NTSR2

Summary

NTSR2 (neurotensin receptor 2, HGNC:8040) is a protein-coding gene on chromosome 2p25.1, encoding Neurotensin receptor type 2 (O95665). Receptor for the tridecapeptide neurotensin.

The protein encoded by this gene belongs to the G protein-coupled receptor family that activate a phosphatidylinositol-calcium second messenger system. Binding and pharmacological studies demonstrate that this receptor binds neurotensin as well as several other ligands already described for neurotensin NT1 receptor. However, unlike NT1 receptor, this gene recognizes, with high affinity, levocabastine, a histamine H1 receptor antagonist previously shown to compete with neurotensin for low-affinity binding sites in brain. These activities suggest that this receptor may be of physiological importance and that a natural agonist for the receptor may exist.

Source: NCBI Gene 23620 — RefSeq curated summary.

At a glance

• GWAS associations: 2
• Clinical variants (ClinVar): 77 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_012344

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:8040
Approved symbol	NTSR2
Name	neurotensin receptor 2
Location	2p25.1
Locus type	gene with protein product
Status	Approved
Aliases	NTR2
Ensembl gene	ENSG00000169006
Ensembl biotype	protein_coding
OMIM	605538
Entrez	23620

Gene structure

Transcript identifiers

Ensembl transcripts: 2 — 2 protein_coding

ENST00000306928, ENST00000950908

RefSeq mRNA: 1 — MANE Select: NM_012344 NM_012344

CCDS: CCDS1681

Canonical transcript exons

ENST00000306928 — 4 exons

Exon	Start	End
ENSE00001136870	11660043	11660133
ENSE00001136874	11661967	11662240
ENSE00001155557	11658178	11658722
ENSE00001155561	11669506	11670195

Expression profiles

Bgee: expression breadth ubiquitous, 113 present calls, max score 94.59.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 1.4532 / max 115.4714, expressed in 103 samples.

FANTOM5 promoters (6 alternative TSS)

Promoter ID	TPM avg	Samples expressed
26927	0.8452	86
26922	0.3101	78
26925	0.1055	54
26924	0.0913	55
26923	0.0624	38
26926	0.0387	30

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
nucleus accumbens	UBERON:0001882	94.59	gold quality
caudate nucleus	UBERON:0001873	93.67	gold quality
putamen	UBERON:0001874	92.43	gold quality
amygdala	UBERON:0001876	92.19	gold quality
substantia nigra	UBERON:0002038	90.93	gold quality
hypothalamus	UBERON:0001898	90.84	gold quality
midbrain	UBERON:0001891	88.88	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	88.30	gold quality
anterior cingulate cortex	UBERON:0009835	88.20	gold quality
cingulate cortex	UBERON:0003027	88.19	gold quality
right frontal lobe	UBERON:0002810	87.36	gold quality
temporal lobe	UBERON:0001871	86.95	gold quality
lateral globus pallidus	UBERON:0002476	86.54	gold quality
Ammon’s horn	UBERON:0001954	85.02	gold quality
Brodmann (1909) area 9	UBERON:0013540	84.32	gold quality
telencephalon	UBERON:0001893	84.30	gold quality
substantia nigra pars reticulata	UBERON:0001966	83.87	gold quality
prefrontal cortex	UBERON:0000451	82.50	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	82.47	gold quality
middle frontal gyrus	UBERON:0002702	82.22	silver quality
entorhinal cortex	UBERON:0002728	81.98	gold quality
frontal cortex	UBERON:0001870	81.87	gold quality
neocortex	UBERON:0001950	81.66	gold quality
cerebral cortex	UBERON:0000956	81.23	gold quality
CA1 field of hippocampus	UBERON:0003881	81.08	gold quality
Brodmann (1909) area 10	UBERON:0013541	81.08	silver quality
substantia nigra pars compacta	UBERON:0001965	80.87	gold quality
forebrain	UBERON:0001890	80.55	gold quality
medial globus pallidus	UBERON:0002477	80.47	gold quality
globus pallidus	UBERON:0001875	80.29	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-GEOD-84465	yes	11.45
E-ANND-3	no	1.97

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

20 targeting NTSR2, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-6885-3P	99.75	70.36	3187
HSA-MIR-3975	99.62	65.97	697
HSA-MIR-6722-3P	99.45	67.62	1919
HSA-MIR-6853-3P	99.36	70.79	1558
HSA-MIR-3606-5P	99.31	69.67	1168
HSA-MIR-580-5P	99.28	70.94	1776
HSA-MIR-100-3P	99.20	67.33	672
HSA-MIR-196A-3P	99.19	67.34	1204
HSA-MIR-1909-3P	99.03	66.56	1662
HSA-MIR-6737-3P	98.95	68.56	1577
HSA-MIR-7157-3P	98.95	68.70	1582
HSA-MIR-4742-5P	98.89	68.41	1542
HSA-MIR-5006-5P	98.79	66.92	1246
HSA-MIR-6131	97.22	66.72	960
HSA-MIR-3972	97.19	66.46	808
HSA-MIR-1202	97.19	66.43	827
HSA-MIR-597-3P	96.46	68.03	1035
HSA-MIR-4474-5P	94.23	67.95	568
HSA-MIR-604	93.13	64.42	299

Literature-anchored findings (GeneRIF, showing 13)

• Recycling ability depends on a single tyrosine residue (PMID:11801734)
• ghrelin receptor, neurotensin receptor 2 and GPR39 display an unusually high degree of constitutive activity, determined by an aromatic cluster on the inner face of the extracellular ends of TMs VI and VII (PMID:15383539)
• NTR1 and NTR2 mRNA were not detected in either pituitary adenomas or normal tissue. (PMID:18624930)
• this study proposes a novel function of NTR2 in the regulation of NTR1 activity. (PMID:19968961)
• NTR2 and NTR3 were upregulated in prostate cancer cells with luminal phenotype (cytokeratin 18+) (PMID:20048080)
• NTSR2 was overexpressed, NTSR1 decreased, and neurotensin was not expressed in B cell leukemia patient’s B-cells, as compared with healthy B cells. (PMID:23109725)
• high expression of NTSR1 is found in clinical NETs and promoter methylation is an important mechanism controlling the differential expression of NTSR1 and silencing of NTSR2 in NET cells (PMID:26298774)
• We showed that expression levels for NTS and NTSR1 varied, that NTSR2 expression was not detectable and that NTSR3 was consistently expressed in all CRC cell lines examined. (PMID:28498396)
• High NTSR2 expression is associated with B-cell chronic lymphocytic leukemia. (PMID:29059151)
• A novel role of NTS in the development of Castration-resistant prostate cancer with Neuroendocrine differentiation (NED), and a possible strategy to prevent the onset of NED by targeting the NTS signaling pathway. (PMID:30770901)
• Characterisation of the Expression of Neurotensin and Its Receptors in Human Colorectal Cancer and Its Clinical Implications. (PMID:32764278)
• Physiological and Pathological Roles of NTSR2 in Several Organs and Diseases (Review). (PMID:37962046)
• Targeting the NTSR2/TrkB oncogenic pathway in chronic lymphocytic leukemia. (PMID:38480783)

Cross-species orthologs

2 orthologs

Organism	Symbol	Gene ID
mus_musculus	Ntsr2	ENSMUSG00000020591
rattus_norvegicus	Ntsr2	ENSRNOG00000049054

Paralogs (15): NTSR1 (ENSG00000101188), BRS3 (ENSG00000102239), MLNR (ENSG00000102539), GHSR (ENSG00000121853), GRPR (ENSG00000126010), NMUR2 (ENSG00000132911), NMBR (ENSG00000135577), EDNRB (ENSG00000136160), EDNRA (ENSG00000151617), GPR37L1 (ENSG00000170075), GPR37 (ENSG00000170775), NMUR1 (ENSG00000171596), GPR148 (ENSG00000173302), TRHR (ENSG00000174417), GPR39 (ENSG00000183840)

Protein

Protein identifiers

Neurotensin receptor type 2 — O95665 (reviewed: O95665)

Alternative names: Levocabastine-sensitive neurotensin receptor

All UniProt accessions (1): O95665

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for the tridecapeptide neurotensin. It is associated with G proteins that activate a phosphatidylinositol-calcium second messenger system.

Subcellular location. Cell membrane.

Tissue specificity. Expressed in prostate (at protein level).

Similarity. Belongs to the G-protein coupled receptor 1 family. Neurotensin receptor subfamily. NTSR2 sub-subfamily.

RefSeq proteins (1): NP_036476* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR003984	NT_rcpt	Family
IPR003986	NT2_rcpt	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (25 total): topological domain 8, transmembrane region 7, sequence conflict 4, sequence variant 2, chain 1, region of interest 1, lipid moiety-binding region 1, disulfide bond 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-O95665-F1	79.25	0.47

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 (1): 377

Disulfide bonds (1): 108–194

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: 76 (showing top): MORF_RAGE, chr2p25, MODY_HIPPOCAMPUS_POSTNATAL, MODULE_45, MODULE_64, MODULE_16, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, LASTOWSKA_COAMPLIFIED_WITH_MYCN, GOMF_PEPTIDE_RECEPTOR_ACTIVITY, MORF_PML, GOBP_SENSORY_PERCEPTION, GOBP_PHOSPHOLIPASE_C_ACTIVATING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, MODULE_18, MODULE_38

GO Biological Process (7): cell surface receptor signaling pathway (GO:0007166), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), neuropeptide signaling pathway (GO:0007218), sensory perception (GO:0007600), regulation of membrane potential (GO:0042391), signal transduction (GO:0007165), G protein-coupled receptor signaling pathway (GO:0007186)

GO Molecular Function (2): G protein-coupled receptor activity (GO:0004930), G protein-coupled neurotensin receptor activity (GO:0016492)

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	3
signal transduction	2
phospholipase C activator activity	1
nervous system process	1
monoatomic ion transmembrane transport	1
regulation of biological quality	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
G protein-coupled receptor activity	1
transmembrane signaling receptor activity	1
neuropeptide receptor activity	1
membrane	1
cell periphery	1
cellular anatomical structure	1

Protein interactions and networks

STRING

1490 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
NTSR2	DHX15	O43143	995
NTSR2	NTS	P30990	994
NTSR2	TFIP11	Q9UBB9	958
NTSR2	COPA	P53621	681
NTSR2	NTRK2	Q16620	676
NTSR2	SORT1	Q99523	668
NTSR2	TUFT1	Q9NNX1	645
NTSR2	NMU	P48645	602
NTSR2	SRSF2	Q01130	549
NTSR2	DHX38	Q92620	522
NTSR2	SLU7	O95391	507
NTSR2	CWC25	Q9NXE8	507
NTSR2	SNRNP200	O75643	506
NTSR2	NTSR1	P30989	500
NTSR2	TAC1	P20366	485

IntAct

0 interactions, top by confidence:

BioGRID (1): NTSR2 (Negative Genetic)

ESM2 similar proteins: A0A6I8PUB9, B2GV46, E9QJ73, F8VQN3, O00155, O00270, O00590, O08707, O08726, O09027, O14842, O14843, O15529, O75388, O88634, O88854, O95665, P0C5I1, P32302, P34997, P46094, P70612, Q04683, Q09QM4, Q13304, Q149R9, Q3UFD7, Q3UJF0, Q3ZC80, Q6NS65, Q6XKD3, Q76JU8, Q76JU9, Q76JV1, Q7TQP4, Q86VZ1, Q8BW93, Q8BYC4, Q8C131, Q8K3T4

Diamond homologs: A0A287A2K5, A5A4K9, A5A4L1, E7EM37, G3M4F8, O00590, O02662, O02666, O02824, O08725, O08786, O15973, O42179, O43193, O54814, O55040, O77408, O77590, O88319, O95665, O97665, O97772, P18090, P20789, P20905, P23944, P25100, P25104, P25962, P26255, P29089, P29755, P30551, P30553, P30555, P30989, P32238, P32239, P32246, P32250

SIGNOR signaling

1 interactions.

A	Effect	B	Mechanism
NTS	down-regulates	NTSR2	binding

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	64
Likely benign	7
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

865 predictions. Top by Δscore:

Variant	Effect	Δscore
2:11660041:A:AC	donor_gain	1.0000
2:11660042:C:CC	donor_gain	1.0000
2:11660042:CT:C	donor_gain	1.0000
2:11661965:A:C	donor_gain	1.0000
2:11660035:ACAC:A	donor_loss	0.9900
2:11660036:CACT:C	donor_loss	0.9900
2:11660037:AC:A	donor_loss	0.9900
2:11660038:CT:C	donor_loss	0.9900
2:11660039:TCACT:T	donor_loss	0.9900
2:11660040:CACTC:C	donor_loss	0.9900
2:11660041:A:T	donor_loss	0.9900
2:11660042:C:G	donor_loss	0.9900
2:11660045:AGT:A	donor_gain	0.9900
2:11660069:G:C	donor_gain	0.9900
2:11660144:T:C	acceptor_gain	0.9900
2:11660144:T:TC	acceptor_gain	0.9900
2:11660165:C:CT	acceptor_gain	0.9900
2:11660166:A:T	acceptor_gain	0.9900
2:11661927:AGGCC:A	donor_gain	0.9900
2:11661964:A:AC	donor_gain	0.9900
2:11663333:C:A	donor_gain	0.9900
2:11669501:CTTAC:C	donor_loss	0.9900
2:11669502:TTACC:T	donor_loss	0.9900
2:11669503:TA:T	donor_loss	0.9900
2:11669504:A:C	donor_loss	0.9900
2:11669505:CCTG:C	donor_loss	0.9900
2:11658719:TGGG:T	acceptor_gain	0.9800
2:11658723:C:CC	acceptor_gain	0.9800
2:11660010:C:A	donor_gain	0.9800
2:11660132:TCC:T	acceptor_loss	0.9800

AlphaMissense

2607 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
2:11662220:G:C	F215L	0.968
2:11662220:G:T	F215L	0.968
2:11662222:A:G	F215L	0.968
2:11658662:G:C	S350R	0.963
2:11658662:G:T	S350R	0.963
2:11658664:T:G	S350R	0.963
2:11669908:G:C	S74R	0.959
2:11669908:G:T	S74R	0.959
2:11669910:T:G	S74R	0.959
2:11658617:G:C	F365L	0.954
2:11658617:G:T	F365L	0.954
2:11658619:A:G	F365L	0.954
2:11660097:G:T	P312Q	0.932
2:11669740:G:C	S130R	0.929
2:11669740:G:T	S130R	0.929
2:11669742:T:G	S130R	0.929
2:11660097:G:C	P312R	0.928
2:11660048:C:A	W328C	0.925
2:11660048:C:G	W328C	0.925
2:11658684:G:A	T343I	0.919
2:11669807:C:G	C108S	0.918
2:11669808:A:T	C108S	0.918
2:11669827:C:A	W101C	0.915
2:11669827:C:G	W101C	0.915
2:11669755:G:C	S125R	0.913
2:11669755:G:T	S125R	0.913
2:11669757:T:G	S125R	0.913
2:11660107:A:G	C309R	0.912
2:11669652:A:G	W160R	0.909
2:11669652:A:T	W160R	0.909

dbSNP variants (sampled 300 via entrez): RS1000167119 (2:11667774 A>G), RS1000498784 (2:11669048 A>C), RS1000783701 (2:11658341 G>C), RS1000794305 (2:11661185 G>A), RS1000825604 (2:11660965 G>C), RS1001055109 (2:11666272 G>A,T), RS1001156345 (2:11671577 A>G), RS1001286670 (2:11661399 C>T), RS1001370742 (2:11660542 G>A), RS1001444406 (2:11660300 C>T), RS1001778841 (2:11661697 CACTGAAA>C), RS1002221564 (2:11665972 T>A,C), RS1002307011 (2:11670817 C>T), RS1002363637 (2:11672169 A>G,T), RS1002375707 (2:11666482 C>A,T)

Disease associations

OMIM: gene MIM:605538 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

2 associations (top):

Study	Trait	p-value
GCST002875_39	Diisocyanate-induced asthma	1.000000e-06
GCST009391_1570	Metabolite levels	6.000000e-06

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0006995	response to diisocyanate
EFO:0010516	orotic acid measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL2111438 (PROTEIN FAMILY), CHEMBL2514 (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: 235 (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
CHEMBL506981	REMINERTANT	3	235

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Neurotensin receptors

Most potent curated ligand interactions (14 total), top 14:

Ligand	Action	Affinity	Parameter
Trp11-neurotensin	Full agonist	9.0	pIC50
neuromedin N	Full agonist	8.8	pIC50
neurotensin	Full agonist	8.8	pKi
xenin	Full agonist	8.8	pIC50
JMV458	Full agonist	8.7	pKi
[125I]neurotensin (human, mouse, rat)	Full agonist	8.6	pKd
[D-Trp11]neurotensin	Full agonist	7.6	pIC50
JMV2004	Full agonist	7.2	pKi
JMV431	Full agonist	7.0	pKd
levocabastine	Full agonist	6.8	pKi
JMV457	Full agonist	6.8	pKi
Thr10contulakin-G	Full agonist	6.8	pIC50
meclinertant	Full agonist	6.4	pKi
contulakin-G	Full agonist	6.1	pIC50

ChEMBL bioactivities

174 potent at pChembl≥5 of 180 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.52	Ki	0.03	nM	CHEMBL4798887
10.05	Ki	0.09	nM	CHEMBL4789659
9.96	Ki	0.11	nM	CHEMBL4742999
9.80	Ki	0.16	nM	CHEMBL4758754
9.64	IC50	0.23	nM	CHEMBL337721
9.59	IC50	0.26	nM	CHEMBL3622802
9.54	Ki	0.29	nM	CHEMBL4744531
9.52	IC50	0.3	nM	CHEMBL336836
9.49	Ki	0.32	nM	CHEMBL4749016
9.48	Ki	0.33	nM	CHEMBL4745899
9.34	Ki	0.46	nM	CHEMBL4597094
9.33	IC50	0.47	nM	CHEMBL258221
9.30	Ki	0.5	nM	CHEMBL4747286
9.26	Ki	0.55	nM	CHEMBL415788
9.21	Ki	0.61	nM	CHEMBL1766935
9.17	IC50	0.67	nM	CHEMBL434227
9.15	IC50	0.7	nM	CHEMBL337644
9.13	Ki	0.74	nM	CHEMBL3786852
9.13	Ki	0.7413	nM	CHEMBL415788
9.13	Ki	0.74	nM	CHEMBL254769
9.11	IC50	0.78	nM	CHEMBL132524
9.05	IC50	0.9	nM	CHEMBL132409
9.02	IC50	0.95	nM	CHEMBL258221
9.02	Ki	0.955	nM	CHEMBL4534768
8.96	IC50	1.1	nM	NEUROTENSIN
8.92	Ki	1.2	nM	CHEMBL415788
8.92	Ki	1.202	nM	CHEMBL4564746
8.92	Kd	1.2	nM	CHEMBL1766928
8.85	Kd	1.4	nM	CHEMBL342252
8.85	Ki	1.4	nM	CHEMBL415788
8.76	Ki	1.72	nM	CHEMBL4742666
8.74	Kd	1.8	nM	CHEMBL415788
8.74	IC50	1.8	nM	CHEMBL337260
8.68	IC50	2.1	nM	CHEMBL430910
8.60	Ki	2.5	nM	CHEMBL3786291
8.57	Ki	2.7	nM	CHEMBL4786574
8.57	IC50	2.7	nM	CHEMBL342252
8.55	IC50	2.8	nM	CHEMBL132507
8.54	Ki	2.86	nM	CHEMBL4740539
8.54	Ki	2.9	nM	CHEMBL6160963
8.52	Ki	3	nM	CHEMBL4762684
8.52	IC50	3	nM	CHEMBL339139
8.51	IC50	3.1	nM	CHEMBL132794
8.49	IC50	3.2	nM	CHEMBL133798
8.46	Ki	3.467	nM	CHEMBL4537266
8.46	IC50	3.5	nM	CHEMBL133850
8.46	IC50	3.5	nM	CHEMBL133340
8.40	Ki	3.981	nM	CHEMBL4457798
8.40	IC50	4	nM	CHEMBL439494
8.39	Ki	4.1	nM	NEUROTENSIN

PubChem BioAssay actives

170 with measured affinity, of 310 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-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(3S)-3-[3-[(4S)-4-[[(2R)-2-[[(2S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-oxo-4,5-dihydro-1H-2-benzazepin-2-yl]propanoylamino]-6-(diaminomethylideneamino)hexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acid	1697037: Displacement of [125I]-neurotensin from human recombinant NTS2 stably expressed in human 1321N1 cell membranes incubated for 60 mins by gamma counter method	ki	<0.0001	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[3-[(4S)-4-[[(2R)-2-[[(2S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-oxo-4,5-dihydro-1H-2-benzazepin-2-yl]propanoylamino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acid	1697037: Displacement of [125I]-neurotensin from human recombinant NTS2 stably expressed in human 1321N1 cell membranes incubated for 60 mins by gamma counter method	ki	<0.0001	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(3S)-3-amino-6-(diaminomethylideneamino)hexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acid	1697037: Displacement of [125I]-neurotensin from human recombinant NTS2 stably expressed in human 1321N1 cell membranes incubated for 60 mins by gamma counter method	ki	0.0001	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[3-[(4S)-4-[[(2R)-2-[[(2S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-oxo-4,5-dihydro-1H-2-benzazepin-2-yl]propanoylamino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acid	1697037: Displacement of [125I]-neurotensin from human recombinant NTS2 stably expressed in human 1321N1 cell membranes incubated for 60 mins by gamma counter method	ki	0.0001	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-6-amino-2-[3-[(4S)-4-[[(2R)-2-[[(2S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-oxo-4,5-dihydro-1H-2-benzazepin-2-yl]propanoylamino]hexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acid	1697037: Displacement of [125I]-neurotensin from human recombinant NTS2 stably expressed in human 1321N1 cell membranes incubated for 60 mins by gamma counter method	ki	0.0002	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-amino-5-[[amino-[[(2S)-2-amino-5-(2-amino-4,5-dihydroimidazol-1-yl)pentanoyl]amino]methylidene]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	147066: Evaluated for binding affinity by inhibiting binding of [125I]Tyr(3)-NT to human Neurotensin receptor 2	ic50	0.0002	uM
(2R)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-2,6-diaminohexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-3-trimethylsilylpropanoic acid	1251024: Displacement of [125I]-Tyr3-NT from human NTS2 receptor expressed in 1321N1 cell membranes incubated for 30 mins by gamma-counting based competitive radioligand binding assay	ic50	0.0003	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-6-amino-2-[3-[(4S)-4-[[(2R)-2-[[(2S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-oxo-4,5-dihydro-1H-2-benzazepin-2-yl]propanoylamino]hexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acid	1697037: Displacement of [125I]-neurotensin from human recombinant NTS2 stably expressed in human 1321N1 cell membranes incubated for 60 mins by gamma counter method	ki	0.0003	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[3-[(4S)-4-[[(2R)-2-[[(2S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-oxo-4,5-dihydro-1H-2-benzazepin-2-yl]propanoylamino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(3-hydroxyphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acid	1697037: Displacement of [125I]-neurotensin from human recombinant NTS2 stably expressed in human 1321N1 cell membranes incubated for 60 mins by gamma counter method	ki	0.0003	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(3S)-7-amino-3-[3-[(4S)-4-[[(2R)-2-[[(2S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-oxo-4,5-dihydro-1H-2-benzazepin-2-yl]propanoylamino]heptanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acid	1697037: Displacement of [125I]-neurotensin from human recombinant NTS2 stably expressed in human 1321N1 cell membranes incubated for 60 mins by gamma counter method	ki	0.0003	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-amino-5-[[amino-[[(2S)-2-amino-5-[[amino(ethylamino)methylidene]amino]pentanoyl]amino]methylidene]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	147066: Evaluated for binding affinity by inhibiting binding of [125I]Tyr(3)-NT to human Neurotensin receptor 2	ic50	0.0003	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acid	1697037: Displacement of [125I]-neurotensin from human recombinant NTS2 stably expressed in human 1321N1 cell membranes incubated for 60 mins by gamma counter method	ki	0.0005	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-6-amino-2-[3-[(4S)-4-[[(2R)-2-[[(2S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-oxo-4,5-dihydro-1H-2-benzazepin-2-yl]propanoylamino]hexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(3-hydroxyphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acid	1697037: Displacement of [125I]-neurotensin from human recombinant NTS2 stably expressed in human 1321N1 cell membranes incubated for 60 mins by gamma counter method	ki	0.0005	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-2,6-diaminohexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	1926231: Inhibition of human NTR2	ic50	0.0005	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	1697037: Displacement of [125I]-neurotensin from human recombinant NTS2 stably expressed in human 1321N1 cell membranes incubated for 60 mins by gamma counter method	ki	0.0006	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(3S)-3-amino-6-(diaminomethylideneamino)hexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	593496: Displacement of [3H]NT from human NTS2 receptor expressed in HEK293 cells	ki	0.0006	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-amino-5-[[amino-(4-aminobutylcarbamoylamino)methylidene]amino]pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid;tetrakis(2,2,2-trifluoroacetic acid)	1289949: Displacement of [3H]NT(8 to 13 residues) from human NTSR2 expressed in HEK293 cell membranes	ki	0.0007	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-amino-5-[[amino-[[(2S)-2,7-diaminoheptanoyl]amino]methylidene]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	147066: Evaluated for binding affinity by inhibiting binding of [125I]Tyr(3)-NT to human Neurotensin receptor 2	ic50	0.0007	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-amino-5-[[amino-[[(2S)-2-amino-5-[(N’-methylcarbamimidoyl)amino]pentanoyl]amino]methylidene]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	147066: Evaluated for binding affinity by inhibiting binding of [125I]Tyr(3)-NT to human Neurotensin receptor 2	ic50	0.0007	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[2-(4-aminobutylamino)acetyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	593496: Displacement of [3H]NT from human NTS2 receptor expressed in HEK293 cells	ki	0.0007	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-amino-5-[[amino-[[(2S)-2-amino-5-(imidazolidin-2-ylamino)pentanoyl]amino]methylidene]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	147066: Evaluated for binding affinity by inhibiting binding of [125I]Tyr(3)-NT to human Neurotensin receptor 2	ic50	0.0008	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-amino-5-[[amino-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]methylidene]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	147066: Evaluated for binding affinity by inhibiting binding of [125I]Tyr(3)-NT to human Neurotensin receptor 2	ic50	0.0009	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-amino-5-[[amino-[2-[2-[2-[6-[(2E)-3,3-dimethyl-2-[(2E,4E)-5-(1,3,3-trimethylindol-1-ium-2-yl)penta-2,4-dienylidene]indol-1-yl]hexanoylamino]ethoxy]ethoxy]ethylcarbamoylamino]methylidene]amino]pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid;2,2,2-trifluoroacetate;tris(2,2,2-trifluoroacetic acid)	1541740: Displacement of [3H] UR-MK300 from human neurotensin receptor 2 in HEK293 cells homogenate incubated in dark after 30 mins by liquid scintillation counter analysis	ki	0.0010	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-4-amino-2-[[(2S)-4-carboxy-2-[[(2S)-3-(4-hydroxyphenyl)-2-[[(2S)-4-methyl-2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]pentanoyl]amino]propanoyl]amino]butanoyl]amino]-4-oxobutanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	1926231: Inhibition of human NTR2	ic50	0.0011	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-amino-5-[[amino-[4-[6-[(2E)-3,3-dimethyl-2-[(2E,4E)-5-(1,3,3-trimethylindol-1-ium-2-yl)penta-2,4-dienylidene]indol-1-yl]hexanoylamino]butylcarbamoylamino]methylidene]amino]pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid;2,2,2-trifluoroacetate;bis(2,2,2-trifluoroacetic acid)	1541740: Displacement of [3H] UR-MK300 from human neurotensin receptor 2 in HEK293 cells homogenate incubated in dark after 30 mins by liquid scintillation counter analysis	ki	0.0012	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxycyclohexa-1,3-dien-1-yl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	593496: Displacement of [3H]NT from human NTS2 receptor expressed in HEK293 cells	kd	0.0012	uM
(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	1055239: Displacement of [3H]NT(8 to 13) from human NTS2 receptor expressed in HEK293 cells	kd	0.0014	uM
(2S)-2-[[(2S)-2-[[(3S)-2-[(2S)-1-[(2S)-2-[[(2S)-2-[3-[(4S)-4-[[(2R)-2-[[(2S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-oxo-4,5-dihydro-1H-2-benzazepin-2-yl]propanoylamino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]-6-hydroxy-3,4-dihydro-1H-isoquinoline-3-carbonyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acid	1697037: Displacement of [125I]-neurotensin from human recombinant NTS2 stably expressed in human 1321N1 cell membranes incubated for 60 mins by gamma counter method	ki	0.0017	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-amino-5-[[amino-[[(2S)-2-amino-6-(methylamino)hexanoyl]amino]methylidene]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	147066: Evaluated for binding affinity by inhibiting binding of [125I]Tyr(3)-NT to human Neurotensin receptor 2	ic50	0.0018	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-amino-5-[[amino-[[(2S)-2,6-diaminohexanoyl]amino]methylidene]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	147066: Evaluated for binding affinity by inhibiting binding of [125I]Tyr(3)-NT to human Neurotensin receptor 2	ic50	0.0021	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-amino-5-[[amino-[4-(propanoylamino)butylcarbamoylamino]methylidene]amino]pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid;tris(2,2,2-trifluoroacetic acid)	1289949: Displacement of [3H]NT(8 to 13 residues) from human NTSR2 expressed in HEK293 cell membranes	ki	0.0025	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-3-(4-hydroxyphenyl)-2-[[(2S)-4-methyl-2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]pentanoyl]amino]propanoyl]amino]propanoyl]amino]-4-oxobutanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	1731235: Displacement of [125I]Tyr3-neurotensin from human recombinant NTS2 stably expressed in human 1321N1 cell membranes incubated for 60 mins by gamma counter analysis	ki	0.0027	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-amino-5-[[amino-[[(2S)-2-amino-6-(dimethylamino)hexanoyl]amino]methylidene]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	147066: Evaluated for binding affinity by inhibiting binding of [125I]Tyr(3)-NT to human Neurotensin receptor 2	ic50	0.0028	uM
(2S)-2-[[(2S)-2-[[(3S)-2-[(2S)-1-[(2S)-6-amino-2-[[(3S)-3,7-diaminoheptanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]-6-hydroxy-3,4-dihydro-1H-isoquinoline-3-carbonyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acid	1697037: Displacement of [125I]-neurotensin from human recombinant NTS2 stably expressed in human 1321N1 cell membranes incubated for 60 mins by gamma counter method	ki	0.0029	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]-3,3-dimethylbutanoyl]amino]-4-methylpentanoic acid	1697037: Displacement of [125I]-neurotensin from human recombinant NTS2 stably expressed in human 1321N1 cell membranes incubated for 60 mins by gamma counter method	ki	0.0030	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-amino-5-[[amino-[[(2S)-2,5-diaminopentanoyl]amino]methylidene]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	147066: Evaluated for binding affinity by inhibiting binding of [125I]Tyr(3)-NT to human Neurotensin receptor 2	ic50	0.0030	uM
[(6S)-6-amino-7-[[N’-[(4S)-4-amino-5-[(2S)-2-[[(2S)-1-[[(2S,3S)-1-[[(1S)-1-carboxy-3-methylbutyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-oxopentyl]carbamimidoyl]amino]-7-oxoheptyl]-trimethylazanium	147066: Evaluated for binding affinity by inhibiting binding of [125I]Tyr(3)-NT to human Neurotensin receptor 2	ic50	0.0031	uM
[(5S)-5-amino-6-[[N’-[(4S)-4-amino-5-[(2S)-2-[[(2S)-1-[[(2S,3S)-1-[[(1S)-1-carboxy-3-methylbutyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-oxopentyl]carbamimidoyl]amino]-6-oxohexyl]-trimethylazanium	147066: Evaluated for binding affinity by inhibiting binding of [125I]Tyr(3)-NT to human Neurotensin receptor 2	ic50	0.0032	uM
4-[2-[(1E,3E,5E)-5-[1-[6-[2-[2-[2-[[N’-[(4S)-4-amino-5-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S,3S)-1-[[(1S)-1-carboxy-3-methylbutyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-oxopentyl]carbamimidoyl]carbamoylamino]ethoxy]ethoxy]ethylamino]-6-oxohexyl]-3,3-dimethyl-5-sulfoindol-2-ylidene]penta-1,3-dienyl]-3,3-dimethylindol-1-ium-1-yl]butane-1-sulfonate;bis(2,2,2-trifluoroacetic acid)	1541740: Displacement of [3H] UR-MK300 from human neurotensin receptor 2 in HEK293 cells homogenate incubated in dark after 30 mins by liquid scintillation counter analysis	ki	0.0035	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-amino-5-[[amino-[[(2S)-2-amino-7-(dimethylamino)heptanoyl]amino]methylidene]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	147066: Evaluated for binding affinity by inhibiting binding of [125I]Tyr(3)-NT to human Neurotensin receptor 2	ic50	0.0035	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-amino-5-[[amino-[[(2S)-2-amino-5-(methylamino)pentanoyl]amino]methylidene]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	147066: Evaluated for binding affinity by inhibiting binding of [125I]Tyr(3)-NT to human Neurotensin receptor 2	ic50	0.0035	uM
4-[2-[(1E,3E,5E)-5-[1-[6-[4-[[N’-[(4S)-4-amino-5-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S,3S)-1-[[(1S)-1-carboxy-3-methylbutyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-oxopentyl]carbamimidoyl]carbamoylamino]butylamino]-6-oxohexyl]-3,3-dimethyl-5-sulfoindol-2-ylidene]penta-1,3-dienyl]-3,3-dimethylindol-1-ium-1-yl]butane-1-sulfonate;bis(2,2,2-trifluoroacetic acid)	1541740: Displacement of [3H] UR-MK300 from human neurotensin receptor 2 in HEK293 cells homogenate incubated in dark after 30 mins by liquid scintillation counter analysis	ki	0.0040	uM
(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-4-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-carboxybutanoyl]amino]-4-methylpentanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]-4-oxobutanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoic acid	147066: Evaluated for binding affinity by inhibiting binding of [125I]Tyr(3)-NT to human Neurotensin receptor 2	ic50	0.0040	uM
(2R)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoyl]amino]-3-(2-aminoethyldisulfanyl)propanoic acid	1890925: Displacement of [3H]NT(8-13) from human NTSR2 expressed in HEK293 cell membranes by radioligand displacement assay	ki	0.0042	uM
(2S)-2-[[(2S,3S)-2-[[2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-2,6-diaminohexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]-[2-(4-hydroxyphenyl)ethyl]amino]acetyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	593496: Displacement of [3H]NT from human NTS2 receptor expressed in HEK293 cells	ki	0.0043	uM
(2S)-2-[[(2S,3S)-2-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2,6-diaminohexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]-[2-(4-hydroxyphenyl)ethyl]amino]acetyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	593496: Displacement of [3H]NT from human NTS2 receptor expressed in HEK293 cells	ki	0.0044	uM
(2S)-2-[[(2S,3S)-2-[[(3S,6S,12S,15S,21E)-15-amino-12-(4-aminobutyl)-25-hydroxy-5,11,14-trioxo-4,10,13,19-tetrazatricyclo[22.3.1.06,10]octacosa-1(28),21,24,26-tetraene-3-carbonyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	1731270: Binding affinity to NTS2 (unknown origin)	ki	0.0045	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-4-amino-2-[[(2S)-4-carboxy-2-[[(2S)-3-(4-hydroxyphenyl)-2-[[(2S)-4-methyl-2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]pentanoyl]amino]propanoyl]amino]butanoyl]amino]-4-oxobutanoyl]amino]hexanoyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	1731235: Displacement of [125I]Tyr3-neurotensin from human recombinant NTS2 stably expressed in human 1321N1 cell membranes incubated for 60 mins by gamma counter analysis	ki	0.0046	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(5R)-1-[(2S)-6-amino-2-[[(2S)-2,6-diaminohexanoyl]amino]hexanoyl]-3,3-dimethyl-1,3-azasilolidine-5-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	1926231: Inhibition of human NTR2	ic50	0.0050	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-amino-5-[[amino-[[(2S)-2-amino-5-(dimethylamino)pentanoyl]amino]methylidene]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid	147066: Evaluated for binding affinity by inhibiting binding of [125I]Tyr(3)-NT to human Neurotensin receptor 2	ic50	0.0051	uM

CTD chemical–gene interactions

8 total (human), top 8 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	increases methylation, affects cotreatment, decreases expression	2
neurotensin 69L	affects binding	1
neurotensin NT79	affects binding	1
Resveratrol	affects cotreatment, decreases expression	1
Benzo(a)pyrene	increases methylation	1
Hydralazine	affects cotreatment, decreases expression	1
Neurotensin	affects binding	1
Plant Extracts	decreases expression, affects cotreatment	1

ChEMBL screening assays

36 unique, capped per target: 33 binding, 3 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4880283	Binding	Neurotensin receptor (h) CEREP ligand profiling	Data for DCP probe ABT-546
CHEMBL857327	Functional	Effect on second messenger (PI or cGMP) turnover at human neurotensin receptor; ND=Not determined	Synthesis of partially non-peptidic neurotensin mimetics — Bioorg Med Chem Lett

Clinical trials (associated diseases)

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