC50	0.0118	nM	CHEMBL4520170
10.89	EC50	0.013	nM	CHEMBL4093931
10.89	EC50	0.013	nM	CHEMBL4095930
10.89	EC50	0.013	nM	CHEMBL3277916
10.85	EC50	0.014	nM	CHEMBL4084223
10.82	EC50	0.015	nM	CHEMBL4078856
10.70	EC50	0.02	nM	CHEMBL3354592
10.70	EC50	0.02	nM	CHEMBL3354571
10.70	EC50	0.02	nM	CHEMBL3353955
10.68	EC50	0.021	nM	CHEMBL4096848
10.60	Ki	0.02512	nM	CHEMBL2037514
10.60	EC50	0.025	nM	CHEMBL3354594
10.57	EC50	0.027	nM	CHEMBL4101771
10.57	EC50	0.027	nM	CHEMBL4065273
10.55	EC50	0.028	nM	CHEMBL4474284
10.52	EC50	0.03	nM	CHEMBL3353942
10.52	EC50	0.03	nM	CHEMBL4094454
10.51	EC50	0.031	nM	CHEMBL4092971
10.51	EC50	0.031	nM	CHEMBL4583231
10.50	Ki	0.03162	nM	CHEMBL2037517
10.50	Ki	0.03162	nM	CHEMBL2037516
10.40	Ki	0.03981	nM	CHEMBL2037507
10.40	EC50	0.04	nM	CHEMBL3354597
10.40	EC50	0.04	nM	CHEMBL3354595
10.40	EC50	0.04	nM	CHEMBL3354588
10.40	EC50	0.04	nM	OXYTOCIN
10.40	EC50	0.04	nM	CHEMBL439044
10.38	EC50	0.042	nM	CHEMBL4080341
10.30	Ki	0.05012	nM	CHEMBL2037515
10.30	Ki	0.05012	nM	CHEMBL2037513
10.30	Ki	0.05012	nM	CHEMBL2037508
10.30	EC50	0.05	nM	CHEMBL3354598
10.30	EC50	0.05	nM	CHEMBL3354589
10.30	EC50	0.05	nM	CHEMBL3353929
10.27	EC50	0.054	nM	CHEMBL4084795
10.25	EC50	0.056	nM	CHEMBL4063150
10.22	EC50	0.06	nM	CHEMBL3353949
10.22	EC50	0.06	nM	CHEMBL3353931
10.22	EC50	0.06	nM	CHEMBL3353935

PubChem BioAssay actives

1215 with measured affinity, of 1879 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
(2R)-2-[(3R,6R)-3-(2,3-dihydro-1H-inden-2-yl)-2,5-dioxo-6-pentan-3-ylpiperazin-1-yl]-2-(2,6-dimethyl-3-pyridinyl)-N,N-dimethylacetamide	664068: Displacement of [3H]oxytocin from human oxytocin receptor	ki	<0.0001	uM
(3R,6R)-3-(2,3-dihydro-1H-inden-2-yl)-1-[(1R)-1-(2,6-dimethyl-3-pyridinyl)-2-morpholin-4-yl-2-oxoethyl]-6-pentan-3-ylpiperazine-2,5-dione	664068: Displacement of [3H]oxytocin from human oxytocin receptor	ki	<0.0001	uM
(2R)-2-[(2R,5R)-2-[(2S)-butan-2-yl]-5-(2,3-dihydro-1H-inden-2-yl)-3,6-dioxopiperazin-1-yl]-2-(4,6-dimethyl-3-pyridinyl)-N,N-dimethylacetamide	664068: Displacement of [3H]oxytocin from human oxytocin receptor	ki	<0.0001	uM
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-N-(cyclopropylmethyl)-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	1178646: Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay	ec50	<0.0001	uM
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-N-cyclobutyl-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	1178646: Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay	ec50	<0.0001	uM
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-N-cyclopentyl-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	1178646: Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay	ec50	<0.0001	uM
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-N-hexyl-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	1178646: Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay	ec50	<0.0001	uM
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-N-(2-methoxyethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	1178646: Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay	ec50	<0.0001	uM
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-N-[(3-methylphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	1178646: Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay	ec50	<0.0001	uM
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-N-[(4-fluorophenyl)methyl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	1178646: Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay	ec50	<0.0001	uM
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-N-(2-pyridin-4-ylethyl)-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	1178646: Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay	ec50	<0.0001	uM
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-N-(thiophen-2-ylmethyl)-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	1178646: Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay	ec50	<0.0001	uM
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-N-(2-thiophen-2-ylethyl)-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	1178646: Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay	ec50	<0.0001	uM
(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-hydroxyphenyl)methyl]-N-(3-hydroxypropyl)-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carboxamide	1178646: Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay	ec50	<0.0001	uM
(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-9-(3-amino-3-oxopropyl)-N-benzyl-12-[(2S)-butan-2-yl]-15-[(4-hydroxyphenyl)methyl]-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carboxamide	1178646: Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay	ec50	<0.0001	uM
(4S,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-N-[(3-methylphenyl)methyl]-6,9,12,15,18-pentaoxo-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	1178646: Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay	ec50	<0.0001	uM
(4S,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-N-[(4-fluorophenyl)methyl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	1178646: Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay	ec50	<0.0001	uM
(2S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-1-oxooctan-2-yl]-1-[(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide	1450439: Agonist activity at human OTR expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay	ec50	<0.0001	uM
(2S,4R)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4,4-dimethyl-1-oxopentan-2-yl]-1-[(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-hydroxyphenyl)methyl]-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carbonyl]-4-hydroxypyrrolidine-2-carboxamide	1450439: Agonist activity at human OTR expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay	ec50	<0.0001	uM
(2S,4S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]-1-[(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]-4-hydroxypyrrolidine-2-carboxamide	1450439: Agonist activity at human OTR expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay	ec50	<0.0001	uM
(2S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4,4-dimethyl-1-oxopentan-2-yl]-1-[(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide	1450439: Agonist activity at human OTR expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay	ec50	<0.0001	uM
(2S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-3-methyl-1-oxobutan-2-yl]-1-[(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide	1450439: Agonist activity at human OTR expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay	ec50	<0.0001	uM
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[(2S)-1-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-N-methyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	1450439: Agonist activity at human OTR expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay	ec50	<0.0001	uM
(2S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-1-oxohexan-2-yl]-1-[(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide	1450439: Agonist activity at human OTR expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay	ec50	<0.0001	uM
(2S,4R)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]-1-[(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-hydroxyphenyl)methyl]-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carbonyl]-4-hydroxypyrrolidine-2-carboxamide	1450439: Agonist activity at human OTR expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay	ec50	<0.0001	uM
(2S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-1-[(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide	1450439: Agonist activity at human OTR expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay	ec50	<0.0001	uM
(2S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-1-oxopropan-2-yl]-1-[(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide	1450439: Agonist activity at human OTR expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay	ec50	<0.0001	uM
N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]-1-[(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]piperidine-2-carboxamide	1450439: Agonist activity at human OTR expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay	ec50	<0.0001	uM
(2S,4R)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]-1-[(3S,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-hydroxyphenyl)methyl]-5,8,11,14,17,20-hexaoxo-1,4,7,10,13,16-hexazacycloicosane-3-carbonyl]-4-hydroxypyrrolidine-2-carboxamide	1450439: Agonist activity at human OTR expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay	ec50	<0.0001	uM
(2S,4R)-1-[(3S,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-hydroxyphenyl)methyl]-5,8,11,14,17,20-hexaoxo-1,4,7,10,13,16-hexazacycloicosane-3-carbonyl]-N-[(2S)-1-(2-carbamoylhydrazinyl)-4-methyl-1-oxopentan-2-yl]-4-hydroxypyrrolidine-2-carboxamide	1450439: Agonist activity at human OTR expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay	ec50	<0.0001	uM
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-N-methyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	1450439: Agonist activity at human OTR expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay	ec50	<0.0001	uM
(2S)-1-[(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]-N-[(2S)-1-(2-carbamoylhydrazinyl)-4-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide	1450439: Agonist activity at human OTR expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay	ec50	<0.0001	uM
(2S,4R)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]-1-[(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]-4-hydroxypyrrolidine-2-carboxamide	1450439: Agonist activity at human OTR expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay	ec50	<0.0001	uM
(2S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-3-cyclohexyl-1-oxopropan-2-yl]-1-[(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide	1450439: Agonist activity at human OTR expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay	ec50	<0.0001	uM
(2S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4,4-dimethyl-1-oxopentan-2-yl]-1-[(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-hydroxyphenyl)methyl]-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carbonyl]pyrrolidine-2-carboxamide	1450439: Agonist activity at human OTR expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay	ec50	<0.0001	uM
(2S)-N-[1-[(2-amino-2-oxoethyl)amino]-1-oxooctan-2-yl]-1-[(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide	1450439: Agonist activity at human OTR expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay	ec50	<0.0001	uM
(4R,7S,10S,13S,16S,19R)-19-amino-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-N-[(4-fluorophenyl)methyl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	1593562: Agonist activity at recombinant human OTR expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method	ec50	<0.0001	uM
N,N’-bis[(5S)-6-[(2-amino-2-oxoethyl)amino]-5-[[(2S)-1-[(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carbonyl]amino]-6-oxohexyl]dodecanediamide	1636598: Agonist activity at human oxytocin receptor C47A mutant high affinity site expressed in HEK293 cells coexpressing Rluc8-tagged Galphaq, N-terminal GFP-tagged Ggamma2 and Gbeta1 protein incubated for 2 mins by Gq protein activation based BRET assay	ec50	<0.0001	uM
N,N’-bis[(5S)-6-[(2-amino-2-oxoethyl)amino]-5-[[(2S)-1-[(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carbonyl]amino]-6-oxohexyl]octanediamide	1636592: Agonist activity at human oxytocin receptor high affinity site expressed in HEK293 cells coexpressing Rluc8-tagged Galphaq, N-terminal GFP-tagged Ggamma2 and Gbeta1 protein incubated for 2 mins by Gq protein activation based BRET assay	ec50	<0.0001	uM
N,N’-bis[(5S)-6-[(2-amino-2-oxoethyl)amino]-5-[[(2S)-1-[(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carbonyl]amino]-6-oxohexyl]decanediamide	1636592: Agonist activity at human oxytocin receptor high affinity site expressed in HEK293 cells coexpressing Rluc8-tagged Galphaq, N-terminal GFP-tagged Ggamma2 and Gbeta1 protein incubated for 2 mins by Gq protein activation based BRET assay	ec50	<0.0001	uM
N,N’-bis[(5S)-6-[(2-amino-2-oxoethyl)amino]-5-[[(2S)-1-[(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carbonyl]amino]-6-oxohexyl]tetradecanediamide	1636598: Agonist activity at human oxytocin receptor C47A mutant high affinity site expressed in HEK293 cells coexpressing Rluc8-tagged Galphaq, N-terminal GFP-tagged Ggamma2 and Gbeta1 protein incubated for 2 mins by Gq protein activation based BRET assay	ec50	<0.0001	uM
(4R,7S,10S,13S,16S,19R)-19-amino-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-N-(3-hydroxypropyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	1593562: Agonist activity at recombinant human OTR expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method	ec50	<0.0001	uM
(2S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]-1-[(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-methoxyphenyl)methyl]-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carbonyl]pyrrolidine-2-carboxamide	1593562: Agonist activity at recombinant human OTR expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method	ec50	<0.0001	uM
Oxytocin	1306776: Agonist activity at human oxytocin receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 90 sec by fluo-4 dye based FLIPR assay	ec50	<0.0001	uM
(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-hydroxyphenyl)methyl]-5,8,11,14,17-pentaoxo-N-(2-phenylethyl)-1-thia-4,7,10,13,16-pentazacycloicosane-3-carboxamide	1178646: Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay	ec50	<0.0001	uM
(2S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]-1-[(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide	1306776: Agonist activity at human oxytocin receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 90 sec by fluo-4 dye based FLIPR assay	ec50	<0.0001	uM
(3R,6R)-3-(2,3-dihydro-1H-inden-2-yl)-1-[(1R)-1-(6-methyl-3-pyridinyl)-2-morpholin-4-yl-2-oxoethyl]-6-pentan-3-ylpiperazine-2,5-dione	664068: Displacement of [3H]oxytocin from human oxytocin receptor	ki	<0.0001	uM
(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-N-[(4-fluorophenyl)methyl]-15-[(4-hydroxyphenyl)methyl]-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carboxamide	1593562: Agonist activity at recombinant human OTR expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method	ec50	<0.0001	uM
(2S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]-1-[(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-hydroxyphenyl)methyl]-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carbonyl]pyrrolidine-2-carboxamide	1450439: Agonist activity at human OTR expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay	ec50	<0.0001	uM
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	1450439: Agonist activity at human OTR expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay	ec50	<0.0001	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Estradiol	increases expression, decreases expression, decreases reaction	3
Asbestos, Crocidolite	decreases expression, increases expression	3
trichostatin A	increases expression	2
Benzo(a)pyrene	affects methylation, decreases methylation	2
Calcitriol	decreases expression, increases expression	2
Silicon Dioxide	increases expression	2
Valproic Acid	decreases expression, increases expression	2
geldanamycin	increases expression	1
methylmercuric chloride	increases expression	1
triphenyl phosphate	affects expression	1
pirinixic acid	affects binding, decreases expression, increases activity	1
bisphenol A	decreases expression	1
2,5,2’,5’-tetrachlorobiphenyl	decreases expression	1
arsenite	increases methylation	1
sodium arsenite	increases methylation	1
butyraldehyde	increases expression	1
zinc chromate	decreases expression, increases abundance	1
potassium chromate(VI)	increases expression	1
2,3-bis(3’-hydroxybenzyl)butyrolactone	affects cotreatment, decreases expression	1
aflatoxin B2	increases methylation	1
S-(1,2-dichlorovinyl)cysteine	affects response to substance, increases expression, affects cotreatment	1
phenethyl isothiocyanate	decreases expression	1
chromium hexavalent ion	increases abundance, decreases expression	1
perfluorooctane sulfonic acid	decreases expression	1
CGP 52608	affects binding, increases reaction	1
abrine	increases expression	1
jinfukang	affects cotreatment, decreases expression	1
malondialdehyde-low density lipoprotein, human	increases expression	1
Resveratrol	affects cotreatment, decreases expression	1
Decitabine	decreases expression, decreases reaction	1

ChEMBL screening assays

249 unique, capped per target: 149 binding, 99 functional, 1 unclassified

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1015247	Binding	Binding affinity to oxytocin receptor	New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists. — J Med Chem
CHEMBL1025690	Functional	Antagonist activity at human recombinant oxytocin receptor expressed in CHO cells by FLIPR assay	Discovery and optimisation of a potent and selective tertiary sulfonamide oxytocin antagonist. — Bioorg Med Chem Lett
CHEMBL1738127	Unclassified	PUBCHEM_BIOASSAY: Late-stage radioligand binding dose response assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screen Ki. (Class of assay: screening) [Related pubchem assays (depositor defined):AID1792, AID1796, AID1823, AID253	PubChem BioAssay data set

Cellosaurus cell lines

9 cell lines: 5 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_D7WC	Ubigene A-549 OXTR KO	Cancer cell line	Male
CVCL_D8RV	Ubigene HCT 116 OXTR KO	Cancer cell line	Male
CVCL_D9LZ	Ubigene HEK293 OXTR KO	Transformed cell line	Female
CVCL_E0JK	Ubigene HeLa OXTR KO	Cancer cell line	Female
CVCL_E3DT	U2OS OXTR HiTSeeker	Cancer cell line	Female
CVCL_H491	CHO-K1/OXTR	Spontaneously immortalized cell line	Female
CVCL_KY73	PathHunter CHO-K1 OXTR beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_LB04	PathHunter U2OS OXTR Activated GPCR Internalization	Cancer cell line	Female
CVCL_ZK65	GeneBLAzer OXTR-Gqo5-NFAT-bla CHO-K1	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT02513940	PHASE4	COMPLETED	Influence of Testosterone Administration on Drug-Induced QT Interval Prolongation and Torsades de Pointes
NCT03834883	PHASE4	COMPLETED	Reducing the Risk of Drug-Induced QT Interval Lengthening in Women
NCT04169100	PHASE4	UNKNOWN	Novel Form of Acquired Long QT Syndrome
NCT04675788	PHASE4	COMPLETED	Novel Approaches for Minimizing Drug-Induced QT Interval Lengthening
NCT00348530	PHASE4	UNKNOWN	Carvedilol Versus Verapamil in Chronic Heart Failure Secondary to Non-Ischemic Cardiomyopathy
NCT00371891	PHASE4	COMPLETED	Ontario Multidetector Computed Tomographic (MDCT) Coronary Angiography Study (OMCAS)
NCT00401856	PHASE4	COMPLETED	CMR to Assess Fibrosis in Cardiomyopathy Using Eplerenone
NCT00559338	PHASE4	COMPLETED	Impact of Nesiritide Infusion for Decompensated Heart Failure in the Emergency Department
NCT00606775	PHASE4	UNKNOWN	The Preventive Efficacy of Carvedilol on Cardiac Dysfunction in Duchenne Muscular Dystrophy
NCT00658203	PHASE4	COMPLETED	Clinical Evaluation on Advanced Resynchronization
NCT00701220	PHASE4	COMPLETED	Statin Therapy for Ischemic and Nonischemic Cardiomyopathy
NCT00800761	PHASE4	COMPLETED	Intensive Combined Chelation Therapy for Iron-Induced Cardiac Disease in Patients With Thalassemia Major
NCT00806390	PHASE4	TERMINATED	Prevention of Anthracycline or Trastuzumab Induced Cardiomyopathy by Metoprolol
NCT01006473	PHASE4	COMPLETED	Exercise Training in Chagas Cardiomyopathy
NCT01261065	PHASE4	COMPLETED	Mechanisms of Improvement With Beta-Blocker Treatment in Heart Failure
NCT01345188	PHASE4	COMPLETED	Ranolazine in Ischemic Cardiomyopathy
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