UTS2R

gene

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Summary

UTS2R (urotensin 2 receptor, HGNC:4468) is a protein-coding gene on chromosome 17q25.3, encoding Urotensin-2 receptor (Q9UKP6). G protein-coupled receptor for the vasoactive neuropeptides urotensin-2 and urotensin-2B.

Predicted to enable urotensin II receptor activity. Predicted to be involved in neuropeptide signaling pathway. Predicted to be located in membrane. Predicted to be active in plasma membrane.

Source: NCBI Gene 2837 — RefSeq curated summary.

At a glance

Clinical variants (ClinVar): 4 total
Druggable target: yes — 1 molecules with ChEMBL bioactivity
MANE Select transcript: NM_018949

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:4468
Approved symbol	UTS2R
Name	urotensin 2 receptor
Location	17q25.3
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000181408
Ensembl biotype	protein_coding
OMIM	600896
Entrez	2837

Gene structure

Transcript identifiers

Ensembl transcripts: 3 — 3 protein_coding

ENST00000313135, ENST00000856767, ENST00000923106

RefSeq mRNA: 2 — MANE Select: NM_018949 NM_001381897, NM_018949

CCDS: CCDS11810

Canonical transcript exons

ENST00000313135 — 3 exons

Exon	Start	End
ENSE00001231793	82374243	82377458
ENSE00003900024	82371765	82372047
ENSE00003903805	82372598	82372783

Expression profiles

Bgee: expression breadth broad, 72 present calls, max score 70.60.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.2114 / max 36.9866, expressed in 84 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
163506	0.1054	45
163508	0.0609	30
163507	0.0450	23

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
upper leg skin	UBERON:0004262	70.60	silver quality
skin of hip	UBERON:0001554	68.69	silver quality
bone marrow cell	CL:0002092	62.99	silver quality
right testis	UBERON:0004534	57.32	gold quality
buccal mucosa cell	CL:0002336	56.43	gold quality
apex of heart	UBERON:0002098	55.67	gold quality
left testis	UBERON:0004533	55.41	gold quality
right atrium auricular region	UBERON:0006631	54.92	gold quality
left lobe of thyroid gland	UBERON:0001120	54.55	gold quality
cardiac atrium	UBERON:0002081	54.55	gold quality
hindlimb stylopod muscle	UBERON:0004252	54.08	silver quality
testis	UBERON:0000473	52.92	gold quality
heart left ventricle	UBERON:0002084	52.79	gold quality
medial globus pallidus	UBERON:0002477	52.69	gold quality
thyroid gland	UBERON:0002046	52.59	gold quality
cardiac ventricle	UBERON:0002082	52.36	gold quality
right lobe of thyroid gland	UBERON:0001119	52.00	gold quality
right frontal lobe	UBERON:0002810	50.44	gold quality
globus pallidus	UBERON:0001875	49.95	gold quality
heart	UBERON:0000948	49.46	gold quality
Brodmann (1909) area 9	UBERON:0013540	47.55	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	47.54	gold quality
prefrontal cortex	UBERON:0000451	47.26	gold quality
frontal cortex	UBERON:0001870	47.07	gold quality
cerebellar vermis	UBERON:0004720	46.54	gold quality
sural nerve	UBERON:0015488	46.15	gold quality
bone marrow	UBERON:0002371	45.64	gold quality
primary visual cortex	UBERON:0002436	45.27	silver quality
neocortex	UBERON:0001950	45.23	gold quality
amniotic fluid	UBERON:0000173	44.15	gold quality

Single-cell (SCXA)

Detected in 4 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-CURD-97	no	183.48
E-MTAB-6379	no	23.46
E-GEOD-81547	no	4.53
E-ANND-3	no	0.39

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): SP1, SP3, TBX5, TP53, YBX1

Literature-anchored findings (GeneRIF, showing 33)

urotensin II receptor (U2R) is up-regulated by interferon-gamma (PMID:14753294)
monocytes and macrophages were the largest producers of GPR14 mRNA, with relatively little expression in foam cells, lymphocytes, and platelets. (PMID:15306183)
Subjects with S89N amino acid substitution are more insulin-resistant and thus more susceptible to type 2 diabetes mellitus development. (PMID:15476949)
Since both mRNA for UT receptor and U-II binding were still present. ANG II receptors were also present as shown by ANG II-induced calcium mobilization. (PMID:15752584)
Diagnostic reagent kits using human rhabdomyosarcoma cells expressing UTS2R were compared. (PMID:17537987)
GPR14 is a candidate for the guanylate cyclase independent receptor for guanylin peptides. (PMID:17595527)
Cloning and functional characterization of the human UT receptor gene promoter revealed the presence of NF-kappaB-binding sites involved in UT receptor gene expression (PMID:17617581)
Data show that both urotensin II and urotensin II receptor are expressed in adrenal tumors and attached non-neoplastic adrenal tissues, and suggest possible roles of UII and UT-R in tumor growth and/or secretion. (PMID:17686550)
REsults describe the differential expression of urotensin II receptors in cardiovascular tissues from rats and humans and suggest that it may account for the diverse vascular actions reported for urotensin-II. (PMID:17905478)
To understand the molecular interactions of hU-II and certain antagonists with the hUT-II receptor, a model of the hUT-II receptor in an active conformation with all its connecting loops was constructed by homology modeling. (PMID:18409194)
Results describe the solution structure of urotensin-II receptor extracellular loop III and characterize its interaction with urotensin-II. (PMID:18423797)
Urotensin II receptor activation in vivo enhanced the adrenocortical expression of immunoreactive aldosterone synthase. (PMID:19001524)
Demonstrate an important role for UTS2R in the pathogenesis of atherosclerosis. The use of UTS2R receptor antagonists may provide a beneficial tool in the management of this debilitating disease process. (PMID:19111831)
This study demonstrates that UT receptor is expressed on the endothelium of HCC. U-II/UT receptor system is involved in HCC function and it involves endothelium and NO pathway. (PMID:19788716)
These findings suggest that the intrahepatic UII/UT system has an important pathophysiological role in cirrhosis and portal hypertension. (PMID:20428787)
An increased sensitivity to U-II in preeclampsia might be achieved by upregulation of placental U-II receptors. (PMID:20479331)
hUII may deteriorate monocrotaline-induced cardiac hypertrophy mainly through a vasoconstriction of the pulmonary artery and partly through the suppression of ANP secretion. (PMID:20870804)
Urotensin II receptor predicts the clinical outcome of prostate cancer patients and is involved in the regulation of motility of prostate adenocarcinoma cells. (PMID:21080343)
presence of functional nuclear UT in various rat and monkey tissues as well as in human cell lines (PMID:22245063)
Data show that vasoactive peptide urotensin II receptor and GABA(A)R are co-expressed in cerebellar glial cells from rat brain slices, in human native astrocytes and in glioma cell line. (PMID:22563490)
Data suggest that UTS2R in aortic endothelium is involved in development of diabetes-associated atherosclerosis; diabetes-associated plaque development is attenuated by urotensin II/UTS2R antagonism in in vitro setting. (PMID:23344731)
Report interaction of urantide with urotensin II receptor. (PMID:24357333)
UTR protein and mRNA levels were increased in colon cancer cell lines and in colon adenoma and adenocarcinoma. UTR appears to be involved in the regulation of colon cancer cell invasion and motility. (PMID:24372535)
family-based analysis of association between blood pressure, glomerular filtration and genes of the urotensin-II pathway (urotensin-II, urotensin-II related peptide, urotensin-II receptor) saturated with 28 tagging single nucleotide polymorphisms (PMID:24391740)
High UTR expression is an independent prognostic factor of good prognosis for non muscle invasive bladder transitional cancer. (PMID:24893613)
Urotensin II can induce the proliferation of BEL-7402 cells via the urotensin receptor mediated PKC/ERK/p38 MAPK signaling pathways. (PMID:25514221)
UTII-R expression on biopsy was associated with Gleason upgrading and pathology upstaging in prostate cancer patients. (PMID:26381851)
The role of Urotensin-II receptor in vasoconstriction and in the development of digestive tract cancers (PMID:27338741)
UII/GPR14 signaling was involved in the DSS-induced colonic inflammation and its inhibition may serve as a potential therapeutic target, which may be associated with the NF-kappaB signaling pathway. (PMID:27600191)
ligand-induced activation of the chemokine receptor CXCR4 and the urotensin 2 receptor UTS2R, triggers a marked reduction in the biogenesis of autophagosomes. (PMID:27715446)
Urotensin II receptor expression in patients with ulcerative colitis: a pilot study. (PMID:31293119)
Novel Mutations in UTS2R are Associated with Adolescent Idiopathic Scoliosis in the Chinese Population. (PMID:33156271)
Lipidated peptides derived from intracellular loops 2 and 3 of the urotensin II receptor act as biased allosteric ligands. (PMID:34389356)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
drosophila_melanogaster	AstC-R1	FBGN0036790
caenorhabditis_elegans		WBGENE00006864
caenorhabditis_elegans		WBGENE00013782
caenorhabditis_elegans		WBGENE00020086

Paralogs (17): OPRK1 (ENSG00000082556), OPRM1 (ENSG00000112038), KISS1R (ENSG00000116014), OPRD1 (ENSG00000116329), OPRL1 (ENSG00000125510), NPBWR2 (ENSG00000125522), SSTR4 (ENSG00000132671), SSTR1 (ENSG00000139874), SSTR5 (ENSG00000162009), GPR149 (ENSG00000174948), SSTR2 (ENSG00000180616), PTGDR2 (ENSG00000183134), CMKLR2 (ENSG00000183671), LTB4R (ENSG00000213903), LTB4R2 (ENSG00000213906), SSTR3 (ENSG00000278195), NPBWR1 (ENSG00000288611)

Protein

Protein identifiers

Urotensin-2 receptor — Q9UKP6 (reviewed: Q9UKP6)

Alternative names: G-protein coupled receptor 14, Urotensin II receptor

All UniProt accessions (1): Q9UKP6

UniProt curated annotations — full annotation on UniProt →

Function. G protein-coupled receptor for the vasoactive neuropeptides urotensin-2 and urotensin-2B. Upon ligand binding, activates intracellular signaling cascades via G-protein coupling, primarily through Gq/11, leading to phospholipase C activation, increased intracellular calcium, and activation of protein kinase C (PKC). Through coupling to G(i)/G(o) alpha subunits, stimulates MAPK/ERK pathways and thereby contributes to regulation of vascular tone, cardiac contractility, and cell proliferation. Ligand binding also triggers a marked reduction in the biogenesis of autophagosomes by inhibiting the recruitment of ATG16L1 to pre-autophagosomal endocytic vesicles.

Subcellular location. Cell membrane.

Tissue specificity. Most abundant expression in the heart and pancreas.

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

RefSeq proteins (2): NP_001368826, NP_061822* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000670	Urot_II_rcpt	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (29 total): topological domain 8, transmembrane region 7, compositionally biased region 5, region of interest 2, glycosylation site 2, sequence variant 2, chain 1, disulfide bond 1, helix 1

Structure

Experimental structures (PDB)

2 structures.

PDB	Method	Resolution (Å)
9JFK	ELECTRON MICROSCOPY	3.23
6HVK	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9UKP6-F1	77.21	0.42

Antibody-complex structures (SAbDab): 1 — 9JFK

Functional residue map

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

Disulfide bonds (1): 123–199

Glycosylation sites (2): 29, 33

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

ID	Pathway
R-HSA-375276	Peptide ligand-binding receptors
R-HSA-416476	G alpha (q) signalling events

MSigDB gene sets: 55 (showing top): GOBP_REGULATION_OF_BLOOD_PRESSURE, GOBP_CIRCULATORY_SYSTEM_PROCESS, GOBP_REGULATION_OF_ANATOMICAL_STRUCTURE_SIZE, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, GOMF_PEPTIDE_RECEPTOR_ACTIVITY, AFFAR_YY1_TARGETS_DN, HAMAI_APOPTOSIS_VIA_TRAIL_DN, NIKOLSKY_BREAST_CANCER_17Q21_Q25_AMPLICON, GOBP_VASCULAR_PROCESS_IN_CIRCULATORY_SYSTEM, NIKOLSKY_MUTATED_AND_AMPLIFIED_IN_BREAST_CANCER, REACTOME_CLASS_A_1_RHODOPSIN_LIKE_RECEPTORS, REACTOME_G_ALPHA_Q_SIGNALLING_EVENTS, GOMF_TRANSMEMBRANE_SIGNALING_RECEPTOR_ACTIVITY, YOSHIMURA_MAPK8_TARGETS_UP

GO Biological Process (6): signal transduction (GO:0007165), neuropeptide signaling pathway (GO:0007218), blood circulation (GO:0008015), regulation of blood pressure (GO:0008217), blood vessel diameter maintenance (GO:0097746), G protein-coupled receptor signaling pathway (GO:0007186)

GO Molecular Function (2): urotensin II receptor activity (GO:0001604), 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
Class A/1 (Rhodopsin-like receptors)	1
GPCR downstream signalling	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
G protein-coupled receptor signaling pathway	2
blood circulation	2
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
circulatory system process	1
regulation of biological quality	1
vascular process in circulatory system	1
regulation of tube diameter	1
G protein-coupled receptor activity	1
signal transduction	1
G protein-coupled peptide receptor activity	1
transmembrane signaling receptor activity	1
membrane	1
cell periphery	1
cellular anatomical structure	1

Protein interactions and networks

STRING

568 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
UTS2R	UTS2	O95399	999
UTS2R	UTS2B	Q765I0	868
UTS2R	GRIP2	Q9C0E4	557
UTS2R	SST	P01166	550
UTS2R	EDN1	P05305	516
UTS2R	UCN	P55089	502
UTS2R	TEX19	Q8NA77	438
UTS2R	HLA-G	P17693	432
UTS2R	GNA13	Q14344	432
UTS2R	SMTNL2	Q2TAL5	422
UTS2R	RASL10B	Q96S79	421
UTS2R	CRH	P06850	412
UTS2R	SCPEP1	Q9HB40	408
UTS2R	PRLH	P81277	385
UTS2R	OGFOD3	Q6PK18	383

IntAct

6 interactions, top by confidence:

A	B	Type	Score
RAMP1	UTS2R	psi-mi:“MI:0915”(physical association)	0.400
RAMP2	UTS2R	psi-mi:“MI:0915”(physical association)	0.400
RAMP3	UTS2R	psi-mi:“MI:0915”(physical association)	0.400

BioGRID (1): UTS2R (Reconstituted Complex)

ESM2 similar proteins: A0A287A2K5, F1MV99, O08858, O43193, O77808, O97772, P28646, P30098, P30552, P30553, P30796, P30872, P30873, P30937, P30938, P31391, P32239, P32300, P32307, P32745, P33533, P35346, P35370, P35377, P41143, P41146, P46095, P46627, P47748, P48044, P49660, P51651, P56481, P58406, P79266, P79292, Q49LX5, Q5D0K2, Q6W5G4, Q6YNI2

Diamond homologs: A1ZAX0, B2ZI34, E7F7V7, F1MV99, F1R332, O08726, O08786, O43603, O54798, O54799, O62709, O88626, O88854, O97666, O97772, O97967, P05363, P08911, P08912, P21451, P21729, P22270, P24053, P24530, P25101, P26684, P28088, P28336, P28646, P30550, P30551, P30552, P30553, P30796, P30872, P30873, P30937, P30974, P31391, P32238

SIGNOR signaling

9 interactions.

A	Effect	B	Mechanism
UTS2R	“up-regulates activity”	GNAS	binding
UTS2R	“up-regulates activity”	GNAL	binding
UTS2R	“up-regulates activity”	GNAI1	binding
UTS2R	“up-regulates activity”	GNAI3	binding
UTS2R	“up-regulates activity”	GNAO1	binding
UTS2R	“up-regulates activity”	GNAZ	binding
UTS2R	“up-regulates activity”	GNAQ	binding
UTS2R	“up-regulates activity”	GNA14	binding
“Urotensin II”	“up-regulates activity”	UTS2R	“chemical activation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	0
Likely benign	1
Benign	3

Top pathogenic / likely-pathogenic (0)

SpliceAI

51 predictions. Top by Δscore:

Variant	Effect	Δscore
17:82374906:TCCC:T	donor_gain	0.6800
17:82374877:A:AG	donor_gain	0.5100
17:82374979:A:AG	acceptor_gain	0.4700
17:82374980:G:GG	acceptor_gain	0.4700
17:82374893:T:TA	donor_gain	0.4300
17:82375284:G:GT	donor_gain	0.4300
17:82374980:GCATC:G	acceptor_gain	0.4100
17:82374898:C:A	donor_gain	0.3600
17:82375239:C:CA	acceptor_gain	0.3600
17:82374569:C:CA	acceptor_gain	0.3400
17:82374814:GGC:G	donor_gain	0.3300
17:82374899:G:GT	donor_gain	0.3100
17:82374980:GC:G	acceptor_gain	0.3000
17:82375242:C:T	donor_gain	0.3000
17:82375285:A:T	donor_gain	0.2900
17:82375333:G:T	donor_gain	0.2700
17:82375334:G:T	donor_gain	0.2700
17:82374981:C:CT	acceptor_gain	0.2500
17:82374995:G:GT	acceptor_gain	0.2500
17:82374991:C:CG	acceptor_gain	0.2400
17:82375248:C:G	donor_gain	0.2400
17:82374283:G:GT	donor_gain	0.2300
17:82374647:T:TA	acceptor_gain	0.2300
17:82374988:G:GC	acceptor_gain	0.2300
17:82374989:G:GA	acceptor_gain	0.2300
17:82374994:G:GC	acceptor_gain	0.2300
17:82375284:G:T	donor_gain	0.2300
17:82375333:G:GT	donor_gain	0.2300
17:82374471:G:GA	donor_gain	0.2200
17:82374682:G:T	donor_gain	0.2200

AlphaMissense

2424 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
17:82374672:G:C	W116C	0.995
17:82374672:G:T	W116C	0.995
17:82374733:A:C	S137R	0.990
17:82374735:C:A	S137R	0.990
17:82374735:C:G	S137R	0.990
17:82374979:A:C	S219R	0.990
17:82374981:C:A	S219R	0.990
17:82374981:C:G	S219R	0.990
17:82374757:A:C	S145R	0.988
17:82374759:C:A	S145R	0.988
17:82374759:C:G	S145R	0.988
17:82375246:A:C	S308R	0.988
17:82375248:C:A	S308R	0.988
17:82375248:C:G	S308R	0.988
17:82375144:T:C	F274L	0.987
17:82375146:C:A	F274L	0.987
17:82375146:C:G	F274L	0.987
17:82374670:T:A	W116R	0.985
17:82374670:T:C	W116R	0.985
17:82375123:T:C	F267L	0.984
17:82375125:C:A	F267L	0.984
17:82375125:C:G	F267L	0.984
17:82375135:T:C	F271L	0.982
17:82375137:C:A	F271L	0.982
17:82375137:C:G	F271L	0.982
17:82374614:A:C	D97A	0.981
17:82374614:A:T	D97V	0.981
17:82374518:G:A	G65D	0.980
17:82374691:T:A	C123S	0.978
17:82374692:G:C	C123S	0.978

dbSNP variants (sampled 300 via entrez): RS1000568351 (17:82373974 G>A), RS1000793021 (17:82369913 C>T), RS1001118765 (17:82373701 T>C), RS1001181229 (17:82370255 A>G), RS1001717180 (17:82377328 G>A,T), RS1002372071 (17:82374147 G>A), RS1002575816 (17:82371237 C>T), RS1002739274 (17:82374023 AG>A,AGG), RS1002945087 (17:82371956 G>A,T), RS1003040821 (17:82376703 G>C), RS1003129598 (17:82370974 G>A), RS1003340585 (17:82376706 C>T), RS1003408728 (17:82375818 C>A,T), RS1003476091 (17:82376852 C>A,G,T), RS1003787051 (17:82375580 C>G)

Disease associations

OMIM: gene MIM:600896 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL3764 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 40 (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
CHEMBL567303	PALOSURAN	2	40

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Urotensin receptor

Most potent curated ligand interactions (28 total), top 25:

Ligand	Action	Affinity	Parameter
[Pen⁵]U-(4-11) (human)	Full agonist	9.7	pKi
[¹²⁵I]U-II (human)	Full agonist	9.62	pKd
U-II-(4-11) (human)	Full agonist	9.6	pKi
[Bz-Phe6]U-II (human)	Full agonist	9.1	pKi
DS37001789	Antagonist	9.05	pIC50
RCI-0879	Antagonist	9.0	pIC50
[3-iodo-Tyr⁶]U-II-(4-11) (human)	Agonist	8.7	pEC50
urotensin-II	Full agonist	8.6	pKi
urotensin II-related peptide	Full agonist	8.6	pIC50
urotensin-II	Full agonist	8.5	pKi
4-Cl-cinnamoyl-c[DCys-4Pal-DTrp-Orn-Val-Cys]-His-amide	Inverse agonist	8.4	pKd
compound 1a [PMID: 18573659]	Antagonist	8.4	pKi
JNJ-39319202	Antagonist	8.4	pKi
urantide	Antagonist	8.3	pKi
Urolinin	Agonist	8.3	pEC50
SR101099	Antagonist	8.0	pIC50
SB-706375	Antagonist	8.0	pKi
tolyacetyl-c[DCys-Apa-DTrp-Orn-Val-Cys]-His-amide	Antagonist	7.7	pKd
FL104	Full agonist	7.5	pEC50
[Orn⁵]URP	Antagonist	7.17	pKi
palosuran	Antagonist	7.1	pIC50
BIM 23127	Antagonist	6.7	pKd
SB-436811	Antagonist	6.7	pKi
AC-7954	Full agonist	6.6	pKi

Binding affinities (BindingDB)

1 measured of 1 human assays (1 total across all organisms); most potent 1 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
Urotensin II	KI	1.2 nM

ChEMBL bioactivities

846 potent at pChembl≥5 of 847 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.70	Ki	0.1995	nM	CHEMBL390094
9.70	Ki	0.1995	nM	CHEMBL3315139
9.60	Ki	0.2512	nM	CHEMBL426020
9.60	Ki	0.2512	nM	CHEMBL218994
9.55	Ki	0.2818	nM	CHEMBL504097
9.52	Ki	0.3	nM	CHEMBL453587
9.40	Ki	0.3981	nM	CHEMBL3315142
9.40	Ki	0.4	nM	CHEMBL257171
9.40	Ki	0.4	nM	CHEMBL255509
9.35	EC50	0.45	nM	CHEMBL4777970
9.22	Ki	0.6	nM	CHEMBL256989
9.22	EC50	0.6	nM	UROTENSIN-II
9.14	Ki	0.7244	nM	CHEMBL3315141
9.11	Ki	0.7762	nM	CHEMBL3315148
9.10	Ki	0.7943	nM	HUMAN UROTENSIN II
9.10	Ki	0.7943	nM	UROTENSIN-II
9.10	Ki	0.7943	nM	CHEMBL509604
9.08	EC50	0.83	nM	CHEMBL4748168
9.05	IC50	0.9	nM	CHEMBL4777970
9.05	Ki	0.8913	nM	CHEMBL510618
9.04	Ki	0.912	nM	CHEMBL2371933
9.00	Ki	1	nM	CHEMBL257415
8.98	Ki	1.047	nM	CHEMBL3315147
8.96	EC50	1.09	nM	HUMAN UROTENSIN II
8.95	Ki	1.122	nM	CHEMBL385281
8.92	Ki	1.2	nM	CHEMBL255462
8.92	EC50	1.2	nM	CHEMBL218994
8.91	Ki	1.23	nM	CHEMBL3315146
8.91	Ki	1.23	nM	CHEMBL218994
8.90	Ki	1.259	nM	CHEMBL2370836
8.90	Ki	1.259	nM	CHEMBL224616
8.90	Ki	1.259	nM	CHEMBL388060
8.84	EC50	1.46	nM	CHEMBL4741230
8.79	Ki	1.622	nM	CHEMBL374468
8.78	Ki	1.66	nM	CHEMBL448403
8.76	Ki	1.738	nM	CHEMBL3315144
8.76	Ki	1.738	nM	CHEMBL4568153
8.76	Ki	1.738	nM	CHEMBL4472928
8.75	Ki	1.778	nM	CHEMBL3315152
8.74	Ki	1.82	nM	CHEMBL3315150
8.74	EC50	1.8	nM	CHEMBL2372899
8.74	EC50	1.8	nM	CHEMBL385616
8.74	EC50	1.8	nM	CHEMBL53181
8.73	EC50	1.862	nM	CHEMBL218994
8.72	EC50	1.9	nM	CHEMBL2372897
8.70	Ki	1.995	nM	CHEMBL3315140
8.70	Ki	2	nM	CHEMBL402520
8.70	Ki	2	nM	CHEMBL257767
8.70	EC50	1.99	nM	CHEMBL4780734
8.70	IC50	2	nM	CHEMBL4741230

PubChem BioAssay actives

870 with measured affinity, of 1399 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
(2S)-2-[[(4R,7S,10S,13S,16S,19R)-10-(4-aminobutyl)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-20,20-dimethyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	1182034: Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method	ki	0.0002	uM
(2S)-2-[[(4R,7S,10S,13S,16S,19S)-10-(4-aminobutyl)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-20,20-dimethyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	213454: Ability to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cells	ki	0.0002	uM
(2S)-2-[[(4R,7S,10S,13S,16S,19R)-10-(4-aminobutyl)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	1182034: Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method	ki	0.0003	uM
(2S)-2-[[(4R,7S,10S,13S,16S,19S)-10-(4-aminobutyl)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	213454: Ability to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cells	ki	0.0003	uM
3-[4-[1-[[2-[3,4-dichloro-N-(cyanomethyl)anilino]acetyl]-methylamino]-2-pyrrolidin-1-ylethyl]phenyl]benzamide	407192: Binding affinity to human urotensin-2 receptor	ki	0.0003	uM
(2S)-2-[[(4R,7S,10S,13S,16S,19S)-10-(4-aminobutyl)-19-[[(2S)-2-amino-3-phenylpropanoyl]amino]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-20,20-dimethyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	375611: Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting	ki	0.0003	uM
(2S)-2-[[(4R,7S,10S,13S,16S,19R)-10-(4-aminobutyl)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-16-benzyl-13-(1H-indol-3-ylmethyl)-20,20-dimethyl-7-(naphthalen-1-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	1182034: Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method	ki	0.0004	uM
(3S)-3-amino-4-[[(4R,7S,10S,13S,16S,19R)-10-(4-aminobutyl)-4-[[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]carbamoyl]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicos-19-yl]amino]-4-oxobutanoic acid	1714259: Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay	ec50	0.0004	uM
6,7-dimethyl-4-[2-oxo-2-[3-phenyl-2-(pyrrolidin-1-ylmethyl)piperidin-1-yl]ethyl]-1,4-benzoxazin-3-one	331335: Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells	ki	0.0004	uM
6,7-dichloro-4-[2-oxo-2-[3-phenyl-2-(pyrrolidin-1-ylmethyl)piperidin-1-yl]ethyl]-1,4-benzoxazin-3-one	331335: Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells	ki	0.0004	uM
6,7-dichloro-1-[2-oxo-2-[3-phenyl-2-(pyrrolidin-1-ylmethyl)piperidin-1-yl]ethyl]quinoxalin-2-one	331335: Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells	ki	0.0006	uM
(4S)-4-amino-5-[[(2S,3R)-1-[(2S)-2-[[(2S)-1-[[(4R,7S,10S,13S,16S,19R)-10-(4-aminobutyl)-16-benzyl-4-[[(1S)-1-carboxy-2-methylpropyl]carbamoyl]-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicos-19-yl]amino]-3-carboxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxobutan-2-yl]amino]-5-oxopentanoic acid	2111137: Modulation of human UTR stably expressed in HEK293 cells assessed as increase in Ca2+ level by Fura 2-AM dye based calcium mobilization assay	ec50	0.0006	uM
(2S)-2-[[(4R,7S,10S,13R,16S,19R)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-10-(3-aminopropyl)-16-benzyl-13-(1H-indol-3-ylmethyl)-20,20-dimethyl-7-(naphthalen-2-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	1182034: Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method	ki	0.0007	uM
(2S)-2-[[(4R,7S,10S,13S,16S,19R)-10-(4-aminobutyl)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-16-benzyl-7-[(3,4-dichlorophenyl)methyl]-13-(1H-indol-3-ylmethyl)-20,20-dimethyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	1182034: Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method	ki	0.0008	uM
(4R,7S,10S,13S,16S,19R)-19-amino-10-(4-aminobutyl)-N-[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	1714259: Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay	ec50	0.0008	uM
(4S)-4-amino-5-[[(2S,3R)-1-[(2R)-2-[[(2S)-1-[[(4R,7S,10R,13S,16R,19S)-10-(4-aminobutyl)-16-benzyl-4-[[(1S)-1-carboxy-2-methylpropyl]carbamoyl]-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicos-19-yl]amino]-3-carboxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxobutan-2-yl]amino]-5-oxopentanoic acid	213454: Ability to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cells	ki	0.0008	uM
(2S)-2-[[(4R,7S,10S,13S,16S,19S)-10-(4-aminobutyl)-19-[[(2S)-2-aminopropanoyl]amino]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-20,20-dimethyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	375611: Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting	ki	0.0008	uM
(2S)-2-[[(4R,7S,10S,13S,16S,19R)-10-(4-aminobutyl)-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-19-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	272688: Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells	ki	0.0009	uM
(2S)-2-[[(4R,7S,10S,13S,16S,19S)-10-(4-aminobutyl)-19-[[(2S)-2-amino-3-(4-chlorophenyl)propanoyl]amino]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-20,20-dimethyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	375611: Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting	ki	0.0009	uM
(2S)-2-[[(4R,7S,10S,13R,16S,19R)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-10-(3-aminopropyl)-16-benzyl-7-[(4-chlorophenyl)methyl]-13-(1H-indol-3-ylmethyl)-20,20-dimethyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	1182034: Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method	ki	0.0010	uM
6,7-dimethyl-1-[2-oxo-2-[3-phenyl-2-(pyrrolidin-1-ylmethyl)piperidin-1-yl]ethyl]quinoxalin-2-one	331335: Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells	ki	0.0010	uM
(2S)-2-[[(4R,7S,10S,13S,16S,19R)-10-(4-aminobutyl)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-16-(1-benzothiophen-3-ylmethyl)-7-benzyl-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	272688: Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells	ki	0.0011	uM
(2S)-2-[[(4R,7S,10S,13S,16S,19R)-10-(4-aminobutyl)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-16-benzyl-7-[(4-chlorophenyl)methyl]-13-(1H-indol-3-ylmethyl)-20,20-dimethyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	1182034: Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method	ki	0.0012	uM
5-chloro-3-[2-oxo-2-[3-phenyl-2-(pyrrolidin-1-ylmethyl)piperidin-1-yl]ethyl]-1,3-benzothiazol-2-one	331335: Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells	ki	0.0012	uM
(2S)-2-[[(4R,7S,10S,13R,16S,19S)-10-(4-aminobutyl)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-20,20-dimethyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	282902: Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells	ki	0.0013	uM
(2S)-2-[[(4R,7S,10S,13R,16S,19S)-10-(4-aminobutyl)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	282902: Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells	ki	0.0013	uM
(2S)-2-[[(4S,7S,10S,13S,16S,19S)-10-(4-aminobutyl)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-3,3,20,20-tetramethyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	213454: Ability to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cells	ki	0.0013	uM
(4S)-4-amino-5-[[(2S,3R)-1-[(2S)-2-[[(2S)-1-[[(4R,7S,10S,13S,16S,19R)-10-(4-aminobutyl)-4-[[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]carbamoyl]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicos-19-yl]amino]-3-carboxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxobutan-2-yl]amino]-5-oxopentanoic acid	1714259: Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay	ec50	0.0015	uM
(2S)-2-[[(4R,7S,10S,13S,16S,19R)-10-(4-aminobutyl)-16-benzyl-19-[[(2S)-3-carboxy-2-(methylamino)propanoyl]amino]-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	272688: Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells	ki	0.0016	uM
(2S)-2-[[(4R,7S,10S,13S,16S,19R)-10-(4-aminobutyl)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-7-(1,3-benzothiazol-2-ylmethyl)-16-benzyl-13-(1H-indol-3-ylmethyl)-20,20-dimethyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	1182034: Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method	ki	0.0017	uM
(2S)-2-[[(4R,7S,10S,13S,16S,19R)-10-(4-aminobutyl)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-14-methyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	1571995: Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay	ki	0.0017	uM
(2S)-2-[[(4R,7S,10S,13S,16S,19R)-10-(4-aminobutyl)-19-[[(2S)-2-aminopropanoyl]-methylamino]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	1571995: Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay	ki	0.0017	uM
(2S)-2-[[(4R,7S,10S,13R,16S,19S)-19-[[(2S)-2-aminopropanoyl]amino]-10-(3-aminopropyl)-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-20,20-dimethyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	375611: Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting	ki	0.0017	uM
(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-amino-3-sulfanylpropanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-sulfanylpropanoyl]amino]-3-methylbutanoic acid	213450: Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor	ec50	0.0018	uM
(2S)-2-[[(4R,7S,10S,13S,16S,19R)-10-(4-aminobutyl)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-16-benzyl-7-[(4-cyanophenyl)methyl]-13-(1H-indol-3-ylmethyl)-20,20-dimethyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	1182034: Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method	ki	0.0018	uM
(2S)-2-[[(4R,7S,10S,13S,16S,19R)-10-(4-aminobutyl)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-16-benzyl-13-(1H-indol-3-ylmethyl)-20,20-dimethyl-7-[(4-nitrophenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	1182034: Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method	ki	0.0018	uM
(4S)-4-amino-5-[[(2S,3R)-1-[(2R)-2-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(1R)-1-carboxy-2-sulfanylethyl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-sulfanylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxobutan-2-yl]amino]-5-oxopentanoic acid	213450: Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor	ec50	0.0018	uM
(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-[[(2R)-1-[(2S,3R)-2-[[(2S)-2-aminopropanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-3-carboxypropanoyl]amino]-3-sulfanylpropanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-sulfanylpropanoyl]amino]-3-methylbutanoic acid	213450: Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor	ec50	0.0018	uM
(4S)-4-amino-5-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2R)-1-[[(1S)-1-carboxy-2-methylpropyl]amino]-1-oxo-3-sulfanylpropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-sulfanylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-5-oxopentanoic acid	213450: Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor	ec50	0.0019	uM
(2S)-2-[[(4R,7S,10S,13S,16S,19R)-10-(4-aminobutyl)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-16-benzyl-13-(1H-indol-3-ylmethyl)-20,20-dimethyl-7-(naphthalen-2-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	1182034: Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method	ki	0.0020	uM
(2S)-2-amino-N-[(4R,7S,10S,13S,16S,19R)-10-(4-aminobutyl)-4-[[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]carbamoyl]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicos-19-yl]pentanediamide	1714259: Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay	ec50	0.0020	uM
6,7-dichloro-4-[2-[2-(morpholin-4-ylmethyl)-3-phenylpiperidin-1-yl]-2-oxoethyl]-1,4-benzoxazin-3-one	331335: Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells	ki	0.0020	uM
2-(3,4-dichloro-N-[2-oxo-2-[3-phenyl-2-(pyrrolidin-1-ylmethyl)piperidin-1-yl]ethyl]anilino)acetonitrile	331335: Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells	ki	0.0020	uM
(2S)-2-[[(4R,7S,10S,13R,16S,19R)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-10-(3-aminopropyl)-16-benzyl-7-[(3,4-dichlorophenyl)methyl]-13-(1H-indol-3-ylmethyl)-20,20-dimethyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	1182034: Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method	ki	0.0022	uM
(2S)-2-[[(4R,7S,10S,13S,16S,19R)-10-(4-aminobutyl)-19-[(2-amino-2-methylpropanoyl)amino]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	272688: Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells	ki	0.0022	uM
(2S)-2-[[(4R,7S,10S,13S,16S,19R)-10-(4-aminobutyl)-19-[[(2S)-2-aminopropanoyl]amino]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-14-methyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	1571995: Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay	ki	0.0022	uM
(2S)-6-amino-N-[(2S)-1-[[(2R)-1-amino-1-oxo-3-sulfanylpropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-amino-3-sulfanylpropanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]hexanamide	213450: Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor	ec50	0.0023	uM
(2S)-2-[[(4R,7S,10S,13S,16S,19R)-10-(4-aminobutyl)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-16-benzyl-7-[(4-hydroxy-3-nitrophenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	272688: Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells	ki	0.0024	uM
(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-[[(2R)-1-[(2S,3R)-2-amino-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-3-carboxypropanoyl]amino]-3-sulfanylpropanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-sulfanylpropanoyl]amino]-3-methylbutanoic acid	213450: Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor	ec50	0.0024	uM
(2S)-2-[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-19-[[(2S)-2-aminopropanoyl]amino]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-[(4-iodophenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid	1662067: Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method	ic50	0.0025	uM

CTD chemical–gene interactions

16 total (human), top 16 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
quercitrin	increases expression	1
S-(1,2-dichlorovinyl)cysteine	affects cotreatment, decreases expression, affects response to substance, increases expression	1
aseanostatin P5	affects binding, increases activity	1
Resveratrol	affects cotreatment, decreases expression	1
Sunitinib	decreases expression	1
Air Pollutants	increases abundance, increases expression	1
Atrazine	increases expression	1
Dimethyl Sulfoxide	affects expression	1
Lipopolysaccharides	decreases expression, affects response to substance, increases expression, affects cotreatment	1
Plant Extracts	affects cotreatment, decreases expression	1
Triclosan	decreases expression	1
Valproic Acid	increases methylation	1
Aflatoxin B1	decreases expression	1
Sodium Selenite	increases expression	1
Particulate Matter	increases expression, increases abundance	1
Endocannabinoids	increases activity, affects binding, decreases reaction	1

ChEMBL screening assays

121 unique, capped per target: 66 binding, 54 functional, 1 toxicity

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1001564	Functional	Antagonist activity at human recombinant urotensin 2 receptor expressed in CHO cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization	Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists. — J Med Chem
CHEMBL1003707	Binding	Binding affinity to urotensin-2 receptor	Sequence-derived three-dimensional pharmacophore models for G-protein-coupled receptors and their application in virtual screening. — J Med Chem
CHEMBL5381640	Toxicity	Binding affinity to urotensin 2 receptor (unknown origin)	Discovery of a Potent and Orally Bioavailable Zwitterionic Series of Selective Estrogen Receptor Degrader-Antagonists. — J Med Chem

Cellosaurus cell lines

4 cell lines: 2 spontaneously immortalized cell line, 2 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_H506	CHO-K1/UT2/Galpha15	Spontaneously immortalized cell line	Female
CVCL_KZ23	PathHunter CHO-K1 UTR2 beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_LB46	PathHunter U2OS UTR2 Total GPCR Internalization	Cancer cell line	Female
CVCL_YK64	U2OS UTS2R HiTSeeker	Cancer cell line	Female

Clinical trials (associated diseases)

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

No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.