NPY4R

Summary

NPY4R (neuropeptide Y receptor Y4, HGNC:9329) is a protein-coding gene on chromosome 10q11.22, encoding Neuropeptide Y receptor type 4 (P50391). G protein-coupled receptor for PPY/pancreatic polypeptide/PP, NPY/neuropeptide Y and PYY/peptide YY that is negatively coupled to cAMP. It is a selective cancer dependency (DepMap: 40.0% of cell lines).

Enables pancreatic polypeptide receptor activity and peptide hormone binding activity. Involved in G protein-coupled receptor signaling pathway. Located in membrane.

Source: NCBI Gene 5540 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 46 total
• Druggable target: yes — 2 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 40.0% of screened cell lines
• MANE Select transcript: NM_005972

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:9329
Approved symbol	NPY4R
Name	neuropeptide Y receptor Y4
Location	10q11.22
Locus type	gene with protein product
Status	Approved
Aliases	Y4, PP1
Ensembl gene	ENSG00000204174
Ensembl biotype	protein_coding
OMIM	601790
Entrez	5540

Gene structure

Transcript identifiers

Ensembl transcripts: 4 — 4 protein_coding

ENST00000374312, ENST00000612632, ENST00000908575, ENST00000908576

RefSeq mRNA: 2 — MANE Select: NM_005972 NM_001278794, NM_005972

CCDS: CCDS73100

Canonical transcript exons

ENST00000374312 — 3 exons

Exon	Start	End
ENSE00001463114	46463730	46463885
ENSE00003793638	46461099	46462694
ENSE00003889990	46465678	46465958

Expression profiles

Bgee: expression breadth broad, 54 present calls, max score 75.24.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.0063 / max 1.6566, expressed in 1 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
109274	0.0063	1

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
rectum	UBERON:0001052	75.24	gold quality
transverse colon	UBERON:0001157	68.06	gold quality
colon	UBERON:0001155	65.65	gold quality
muscle layer of sigmoid colon	UBERON:0035805	64.38	gold quality
intestine	UBERON:0000160	63.29	gold quality
duodenum	UBERON:0002114	62.82	gold quality
mucosa of transverse colon	UBERON:0004991	61.98	gold quality
smooth muscle tissue	UBERON:0001135	58.63	gold quality
small intestine	UBERON:0002108	57.84	gold quality
small intestine Peyer’s patch	UBERON:0003454	57.24	gold quality
skin of abdomen	UBERON:0001416	56.97	gold quality
zone of skin	UBERON:0000014	55.98	gold quality
skin of leg	UBERON:0001511	55.22	gold quality
vermiform appendix	UBERON:0001154	52.23	gold quality
cortical plate	UBERON:0005343	50.91	silver quality
stomach	UBERON:0000945	49.64	gold quality
body of stomach	UBERON:0001161	49.49	gold quality
omental fat pad	UBERON:0010414	47.11	gold quality
fundus of stomach	UBERON:0001160	46.62	gold quality
prostate gland	UBERON:0002367	45.96	gold quality
right hemisphere of cerebellum	UBERON:0014890	45.01	gold quality
upper lobe of left lung	UBERON:0008952	44.57	gold quality
cerebellum	UBERON:0002037	44.27	silver quality
cerebellar cortex	UBERON:0002129	44.18	silver quality
cerebellar hemisphere	UBERON:0002245	44.16	silver quality
vagina	UBERON:0000996	43.61	gold quality
lung	UBERON:0002048	42.59	gold quality
colonic epithelium	UBERON:0000397	40.96	gold quality
adipose tissue	UBERON:0001013	40.37	gold quality
ventricular zone	UBERON:0003053	39.82	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-ANND-3	no	1.48

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

16 targeting NPY4R, 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-629-3P	99.85	67.99	1875
HSA-MIR-4698	99.84	71.41	4303
HSA-MIR-4713-5P	99.78	67.80	1794
HSA-MIR-4708-3P	99.51	67.99	870
HSA-MIR-12117	99.50	67.57	868
HSA-MIR-1207-5P	99.49	69.11	2983
HSA-MIR-4763-3P	99.10	67.83	2649
HSA-MIR-6737-3P	98.95	68.56	1577
HSA-MIR-7157-3P	98.95	68.70	1582
HSA-MIR-367-5P	98.84	67.18	902
HSA-MIR-5008-3P	98.73	67.50	1433
HSA-MIR-6840-3P	98.68	65.95	1923
HSA-MIR-1304-3P	98.29	66.44	1207
HSA-MIR-6880-5P	98.08	65.59	1282
HSA-MIR-4456	97.50	64.88	1678
HSA-MIR-3194-5P	96.80	64.90	1027

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 40.0% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 12)

• The pharmacologic insensitivity of pancreatic polypeptide responses to either NPY1- or NPY2-receptor antagonism, or to tetrodotoxin, indicates that NPY4 receptors are involved and that they are predominantly post-junctional in colon mucosa. (PMID:11906964)
• PP1 is targeted to DNA polymerase III via an interaction with the p68 subunit. (PMID:18826257)
• Results suggest that rabbit and human Y1, Y2 and Y5 receptor subtypes are well conserved, whereas Y4 receptors are less well conserved. (PMID:19481128)
• Results report on the functional reconstitution of the hY(2)R and the hY(4)R in Sf9 insect cells using the baculovirus system. (PMID:21745157)
• structure determination of transmembrane segments of Y4 and the yeast Ste2p G-protein-coupled receptors (PMID:22947943)
• Pancreatic polypeptide is recognized by two hydrophobic domains of the human Y4 receptor binding pocket. (PMID:24375409)
• These data demonstrate glucose-regulated secretion of PP and its effects on glucagon release through PPYR1 receptors expressed by alpha-cells. (PMID:25445712)
• Data suggest that repression of JNK-c-Jun signaling through pancreatic polypeptide receptor 1 (PP1) is one of the key anti-tumor mechanisms of neuronal membrane cytoskeletal protein 4.1 (4.1N). (PMID:26575790)
• A copy number variation (CNV) analysis demonstrated a significantly higher frequency of NPY4R containing 10q11.22 CNV loss in the patient population, while CNV gain in this region was more prevalent in the control population. Mutation analysis resulted in the identification of 15 rare non-synonymous heterozygous variants. Two variants in the patient population demonstrated receptor dysfunction and a pathogenic effect. (PMID:26921218)
• the internalization motif for the human neuropeptide Y4 receptor, which regulates arrestin-3 recruitment and receptor endocytosis, was identified. (PMID:27818291)
• Our results suggest that NPY4R genetic variation influences body weight in women, but the exact role of this receptor appears to be more complex than previously proposed. (PMID:29621259)
• Theoretical study of the interactions between peptide tyrosine tyrosine [PYY (1-36)], a newly identified modulator in type 2 diabetes pathophysiology, with receptors NPY1R and NPY4R. (PMID:33782920)

Cross-species orthologs

1 orthologs

Organism	Symbol	Gene ID
mus_musculus	Npy4r	ENSMUSG00000048337

Paralogs (33): TACR2 (ENSG00000075073), PROKR2 (ENSG00000101292), GPR50 (ENSG00000102195), TACR1 (ENSG00000115353), GPR75 (ENSG00000119737), PRLHR (ENSG00000119973), GPR83 (ENSG00000123901), MCHR1 (ENSG00000128285), OR11H1 (ENSG00000130538), MTNR1B (ENSG00000134640), MCHR2 (ENSG00000152034), NPY1R (ENSG00000164128), NPY5R (ENSG00000164129), MTNR1A (ENSG00000168412), PROKR1 (ENSG00000169618), TACR3 (ENSG00000169836), OR9G1 (ENSG00000174914), OR11H4 (ENSG00000176198), OR11H6 (ENSG00000176219), OR9A2 (ENSG00000179468), GPR88 (ENSG00000181656), GPR19 (ENSG00000183150), NPY2R (ENSG00000185149), OR11G2 (ENSG00000196832), OR11A1 (ENSG00000204694), OR9A1P (ENSG00000237621), OR11H12 (ENSG00000257115), OR9A4 (ENSG00000258083), OR11H2 (ENSG00000258453), OR11H7 (ENSG00000258806), NPY4R2 (ENSG00000264717), OR10X1 (ENSG00000279111), OR51F1 (ENSG00000280021)

Protein

Protein identifiers

Neuropeptide Y receptor type 4 — P50391 (reviewed: P50391)

Alternative names: Pancreatic polypeptide receptor 1

All UniProt accessions (1): P50391

UniProt curated annotations — full annotation on UniProt →

Function. G protein-coupled receptor for PPY/pancreatic polypeptide/PP, NPY/neuropeptide Y and PYY/peptide YY that is negatively coupled to cAMP. The rank order of affinity for these polypeptides and their derivatives is PP, PP (2-36) and [Ile-31, Gln-34] PP > [Pro-34] PYY > PYY and [Leu-31, Pro-34] NPY > NPY > PYY (3-36) and NPY (2-36) > PP (13-36) > PP (31-36) > NPY free acid.

Subcellular location. Cell membrane.

Tissue specificity. Highest levels found in brain, coronary artery and ileum. Low levels in pancreas and kidney. Detected in colon and small intestine.

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

RefSeq proteins (2): NP_001265723, NP_005963* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000611	NPY_rcpt	Family
IPR001933	NPY4_rcpt	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (40 total): helix 13, topological domain 8, transmembrane region 7, glycosylation site 4, sequence variant 2, turn 2, chain 1, lipid moiety-binding region 1, disulfide bond 1, strand 1

Structure

Experimental structures (PDB)

1 structures.

PDB	Method	Resolution (Å)
7X9C	ELECTRON MICROSCOPY	3

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P50391-F1	80.43	0.56

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): 340

Disulfide bonds (1): 114–201

Glycosylation sites (4): 2, 19, 29, 187

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

ID	Pathway
R-HSA-375276	Peptide ligand-binding receptors
R-HSA-418594	G alpha (i) signalling events

MSigDB gene sets: 74 (showing top): REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, MARTINEZ_RB1_TARGETS_DN, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, GOMF_PEPTIDE_RECEPTOR_ACTIVITY, GOCC_NEURON_PROJECTION, LEE_CALORIE_RESTRICTION_MUSCLE_UP, MARTINEZ_RB1_AND_TP53_TARGETS_UP, MULLIGHAN_MLL_SIGNATURE_1_UP, REACTOME_CLASS_A_1_RHODOPSIN_LIKE_RECEPTORS, GOMF_TRANSMEMBRANE_SIGNALING_RECEPTOR_ACTIVITY, GOMF_AMIDE_BINDING, GOMF_PEPTIDE_HORMONE_BINDING, GOMF_G_PROTEIN_COUPLED_RECEPTOR_ACTIVITY, MIKKELSEN_MEF_ICP_WITH_H3K27ME3, MIKKELSEN_ES_ICP_WITH_H3K4ME3

GO Biological Process (5): G protein-coupled receptor signaling pathway (GO:0007186), cell communication (GO:0007154), signal transduction (GO:0007165), neuropeptide signaling pathway (GO:0007218), signaling (GO:0023052)

GO Molecular Function (5): pancreatic polypeptide receptor activity (GO:0001602), G protein-coupled receptor activity (GO:0004930), peptide hormone binding (GO:0017046), neuropeptide binding (GO:0042923), neuropeptide Y receptor activity (GO:0004983)

GO Cellular Component (3): plasma membrane (GO:0005886), membrane (GO:0016020), neuron projection (GO:0043005)

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
cellular process	2
G protein-coupled receptor signaling pathway	2
G protein-coupled receptor activity	1
signal transduction	1
cell communication	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
regulation of biological process	1
neuropeptide Y receptor activity	1
transmembrane signaling receptor activity	1
hormone binding	1
peptide binding	1
neuropeptide receptor activity	1
membrane	1
cell periphery	1
cellular anatomical structure	1
plasma membrane bounded cell projection	1

Protein interactions and networks

STRING

0 interactions, top by confidence (×1000):

IntAct

6 interactions, top by confidence:

A	B	Type	Score
NPY4R	RAMP1	psi-mi:“MI:0915”(physical association)	0.400
RAMP2	NPY4R	psi-mi:“MI:0915”(physical association)	0.400
NPY4R	RAMP2	psi-mi:“MI:0915”(physical association)	0.400
RAMP3	NPY4R	psi-mi:“MI:0915”(physical association)	0.400

BioGRID (9): NPY4R (Affinity Capture-MS), NPY4R (Negative Genetic), NPY4R (Positive Genetic), NPY4R (Positive Genetic), NPY4R (Positive Genetic), TPSAB1 (Positive Genetic), NPY4R (Positive Genetic), NPY4R (Positive Genetic), NPY4R (Positive Genetic)

ESM2 similar proteins: O02813, O02835, O02836, O43614, O62809, O93603, P0C0L6, P0DQD5, P21555, P21761, P25929, P28647, P30731, P34981, P34992, P35382, P47751, P49146, P50391, P56719, P58308, P70031, P79113, P79217, P79945, P97295, Q04573, Q1RMU8, Q28596, Q56H79, Q5IS62, Q61041, Q61212, Q61618, Q63447, Q6W5P4, Q8BZP8, Q8K458, Q8NFJ6, Q8SPN1

Diamond homologs: A5A4K9, A5A4L1, C3ZQF9, F1MV99, G4WMX4, O02835, O02836, O08725, O42179, O43614, O54799, O62729, O62809, O70342, O77408, P0DQD5, P11617, P20288, P22270, P24053, P24628, P25929, P25931, P28336, P29274, P30731, P30938, P30975, P32251, P35346, P35371, P41143, P47211, P47751, P49146, P49219, P49285, P49288, P49683, P50391

SIGNOR signaling

3 interactions.

A	Effect	B	Mechanism
PPY	up-regulates	NPY4R	binding
NPY	up-regulates	NPY4R	binding
PYY	up-regulates	NPY4R	binding

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	36
Likely benign	0
Benign	9

Top pathogenic / likely-pathogenic (0)

SpliceAI

192 predictions. Top by Δscore:

Variant	Effect	Δscore
10:46462693:GGC:G	acceptor_gain	1.0000
10:46465678:G:GT	donor_gain	1.0000
10:46462693:G:GG	acceptor_gain	0.9900
10:46462694:A:AC	acceptor_loss	0.9900
10:46462694:A:AG	acceptor_gain	0.9900
10:46462696:GTA:G	acceptor_loss	0.9900
10:46462697:TGTAG:T	acceptor_loss	0.9900
10:46462698:TTGTA:T	acceptor_loss	0.9900
10:46465674:T:A	donor_loss	0.9900
10:46465676:GGT:G	donor_loss	0.9900
10:46465677:AGGTA:A	donor_loss	0.9900
10:46465679:GGAG:G	donor_gain	0.9900
10:46465695:G:GG	donor_gain	0.9700
10:46462693:GG:G	acceptor_gain	0.9600
10:46462694:AG:A	acceptor_gain	0.9600
10:46465678:GAG:G	donor_gain	0.9600
10:46462693:GGCGT:G	acceptor_gain	0.9400
10:46465675:G:GG	donor_gain	0.9400
10:46462693:GGCG:G	acceptor_gain	0.9300
10:46462694:AGGC:A	acceptor_gain	0.9300
10:46465678:G:T	donor_gain	0.9100
10:46465679:GGAGG:G	donor_gain	0.8900
10:46465680:AGGAG:A	donor_gain	0.8900
10:46462706:T:A	acceptor_loss	0.8700
10:46463776:TT:T	donor_gain	0.8500
10:46463777:GT:G	donor_gain	0.8500
10:46462697:T:TA	acceptor_gain	0.8200
10:46463884:G:GT	acceptor_loss	0.8000
10:46463885:A:AT	acceptor_loss	0.8000
10:46463886:CA:C	acceptor_loss	0.8000

AlphaMissense

2457 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
10:46462021:C:A	W205C	0.998
10:46462021:C:G	W205C	0.998
10:46461814:A:C	F274L	0.997
10:46461814:A:T	F274L	0.997
10:46461816:A:G	F274L	0.997
10:46461797:G:C	P280R	0.993
10:46462295:C:G	C114S	0.993
10:46462296:A:T	C114S	0.993
10:46462315:C:A	W107C	0.993
10:46462315:C:G	W107C	0.993
10:46461717:A:G	C307R	0.992
10:46462034:C:G	C201S	0.992
10:46462035:A:T	C201S	0.992
10:46462146:A:G	W164R	0.991
10:46462146:A:T	W164R	0.991
10:46462390:G:C	N82K	0.991
10:46462390:G:T	N82K	0.991
10:46461797:G:T	P280H	0.990
10:46462023:A:G	W205R	0.990
10:46462023:A:T	W205R	0.990
10:46462489:G:C	S49R	0.990
10:46462489:G:T	S49R	0.990
10:46462491:T:G	S49R	0.990
10:46461704:G:T	A311D	0.989
10:46461804:A:G	W278R	0.989
10:46461804:A:T	W278R	0.989
10:46462035:A:G	C201R	0.989
10:46462317:A:G	W107R	0.989
10:46462317:A:T	W107R	0.989
10:46462295:C:T	C114Y	0.987

dbSNP variants (sampled 300 via entrez): RS1048156 (10:46462048 C>T), RS113117352 (10:46461898 G>A), RS113864611 (10:46460923 G>A), RS114592738 (10:46461920 C>T), RS115280230 (10:46461607 G>A), RS115386214 (10:46466011 G>A), RS115443559 (10:46461899 C>T), RS1156316906 (10:46466175 CTT>C,CTTTT), RS1156409640 (10:46466312 C>T), RS1156829474 (10:46465707 A>T), RS1156937288 (10:46465651 C>A), RS1157432930 (10:46460709 T>A,C), RS1157503498 (10:46462002 T>C), RS1158024416 (10:46461030 C>G,T), RS1158416848 (10:46467545 G>A)

Disease associations

OMIM: gene MIM:601790 | 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): CHEMBL4877 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 11 (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
CHEMBL4540843	PANCREATIC POLYPEPTIDE	2	1
CHEMBL438945	HUMAN NEUROPEPTIDE Y	1	10

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Neuropeptide Y receptors

Most potent curated ligand interactions (29 total), top 25:

Ligand	Action	Affinity	Parameter
pancreatic polypeptide	Full agonist	10.9	pKi
PP-(2-36) (human)	Full agonist	10.4	pKi
[Leu31,Pro34]PYY (human)	Full agonist	10.2	pKi
pancreatic polypeptide	Full agonist	10.0	pKi
[125I]PYY (pig)	Full agonist	9.8	pKd
GR231118	Full agonist	9.8	pKi
[125I]GR231118	Full agonist	9.6	pKd
[Ile31,Gln34]PP (human)	Full agonist	9.2	pKi
PP-(13-36) (human)	Full agonist	9.0	pKi
[Pro34]PYY (human)	Full agonist	8.9	pKi
peptide YY	Full agonist	8.8	pKi
NPY	Full agonist	8.7	pKi
pancreatic polypeptide	Full agonist	8.6	pIC50
peptide YY	Full agonist	8.5	pIC50
[Leu31,Pro34]NPY (pig)	Full agonist	8.4	pIC50
PP-(20-36) (human)	Full agonist	8.1	pKi
neuropeptide Y	Full agonist	8.0	pKi
[Leu31,Pro34]PYY (pig)	Full agonist	8.0	pIC50
NPY-(3-36) (pig)	Full agonist	7.7	pKi
[Leu31,Pro34]NPY	Full agonist	7.7	pKi
PYY-(3-36)	Full agonist	7.6	pKi
PYY-(13-36) (mouse, rat, pig)	Full agonist	7.5	pKi
NPY-(2-36) (pig)	Full agonist	7.4	pKi
NPY-(2-36)	Full agonist	7.1	pIC50
VU0506013	Positive	6.9	pEC50

Binding affinities (BindingDB)

24 measured of 25 human assays (35 total across all organisms); most potent 24 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
P34-PYY,human	KI	0.14 nM
CAS_118997-30-1	KI	0.17 nM
Des-AA11-18[Cys7,21,D-Lys9 (Ac), Pro34]-NPY	KI	0.2 nM
Des-AA11-18[Cys7,21,D-Lys9 (Ac)]-NPY	KI	0.7 nM
[D-Arg25]-NPY	KI	0.9 nM
Des-AA11-18[Cys7,21,D-Lys9 (Ac), D-His26, Pro34]-NPY	KI	1.2 nM
[D-His26]-NPY	KI	2 nM
Des-AA11-18[Cys7,21,D-Lys9 (Ac), D-His26]-NPY	KI	2.2 nM
[D-Arg25, D-His26]-NPY	KI	9.7 nM
I31,G34-PP,human	KI	20 nM
PYY 3-36, rat	KI	33.1 nM
Des-AA10-17[Cys7,21, Pro34]-NPY	KI	37 nM
PYY3-36, human	KI	45.7 nM
CAS_59763-91-6	KI	97.7 nM
PP2-36, HUMAN	KI	100 nM
PP13-36, HUMAN	KI	100 nM
CAS_59763-91-6	KI	170 nM
CAS_59763-91-6	KI	209 nM
NPY, free acid, human	KI	398 nM
NSC_41735	KI	468 nM
PP [cPP(1-7), NPY(19-23), Ala31, Aib32, Gln34], human	KI	530 nM
NPY [Ala31, Aib32], porcine	KI	700 nM
PYY 3-36	KI	760 nM
NPY [hPP(1-17), Ala31,Aib32], human	KI	1000 nM

ChEMBL bioactivities

753 potent at pChembl≥5 of 760 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
11.00	Ki	0.01	nM	CHEMBL4276961
11.00	Ki	0.01	nM	CHEMBL4286615
11.00	Ki	0.01	nM	CHEMBL5423253
10.96	Ki	0.011	nM	CHEMBL4873376
10.92	Kd	0.01202	nM	CHEMBL5395013
10.92	Kd	0.012	nM	CHEMBL5395013
10.85	Kd	0.014	nM	CHEMBL5395013
10.64	Ki	0.023	nM	PANCREATIC POLYPEPTIDE
10.61	Ki	0.02455	nM	CHEMBL5437701
10.59	Ki	0.026	nM	CHEMBL5437701
10.52	EC50	0.03	nM	CHEMBL3559801
10.52	Ki	0.0302	nM	CHEMBL5422869
10.51	EC50	0.0307	nM	CHEMBL5420881
10.51	Ki	0.031	nM	CHEMBL5422869
10.50	Ki	0.03162	nM	CHEMBL5423253
10.48	Ki	0.03311	nM	CHEMBL4856311
10.48	Ki	0.033	nM	CHEMBL4856311
10.44	Ki	0.036	nM	CHEMBL5423253
10.44	Ki	0.03631	nM	PANCREATIC POLYPEPTIDE
10.43	Ki	0.037	nM	PANCREATIC POLYPEPTIDE
10.40	EC50	0.03981	nM	CHEMBL3559801
10.40	Ki	0.03981	nM	CHEMBL5435492
10.39	Ki	0.041	nM	CHEMBL5435492
10.36	Ki	0.04365	nM	CHEMBL4873376
10.32	Ki	0.048	nM	CHEMBL4873376
10.30	Ki	0.05	nM	CHEMBL2371908
10.30	EC50	0.05012	nM	CHEMBL5437695
10.20	Ki	0.0631	nM	CHEMBL3559801
10.20	EC50	0.063	nM	CHEMBL5437695
10.18	Ki	0.06607	nM	CHEMBL5437695
10.18	Ki	0.066	nM	CHEMBL5437695
10.13	Ki	0.07413	nM	CHEMBL4873376
10.12	Ki	0.076	nM	CHEMBL4873376
10.10	Ki	0.08	nM	CHEMBL429531
10.08	Ki	0.08318	nM	CHEMBL5423253
10.06	Ki	0.088	nM	CHEMBL5423253
10.05	Kd	0.09	nM	CHEMBL5395013
10.04	Ki	0.0912	nM	CHEMBL5421880
10.03	Ki	0.093	nM	CHEMBL5421880
10.02	Ki	0.0955	nM	PANCREATIC POLYPEPTIDE
10.00	Ki	0.1	nM	CHEMBL4278700
10.00	Ki	0.1	nM	PANCREATIC POLYPEPTIDE
10.00	EC50	0.1	nM	CHEMBL5430318
9.98	Kd	0.1047	nM	CHEMBL5395013
9.97	Ki	0.1072	nM	CHEMBL5396128
9.96	Ki	0.11	nM	CHEMBL5396128
9.96	Ki	0.1096	nM	CHEMBL5430318
9.96	EC50	0.11	nM	CHEMBL5430318
9.96	Kd	0.11	nM	CHEMBL5395013
9.93	Ki	0.1175	nM	CHEMBL4857577

PubChem BioAssay actives

1494 with measured affinity, of 2695 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
(4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-5-carbamimidamido-1-[(2S)-2-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]amino]-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-aminopropanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]propanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoic acid	1418831: Displacement of [125I]-PP from human Y4R expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay	ki	<0.0001	uM
(4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(3S)-6-amino-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]amino]-1-oxopentan-2-yl]amino]-1,6-dioxohexan-3-yl]-methylamino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-aminopropanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]propanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoic acid	1418831: Displacement of [125I]-PP from human Y4R expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay	ki	<0.0001	uM
2-(4-tert-butylphenoxy)cyclohexan-1-ol	1450957: Positive allosteric modulation of human NY4 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of pancreatic polypeptide induced-calcium flux by measuring pancreatic polypeptide EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of pancreatic polypeptide after 140 secs by Fluo2-AM fluorescent dye based-assay (Rvb = 0.1 nM)	ec50	<0.0001	uM
(9S,12S,15S)-4-amino-N-[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-15-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-2,11,14,17,20-pentaoxo-1,3,5,10,13,16,21-heptazacyclopentacos-4-ene-9-carboxamide	1782295: Displacement of [3H]UR-KK200 from human neuropeptide Y Y4 receptor expressed in CHO-mtAEQ cells co-expressing Gqi5 measured after 90 mins by scintillation counting analysis	ki	<0.0001	uM
(9S,12S,15S)-4-amino-N-[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-15-[3-(diaminomethylideneamino)propyl]-12-(1H-indol-3-ylmethyl)-2,11,14,17,20-pentaoxo-1,3,5,10,13,16,21-heptazacyclopentacos-4-ene-9-carboxamide	1782295: Displacement of [3H]UR-KK200 from human neuropeptide Y Y4 receptor expressed in CHO-mtAEQ cells co-expressing Gqi5 measured after 90 mins by scintillation counting analysis	ki	<0.0001	uM
(9S,12S,15S,19R)-4-amino-N-[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-15-[3-(diaminomethylideneamino)propyl]-19-[4-(2,3-ditritiopropanoylamino)butanoylamino]-12-[(4-hydroxyphenyl)methyl]-2,11,14,17,20-pentaoxo-1,3,5,10,13,16,21-heptazacyclopentacos-4-ene-9-carboxamide	2019073: Binding affinity to human Y4R expressed in CHO cells co-expressing Gqi5-mtAEQ under sodium free buffer condition	kd	<0.0001	uM
(9S,12S,15S,18R)-4,18-diamino-N-[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-15-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-2,11,14,17,20-pentaoxo-1,3,5,10,13,16,21-heptazacyclopentacos-4-ene-9-carboxamide;tetrakis(2,2,2-trifluoroacetic acid)	2019062: Displacement of [3H]UR-KK200 from human Y4R expressed in CHO cells co-expressing Gqi5-mtAEQ	ki	<0.0001	uM
(9S,12S,15S,19R)-4-amino-N-[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-15-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-2,11,14,17,20-pentaoxo-19-[4-(propanoylamino)butanoylamino]-1,3,5,10,13,16,21-heptazacyclopentacos-4-ene-9-carboxamide;tris(2,2,2-trifluoroacetic acid)	2019062: Displacement of [3H]UR-KK200 from human Y4R expressed in CHO cells co-expressing Gqi5-mtAEQ	ki	<0.0001	uM
(9S,12S,15S,19R)-4,19-diamino-N-[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-15-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-2,11,14,17,20-pentaoxo-1,3,5,10,13,16,21-heptazacyclopentacos-4-ene-9-carboxamide;tetrakis(2,2,2-trifluoroacetic acid)	2019062: Displacement of [3H]UR-KK200 from human Y4R expressed in CHO cells co-expressing Gqi5-mtAEQ	ki	<0.0001	uM
(9S,12S,15S,19S)-4,19-diamino-N-[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-15-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-2,11,14,17,20-pentaoxo-1,3,5,10,13,16,21-heptazacyclopentacos-4-ene-9-carboxamide;tetrakis(2,2,2-trifluoroacetic acid)	2019062: Displacement of [3H]UR-KK200 from human Y4R expressed in CHO cells co-expressing Gqi5-mtAEQ	ki	<0.0001	uM
(4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-aminopropanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]propanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoic acid	2019089: Displacement of [3H]-(9S,12S,15S,19R,E)-4-amino-N-((S)-1-(((S)-1-(((S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)amino)-5-guanidino-1-oxopentan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)-15-(3-guanidinopropyl)-12-(4-hydroxybenzyl)-2,11,14,17,20-pentaoxo-19-(4-(propanamido-2,3-t2)butanamido)-1,3,5,10,13,16,21-heptaazacyclopentacos-3-ene-9-carboxamide from human Y4R expressed in CHO cells coexpressing Gqi5-mtAEQ under hypotonic sodium free buffer condition	ki	<0.0001	uM
N-[1-methyl-2-oxo-5-(pyrrolidine-1-carbonyl)-3-pyridinyl]-2-(2-methylphenoxy)acetamide	1981609: Positive allosteric modulation of YFP tagged human Y4 receptor transfected with COS-7 cells co-transfected with delta6Galphaqi4-myr measured after 24 hrs by calcium 2+ flux assay (Rvb = 91.1 pM )	ec50	<0.0001	uM
(4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]amino]-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-aminopropanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]propanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoic acid	1418831: Displacement of [125I]-PP from human Y4R expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay	ki	0.0001	uM
(15S,18S,21S)-2-amino-N-[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-15-[3-(diaminomethylideneamino)propyl]-18-[(4-hydroxyphenyl)methyl]-4,10,13,16,19-pentaoxo-1,3,5,9,14,17,20-heptazacyclotetracosene-21-carboxamide	1782295: Displacement of [3H]UR-KK200 from human neuropeptide Y Y4 receptor expressed in CHO-mtAEQ cells co-expressing Gqi5 measured after 90 mins by scintillation counting analysis	ki	0.0001	uM
(9S,12S,15S,18S)-4-amino-N-[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-15-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-2,11,14,17,20-pentaoxo-18-(propanoylamino)-1,3,5,10,13,16,21-heptazacyclopentacos-4-ene-9-carboxamide;tris(2,2,2-trifluoroacetic acid)	2019062: Displacement of [3H]UR-KK200 from human Y4R expressed in CHO cells co-expressing Gqi5-mtAEQ	ki	0.0001	uM
(9S,12S,15S,19S)-4-amino-N-[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-15-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-2,11,14,17,20-pentaoxo-19-(propanoylamino)-1,3,5,10,13,16,21-heptazacyclopentacos-4-ene-9-carboxamide;tris(2,2,2-trifluoroacetic acid)	2019062: Displacement of [3H]UR-KK200 from human Y4R expressed in CHO cells co-expressing Gqi5-mtAEQ	ki	0.0001	uM
(9S,12S,15S,19R)-4-amino-19-(4-aminobutanoylamino)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-15-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-2,11,14,17,20-pentaoxo-1,3,5,10,13,16,21-heptazacyclopentacos-4-ene-9-carboxamide;tetrakis(2,2,2-trifluoroacetic acid)	2019062: Displacement of [3H]UR-KK200 from human Y4R expressed in CHO cells co-expressing Gqi5-mtAEQ	ki	0.0001	uM
(9S,12S,15S,18R)-4-amino-N-[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-15-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-2,11,14,17,20-pentaoxo-18-(propanoylamino)-1,3,5,10,13,16,21-heptazacyclopentacos-4-ene-9-carboxamide;tris(2,2,2-trifluoroacetic acid)	2019062: Displacement of [3H]UR-KK200 from human Y4R expressed in CHO cells co-expressing Gqi5-mtAEQ	ki	0.0001	uM
(9S,12S,15S,19R)-4-amino-N-[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-15-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-2,11,14,17,20-pentaoxo-19-(propanoylamino)-1,3,5,10,13,16,21-heptazacyclopentacos-4-ene-9-carboxamide;tris(2,2,2-trifluoroacetic acid)	2019062: Displacement of [3H]UR-KK200 from human Y4R expressed in CHO cells co-expressing Gqi5-mtAEQ	ki	0.0001	uM
(4S)-4-[[2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-2-[[(2S)-1-[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-5-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-5-oxopentanoic acid	143554: Affinity for cloned Y4 receptor using [125I]PP as radioligand	ki	0.0001	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,7S)-2,7-diamino-8-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-8-oxooctanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-(4-hydroxyphenyl)propanoic acid	263165: Displacement of [125I]hPP from human NPY4 receptor expressed in CHO cells	ki	0.0001	uM
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]amino]-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]-methylamino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-4-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S,3S)-2-amino-3-methylpentanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-4-carboxybutanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-5-oxopentanoic acid	1418831: Displacement of [125I]-PP from human Y4R expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay	ki	0.0002	uM
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-5-carbamimidamido-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]amino]-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-methylamino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-4-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S,3S)-2-amino-3-methylpentanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-4-carboxybutanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-5-oxopentanoic acid	1418831: Displacement of [125I]-PP from human Y4R expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay	ki	0.0002	uM
(2R,7R)-2,7-diamino-N,N’-bis[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]octanediamide	1635411: Displacement of [3H]18 from human NPY Y4 receptor expressed in CHO cells co-expressing Gqi5-mtAEQ after 90 mins by liquid scintillation counting	ki	0.0002	uM
(9S,12S,15S)-4-amino-15-(4-aminobutyl)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-12-[(4-hydroxyphenyl)methyl]-2,11,14,17,20-pentaoxo-1,3,5,10,13,16,21-heptazacyclopentacos-4-ene-9-carboxamide	1782295: Displacement of [3H]UR-KK200 from human neuropeptide Y Y4 receptor expressed in CHO-mtAEQ cells co-expressing Gqi5 measured after 90 mins by scintillation counting analysis	ki	0.0002	uM
(12S,15S,18S,21S)-2,12-diamino-N-[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-15-[3-(diaminomethylideneamino)propyl]-18-[(4-hydroxyphenyl)methyl]-4,9,13,16,19-pentaoxo-1,3,5,8,14,17,20-heptazacyclotetracosene-21-carboxamide;tetrakis(2,2,2-trifluoroacetic acid)	2019062: Displacement of [3H]UR-KK200 from human Y4R expressed in CHO cells co-expressing Gqi5-mtAEQ	ki	0.0002	uM
N’-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-6-[[(E)-N’-[4-(2,3-ditritiopropanoylamino)butylcarbamoyl]carbamimidoyl]amino]-1-oxohexan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]octanediamide	2019089: Displacement of [3H]-(9S,12S,15S,19R,E)-4-amino-N-((S)-1-(((S)-1-(((S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)amino)-5-guanidino-1-oxopentan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)-15-(3-guanidinopropyl)-12-(4-hydroxybenzyl)-2,11,14,17,20-pentaoxo-19-(4-(propanamido-2,3-t2)butanamido)-1,3,5,10,13,16,21-heptaazacyclopentacos-3-ene-9-carboxamide from human Y4R expressed in CHO cells coexpressing Gqi5-mtAEQ under hypotonic sodium free buffer condition	ki	0.0002	uM
(2S,7S)-2-amino-N,N’-bis[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]-7-(propanoylamino)octanediamide	1635411: Displacement of [3H]18 from human NPY Y4 receptor expressed in CHO cells co-expressing Gqi5-mtAEQ after 90 mins by liquid scintillation counting	ki	0.0003	uM
(12S,15S,18S,21S)-2-amino-N-[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-15-[3-(diaminomethylideneamino)propyl]-18-[(4-hydroxyphenyl)methyl]-4,9,13,16,19-pentaoxo-12-(propanoylamino)-1,3,5,8,14,17,20-heptazacyclotetracosene-21-carboxamide;tetrakis(2,2,2-trifluoroacetic acid)	2019062: Displacement of [3H]UR-KK200 from human Y4R expressed in CHO cells co-expressing Gqi5-mtAEQ	ki	0.0003	uM
(9S,12S,15S,18S)-4,18-diamino-N-[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-15-[3-(diaminomethylideneamino)propyl]-12-[(4-hydroxyphenyl)methyl]-2,11,14,17,20-pentaoxo-1,3,5,10,13,16,21-heptazacyclopentacos-4-ene-9-carboxamide;tetrakis(2,2,2-trifluoroacetic acid)	2019062: Displacement of [3H]UR-KK200 from human Y4R expressed in CHO cells co-expressing Gqi5-mtAEQ	ki	0.0003	uM
(3S,9S,12S,18S,24S,27S)-9-N,24-N-bis[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]-3,18-bis[[(2S,3S)-2-amino-3-methylpentanoyl]amino]-2,6,11,17,21,26-hexaoxo-1,7,10,16,22,25-hexazatricyclo[25.3.0.012,16]triacontane-9,24-dicarboxamide	143554: Affinity for cloned Y4 receptor using [125I]PP as radioligand	ki	0.0003	uM
(2R,7R)-2-amino-N,N’-bis[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]-7-(2,3-ditritiopropanoylamino)octanediamide	2019089: Displacement of [3H]-(9S,12S,15S,19R,E)-4-amino-N-((S)-1-(((S)-1-(((S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)amino)-5-guanidino-1-oxopentan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)-15-(3-guanidinopropyl)-12-(4-hydroxybenzyl)-2,11,14,17,20-pentaoxo-19-(4-(propanamido-2,3-t2)butanamido)-1,3,5,10,13,16,21-heptaazacyclopentacos-3-ene-9-carboxamide from human Y4R expressed in CHO cells coexpressing Gqi5-mtAEQ under hypotonic sodium free buffer condition	ki	0.0004	uM
(3S,12S,18S,27S)-9-N,24-N-bis[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]-3,18-bis[[(2S,3S)-2-amino-3-methylpentanoyl]amino]-2,6,11,17,21,26-hexaoxo-1,7,10,16,22,25-hexazatricyclo[25.3.0.012,16]triacontane-9,24-dicarboxamide	1660937: Displacement of [3H]UR-KK200 from human Y4 receptor expressed in CHO cells co-expressing Gqi5-mtAEQ measured after 90 mins by scintillation counting analysis	ki	0.0004	uM
(4S)-4-[[2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-2-[[(2S)-1-[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-5-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-5-oxopentanoic acid	460480: Displacement of [125I]Pancreatic polypeptide from human neuropeptide Y4 receptor in human HEK293 cells after 40 mins	ki	0.0004	uM
(4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-5-carbamimidamido-1-[(2S)-2-[[(2R)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]amino]-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-1-[(2S,3S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[2-[[(2S)-1-[(2R)-2-[[(2R)-2-[[(2R)-1-[(2R)-2-[[(2R)-2-[[(2R)-1-[(2S)-2-aminopropanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]propanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoic acid	1289951: Displacement of S0586[K4]hpp from human NPY4 receptor expressed in CHO cells co-expressing Gqi5-mtAEQ by flow cytometric analysis	ki	0.0005	uM
(4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(1S)-1-amino-2-(4-hydroxyphenyl)ethyl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-aminopropanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]propanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoic acid	776960: Binding affinity to human Y4 receptor	ki	0.0005	uM
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-5-carbamimidamidopentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-N-[(2S)-1-[[(2S,3S)-1-[[(1R,3S)-3-[[(2S)-1-[[(1R,3S)-3-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]-2,2-dimethylcyclobutyl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]-2,2-dimethylcyclobutyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]butanediamide	776959: Displacement of Cy5-[K4]hPP from human Y4 receptor expressed in CHO cells after 90 to 120 mins by flow cytometry	ki	0.0005	uM
4-[[(2S)-1-[[(2S)-1-[[(2S)-5-[[amino-(3-aminopropylcarbamoylamino)methylidene]amino]-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-oxobutanoic acid	1782295: Displacement of [3H]UR-KK200 from human neuropeptide Y Y4 receptor expressed in CHO-mtAEQ cells co-expressing Gqi5 measured after 90 mins by scintillation counting analysis	ki	0.0006	uM
(1R,2S,3R)-2-[[[(2S)-2-acetamido-5-(diaminomethylideneamino)pentanoyl]amino]methyl]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-3-phenylcyclobutane-1-carboxamide	1982887: Displacement of [3H]UR-KK200 from human Y4 receptor expressed in CHO-Gqi5-mtAQE cells measured after 90 mins by MicroBeta plate counter based competition binding assay	ki	0.0006	uM
N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]-N’-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-5-[[(E)-N’-[4-(propanoylamino)butylcarbamoyl]carbamimidoyl]amino]pentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]octanediamide	1635411: Displacement of [3H]18 from human NPY Y4 receptor expressed in CHO cells co-expressing Gqi5-mtAEQ after 90 mins by liquid scintillation counting	ki	0.0007	uM
2,7-diamino-N,N’-bis[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]octanediamide	1635423: Displacement of [3H]18 from human NPY Y4 receptor expressed in CHO cells co-expressing Gqi5-mtAEQ by liquid scintillation counting	kd	0.0007	uM
N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]-N’-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-[[N-[4-(2,3-ditritiopropanoylamino)butylcarbamoyl]carbamimidoyl]amino]-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]octanediamide	1635413: Binding affinity to human NPY Y4 receptor expressed in CHO cells co-expressing Gqi5-mtAEQ after 90 mins in presence of sodium-free HEPES buffer by liquid scintillation counting	kd	0.0007	uM
(2S,7S)-2-amino-N,N’-bis[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]-7-(2,3-ditritiopropanoylamino)octanediamide	1635413: Binding affinity to human NPY Y4 receptor expressed in CHO cells co-expressing Gqi5-mtAEQ after 90 mins in presence of sodium-free HEPES buffer by liquid scintillation counting	kd	0.0007	uM
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-5-carbamimidamido-1-[[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]amino]-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-4-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S,3S)-2-[[(2S)-1-[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-4-carboxybutanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-5-oxopentanoic acid	1418831: Displacement of [125I]-PP from human Y4R expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay	ki	0.0008	uM
(4S)-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-aminopropanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-6-(2,3-ditritiopropanoylamino)hexanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]propanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoic acid	2019055: Binding affinity to human Y4R under sodium free condition	kd	0.0011	uM
N’-[(2S)-1-[[(2S)-5-[[(E)-N’-(4-aminobutylcarbamoyl)carbamimidoyl]amino]-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]octanediamide	1635408: Displacement of 3H-10 from human NPY Y4 receptor expressed in CHO cells co-expressing Gqi5-mtAEQ after 90 mins in presence of sodium-free HEPES buffer by liquid scintillation counting	ki	0.0012	uM
4-[[(2S)-1-[[(2S)-1-[[(2S)-5-[[amino-(4-aminobutylcarbamoylamino)methylidene]amino]-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-oxobutanoic acid	1782295: Displacement of [3H]UR-KK200 from human neuropeptide Y Y4 receptor expressed in CHO-mtAEQ cells co-expressing Gqi5 measured after 90 mins by scintillation counting analysis	ki	0.0013	uM
(3R,9R,12S,18S,24S,27S)-9-N,24-N-bis[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]-3,18-bis[[(2S,3S)-2-amino-3-methylpentanoyl]amino]-2,6,11,17,21,26-hexaoxo-1,7,10,16,22,25-hexazatricyclo[25.3.0.012,16]triacontane-9,24-dicarboxamide	1635411: Displacement of [3H]18 from human NPY Y4 receptor expressed in CHO cells co-expressing Gqi5-mtAEQ after 90 mins by liquid scintillation counting	ki	0.0013	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-N-[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-methylpentanamide	1660937: Displacement of [3H]UR-KK200 from human Y4 receptor expressed in CHO cells co-expressing Gqi5-mtAEQ measured after 90 mins by scintillation counting analysis	ki	0.0014	uM
(9S,12S)-4-amino-N-[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-12-[3-(diaminomethylideneamino)propyl]-2,11,14,17-tetraoxo-1,3,5,10,13,18-hexazacyclodocos-4-ene-9-carboxamide	1782295: Displacement of [3H]UR-KK200 from human neuropeptide Y Y4 receptor expressed in CHO-mtAEQ cells co-expressing Gqi5 measured after 90 mins by scintillation counting analysis	ki	0.0014	uM

CTD chemical–gene interactions

14 total (human), top 14 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Aflatoxin B1	decreases methylation, increases expression	2
bisphenol F	affects cotreatment, increases expression	1
hydroxyhydroquinone	decreases expression	1
sulforaphane	decreases expression	1
abrine	decreases expression	1
licochalcone B	decreases expression	1
Benzo(a)pyrene	increases expression	1
Dexamethasone	affects cotreatment, increases expression	1
Indomethacin	affects cotreatment, increases expression	1
Phthalic Acids	increases methylation	1
Tobacco Smoke Pollution	decreases expression	1
1-Methyl-3-isobutylxanthine	affects cotreatment, increases expression	1
Okadaic Acid	decreases expression	1
S-Nitrosoglutathione	increases expression	1

ChEMBL screening assays

199 unique, capped per target: 134 binding, 65 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1001160	Binding	Binding affinity to NPY Y4 receptor	Design, syntheses, and structure-activity relationships of novel NPY Y5 receptor antagonists: 2-{3-Oxospiro[isobenzofuran-1(3H),4’-piperidin]-1’-yl}benzimidazole derivatives. — Bioorg Med Chem Lett
CHEMBL1053234	Functional	Antagonist activity at human neuropeptide Y4 receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay	Design, synthesis and evaluation of a novel cyclohexanamine class of neuropeptide Y Y1 receptor antagonists. — Bioorg Med Chem Lett

Cellosaurus cell lines

5 cell lines: 3 spontaneously immortalized cell line, 1 cancer cell line, 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B1YY	Abcam HeLa NPY4R KO	Cancer cell line	Female
CVCL_C0TJ	ACTOne PPYR1	Transformed cell line	Female
CVCL_H481	CHO-K1/NPY4/Galpha15	Spontaneously immortalized cell line	Female
CVCL_KV64	cAMP Hunter CHO-K1 PPYR1 Gi	Spontaneously immortalized cell line	Female
CVCL_KY82	PathHunter CHO-K1 PPYR1 beta-arrestin	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

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