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AVPR1A

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Summary

AVPR1A (arginine vasopressin receptor 1A, HGNC:895) is a protein-coding gene on chromosome 12q14.2, encoding Vasopressin V1a receptor (P37288). Receptor for arginine vasopressin.

The protein encoded by this gene acts as receptor for arginine vasopressin. This receptor belongs to the subfamily of G-protein coupled receptors which includes AVPR1B, V2R and OXT receptors. Its activity is mediated by G proteins which stimulate a phosphatidylinositol-calcium second messenger system. The receptor mediates cell contraction and proliferation, platelet aggregation, release of coagulation factor and glycogenolysis.

Source: NCBI Gene 552 — RefSeq curated summary.

At a glance

  • Gene–disease (curated): autism spectrum disorder (Limited, GenCC)
  • GWAS associations: 8
  • Clinical variants (ClinVar): 66 total — 2 pathogenic
  • Druggable target: yes — 46 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_000706

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:895
Approved symbolAVPR1A
Namearginine vasopressin receptor 1A
Location12q14.2
Locus typegene with protein product
StatusApproved
Ensembl geneENSG00000166148
Ensembl biotypeprotein_coding
OMIM600821
Entrez552

Gene structure

Transcript identifiers

Ensembl transcripts: 2 — 2 protein_coding

ENST00000299178, ENST00000550940

RefSeq mRNA: 1 — MANE Select: NM_000706 NM_000706

CCDS: CCDS8965

Canonical transcript exons

ENST00000299178 — 2 exons

ExonStartEnd
ENSE000011002336314275963147645
ENSE000011002366314986763151201

Expression profiles

Bgee: expression breadth ubiquitous, 202 present calls, max score 89.92.

FANTOM5 (CAGE): breadth broad, TPM avg 1.0002 / max 161.3604, expressed in 218 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter IDTPM avgSamples expressed
1318390.5453153
1318380.2855107
1318370.093746
1318360.075829

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
left adrenal glandUBERON:000123489.92gold quality
left adrenal gland cortexUBERON:003582589.36gold quality
adrenal cortexUBERON:000123588.62gold quality
popliteal arteryUBERON:000225088.16gold quality
tibial arteryUBERON:000761088.13gold quality
adrenal glandUBERON:000236987.17gold quality
parietal pleuraUBERON:000240086.59gold quality
right adrenal glandUBERON:000123386.01gold quality
skin of hipUBERON:000155485.45gold quality
right adrenal gland cortexUBERON:003582785.39gold quality
adipose tissueUBERON:000101384.34gold quality
adipose tissue of abdominal regionUBERON:000780883.53gold quality
connective tissueUBERON:000238483.16gold quality
omental fat padUBERON:001041483.14gold quality
peritoneumUBERON:000235883.07gold quality
subcutaneous adipose tissueUBERON:000219082.83gold quality
superficial temporal arteryUBERON:000161482.22gold quality
seminal vesicleUBERON:000099881.45gold quality
liverUBERON:000210781.13gold quality
calcaneal tendonUBERON:000370180.80gold quality
pericardiumUBERON:000240780.29gold quality
pleuraUBERON:000097779.73gold quality
endometriumUBERON:000129579.68gold quality
right lobe of liverUBERON:000111479.65gold quality
smooth muscle tissueUBERON:000113577.68gold quality
synovial jointUBERON:000221777.54gold quality
hindlimb stylopod muscleUBERON:000425277.39gold quality
gall bladderUBERON:000211077.18gold quality
myometriumUBERON:000129676.77gold quality
uterusUBERON:000099576.51gold quality

Single-cell (SCXA)

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

ExperimentMarker?Max mean expression
E-ANND-3yes9.13

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): AR

miRNA regulators (miRDB)

148 targeting AVPR1A, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-3613-3P100.0076.367965
HSA-MIR-6867-5P100.0082.213464
HSA-MIR-3924100.0072.092394
HSA-MIR-5692B100.0071.322622
HSA-MIR-5692C100.0071.322622
HSA-MIR-4795-3P100.0074.624024
HSA-MIR-1277-5P100.0073.955056
HSA-MIR-3163100.0077.238605
HSA-MIR-656-3P100.0072.152788
HSA-MIR-5692A100.0074.406850
HSA-MIR-200B-3P100.0073.312693
HSA-MIR-200C-3P100.0073.352685
HSA-MIR-429100.0073.442698
HSA-MIR-196A-1-3P99.9972.152772
HSA-MIR-548C-3P99.9974.017587
HSA-MIR-513B-5P99.9969.962150
HSA-MIR-6759-5P99.9966.54785
HSA-MIR-428299.9975.366408
HSA-MIR-477599.9875.006394
HSA-MIR-499A-5P99.9870.791323
HSA-MIR-480399.9871.993117
HSA-MIR-302C-5P99.9772.563642
HSA-MIR-314899.9775.066478
HSA-MIR-3065-5P99.9771.563281
HSA-MIR-590-3P99.9674.346478
HSA-MIR-1468-3P99.9672.743797
HSA-MIR-1250-3P99.9670.044038
HSA-MIR-570-3P99.9672.414910
HSA-MIR-4666A-3P99.9671.713434
HSA-MIR-551B-5P99.9671.283493

Literature-anchored findings (GeneRIF, showing 40)

  • transmission disequilibrium testing of polymorphism in autism (PMID:12082568)
  • residue Phe225, located in transmembrane domain V, directly participates in the binding of the V1a-selective nonpeptide antagonist SR49059 (PMID:12869559)
  • In the wildtype V1aR, Arg46 constrains the inactive conformation of the receptor; on binding AVP this constraint is alleviated, promoting the transition to active V1aR (PMID:14622255)
  • examination of interaction with beta-arrestin and trafficking patterns by heterodimerization with V2 vasopressin receptor (PMID:14757828)
  • AVPR1a’s exons were screened in 125 independent autistic probands. 2 promoter polymorphisms were typed in 65 autism-affected sibling-pair families. Linkage & linkage disequilibrium were seen in a subset with relatively less severe language impairment. (PMID:15098001)
  • Glu54 is critical for arginine vasopressin binding by V1aR. (PMID:15994199)
  • Association between AVPR1a and SLC6A4 reflects the social communication, courtship, and spiritual facets of the dancing phenotype. (PMID:16205790)
  • molecular dynamics analysis of mechanism of desmopressin binding in vasopressin V2 receptor versus vasopressin V1a and oxytocin receptors (PMID:16333859)
  • This study confirms an association between the AVPR1a gene and autism spectrum disorders and identifies a third microsatellite associated with autism spectrum disorders as well as haplotypes consisting of all three markers. (PMID:16520824)
  • analysis of a pharmacological chaperone ligand that acts on misfolded mutant V(1a) receptors (PMID:16565083)
  • These results suggest that the four SNPs in the promoter region of the V1aR gene may not be useful as genetic markers for platelet aggregation heterogeneity. (PMID:16721832)
  • There is an association of the V1aR SNP-6951 with essential hypertension in nonobese individuals. (PMID:17653244)
  • This gene contributes to social bonding in lower animals and in human behavior, suggesting a common evolutionary mechanism. (PMID:17696996)
  • study is the first to report associations between AVPR1A and OXTR genetic variation with life history traits in humans (PMID:17939166)
  • human amygdala function is strongly associated with genetic variation in AVPR1A. (PMID:18490926)
  • AVPR1a has been linked to eating behaviour in both clinical and non-clinical groups, reflecting the social and ritualistic side of eating behaviour.[REVIEW] (PMID:18655900)
  • report an association between one of the human AVPR1A repeat polymorphisms (RS3) and traits reflecting pair-bonding behavior in men (PMID:18765804)
  • Genetic variation of the human arginine vasopressin 1A (AVPR1A) gene is associated with uncoupling of the usual direct relation between glucose and triglycerides and an increased prevalence of diabetes in subjects with a high fat intake or who are obese (PMID:19056558)
  • A role of the AVPR1a gene in contributing to the prepulse inhibition response to auditory stimuli. (PMID:19195791)
  • The amplified region was polymorphic in length in all species investigated. This region could be a marker to further survey functional difference between and within species. (PMID:19350216)
  • AVPR1A haplotype AVR+RS1 further suggested a positive association with creative functions in music using haplotype-based association test HBAT. (PMID:19461995)
  • polymorphism rs1042615 of the V1a receptor altered body mass index and diastolic pressure in middle-aged and older men and the training-induced responses of DBP and low-density lipoprotein cholesterol, whereas women did not show any of these responses (PMID:20142561)
  • Possible roles of oxytocin receptor and vasopressin-1alpha receptor in the pathomechanism of dysperistalsis and dysmenorrhea in patients with adenomyosis uteri. (PMID:20413116)
  • The results of this study found a statistically significant association between microsatellites and Korean autism spectrum disorders. (PMID:20452058)
  • Evidence provided for a possible association between these SNPs and the phenotype of autism spectrum disorders. (PMID:20546835)
  • The importance of subtle, quantitative measures of endophenotype are emphasized in this review of the neural distribution of vasopressin 1a receptor (V1aR), a recent focus for studies of social behavior. (PMID:20889332)
  • A positive association between the AVPR1A haplotype (RS1 and AVR) and active current listening to music (permuted P=0.0019) was observed. (PMID:21307861)
  • report finds an association between AVPR1A and the risk for DUD. (PMID:21514569)
  • Our results demonstrate a role for V1A-mediated signaling in the development of heart failure. (PMID:21747049)
  • AVPR1A variant associated with preschoolers’ lower altruistic behavior. (PMID:21980412)
  • data suggest a possible interrelation between AVR and RS3 gene variants of the AVPR1A gene and impulsive aggression in patients with borderline personality disorder (PMID:22008661)
  • In a sample of European mothers, a microsatellite variant RS3 of the vasopressin 1a receptor gene is associated with maternal sensitivity; this association is strongest under conditions of high maternal early adversity. (PMID:22288734)
  • analysis of AVPR1A and SLC6A4 polymorphisms in choral singers and non-musicians (PMID:22384070)
  • greater perceived threat predicted lower commitment to civic duty for individuals with one or two short alleles for AVPR1a rs1, but not for individuals with only long alleles (PMID:22457427)
  • Human maternal behaviour is associated with arginine vasopressin receptor 1A gene (PMID:22764113)
  • There was moderate statistical evidence for interactions shoulder pain phenotypes between AVPR1A and depressive symptoms, pain catastrophizing, or kinesiophobia (PMID:24373571)
  • Early caregiving combined with genetic liability along the axis of vasopressin-oxytocin gene pathways: G x E contributions to PTSD. (PMID:24618689)
  • Men, but not women, with high levels of poststressor AVP and the 320 allele of the RS1 polymorphism reported more poststressor anger than noncarriers. (PMID:24660771)
  • Gene-level tests showed that DRD2 was associated with vocabulary, ASPM with vocabulary and reading decoding, and AVPR1A with all three endophenotypes. (PMID:24849541)
  • humanized AVPR1A mice displayed increased reciprocal social interactions compared with wild-type animals. (PMID:24924430)

Cross-species orthologs

5 orthologs

OrganismSymbolGene ID
danio_rerioavpr1abENSDARG00000045788
danio_rerioavpr1aaENSDARG00000077083
mus_musculusAvpr1aENSMUSG00000020123
rattus_norvegicusAvpr1aENSRNOG00000004400
drosophila_melanogasterCCAP-RFBGN0039396

Paralogs (16): NPFFR2 (ENSG00000056291), GNRHR (ENSG00000109163), CCKBR (ENSG00000110148), HCRTR1 (ENSG00000121764), AVPR2 (ENSG00000126895), GALR3 (ENSG00000128310), HCRTR2 (ENSG00000137252), NPFFR1 (ENSG00000148734), CCKAR (ENSG00000163394), GALR1 (ENSG00000166573), GPR22 (ENSG00000172209), GPR150 (ENSG00000178015), OXTR (ENSG00000180914), FFAR4 (ENSG00000186188), QRFPR (ENSG00000186867), AVPR1B (ENSG00000198049)

Protein

Protein identifiers

Vasopressin V1a receptor — P37288 (reviewed: P37288)

Alternative names: AVPR V1a, Antidiuretic hormone receptor 1a, Vascular/hepatic-type arginine vasopressin receptor

All UniProt accessions (3): P37288, F8VW98, X5D2B0

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for arginine vasopressin. The activity of this receptor is mediated by G proteins which activate a phosphatidyl-inositol-calcium second messenger system. Has been involved in social behaviors, including affiliation and attachment.

Subcellular location. Cell membrane.

Miscellaneous. Differences in regional receptor expression in the brain as well as differences in social behavior may result from a highly variable repetitive sequence in the 5’ flanking region of AVPR1A. One such allelic variant has been linked to autism.

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

RefSeq proteins (1): NP_000697* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR000276GPCR_RhodpsnFamily
IPR001224Vprs_V1A_rcptFamily
IPR001817Vasoprsn_rcptFamily
IPR015076V1R_CDomain
IPR017452GPCR_Rhodpsn_7TMDomain

Pfam: PF00001, PF08983

UniProt features (26 total): topological domain 8, transmembrane region 7, region of interest 2, lipid moiety-binding region 2, glycosylation site 2, chain 1, compositionally biased region 1, modified residue 1, disulfide bond 1, sequence variant 1

Structure

Experimental structures (PDB)

5 structures.

PDBMethodResolution (Å)
1YTVX-RAY DIFFRACTION1.8
9UWLELECTRON MICROSCOPY2.6
9UWIELECTRON MICROSCOPY2.8
9XB1ELECTRON MICROSCOPY2.8
9UWJELECTRON MICROSCOPY3

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-P37288-F174.110.33

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 (3): 404, 365, 366

Disulfide bonds (1): 124–203

Glycosylation sites (2): 27, 196

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

IDPathway
R-HSA-388479Vasopressin-like receptors
R-HSA-416476G alpha (q) signalling events
R-HSA-5619099Defective AVP does not bind AVPR1A,B and causes neurohypophyseal diabetes insipidus (NDI)

MSigDB gene sets: 304 (showing top): GOBP_GLUTAMATE_SECRETION, GOBP_BEHAVIOR, GOBP_REGULATION_OF_BLOOD_PRESSURE, GOBP_CIRCULATORY_SYSTEM_PROCESS, GOBP_REGULATION_OF_ORGANIC_ACID_TRANSPORT, GOBP_RESPONSE_TO_ACID_CHEMICAL, GOBP_RESPONSE_TO_CORTICOSTEROID, MODULE_64, GRAESSMANN_APOPTOSIS_BY_SERUM_DEPRIVATION_UP, GOBP_GROWTH, GOBP_STRIATED_MUSCLE_CELL_DIFFERENTIATION, GOBP_REGULATION_OF_SYSTEMIC_ARTERIAL_BLOOD_PRESSURE, GOBP_NEGATIVE_REGULATION_OF_NERVOUS_SYSTEM_PROCESS, GOBP_CELLULAR_RESPONSE_TO_ACID_CHEMICAL, GOBP_MONOCARBOXYLIC_ACID_METABOLIC_PROCESS

GO Biological Process (30): regulation of systemic arterial blood pressure by vasopressin (GO:0001992), maternal aggressive behavior (GO:0002125), positive regulation of systemic arterial blood pressure (GO:0003084), generation of precursor metabolites and energy (GO:0006091), G protein-coupled receptor signaling pathway (GO:0007186), positive regulation of cytosolic calcium ion concentration (GO:0007204), negative regulation of female receptivity (GO:0007621), grooming behavior (GO:0007625), blood circulation (GO:0008015), positive regulation of cell population proliferation (GO:0008284), positive regulation of heart rate (GO:0010460), positive regulation of glutamate secretion (GO:0014049), myotube differentiation (GO:0014902), calcium-mediated signaling (GO:0019722), telencephalon development (GO:0021537), positive regulation of cell growth (GO:0030307), positive regulation of prostaglandin biosynthetic process (GO:0031394), obsolete positive regulation of cellular pH reduction (GO:0032849), cellular response to hormone stimulus (GO:0032870), social behavior (GO:0035176), cellular response to water deprivation (GO:0042631), maternal behavior (GO:0042711), sperm ejaculation (GO:0042713), positive regulation of vasoconstriction (GO:0045907), response to corticosterone (GO:0051412), negative regulation of transmission of nerve impulse (GO:0051970), transport across blood-brain barrier (GO:0150104), signal transduction (GO:0007165), regulation of blood pressure (GO:0008217), positive regulation of blood pressure (GO:0045777)

GO Molecular Function (7): vasopressin receptor activity (GO:0005000), protein kinase C binding (GO:0005080), peptide hormone binding (GO:0017046), V1A vasopressin receptor binding (GO:0031894), G protein-coupled receptor activity (GO:0004930), protein binding (GO:0005515), G protein-coupled peptide receptor activity (GO:0008528)

GO Cellular Component (4): endosome (GO:0005768), plasma membrane (GO:0005886), endocytic vesicle (GO:0030139), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-3 pathways:

CategoryPathways
Peptide ligand-binding receptors1
GPCR downstream signalling1
SLC transporter disorders1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
G protein-coupled receptor activity2
behavior2
positive regulation of cellular process2
cytoplasmic vesicle2
regulation of systemic arterial blood pressure by hormone1
aggressive behavior1
regulation of systemic arterial blood pressure1
positive regulation of blood pressure1
metabolic process1
signal transduction1
regulation of biological quality1
regulation of female receptivity1
circulatory system process1
cell population proliferation1
regulation of cell population proliferation1
regulation of heart rate1
positive regulation of heart contraction1
glutamate secretion1
regulation of glutamate secretion1
positive regulation of organic acid transport1
positive regulation of amino acid transport1
positive regulation of secretion by cell1
striated muscle cell differentiation1
intracellular signaling cassette1
forebrain development1
anatomical structure development1
regulation of cell growth1
cell growth1
positive regulation of growth1
prostaglandin biosynthetic process1
regulation of prostaglandin biosynthetic process1
positive regulation of unsaturated fatty acid biosynthetic process1
response to hormone1
cellular response to chemical stimulus1
cellular response to endogenous stimulus1
biological process involved in intraspecies interaction between organisms1
G protein-coupled peptide receptor activity1
protein kinase binding1
hormone binding1
vasopressin receptor binding1

Protein interactions and networks

STRING

992 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
AVPR1AOXTP01178987
AVPR1AAVPP01185926
AVPR1APOMCP01189758
AVPR1AACKR3P25106669
AVPR1ASLC6A4P31645658
AVPR1AGIPRP48546640
AVPR1AOXTRP30559632
AVPR1ADRD4P21917625
AVPR1AVIPP01282593
AVPR1AADRA1AP35348571
AVPR1AGNAQP50148560
AVPR1AAVPR2P30518542
AVPR1ACRHR1P34998537
AVPR1AAGTP01019532
AVPR1AGNA14O95837520

IntAct

14 interactions, top by confidence:

ABTypeScore
ACKR3AVPR1Apsi-mi:“MI:2364”(proximity)0.570
ACKR3AVPR1Apsi-mi:“MI:0915”(physical association)0.570
AVPR1AACKR3psi-mi:“MI:2364”(proximity)0.570
AVPR1AACKR3psi-mi:“MI:0914”(association)0.570
AVPR1ACXCR4psi-mi:“MI:2364”(proximity)0.420
ACKR3psi-mi:“MI:2364”(proximity)0.410
AVPR1AAVPpsi-mi:“MI:0915”(physical association)0.400
VIPAVPR1Apsi-mi:“MI:0915”(physical association)0.400
AVPR1ARAMP1psi-mi:“MI:0915”(physical association)0.400
RAMP2AVPR1Apsi-mi:“MI:0915”(physical association)0.400
AVPR1ARAMP3psi-mi:“MI:0915”(physical association)0.400

BioGRID (3): AVPR1A (Affinity Capture-MS), AVPR1A (Affinity Capture-Western), AVPR1A (Affinity Capture-Western)

ESM2 similar proteins: A1ZAX0, O02835, O02836, O08786, O43613, O43614, O46639, O62809, O93603, O97772, P0C0L6, P21761, P25931, P28646, P30551, P30560, P30872, P30873, P30975, P32238, P32247, P34981, P37288, P47751, P48043, P49146, P56719, P58307, P58308, P70031, P79113, P97295, Q1RMU8, Q28596, Q49LX5, Q4V622, Q5D0K2, Q5IS62, Q61041, Q62463

Diamond homologs: A0A2L0VBG2, O18821, O42329, O77808, O88721, P30518, P30560, P30968, P30969, P32236, P32237, P32307, P37288, P48044, P49922, P70536, P97266, Q00788, Q01776, Q18775, Q19PY9, Q24563, Q25188, Q2V2K5, Q5QD12, Q5QD21, Q63384, Q8CH60, Q8IS44, Q8SPZ1, Q90252, Q90334, Q923X8, Q923Y2, Q93126, Q95JG1, Q95MG6, Q95MH6, Q96P88, Q9BZJ6

SIGNOR signaling

4 interactions.

AEffectBMechanism
AVPR1A“up-regulates activity”GNASbinding
AVPR1A“up-regulates activity”GNALbinding
AVPR1A“up-regulates activity”GNAQbinding
vasopressin“up-regulates activity”AVPR1A“chemical activation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic2
Likely pathogenic0
Uncertain significance53
Likely benign3
Benign3

Top pathogenic / likely-pathogenic (2)

Variant IDHGVSClassification
150076GRCh38/hg38 12q14.1-14.3(chr12:60907151-66568077)x1Pathogenic
2685437GRCh37/hg19 12q14.1-15(chr12:61755618-70035424)x1Pathogenic

SpliceAI

298 predictions. Top by Δscore:

VariantEffectΔscore
12:63149844:T:Adonor_gain1.0000
12:63149863:GTA:Gdonor_loss1.0000
12:63149865:A:ACdonor_gain1.0000
12:63149866:C:CCdonor_gain1.0000
12:63147646:C:CCacceptor_gain0.9900
12:63147650:A:Cacceptor_gain0.9900
12:63149866:CCGGT:Cdonor_gain0.9900
12:63147425:A:ACdonor_gain0.9800
12:63147426:C:CCdonor_gain0.9800
12:63147476:A:ACdonor_gain0.9800
12:63147477:C:CCdonor_gain0.9800
12:63147650:A:ACacceptor_gain0.9700
12:63147643:ATTCT:Aacceptor_loss0.9600
12:63147644:TT:Tacceptor_gain0.9600
12:63147644:TTCTG:Tacceptor_loss0.9600
12:63147645:TCTGC:Tacceptor_loss0.9600
12:63147646:CT:Cacceptor_loss0.9600
12:63147647:T:Aacceptor_loss0.9600
12:63149966:TC:Tdonor_gain0.9600
12:63147641:CGATT:Cacceptor_gain0.9500
12:63147649:CA:Cacceptor_gain0.9500
12:63149865:AC:Adonor_gain0.9300
12:63149866:CC:Cdonor_gain0.9300
12:63149898:C:CTdonor_gain0.9300
12:63149896:G:Tdonor_gain0.9200
12:63149866:CCG:Cdonor_gain0.8900
12:63149832:ATC:Adonor_gain0.8700
12:63147659:A:Cacceptor_gain0.8500
12:63147561:C:CCacceptor_gain0.8300
12:63149866:CCGG:Cdonor_gain0.8300

AlphaMissense

2761 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
12:63150270:G:CF189L0.998
12:63150270:G:TF189L0.998
12:63150272:A:GF189L0.998
12:63150303:G:CS178R0.997
12:63150303:G:TS178R0.997
12:63150305:T:GS178R0.997
12:63150555:G:CS94R0.997
12:63150555:G:TS94R0.997
12:63150557:T:GS94R0.997
12:63147580:A:GW346R0.996
12:63147580:A:TW346R0.996
12:63150291:G:CS182R0.996
12:63150291:G:TS182R0.996
12:63150293:T:GS182R0.996
12:63150466:C:GC124S0.996
12:63150467:A:TC124S0.996
12:63150486:G:CF117L0.996
12:63150486:G:TF117L0.996
12:63150487:A:CF117C0.996
12:63150488:A:GF117L0.996
12:63147593:G:CS341R0.995
12:63147593:G:TS341R0.995
12:63147595:T:GS341R0.995
12:63150228:G:CC203W0.995
12:63150229:C:TC203Y0.994
12:63150314:A:GW175R0.994
12:63150314:A:TW175R0.994
12:63150466:C:TC124Y0.994
12:63149930:A:GC303R0.993
12:63150229:C:GC203S0.993

dbSNP variants (sampled 300 via entrez): RS1000074731 (12:63144923 G>T), RS1000557231 (12:63142998 A>C,G), RS1000588313 (12:63143325 T>C), RS1001235000 (12:63149078 T>C), RS1001292278 (12:63148705 T>C), RS1001330408 (12:63150934 G>A,C,T), RS1001549454 (12:63148225 T>C), RS1001884762 (12:63149579 CACT>C), RS1002408769 (12:63143990 C>G), RS1002481852 (12:63147141 G>T), RS1003674860 (12:63145647 C>G,T), RS1004220949 (12:63152839 CTTTCT>C), RS1004235505 (12:63151238 C>T), RS1004581366 (12:63144443 T>A,C), RS1004701894 (12:63152621 G>A)

Disease associations

OMIM: gene MIM:600821 | disease phenotypes:

GenCC curated gene-disease

DiseaseClassificationInheritance
autism spectrum disorderLimitedAutosomal dominant

ClinGen Gene-Disease Validity (1)

Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.

DiseaseClassificationInheritance
autism spectrum disorderDisputedUD

Mondo (1): autism spectrum disorder (MONDO:0005258)

Orphanet (0):

HPO phenotypes

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

GWAS associations

8 associations (top):

StudyTraitp-value
GCST006134_7Hippocampal volume7.000000e-06
GCST006190_64Diastolic blood pressure x smoking status (ever vs never) interaction (2df test)3.000000e-08
GCST006190_85Diastolic blood pressure x smoking status (ever vs never) interaction (2df test)5.000000e-08
GCST007565_15Morning person2.000000e-16
GCST007565_69Morning person4.000000e-18
GCST007576_361Chronotype4.000000e-18
GCST007576_395Chronotype1.000000e-17
GCST008114_8Type 2 diabetes8.000000e-06

EFO canonical traits (4, from GWAS)

EFO IDTrait name
EFO:0005035hippocampal volume
EFO:0006336diastolic blood pressure
EFO:0006527smoking status measurement
EFO:0008328chronotype measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (4): CHEMBL1889 (SINGLE PROTEIN), CHEMBL2111456 (PROTEIN FAMILY), CHEMBL2363078 (PROTEIN FAMILY), CHEMBL4523980 (SELECTIVITY GROUP)

Molecules with ChEMBL bioactivity

46 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 537,356 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL111RIMONABANT415,726
CHEMBL1112ARIPIPRAZOLE424,205
CHEMBL114SAQUINAVIR439,899
CHEMBL1171837PONATINIB48,955
CHEMBL1201303PYRVINIUM41,797
CHEMBL1201304INDOCYANINE GREEN ACID FORM47,044
CHEMBL1201346BALSALAZIDE48,319
CHEMBL1401NITAZOXANIDE49,504
CHEMBL1423PIMOZIDE417,310
CHEMBL1429DESMOPRESSIN4122
CHEMBL1617RIFAXIMIN413,380
CHEMBL163RITONAVIR453,773
CHEMBL1755CONIVAPTAN43,108
CHEMBL178DAUNORUBICIN4203,756
CHEMBL2135460TERLIPRESSIN411,801
CHEMBL288441BOSUTINIB412,255
CHEMBL3301668CARBETOCIN41,721
CHEMBL344159TOLVAPTAN43,645
CHEMBL373742VASOPRESSIN47,202
CHEMBL374478RIFAMPIN493,834
CHEMBL382301ATOSIBAN4
CHEMBL395429OXYTOCIN4
CHEMBL411DIETHYLSTILBESTROL4
CHEMBL420762MOZAVAPTAN4
CHEMBL46516FLUSPIRILENE4
CHEMBL56337EPALRESTAT4
CHEMBL76370TEGASEROD4
CHEMBL790CHLORHEXIDINE4
CHEMBL1254025NOLASIBAN3
CHEMBL2103773OTILONIUM BROMIDE3

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 (66 total), top 25:

LigandActionAffinityParameter
[125I]OH-LVAAntagonist10.4pKd
[3H]AVP (human, mouse, rat)Full agonist10.2pKd
[125I]3-N3-Phpa-LVAAntagonist9.9pKd
3-N3-Phpa-LVAAntagonist9.6pKi
SRX246Antagonist9.52pKi
YM 218Antagonist9.5pKi
vasopressinFull agonist9.3pKi
relcovaptanAntagonist9.3pKi
OH-LVAAntagonist9.3pKi
d(CH2)5[Tyr(Me)2,Thr4,Phe(3125I,4N3)-NH29]OVTAntagonist9.3pKd
d[D-Phe2]AVPFull agonist9.2pKi
YM 471Antagonist9.2pKi
[Phaa1,D-Tyr2,Val4,Arg6,Arg-NH29]AVPAntagonist9.2pKi
d(CH2)5[Tyr(Me)2]AVPAntagonist9.2pKi
[Phaa1,D-Tyr(Et)2,Lys6,des-Gly9]AVPAntagonist9.1pKi
[Phaa1,D-Tyr(Me)2,Arg6,Tyr-NH29]AVPAntagonist9.1pKi
[tBaa1,D-Tyr(Et)2,Val4,Lys6,Arg-NH28,des-Gly9]AVPAntagonist9.1pKi
d(CH2)5[D-Tyr(Et)2,Val4,Tyr-NH29]AVPAntagonist9.1pKi
d(CH2)5[Tyr(Et)2,Val4,des-Gly9]AVPAntagonist9.1pKi
d[Pen1,Tyr(Me)2]AVPAntagonist9.1pKi
d(CH2)5[Tyr(Me)2,Thr4,Tyr(3125I)-NH29]OVTAntagonist9.0pKd
[3H]d(CH2)5[Tyr(Me)2]AVPAntagonist9.0pKd
d(CH2)5[Tyr(Me)2,Arg8]VPAntagonist9.0pKi
Ro5028442Antagonist9.0pKi
d(CH2)5[Tyr(Me)2,Thr4,Phe(3I,4N3)-NH29]OVTAntagonist8.9pKi

Binding affinities (BindingDB)

310 measured of 312 human assays (313 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValuePatent
(5E)-5-[1-(4-chlorophenyl)-2-fluoroethylidene]-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI0.398 nMUS-10092551: Spiro-thiazolones
(5Z)-5-[1-(6-chloro-3-pyridinyl)ethylidene]-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI0.398 nMUS-10092551: Spiro-thiazolones
CAS_50-56-6KI0.5 nM
(5Z)-5-[1-(4-chlorophenyl)ethylidene]-2-spiro[7H-furo[3,4-b]pyridine-5,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI0.501 nMUS-10092551: Spiro-thiazolones
(5Z)-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-5-(6,7,8,9-tetrahydrobenzo[7]annulen-5-ylidene)-1,3-thiazol-4-oneKI0.501 nMUS-10092551: Spiro-thiazolones
(5E)-5-(2-hydroxy-1-phenylethylidene)-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI0.501 nMUS-10092551: Spiro-thiazolones
1’-[(5Z)-4-oxo-5-(1-phenylethylidene)-1,3-thiazol-2-yl]spiro[2-benzofuran-3,4’-piperidine]-1-oneKI0.501 nMUS-10092551: Spiro-thiazolones
tert-butyl N-[(2E)-2-(4-oxo-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-5-ylidene)-2-phenylethyl]carbamateKI0.501 nMUS-10092551: Spiro-thiazolones
(5Z)-5-[1-(6-chloro-3-pyridinyl)-2,2,2-trideuterioethylidene]-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI0.501 nMUS-10092551: Spiro-thiazolones
(5Z)-5-[1-(4-chlorophenyl)ethylidene]-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI0.631 nMUS-10092551: Spiro-thiazolones
(5Z)-5-(1-phenylethylidene)-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI0.631 nMUS-10092551: Spiro-thiazolones
(5Z)-5-[1-(1H-pyrrol-2-yl)ethylidene]-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI0.631 nMUS-10092551: Spiro-thiazolones
(5Z)-5-[1-(6-chloro-3-pyridinyl)propylidene]-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI0.631 nMUS-10092551: Spiro-thiazolones
(5Z)-5-[1-(4-chlorophenyl)propylidene]-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI0.794 nMUS-10092551: Spiro-thiazolones
(5E)-5-[1-(4-chlorophenyl)-2,2,2-trifluoroethylidene]-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI0.794 nMUS-10092551: Spiro-thiazolones
(5Z)-5-[1-(1-methylpyrrol-2-yl)ethylidene]-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI0.794 nMUS-10092551: Spiro-thiazolones
(5Z)-5-[1-(2-fluoro-3-pyridinyl)ethylidene]-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI0.794 nMUS-10092551: Spiro-thiazolones
[3-[[2-[3-(4-chlorophenyl)-5-oxo-4-[(2S)-3,3,3-trifluoro-2-hydroxypropyl]-1,2,4-triazol-1-yl]acetyl]amino]-2-[2-(trifluoromethyl)phenyl]propyl] carbamateIC501 nMUS-9180120: Substituted N-phenethyltriazoloneacetamides and use thereof
(5Z)-5-[1-(4-chlorophenyl)ethylidene]-2-spiro[5H-furo[3,4-b]pyridine-7,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1 nMUS-10092551: Spiro-thiazolones
1’-[(5Z)-5-[1-(4-chlorophenyl)ethylidene]-4-oxo-1,3-thiazol-2-yl]spiro[2-benzofuran-3,4’-piperidine]-1-oneKI1 nMUS-10092551: Spiro-thiazolones
(5Z)-5-[1-(4-chlorophenyl)ethylidene]-2-spiro[1H-furo[3,4-c]pyridine-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1 nMUS-10092551: Spiro-thiazolones
(5Z)-5-(7-chloro-3,4-dihydro-2H-naphthalen-1-ylidene)-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1 nMUS-10092551: Spiro-thiazolones
(5Z)-5-[1-(2-fluorophenyl)ethylidene]-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1 nMUS-10092551: Spiro-thiazolones
(5Z)-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-5-[1-(1,3-thiazol-2-yl)ethylidene]-1,3-thiazol-4-oneKI1 nMUS-10092551: Spiro-thiazolones
(5Z)-5-(3-chloro-6,7,8,9-tetrahydrobenzo[7]annulen-5-ylidene)-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1 nMUS-10092551: Spiro-thiazolones
(5E)-5-(2-methoxy-1-phenylethylidene)-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1 nMUS-10092551: Spiro-thiazolones
5-[bis(1H-pyrrol-2-yl)methylidene]-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1 nMUS-10092551: Spiro-thiazolones
(5Z)-5-(2-hydroxy-1-phenylethylidene)-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1 nMUS-10092551: Spiro-thiazolones
1’-[(5Z)-5-[1-(6-chloro-3-pyridinyl)propylidene]-4-oxo-1,3-thiazol-2-yl]spiro[2-benzofuran-3,4’-piperidine]-1-oneKI1 nMUS-10092551: Spiro-thiazolones
(5E)-5-(1-phenylethylidene)-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1 nMUS-10092551: Spiro-thiazolones
cis-2-[2-(3-Chlorophenyl)-4-oxo-6-[3-(1-piperidylmethyl)cyclobutyl]quinazolin-3-yl]-N-[(1R)-2,2,2-trifluoro-1-methyl-ethyl]acetamideKI1 nMUS-9617226: Fused heterocyclic or carbocyclic compounds carrying a substituted cycloaliphatic radical and use thereof for treating vasopressin-related diseases
(1’S,5’R)-8’-[(5Z)-5-[1-(4-chlorophenyl)ethylidene]-4-oxo-1,3-thiazol-2-yl]spiro[2-benzofuran-3,3’-8-azabicyclo[3.2.1]octane]-1-oneKI1.26 nMUS-10092551: Spiro-thiazolones
(5Z)-5-[1-(6-methyl-3-pyridinyl)ethylidene]-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1.26 nMUS-10092551: Spiro-thiazolones
(5Z)-5-[1-(furan-2-yl)ethylidene]-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1.26 nMUS-10092551: Spiro-thiazolones
(5Z)-5-(1-pyridin-3-ylethylidene)-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1.26 nMUS-10092551: Spiro-thiazolones
(5Z)-5-[1-(2,4-dimethyl-1,3-oxazol-5-yl)ethylidene]-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1.26 nMUS-10092551: Spiro-thiazolones
(5E)-5-(1H-isochromen-4-ylidene)-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1.26 nMUS-10092551: Spiro-thiazolones
5-heptan-4-ylidene-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1.26 nMUS-10092551: Spiro-thiazolones
5-(dicyclopropylmethylidene)-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1.26 nMUS-10092551: Spiro-thiazolones
(5E)-5-[1-(6-chloro-3-pyridinyl)-2-hydroxyethylidene]-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1.26 nMUS-10092551: Spiro-thiazolones
1’-[(5E)-5-[2-[tert-butyl(dimethyl)silyl]oxy-1-phenylethylidene]-4-oxo-1,3-thiazol-2-yl]spiro[2-benzofuran-3,4’-piperidine]-1-oneKI1.26 nMUS-10092551: Spiro-thiazolones
(5E)-5-[1-(6-chloro-3-pyridinyl)-2,2,2-trideuterioethylidene]-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1.26 nMUS-10092551: Spiro-thiazolones
5-(1,3-dimethoxypropan-2-ylidene)-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1.58 nMUS-10092551: Spiro-thiazolones
(5Z)-5-(1-pyridin-2-ylethylidene)-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1.58 nMUS-10092551: Spiro-thiazolones
(5Z)-5-(1-cyclopentylethylidene)-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1.58 nMUS-10092551: Spiro-thiazolones
(5Z)-5-(2-methoxycyclohexylidene)-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1.58 nMUS-10092551: Spiro-thiazolones
(5Z)-5-[1-(2-chloro-3-pyridinyl)ethylidene]-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1.58 nMUS-10092551: Spiro-thiazolones
5-(2,4-dimethylpentan-3-ylidene)-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-1,3-thiazol-4-oneKI1.58 nMUS-10092551: Spiro-thiazolones
1’-[(5E)-5-(2-hydroxy-1-phenylethylidene)-4-oxo-1,3-thiazol-2-yl]spiro[2-benzofuran-3,4’-piperidine]-1-oneKI1.58 nMUS-10092551: Spiro-thiazolones
(5Z)-2-spiro[1H-2-benzofuran-3,4’-piperidine]-1’-yl-5-[2,2,2-trideuterio-1-(6-methyl-3-pyridinyl)ethylidene]-1,3-thiazol-4-oneKI1.58 nMUS-10092551: Spiro-thiazolones

ChEMBL bioactivities

2117 potent at pChembl≥5 of 2183 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
10.49Ki0.032nMCHEMBL394602
10.47EC500.034nMCHEMBL4094454
10.44Ki0.036nMCHEMBL394602
10.43Ki0.03715nMCHEMBL1807272
10.40Ki0.04nMCHEMBL6087371
10.40Ki0.03981nMCHEMBL1807267
10.30Ki0.05nMCHEMBL1083094
10.22Ki0.06nMCHEMBL1084823
10.20Ki0.063nMCHEMBL6027125
10.15Ki0.07nMCHEMBL540192
10.10Ki0.08nMCHEMBL269012
10.05Ki0.09nMCHEMBL1161978
10.02Ki0.0955nMCHEMBL1807270
10.00Ki0.1nMCHEMBL5549819
10.00Ki0.1nMCHEMBL5573173
10.00Ki0.1nMCHEMBL5565555
10.00Ki0.1nMCHEMBL6150478
10.00Ki0.1nMCHEMBL1084008
9.92EC500.12nMCHEMBL4094454
9.90EC500.1259nMCHEMBL3342789
9.90EC500.1259nMCHEMBL4165132
9.89Ki0.13nMCHEMBL6101825
9.85Ki0.14nMCHEMBL6108956
9.85EC500.1413nMCHEMBL1819540
9.85EC500.14nMCHEMBL1819540
9.82Ki0.15nMATOSIBAN
9.82EC500.15nMCHEMBL1819441
9.81EC500.1549nMCHEMBL1819441
9.80EC500.1585nMCHEMBL3342790
9.80EC500.1585nMCHEMBL4173036
9.77Ki0.17nMCHEMBL412210
9.77Ki0.17nMCHEMBL430272
9.77EC500.17nMCHEMBL4096848
9.77Ki0.17nMCHEMBL6108984
9.74EC500.18nMOXYTOCIN
9.74Ki0.182nMCHEMBL1807266
9.72EC500.19nMOXYTOCIN
9.72Ki0.19nMRELCOVAPTAN
9.70Ki0.2nMCHEMBL4281963
9.70Ki0.2nMCHEMBL397179
9.70Ki0.2nMCHEMBL5575561
9.70Ki0.2nMCHEMBL5575281
9.70Ki0.2nMCHEMBL5563095
9.70Ki0.2nMCHEMBL5569717
9.70Ki0.2nMCHEMBL5571184
9.70Ki0.2nMCHEMBL5542954
9.70Ki0.2nMCHEMBL5574628
9.70Ki0.2nMCHEMBL5575102
9.70Ki0.2nMCHEMBL5975276
9.70Ki0.2nMCHEMBL6102315

PubChem BioAssay actives

1606 with measured affinity, of 3837 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.

CompoundAssayTypeValueUnit
(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-carboxamide1450441: Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayec50<0.0001uM
(2S)-N-[(2S)-4-amino-1-[[(2S)-1-[(3S)-3-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]-2-[[(2S)-2-[[(2R)-3-(4-hydroxyphenyl)-2-[[2-(4-hydroxyphenyl)acetyl]-methylamino]propanoyl]amino]-3-phenylpropanoyl]amino]pentanediamide298221: Inhibition of human vasopressin V1a receptor expressed in CHO cells by polarisation binding assay using 96-well plate membraneski<0.0001uM
1-(4-chlorophenyl)-N-[(2R)-3-(4-chlorophenyl)-1-[[4-(dimethylamino)cyclohexyl]amino]-1-oxopropan-2-yl]cyclopropane-1-carboxamide608204: Displacement of [3H]AVP from human V1A receptor expressed in CHO cellski<0.0001uM
N-[(2R)-3-(4-chlorophenyl)-1-[[4-(dimethylamino)cyclohexyl]amino]-1-oxopropan-2-yl]-1-(4-fluorophenyl)cyclopentane-1-carboxamide608204: Displacement of [3H]AVP from human V1A receptor expressed in CHO cellski<0.0001uM
vasopressin1593564: Agonist activity at recombinant human V1a receptor 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 methodec50<0.0001uM
(5S)-8-chloro-5-(fluoromethyl)-1-(4-pyridin-2-yloxycyclohexyl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine2093664: Displacement of [3H]vasopressin from human V1A receptor assessed as inhibition constant by Cheng-Prusoff equation analysiski0.0001uM
(5R)-8-chloro-5-(fluoromethyl)-1-(4-pyridin-2-yloxycyclohexyl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine2093664: Displacement of [3H]vasopressin from human V1A receptor assessed as inhibition constant by Cheng-Prusoff equation analysiski0.0001uM
8’-chloro-1’-(4-pyridin-2-yloxycyclohexyl)spiro[1,3-dioxepane-2,5’-4,6-dihydro-[1,2,4]triazolo[4,3-a][1]benzazepine]2093664: Displacement of [3H]vasopressin from human V1A receptor assessed as inhibition constant by Cheng-Prusoff equation analysiski0.0001uM
4-chloro-N-(2-methylpyrazol-3-yl)benzenesulfonamide1507372: Antagonist activity at human vasopressin 1a receptor expressed in HEK293 cell membranes assessed as inhibition of AVP-induced increase in Ca2+ flux preincubated for 5 mins followed by AVP addition measured after 5 mins for every 2 secs by Ca5 dye based FLIPR assayec500.0001uM
(2S)-N-[(2S)-4-amino-1-[[(2S)-1-[(2S)-2-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]-2-[[(2S)-2-[[(2R)-3-(4-hydroxyphenyl)-2-[[2-(4-hydroxyphenyl)acetyl]-methylamino]propanoyl]amino]-3-phenylpropanoyl]amino]pentanediamide217092: Displacement of [125I]- HO-LVA from human Vasopressin V1a receptor in membranes of CHO cellski0.0001uM
(2S)-N-[(2S)-4-amino-1-[[(2S)-1-[(2S)-2-[[3’,6’-bis(dimethylamino)-3-oxospiro[2-benzofuran-1,9’-xanthene]-5-carbonyl]-[(2S)-1,6-diamino-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]-2-[[(2S)-2-[[(2R)-3-(4-hydroxyphenyl)-2-[3-(4-hydroxyphenyl)propanoyl-methylamino]propanoyl]amino]-3-phenylpropanoyl]amino]pentanediamide217092: Displacement of [125I]- HO-LVA from human Vasopressin V1a receptor in membranes of CHO cellski0.0001uM
4-[2-[[6-[[(3S)-1-[(2S)-2-[[(2S)-4-amino-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2R)-3-(4-hydroxyphenyl)-2-[3-(4-hydroxyphenyl)propanoyl-methylamino]propanoyl]amino]-3-phenylpropanoyl]amino]-5-oxopentanoyl]amino]-4-oxobutanoyl]amino]-5-carbamimidamidopentanoyl]pyrrolidine-3-carbonyl]-[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethyl]sulfanyl-2,3,5-trichloro-6-(7,7,9,17,19,19-hexamethyl-4,22-disulfo-2-oxa-6,20-diazapentacyclo[12.8.0.03,12.05,10.016,21]docosa-1(14),5,12,15,21-pentaen-13-yl)benzoic acid298215: Displacement of [3H]AVP from human vasopressin V1a receptor expressed in CHO cellski0.0001uM
[4-(2-methylphenyl)phenyl]-[(1S,5R)-1,3,3-trimethyl-6-azabicyclo[3.2.1]octan-6-yl]methanone483981: Displacement [3H]Arg human recombinant Vasopressin V1a receptorki0.0001uM
[3-methyl-4-(2-methylphenyl)phenyl]-[(1S,5R)-1,3,3-trimethyl-6-azabicyclo[3.2.1]octan-6-yl]methanone483981: Displacement [3H]Arg human recombinant Vasopressin V1a receptorki0.0001uM
[4-(1H-indol-3-yl)-3-methoxyphenyl]-[(1S,5R)-1,3,3-trimethyl-6-azabicyclo[3.2.1]octan-6-yl]methanone483981: Displacement [3H]Arg human recombinant Vasopressin V1a receptorki0.0001uM
(2S)-N-[(2S)-5-amino-1-[(2-amino-2-oxoethyl)amino]-1-oxopentan-2-yl]-1-[(4R,7S,10S,13S,16R)-7-(2-amino-2-oxoethyl)-13-[(2S)-butan-2-yl]-16-[(4-ethoxyphenyl)methyl]-10-[(1R)-1-hydroxyethyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide317413: Binding affinity to human vasopressin V1a receptorki0.0001uM
(2S)-1-[(4R,7S,10S,13S,16S,19R)-19-amino-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13,16-dibenzyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]pyrrolidine-2-carboxamide613479: Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayec500.0001uM
(2S)-N-[(2S)-5-amino-1-[(2-amino-2-oxoethyl)amino]-1-oxopentan-2-yl]-1-[(4R,7S,10S,13S,16S,19R)-19-amino-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13,16-dibenzyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide613479: Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayec500.0001uM
1-(4-chlorophenyl)-N-[(2R)-3-(4-chlorophenyl)-1-[[4-(dimethylamino)cyclohexyl]amino]-1-oxopropan-2-yl]cyclobutane-1-carboxamide608204: Displacement of [3H]AVP from human V1A receptor expressed in CHO cellski0.0001uM
4-chloro-N-(2-pyridin-2-ylpyrazol-3-yl)benzenesulfonamide1507372: Antagonist activity at human vasopressin 1a receptor expressed in HEK293 cell membranes assessed as inhibition of AVP-induced increase in Ca2+ flux preincubated for 5 mins followed by AVP addition measured after 5 mins for every 2 secs by Ca5 dye based FLIPR assayec500.0001uM
(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-carboxamide1450441: Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayec500.0002uM
(2S)-N-[(2S)-4-amino-1-[[(2S)-1-[(2S)-2-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]-2-[[(2S)-2-[[(2R)-2-[3-(4-hydroxyphenyl)propanoylamino]-3-(4-methoxyphenyl)propanoyl]amino]-3-phenylpropanoyl]amino]pentanediamide1409547: Displacement of [Se-Se]-AVP from human V1A receptor expressed in CHO cells after 4 hrs by RP-LC-ICPMS analysiski0.0002uM
(5R)-8-chloro-5-methoxy-1-(4-pyridin-2-yloxycyclohexyl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine2093664: Displacement of [3H]vasopressin from human V1A receptor assessed as inhibition constant by Cheng-Prusoff equation analysiski0.0002uM
N-[(5R)-8-chloro-1-(4-pyridin-2-yloxycyclohexyl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl]-3-(dimethylamino)propanamide2093664: Displacement of [3H]vasopressin from human V1A receptor assessed as inhibition constant by Cheng-Prusoff equation analysiski0.0002uM
8’-bromo-1’-(4-pyridin-2-yloxycyclohexyl)spiro[1,3-dioxolane-2,5’-4,6-dihydro-[1,2,4]triazolo[4,3-a][1]benzazepine]2093664: Displacement of [3H]vasopressin from human V1A receptor assessed as inhibition constant by Cheng-Prusoff equation analysiski0.0002uM
8’-fluoro-1’-(4-pyridin-2-yloxycyclohexyl)spiro[1,3-dioxolane-2,5’-4,6-dihydro-[1,2,4]triazolo[4,3-a][1]benzazepine]2093664: Displacement of [3H]vasopressin from human V1A receptor assessed as inhibition constant by Cheng-Prusoff equation analysiski0.0002uM
[4-(8’-chlorospiro[1,3-dioxolane-2,5’-4,6-dihydro-[1,2,4]triazolo[4,3-a][1]benzazepine]-1’-yl)cyclohexyl]-morpholin-4-ylmethanone2093664: Displacement of [3H]vasopressin from human V1A receptor assessed as inhibition constant by Cheng-Prusoff equation analysiski0.0002uM
8’-chloro-1’-(4-methoxy-4-methylcyclohexyl)spiro[1,3-dioxolane-2,5’-4,6-dihydro-[1,2,4]triazolo[4,3-a][1]benzazepine]2093664: Displacement of [3H]vasopressin from human V1A receptor assessed as inhibition constant by Cheng-Prusoff equation analysiski0.0002uM
8’-methyl-1’-(4-pyridin-2-yloxycyclohexyl)spiro[1,3-dioxolane-2,5’-4,6-dihydro-[1,2,4]triazolo[4,3-a][1]benzazepine]2093664: Displacement of [3H]vasopressin from human V1A receptor assessed as inhibition constant by Cheng-Prusoff equation analysiski0.0002uM
8-chloro-1-(4-pyridin-2-yloxycyclohexyl)spiro[4,6-dihydro-[1,2,4]triazolo[4,3-a][1]benzazepine-5,4’-oxane]2093664: Displacement of [3H]vasopressin from human V1A receptor assessed as inhibition constant by Cheng-Prusoff equation analysiski0.0002uM
Oxytocin1591640: Agonist activity at human V1A receptor expressed in HEK293 cells assessed as intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric methodec500.0002uM
(2S)-N-[(2S)-4-amino-1-[[(2S)-5-(diaminomethylideneamino)-1-[(2S)-2-[[(2S)-1,6-diamino-1-oxohexan-2-yl]-(3’,6’-dihydroxy-1-oxospiro[2-benzofuran-3,9’-xanthene]-5-carbonyl)carbamoyl]pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]-2-[[(2S)-2-[[(2R)-3-(4-hydroxyphenyl)-2-[3-(4-hydroxyphenyl)propanoyl-methylamino]propanoyl]amino]-3-phenylpropanoyl]amino]pentanediamide217092: Displacement of [125I]- HO-LVA from human Vasopressin V1a receptor in membranes of CHO cellski0.0002uM
(2S)-N-[(2S)-4-amino-1-[[(2S)-1-[(2S)-2-[[3’,6’-bis(dimethylamino)-1-oxospiro[2-benzofuran-3,9’-xanthene]-5-carbonyl]-[(2S)-1,6-diamino-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]-2-[[(2S)-2-[[(2R)-3-(4-hydroxyphenyl)-2-[3-(4-hydroxyphenyl)propanoyl-methylamino]propanoyl]amino]-3-phenylpropanoyl]amino]pentanediamide217092: Displacement of [125I]- HO-LVA from human Vasopressin V1a receptor in membranes of CHO cellski0.0002uM
(2S)-N-[(2S)-4-amino-1-[[(2S)-5-(diaminomethylideneamino)-1-[(2S)-2-[[(2S)-1,6-diamino-1-oxohexan-2-yl]-(3’,6’-dihydroxy-3-oxospiro[2-benzofuran-1,9’-xanthene]-5-carbonyl)carbamoyl]pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]-2-[[(2S)-2-[[(2R)-3-(4-hydroxyphenyl)-2-[3-(4-hydroxyphenyl)propanoyl-methylamino]propanoyl]amino]-3-phenylpropanoyl]amino]pentanediamide217092: Displacement of [125I]- HO-LVA from human Vasopressin V1a receptor in membranes of CHO cellski0.0002uM
(2S)-5-(4-cyclohexylpiperazin-1-yl)-N-[[2-fluoro-3-(trifluoromethyl)phenyl]methyl]-5-oxo-2-[(3S,4R)-2-oxo-3-[(4S)-2-oxo-4-phenyl-1,3-oxazolidin-3-yl]-4-[(E)-2-phenylethenyl]azetidin-1-yl]pentanamide293624: Binding affinity for human cloned vasopressin V1a receptor expressed in CHO cellski0.0002uM
N-(2-methylpyrazol-3-yl)-4-(trifluoromethyl)benzenesulfonamide1507372: Antagonist activity at human vasopressin 1a receptor expressed in HEK293 cell membranes assessed as inhibition of AVP-induced increase in Ca2+ flux preincubated for 5 mins followed by AVP addition measured after 5 mins for every 2 secs by Ca5 dye based FLIPR assayec500.0002uM
(2S)-1-[(4R,7S,10S,13S,16S,19R)-19-amino-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-16-benzyl-13-[(2S)-butan-2-yl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-1-oxo-5-(propylamino)pentan-2-yl]pyrrolidine-2-carboxamide613479: Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayec500.0002uM
N-[(2R)-3-(4-chlorophenyl)-1-[[4-(dimethylamino)cyclohexyl]amino]-1-oxopropan-2-yl]-1-(4-fluorophenyl)cyclopropane-1-carboxamide608204: Displacement of [3H]AVP from human V1A receptor expressed in CHO cellski0.0002uM
(2R)-N-[(1S,5R)-8-azabicyclo[3.2.1]octan-3-yl]-3-(4-chlorophenyl)-2-[[2-(4-chlorophenyl)acetyl]amino]propanamide596611: Displacement of [3H]AVP from human V1A receptor expressed in CHO cellski0.0002uM
(2S)-N-[(2S)-5-amino-1-[(2-amino-2-oxoethyl)amino]-1-oxopentan-2-yl]-1-[(4R,7S,10S,13S,16S,19R)-19-amino-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-carboxamide613479: Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayec500.0002uM
(2R)-3-(4-chlorophenyl)-2-[[2-(4-chlorophenyl)acetyl]amino]-N-(2-hydroxycyclohexyl)propanamide608204: Displacement of [3H]AVP from human V1A receptor expressed in CHO cellski0.0002uM
(2R)-3-(4-chlorophenyl)-2-[[2-(4-chlorophenyl)acetyl]amino]-N-[4-(dimethylamino)cyclohexyl]propanamide608204: Displacement of [3H]AVP from human V1A receptor expressed in CHO cellski0.0002uM
(2S)-1-[(2R,3S)-5-chloro-3-(2-chlorophenyl)-1-(3,4-dimethoxyphenyl)sulfonyl-3-hydroxy-2H-indole-2-carbonyl]pyrrolidine-2-carboxamide298224: Inhibition of human vasopressin V1a receptor expressed in COS7 cells by HTRF-FRET assay using 96-well plate membraneski0.0002uM
N-(2-pyridin-2-ylpyrazol-3-yl)-4-(trifluoromethyl)benzenesulfonamide1507372: Antagonist activity at human vasopressin 1a receptor expressed in HEK293 cell membranes assessed as inhibition of AVP-induced increase in Ca2+ flux preincubated for 5 mins followed by AVP addition measured after 5 mins for every 2 secs by Ca5 dye based FLIPR assayec500.0002uM
8-chloro-1-(4-pyridin-2-yloxycyclohexyl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-ol1820284: Displacement of [3H]-arginine-vasopressin from human V1A receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayki0.0003uM
(2S)-N-[(2S)-4-amino-1-[[(2S)-1-[(2S)-2-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]-2-[[(2S)-2-[[(2R)-2-[[2-(4-hydroxyphenyl)selanylacetyl]amino]-3-(4-methoxyphenyl)propanoyl]amino]-3-phenylpropanoyl]amino]pentanediamide1409545: Binding affinity to human V1A receptor expressed in CHO cells after 4 hrs by RP-LC-ICPMS analysiskd0.0003uM
[(5S)-8-chloro-1-(4-pyridin-2-yloxycyclohexyl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl]methanol2093664: Displacement of [3H]vasopressin from human V1A receptor assessed as inhibition constant by Cheng-Prusoff equation analysiski0.0003uM
[(5R)-8-chloro-1-(4-pyridin-2-yloxycyclohexyl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl]methanol2093664: Displacement of [3H]vasopressin from human V1A receptor assessed as inhibition constant by Cheng-Prusoff equation analysiski0.0003uM
(5R)-8-chloro-N-ethyl-1-(4-pyridin-2-yloxycyclohexyl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine2093664: Displacement of [3H]vasopressin from human V1A receptor assessed as inhibition constant by Cheng-Prusoff equation analysiski0.0003uM
8’-chloro-1’-(4-pyridin-2-yloxycyclohexyl)spiro[1,3-dioxane-2,5’-4,6-dihydro-[1,2,4]triazolo[4,3-a][1]benzazepine]2093664: Displacement of [3H]vasopressin from human V1A receptor assessed as inhibition constant by Cheng-Prusoff equation analysiski0.0003uM

CTD chemical–gene interactions

24 total (human), top 24 by PubMed support.

ChemicalActions (top 5)PubMed papers
Benzo(a)pyreneaffects methylation, decreases expression, decreases methylation2
arseniteincreases methylation1
mono-(2-ethylhexyl)phthalateincreases expression1
vasopressin, 1-(1-mercaptocyclohexaneacetic acid)-2-(O- methyl-L-tyrosine)-8-L-arginine-decreases reaction, increases activity1
relcovaptandecreases activity1
CGP 52608affects binding, increases reaction1
2,7-dihydroxynaphthalenedecreases expression1
F-180 vasoconstrictor peptideaffects activity1
bardoxolone methyldecreases activity1
GW 7647increases expression1
gypenosidedecreases expression1
vasopressin, Phe(2)-Ile(3)-Hgn(4)-Orn(iPr)(8)-affects binding, increases activity1
Arginine Vasopressinincreases activity, decreases reaction1
Carmustineincreases expression1
Cycloheximidedecreases expression, decreases reaction1
Doxorubicinincreases expression1
Chlorpyrifosaffects expression, affects response to substance1
Etoposideincreases expression1
Monobactamsaffects binding1
Progesteroneincreases expression1
Tetrachlorodibenzodioxindecreases expression, decreases reaction1
Valproic Acidincreases expression1
Aflatoxin B1decreases methylation1
Okadaic Aciddecreases expression1

ChEMBL screening assays

437 unique, capped per target: 321 binding, 108 functional, 8 admet

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1001061BindingBinding affinity to vasopressin 1A receptorSynthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists. — J Med Chem
CHEMBL1015245FunctionalAgonist activity at human vasopressin V1a receptor upto 10 uM by reporter gene assayNew benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists. — J Med Chem
CHEMBL4018362ADMETAgonist activity at human V1a receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayPotent and selective oxytocin receptor agonists without disulfide bridges. — Bioorg Med Chem Lett

Cellosaurus cell lines

5 cell lines: 2 spontaneously immortalized cell line, 2 cancer cell line, 1 transformed cell line

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

CellosaurusNameCategorySex
CVCL_H507CHO-K1/V1ASpontaneously immortalized cell lineFemale
CVCL_KZ75PathHunter U2OS AVPR1A beta-arrestinCancer cell lineFemale
CVCL_KZ76PathHunter U2OS AVPR1A Total GPCR InternalizationCancer cell lineFemale
CVCL_LB56GeneBLAzer AVPR1a-NFAT-bla CHO-K1Spontaneously immortalized cell lineFemale
CVCL_YK01HEK293 AVPR1A HiTSeekerTransformed cell lineFemale

Clinical trials (associated diseases)

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

TrialPhaseStatusTitle
NCT00391261PHASE4COMPLETEDAn Open-label Trial of Metformin for Weight Control of Pediatric Patients on Antipsychotic Medications.
NCT01028820PHASE4COMPLETEDFMRI Brain Activation of Aripiprazole Treatment in Autism Spectrum Disorders
NCT01333865PHASE4COMPLETEDA Study of Memantine Hydrochloride (Namenda®) for Cognitive and Behavioral Impairment in Adults With Autism Spectrum Disorders
NCT01337700PHASE4COMPLETEDMilnacipran in Autism and the Functional Locus Coeruleus and Noradrenergic Model of Autism
NCT01695200PHASE4COMPLETEDOmega-3 Fatty Acids in Autism Spectrum Disorders
NCT02096952PHASE4COMPLETEDMethylphenidate ER Liquid Formulation in Adults With ASD and ADHD
NCT02235467PHASE4COMPLETEDMultisite Study: Parental Training Using Video Modelling to Develop Social Skills in Children With Autism
NCT02940574PHASE4COMPLETEDNeural and Behavioral Effects of Oxytocin in Autism Spectrum Disorders
NCT03333629PHASE4COMPLETEDPromoting Positive Outcomes for Individuals With ASD: Linking Early Detection, Treatment, and Long-term Outcomes
NCT03337646PHASE4COMPLETEDEvaluation of the Effect and Safety of Lisdexamfetamine in Children Aged 6-12 With ADHD and Autism
NCT03538431PHASE4COMPLETEDImproving Driving in Young People With Autism Spectrum Disorders
NCT03757585PHASE4COMPLETEDNatural Treatments for the Management of Emotional Dysregulation in Youth With Non-verbal Learning Disability (NVLD) and/or Autism Spectrum Disorders (ASD)
NCT04903353PHASE4COMPLETEDPragmatic Trial Comparing Weight Gain in Children With Autism Taking Risperidone Versus Aripiprazole
NCT05063656PHASE4COMPLETEDBiomarker-Driven Pharmacological Treatment of Adolescents With Autism Spectrum Disorder With Gabapentin
NCT05146245PHASE4UNKNOWNSafety and Pharmacokinetics of Antipsychotics in Children 2: Studying TDM in an RCT
NCT05916339PHASE4RECRUITINGAWARE: Management of ADHD in Autism Spectrum Disorder
NCT05954052PHASE4TERMINATEDA Study of Glutathione in Children With Autism Spectrum Disorder
NCT06853665PHASE4RECRUITINGThe TEAM Study - Treatment Efficacy for Autism/Attention Using Mixed Amphetamine
NCT07054697PHASE4COMPLETEDPilot-RCT With Individualized Homeopathic Treatment in the Children With Autism Spectrum Disorder
NCT07161804PHASE4COMPLETEDPilot RCT Using Homeopathic Medicines in ASD
NCT07439042PHASE4NOT_YET_RECRUITINGBuspirone for Anxiety in Autistic Youth
NCT01302964PHASE3COMPLETEDMirtazapine Treatment of Anxiety in Children and Adolescents With Pervasive Developmental Disorders
NCT01706523PHASE3TERMINATEDOpen Label Extension Study of STX209 (Arbaclofen) in Autism Spectrum Disorders
NCT01825798PHASE3COMPLETEDTreatment of Overweight Induced by Antipsychotic Medication in Young People With Autism Spectrum Disorders (ASD)
NCT01972074PHASE3COMPLETEDBehavioral and Neural Response to Memantine in Adolescents With Autism Spectrum Disorder
NCT02985749PHASE3COMPLETEDA Study of Oxytocin for the Treatment of Social Impairment in Individuals With High Functioning Autism Spectrum Disorder
NCT03197922PHASE3COMPLETEDTreatment of Encopresis in Children With Autism Spectrum Disorders
NCT03504917PHASE3TERMINATEDA Study of Balovaptan in Adults With Autism Spectrum Disorder With a 2-Year Open-Label Extension
NCT03553875PHASE3TERMINATEDMemantine for the Treatment of Social Deficits in Youth With Disorders of Impaired Social Interactions
NCT03640156PHASE3COMPLETEDModulating Socially Adaptive Mirror System Functioning in Autism by Oxytocin
NCT03715153PHASE3TERMINATEDEfficacy and Safety of Bumetanide Oral Liquid Formulation in Children Aged From 2 to Less Than 7 Years Old With Autism Spectrum Disorder.
NCT03715166PHASE3TERMINATEDEfficacy and Safety of Bumetanide Oral Liquid Formulation in Children and Adolescents Aged From 7 to Less Than 18 Years Old With Autism Spectrum Disorder
NCT04233502PHASE3WITHDRAWNEfficacy and Safety of Slenyto for Insomnia in Children With ASD
NCT04578756PHASE3COMPLETEDOpen-Label, Flexible-dose Study to Evaluate the Long-Term Safety and Tolerability of Cariprazine in the Treatment of Pediatric Participants With Schizophrenia, Bipolar I Disorder, or Autism Spectrum Disorder
NCT04623398PHASE3COMPLETEDEffect of Lithium in Patients With Autism Spectrum Disorder and Phelan-McDermid Syndrome (SHANK3 Haploinsufficiency)
NCT04725383PHASE3TERMINATEDAmitriptyline for Repetitive Behaviors in Autism Spectrum Disorders
NCT05212493PHASE3COMPLETEDThe Effects of Medical Cannabis in Children With Autistic Spectrum Disorder
NCT05361707PHASE3UNKNOWNEvaluating the Effects of Tasimelteon in Individuals With Autism Spectrum Disorder (ASD) and Sleep Disturbances
NCT05439616PHASE3COMPLETEDStudy of Cariprazine Oral Capsules or Solution to Assess Adverse Events and Change in Irritability Due to Autism Spectrum Disorder (ASD) in Participants Aged 5-17 Years With ASD
NCT06229210PHASE3RECRUITINGSafety and Tolerability Trial of Lumateperone in Pediatric Patients With Schizophrenia, Bipolar Disorder or Autism Spectrum Disorder

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Sources 81

This page pulls from 81 datasets indexed by BioBTree:

alphafoldalphamissenseantibodybgeebgee_evidencebindingdbbiogrid_interactionbrendabrenda_kineticsccdscellosauruschembl_activitychembl_assaychembl_documentchembl_moleculechembl_targetciviccivic_evidenceclingen_dosageclingen_gene_validityclinical_trialsclinvarcollectrictd_gene_interactiondbsnpdepmapdiamond_similarityefoensemblentrezesm2_similarityexonfantom5_genefantom5_promotergenccgenerifgogoparentgtopdbgtopdb_interactiongwasgwas_studyhgnchpointactinterprointogenjasparmeshmimmirdbmondomsigdborphanetorthologparalogpatentpatent_compoundpdbpfampharmgkb_clinicalpharmgkb_genepharmgkb_guidelinepharmgkb_variantpubchempubchem_activitypubchem_assaypubmedreactomereactomeparentrefseqrhearnacentralscxa_expressionscxa_gene_experimentsignorspliceaistring_interactiontranscriptufeatureuniprot