NPBWR1

gene

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Summary

NPBWR1 (neuropeptides B and W receptor 1, HGNC:4522) is a protein-coding gene on chromosome 8q11.23, encoding Neuropeptides B/W receptor type 1 (P48145). Interacts specifically with a number of opioid ligands.

Predicted to enable G protein-coupled receptor activity and neuropeptide binding activity. Involved in G protein-coupled receptor signaling pathway. Predicted to be located in membrane. Predicted to be active in neuron projection and plasma membrane.

Source: NCBI Gene 2831 — RefSeq curated summary.

At a glance

GWAS associations: 3
Clinical variants (ClinVar): 57 total
Druggable target: yes
MANE Select transcript: NM_005285

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:4522
Approved symbol	NPBWR1
Name	neuropeptides B and W receptor 1
Location	8q11.23
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000288611
Ensembl biotype	protein_coding
OMIM	600730
Entrez	2831

Gene structure

Transcript identifiers

Ensembl transcripts: 1 — 1 protein_coding

ENST00000674939

RefSeq mRNA: 1 — MANE Select: NM_005285 NM_005285

CCDS: CCDS6151

Canonical transcript exons

ENST00000674939 — 2 exons

Exon	Start	End
ENSE00001315782	52939182	52939366
ENSE00003903177	52939711	52943734

Expression profiles

Bgee: expression breadth broad, 61 present calls, max score 70.35.

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	70.35	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	66.05	gold quality
secondary oocyte	CL:0000655	60.81	gold quality
gall bladder	UBERON:0002110	59.84	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	59.11	gold quality
prefrontal cortex	UBERON:0000451	56.68	gold quality
buccal mucosa cell	CL:0002336	55.75	gold quality
Brodmann (1909) area 46	UBERON:0006483	55.01	gold quality
parotid gland	UBERON:0001831	54.84	gold quality
right lobe of liver	UBERON:0001114	54.80	gold quality
nasal cavity epithelium	UBERON:0005384	52.25	gold quality
nasal cavity mucosa	UBERON:0001826	51.22	gold quality
anterior cingulate cortex	UBERON:0009835	51.22	gold quality
liver	UBERON:0002107	51.05	gold quality
frontal cortex	UBERON:0001870	50.99	gold quality
neocortex	UBERON:0001950	50.30	gold quality
Brodmann (1909) area 9	UBERON:0013540	49.72	gold quality
hypothalamus	UBERON:0001898	49.17	gold quality
cerebellar vermis	UBERON:0004720	48.93	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	48.49	gold quality
right frontal lobe	UBERON:0002810	47.73	gold quality
cerebral cortex	UBERON:0000956	46.98	gold quality
quadriceps femoris	UBERON:0001377	46.52	gold quality
skin of abdomen	UBERON:0001416	46.50	gold quality
vastus lateralis	UBERON:0001379	45.68	gold quality
lymph node	UBERON:0000029	44.26	gold quality
oocyte	CL:0000023	43.85	gold quality
zone of skin	UBERON:0000014	43.69	gold quality
leukocyte	CL:0000738	43.39	silver quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	43.37	gold quality

Regulation

Is transcription factor: no

Literature-anchored findings (GeneRIF, showing 9)

neuropeptide B, a neuropeptide modified with bromine is an endogenous ligand for GPR7 (PMID:12118011)
distribution in central nervous system and peripheral tissues with precursor peptides (PMID:12401809)
characterization of a family of endogenous neuropeptide ligands for this G protein-coupled receptor (PMID:12719537)
These results suggest a relationship between the pathogenesis of inflammatory/immune-mediated neuropathies, GPR7 receptor expression, and pain transmission. (PMID:15607941)
Expressed in the zona glomerulosa and zona fasciculata-reticularis ( cells of the human adrenal cortex. (PMID:15797961)
methylation of the GPR7 is significantly associated with prostate cancer prognosis. (PMID:17437806)
A single nucleotide polymorphism of NPBWR1 changed the receptor function of this molecule at the cellular level, and, at the behavioral level, could influence personality difference in the context of social interaction. (PMID:22545105)
screening of GPR7 gene mutations among lean and obese subjects revealed a Tyr135Phe allelic variant that is fairly common in the study population. This variant is unlikely to cause a functional derangement of the receptor (PMID:23563248)
hypermethylation of HIST1H4F, PCDHGB6, NPBWR1, ALX1, and HOXA9 was significantly associated with shorter survival in stage 1 Non-small-cell lung cancer (PMID:24081945)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
mus_musculus	Npbwr1	ENSMUSG00000033774
rattus_norvegicus	Npbwr1	ENSRNOG00000071533
drosophila_melanogaster	Rh7	FBGN0036260
caenorhabditis_elegans	trhr-1	WBGENE00016265

Paralogs (17): OPRK1 (ENSG00000082556), OPRM1 (ENSG00000112038), KISS1R (ENSG00000116014), OPRD1 (ENSG00000116329), OPRL1 (ENSG00000125510), NPBWR2 (ENSG00000125522), SSTR4 (ENSG00000132671), SSTR1 (ENSG00000139874), SSTR5 (ENSG00000162009), GPR149 (ENSG00000174948), SSTR2 (ENSG00000180616), UTS2R (ENSG00000181408), PTGDR2 (ENSG00000183134), CMKLR2 (ENSG00000183671), LTB4R (ENSG00000213903), LTB4R2 (ENSG00000213906), SSTR3 (ENSG00000278195)

Protein

Protein identifiers

Neuropeptides B/W receptor type 1 — P48145 (reviewed: P48145)

Alternative names: G-protein coupled receptor 7

All UniProt accessions (2): P48145, H9NIL7

UniProt curated annotations — full annotation on UniProt →

Function. Interacts specifically with a number of opioid ligands. Receptor for neuropeptides B and W, which may be involved in neuroendocrine system regulation, food intake and the organization of other signals. Has a higher affinity for neuropeptide B.

Subcellular location. Cell membrane.

Tissue specificity. Found in cerebellum and frontal cortex. Detected at high levels in hippocampus, amygdala and trachea; at moderate levels in fetal brain, pituitary gland and prostate. Not in caudate, accumbens, kidney or liver. Also detected at high levels in lung carcinoma.

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

RefSeq proteins (1): NP_005276* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR009150	Neuropept_B/W_rcpt	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (24 total): topological domain 8, transmembrane region 7, glycosylation site 3, sequence variant 3, chain 1, disulfide bond 1, sequence conflict 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P48145-F1	83.74	0.52

Functional residue map

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

Disulfide bonds (1): 109–188

Glycosylation sites (3): 3, 13, 25

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: 30 (showing top): GOBP_CELL_CELL_SIGNALING, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, GOBP_SYNAPTIC_SIGNALING, GOMF_PEPTIDE_RECEPTOR_ACTIVITY, GOCC_NEURON_PROJECTION, ACEVEDO_METHYLATED_IN_LIVER_CANCER_DN, chr8q11, GOCC_SYNAPSE, REACTOME_CLASS_A_1_RHODOPSIN_LIKE_RECEPTORS, GOMF_TRANSMEMBRANE_SIGNALING_RECEPTOR_ACTIVITY, GOMF_G_PROTEIN_COUPLED_RECEPTOR_ACTIVITY, GOBP_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, GOBP_G_PROTEIN_COUPLED_OPIOID_RECEPTOR_SIGNALING_PATHWAY, GOMF_G_PROTEIN_COUPLED_OPIOID_RECEPTOR_ACTIVITY

GO Biological Process (5): G protein-coupled receptor signaling pathway (GO:0007186), neuropeptide signaling pathway (GO:0007218), chemical synaptic transmission (GO:0007268), signal transduction (GO:0007165), G protein-coupled opioid receptor signaling pathway (GO:0038003)

GO Molecular Function (5): G protein-coupled receptor activity (GO:0004930), G protein-coupled opioid receptor activity (GO:0004985), neuropeptide receptor activity (GO:0008188), neuropeptide binding (GO:0042923), protein binding (GO:0005515)

GO Cellular Component (4): plasma membrane (GO:0005886), membrane (GO:0016020), neuron projection (GO:0043005), synapse (GO:0045202)

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

Protein interactions and networks

STRING

628 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
NPBWR1	NPW	Q8N729	999
NPBWR1	NPB	Q8NG41	999
NPBWR1	MC4R	P32245	708
NPBWR1	PCDHGB6	Q9Y5F9	695
NPBWR1	ALX1	Q15699	580
NPBWR1	NPY	P01303	537
NPBWR1	EPHX3	Q9H6B9	504
NPBWR1	ESR1	P03372	412
NPBWR1	DRD2	P14416	381
NPBWR1	RXFP1	Q9HBX9	378
NPBWR1	HTR1D	P28221	376
NPBWR1	TMEM68	Q96MH6	373
NPBWR1	C4orf51	C9J302	370
NPBWR1	HOXA9	P31269	370
NPBWR1	PCDHGC5	Q9Y5F6	350

IntAct

4 interactions, top by confidence:

A	B	Type	Score
NPBWR1	UBQLN2	psi-mi:“MI:0915”(physical association)	0.560
UBQLN2	NPBWR1	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (4): UBQLN2 (Two-hybrid), NPW (Reconstituted Complex), NPB (Reconstituted Complex), SAFB2 (Cross-Linking-MS (XL-MS))

ESM2 similar proteins: A0A287A2K5, F1MV99, O08858, O42179, P28646, P30552, P30553, P30680, P30796, P30872, P30873, P30874, P30875, P30936, P30937, P30938, P31391, P32239, P32300, P32745, P33533, P33534, P33535, P34975, P34993, P34994, P35346, P35370, P35377, P41143, P41144, P41145, P41146, P42866, P46627, P47748, P48145, P48146, P49660, P49681

Diamond homologs: A0T2N3, A1ZAX0, E7F7V7, F1MV99, F1R332, O08726, O08858, O43603, O60755, O88626, O88853, O88854, O97666, P14600, P21109, P25024, P25025, P25103, P28646, P30547, P30548, P30680, P30731, P30872, P30873, P30874, P30875, P30937, P30938, P30974, P30975, P31391, P32300, P32303, P32745, P33396, P33533, P33534, P33535, P34975

SIGNOR signaling

3 interactions.

A	Effect	B	Mechanism
NPBWR1	“up-regulates activity”	GNAI1	binding
NPBWR1	“up-regulates activity”	GNAI3	binding
“Neuropeptide W-30”	“up-regulates activity”	NPBWR1	“chemical activation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	52
Likely benign	4
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

101 predictions. Top by Δscore:

Variant	Effect	Δscore
8:52939709:A:AG	acceptor_gain	0.9900
8:52939710:G:GG	acceptor_gain	0.9900
8:52939710:GCCCC:G	acceptor_gain	0.9800
8:52939710:GCC:G	acceptor_gain	0.9700
8:52939363:CCAG:C	donor_loss	0.9600
8:52939365:AG:A	donor_loss	0.9600
8:52939366:GGT:G	donor_loss	0.9600
8:52939367:GTAA:G	donor_loss	0.9600
8:52939368:T:G	donor_loss	0.9600
8:52939705:TTCCA:T	acceptor_loss	0.9600
8:52939706:TCCA:T	acceptor_loss	0.9600
8:52939708:CAGCC:C	acceptor_loss	0.9600
8:52939709:AGCCC:A	acceptor_loss	0.9600
8:52939710:GC:G	acceptor_gain	0.9600
8:52939362:GCCAG:G	donor_gain	0.9500
8:52939710:GCCC:G	acceptor_gain	0.9400
8:52939338:A:T	donor_gain	0.9200
8:52939698:T:G	acceptor_loss	0.9100
8:52939697:A:AG	acceptor_loss	0.8700
8:52939367:G:GG	donor_gain	0.8300
8:52939605:G:GT	donor_gain	0.7500
8:52939337:G:GT	donor_gain	0.7400
8:52939583:AGC:A	donor_gain	0.7400
8:52939472:G:GT	donor_gain	0.7200
8:52939490:G:T	donor_gain	0.6800
8:52939375:A:AG	donor_gain	0.6400
8:52939365:AGG:A	donor_gain	0.6200
8:52939366:GG:G	donor_gain	0.6100
8:52939367:G:C	donor_gain	0.6100
8:52939376:A:G	donor_gain	0.6100

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000264288 (8:52939117 A>G,T), RS1000487729 (8:52941677 C>T), RS1000614739 (8:52938846 G>C), RS1000792211 (8:52940343 C>G,T), RS1001387605 (8:52939442 C>A), RS1001740499 (8:52941010 G>A,C), RS1002580683 (8:52939700 C>A,T), RS1003180345 (8:52940639 C>G,T), RS1003482349 (8:52939456 G>A), RS1003817956 (8:52939656 A>C,G,T), RS1004732502 (8:52944053 G>A,C), RS1005080690 (8:52938415 A>G,T), RS1005564165 (8:52938222 A>G), RS1005583189 (8:52941329 T>A), RS1005703342 (8:52940978 G>A,C,T)

Disease associations

OMIM: gene MIM:600730 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

3 associations (top):

Study	Trait	p-value
GCST002541_65	Menarche (age at onset)	1.000000e-08
GCST007398_1	Mitochondrial DNA copy number (white blood cells)	2.000000e-06
GCST010002_299	Refractive error	7.000000e-25

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0004703	age at menarche
EFO:0006312	mitochondrial DNA measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL1293293 (SINGLE PROTEIN)

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Neuropeptide W/neuropeptide B receptors

Most potent curated ligand interactions (9 total), top 9:

Ligand	Action	Affinity	Parameter
neuropeptide W-30	Full agonist	10.6	pIC50
[¹²⁵I][Tyr¹¹]des-Br-NPB-23	Full agonist	10.4	pKd
neuropeptide W-23	Full agonist	10.0	pIC50
des-Br-neuropeptide B-29	Full agonist	9.5	pIC50
neuropeptide B-29	Full agonist	9.5	pIC50
Ava3	Full agonist	9.43	pKi
[¹²⁵I]NPW-23 (human)	Agonist	9.4	pKd
Ava5	Full agonist	9.0	pKi
des-Br-neuropeptide B-23	Full agonist	8.8	pIC50

Binding affinities (BindingDB)

7 measured of 7 human assays (11 total across all organisms); most potent 7 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
BREMAZOCINE(-)	KI	0.9 nM
Beta-Funeltrexamine	KI	93 nM
U50,488H	KI	100 nM
Tyr-Pro-Phe-Pro-NH2	KI	145 nM
CTOP	KI	1000 nM
NALTRINDOLE	KI	1230 nM
Beta-Endorphin (6-31)	KI	2400 nM

ChEMBL bioactivities

295 potent at pChembl≥5 of 359 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.57	EC50	2.7	nM	CHEMBL5187335
8.46	EC50	3.5	nM	CHEMBL5170622
8.38	IC50	4.2	nM	CHEMBL1940537
8.29	EC50	5.1	nM	CHEMBL5204006
8.26	EC50	5.5	nM	CHEMBL5197385
8.23	IC50	5.9	nM	CHEMBL1940539
8.22	IC50	6	nM	CHEMBL1940543
8.10	EC50	8	nM	CHEMBL5170622
8.10	EC50	8	nM	CHEMBL5187335
7.96	EC50	10.9	nM	CHEMBL5194519
7.96	EC50	11	nM	CHEMBL5178929
7.96	IC50	11	nM	CHEMBL1940539
7.89	EC50	13	nM	CHEMBL5172042
7.89	EC50	13	nM	CHEMBL5206425
7.85	EC50	14	nM	CHEMBL5177662
7.75	IC50	18	nM	CHEMBL1940542
7.70	EC50	20	nM	CHEMBL5188323
7.68	IC50	21	nM	CHEMBL1940536
7.66	EC50	22	nM	CHEMBL5191528
7.66	EC50	22	nM	CHEMBL5179908
7.64	EC50	23	nM	CHEMBL5204006
7.60	EC50	25	nM	CHEMBL5197385
7.52	IC50	30	nM	CHEMBL4757321
7.46	IC50	35	nM	CHEMBL1940538
7.41	IC50	39	nM	CHEMBL1940538
7.40	IC50	40	nM	CHEMBL1940537
7.39	EC50	41	nM	CHEMBL5208352
7.32	EC50	48	nM	CHEMBL5174290
7.28	IC50	53	nM	CHEMBL4796786
7.24	EC50	57	nM	CHEMBL5189212
7.23	EC50	59	nM	CHEMBL5195844
7.20	EC50	63	nM	CHEMBL5194208
7.16	IC50	70	nM	CHEMBL4779758
7.16	IC50	70	nM	CHEMBL1940543
7.15	IC50	71	nM	CHEMBL5196275
7.03	EC50	93	nM	CHEMBL5185639
7.02	IC50	95	nM	CHEMBL1940541
7.01	EC50	98	nM	CHEMBL5200286
7.00	IC50	100	nM	CHEMBL2314291
6.96	IC50	110	nM	CHEMBL1940536
6.95	EC50	112	nM	CHEMBL5191389
6.95	IC50	113	nM	CHEMBL5198182
6.92	IC50	120	nM	CHEMBL1972527
6.85	IC50	140	nM	CHEMBL2314320
6.80	IC50	160	nM	CHEMBL2207117
6.71	EC50	194	nM	CHEMBL5180015
6.71	IC50	197	nM	CHEMBL1940542
6.69	IC50	205	nM	CHEMBL4744579
6.68	IC50	210	nM	CHEMBL2207121
6.66	IC50	220	nM	CHEMBL2314323

PubChem BioAssay actives

212 with measured affinity, of 322 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)-6-amino-N-[5-[[5-[[5-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentyl]amino]-5-oxopentyl]amino]-5-oxopentyl]-2-[[(2S)-3-(4-hydroxyphenyl)-2-[[(2S)-3-(1H-indol-3-yl)-2-[3-(1H-indol-3-yl)propanoylamino]propanoyl]amino]propanoyl]amino]hexanamide	1901684: Agonist activity at human NPBWR1 expressed in CHO cells measured by LANCE Ultra cAMP kit-based TR-FRET assay	ec50	0.0027	uM
(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]hexanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-methylbutanoyl]amino]propanoyl]amino]-3-hydroxypropanoyl]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]pyrrolidine-2-carboxamide	1901684: Agonist activity at human NPBWR1 expressed in CHO cells measured by LANCE Ultra cAMP kit-based TR-FRET assay	ec50	0.0035	uM
[4-(1,3-benzoxazol-2-yl)piperazin-1-yl]-[(1S,2S,4R)-4-[[1-(4-methoxyphenyl)cyclobutyl]amino]-2-thiophen-3-ylcyclohexyl]methanone	640504: Displacement of [125]-hNPW23 from human NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ic50	0.0042	uM
(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-N-[5-[[5-[[5-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentyl]amino]-5-oxopentyl]amino]-5-oxopentyl]hexanamide	1901684: Agonist activity at human NPBWR1 expressed in CHO cells measured by LANCE Ultra cAMP kit-based TR-FRET assay	ec50	0.0051	uM
(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-N-[5-[[5-[[5-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentyl]amino]-5-oxopentyl]amino]-5-oxopentyl]hexanamide	1901684: Agonist activity at human NPBWR1 expressed in CHO cells measured by LANCE Ultra cAMP kit-based TR-FRET assay	ec50	0.0055	uM
[4-(1H-benzimidazol-2-yl)piperazin-1-yl]-[(1S,2S,4R)-4-[[1-(4-methoxyphenyl)cyclobutyl]amino]-2-thiophen-3-ylcyclohexyl]methanone	640504: Displacement of [125]-hNPW23 from human NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ic50	0.0059	uM
[(1S,2S,4R)-4-[[1-(4-methoxyphenyl)cyclobutyl]amino]-2-thiophen-3-ylcyclohexyl]-[4-(5-methyl-1,3-benzoxazol-2-yl)piperazin-1-yl]methanone	640504: Displacement of [125]-hNPW23 from human NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ic50	0.0060	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]hexanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-methylbutanoyl]amino]propanoyl]amino]-3-hydroxypropanoyl]pyrrolidine-2-carbonyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-3-methylbutanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]propanoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-3-(1H-indol-3-yl)propanoic acid	1901680: Agonist activity at human NPBWR1 expressed in CHO-RD-HGA16 cells measured by calcium mobilization assay	ec50	0.0109	uM
(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-N-[5-[[5-[[5-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentyl]amino]-5-oxopentyl]amino]-5-oxopentyl]hexanamide	1901680: Agonist activity at human NPBWR1 expressed in CHO-RD-HGA16 cells measured by calcium mobilization assay	ec50	0.0110	uM
(2S)-1-[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]hexanoyl]-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]pyrrolidine-2-carboxamide	1901680: Agonist activity at human NPBWR1 expressed in CHO-RD-HGA16 cells measured by calcium mobilization assay	ec50	0.0130	uM
(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-N-[5-[[5-[[5-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentyl]amino]-5-oxopentyl]amino]-5-oxopentyl]hexanamide	1901680: Agonist activity at human NPBWR1 expressed in CHO-RD-HGA16 cells measured by calcium mobilization assay	ec50	0.0130	uM
(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-N-[5-[[5-[[5-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentyl]amino]-5-oxopentyl]amino]-5-oxopentyl]hexanamide	1901680: Agonist activity at human NPBWR1 expressed in CHO-RD-HGA16 cells measured by calcium mobilization assay	ec50	0.0140	uM
[4-(5-bromo-1,3,4-thiadiazol-2-yl)piperazin-1-yl]-[(1S,2S,4R)-4-[[1-(4-methoxyphenyl)cyclobutyl]amino]-2-thiophen-3-ylcyclohexyl]methanone	640504: Displacement of [125]-hNPW23 from human NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ic50	0.0180	uM
(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-N-[5-[[5-[[5-[[2-[[(2S)-1-[[(2S)-1-[[1-[[2-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-2-methyl-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentyl]amino]-5-oxopentyl]amino]-5-oxopentyl]hexanamide	1901680: Agonist activity at human NPBWR1 expressed in CHO-RD-HGA16 cells measured by calcium mobilization assay	ec50	0.0200	uM
[4-(1,3-benzoxazol-2-yl)piperazin-1-yl]-[(1S,2S,4R)-4-[2-(4-methoxyphenyl)propan-2-ylamino]-2-thiophen-3-ylcyclohexyl]methanone	640504: Displacement of [125]-hNPW23 from human NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ic50	0.0210	uM
(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-N-[5-[[5-[[5-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentyl]amino]-5-oxopentyl]amino]-5-oxopentyl]hexanamide	1901680: Agonist activity at human NPBWR1 expressed in CHO-RD-HGA16 cells measured by calcium mobilization assay	ec50	0.0220	uM
(2S)-6-amino-N-[5-[[5-[[5-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentyl]amino]-5-oxopentyl]amino]-5-oxopentyl]-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]hexanamide	1901680: Agonist activity at human NPBWR1 expressed in CHO-RD-HGA16 cells measured by calcium mobilization assay	ec50	0.0220	uM
2-[2,6-dichloro-4-(1H-pyrazol-4-yl)phenyl]-6-(trifluoromethyl)-1H-benzimidazole	1696996: Antagonist activity at human NPBWR1 assessed as inhibition of agonist-induced cAMP accumulation by cAMP assay	ic50	0.0300	uM
[4-(1H-benzimidazol-2-yl)piperazin-1-yl]-[(1S,2S,4R)-4-[2-(4-methoxyphenyl)propan-2-ylamino]-2-thiophen-3-ylcyclohexyl]methanone	640504: Displacement of [125]-hNPW23 from human NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ic50	0.0350	uM
(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-N-[5-[[5-[[5-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S,3S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentyl]amino]-5-oxopentyl]amino]-5-oxopentyl]hexanamide	1901680: Agonist activity at human NPBWR1 expressed in CHO-RD-HGA16 cells measured by calcium mobilization assay	ec50	0.0410	uM
(2S)-6-amino-N-[5-[[5-[[5-[[2-[[(2S)-1-[[(2S)-1-[[2-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentyl]amino]-5-oxopentyl]amino]-5-oxopentyl]-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]hexanamide	1901680: Agonist activity at human NPBWR1 expressed in CHO-RD-HGA16 cells measured by calcium mobilization assay	ec50	0.0480	uM
5-[3,5-dichloro-4-[6-(trifluoromethyl)-1H-benzimidazol-2-yl]phenyl]pyridin-2-amine	1696996: Antagonist activity at human NPBWR1 assessed as inhibition of agonist-induced cAMP accumulation by cAMP assay	ic50	0.0530	uM
(2S)-6-amino-N-[2-[2-[2-[2-[2-[2-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethyl]-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]hexanamide	1901680: Agonist activity at human NPBWR1 expressed in CHO-RD-HGA16 cells measured by calcium mobilization assay	ec50	0.0570	uM
(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-N-[5-[[5-[[5-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentyl]amino]-5-oxopentyl]amino]-5-oxopentyl]hexanamide	1901680: Agonist activity at human NPBWR1 expressed in CHO-RD-HGA16 cells measured by calcium mobilization assay	ec50	0.0590	uM
(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-N-[5-[[5-[[5-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-3,3-dimethyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentyl]amino]-5-oxopentyl]amino]-5-oxopentyl]hexanamide	1901680: Agonist activity at human NPBWR1 expressed in CHO-RD-HGA16 cells measured by calcium mobilization assay	ec50	0.0630	uM
[4-[3,5-dichloro-4-[6-(trifluoromethyl)-1H-benzimidazol-2-yl]phenyl]phenyl]methanamine	1696996: Antagonist activity at human NPBWR1 assessed as inhibition of agonist-induced cAMP accumulation by cAMP assay	ic50	0.0700	uM
N-[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[5-[[5-[[5-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentyl]amino]-5-oxopentyl]amino]-5-oxopentyl]amino]-1-oxohexan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]hexadecanamide	1901683: Antagonist activity at human NPBWR1 expressed in CHO-RD-HGA16 cells measured by calcium mobilization assay	ic50	0.0710	uM
(2S)-6-amino-2-[[(2S)-2-[[(2R)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-N-[5-[[5-[[5-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentyl]amino]-5-oxopentyl]amino]-5-oxopentyl]hexanamide	1901680: Agonist activity at human NPBWR1 expressed in CHO-RD-HGA16 cells measured by calcium mobilization assay	ec50	0.0930	uM
[(1S,2S,4R)-4-[[1-(4-methoxyphenyl)cyclobutyl]amino]-2-thiophen-3-ylcyclohexyl]-[4-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]piperazin-1-yl]methanone	640504: Displacement of [125]-hNPW23 from human NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ic50	0.0950	uM
(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-6-amino-N-[5-[[5-[[5-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentyl]amino]-5-oxopentyl]amino]-5-oxopentyl]hexanamide	1901680: Agonist activity at human NPBWR1 expressed in CHO-RD-HGA16 cells measured by calcium mobilization assay	ec50	0.0980	uM
5-chloro-4-(4-ethoxyphenoxy)-2-(naphthalen-1-ylmethyl)pyridazin-3-one	724071: Antagonist activity against human NPBWR1 expressed in HEK293 cells co-expressing Gqi3 assessed as inhibition of agonist-induced response by FLIPR assay	ic50	0.1000	uM
(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-N-[5-[[5-[[5-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentyl]amino]-5-oxopentyl]amino]-5-oxopentyl]-6-[(2,2,2-trifluoroacetyl)amino]hexanamide	1901680: Agonist activity at human NPBWR1 expressed in CHO-RD-HGA16 cells measured by calcium mobilization assay	ec50	0.1120	uM
N-[(5S)-5-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-6-[[5-[[5-[[5-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentyl]amino]-5-oxopentyl]amino]-5-oxopentyl]amino]-6-oxohexyl]hexadecanamide	1901683: Antagonist activity at human NPBWR1 expressed in CHO-RD-HGA16 cells measured by calcium mobilization assay	ic50	0.1130	uM
5-chloro-2-(9H-fluoren-9-yl)-4-(4-methoxyphenoxy)pyridazin-3-one	724071: Antagonist activity against human NPBWR1 expressed in HEK293 cells co-expressing Gqi3 assessed as inhibition of agonist-induced response by FLIPR assay	ic50	0.1200	uM
5-chloro-4-(4-methoxyphenoxy)-2-(naphthalen-1-ylmethyl)pyridazin-3-one	724071: Antagonist activity against human NPBWR1 expressed in HEK293 cells co-expressing Gqi3 assessed as inhibition of agonist-induced response by FLIPR assay	ic50	0.1400	uM
5-chloro-4-(4-methoxyphenoxy)-2-naphthalen-2-ylpyridazin-3-one	719325: Antagonist activity at human NPBWR1 expressed in HEK293T cells co-expressing Galphaqi3 assessed as calcium release after 15 mins by FLIPR assay assay	ic50	0.1600	uM
(2R)-6-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-N-[5-[[5-[[5-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentyl]amino]-5-oxopentyl]amino]-5-oxopentyl]hexanamide	1901680: Agonist activity at human NPBWR1 expressed in CHO-RD-HGA16 cells measured by calcium mobilization assay	ec50	0.1940	uM
2-(2,4-dichloro-6-iodophenyl)-6-nitro-1H-benzimidazole	1696996: Antagonist activity at human NPBWR1 assessed as inhibition of agonist-induced cAMP accumulation by cAMP assay	ic50	0.2050	uM
5-chloro-2-(3,5-dimethylphenyl)-4-(4-ethoxyphenoxy)pyridazin-3-one	719325: Antagonist activity at human NPBWR1 expressed in HEK293T cells co-expressing Galphaqi3 assessed as calcium release after 15 mins by FLIPR assay assay	ic50	0.2100	uM
5-chloro-4-(4-methoxyphenoxy)-2-[(2-methylnaphthalen-1-yl)methyl]pyridazin-3-one	724071: Antagonist activity against human NPBWR1 expressed in HEK293 cells co-expressing Gqi3 assessed as inhibition of agonist-induced response by FLIPR assay	ic50	0.2200	uM
5-chloro-4-(4-methoxyphenoxy)-2-[(2-pyrazol-1-ylphenyl)methyl]pyridazin-3-one	724071: Antagonist activity against human NPBWR1 expressed in HEK293 cells co-expressing Gqi3 assessed as inhibition of agonist-induced response by FLIPR assay	ic50	0.2200	uM
(2S)-6-amino-N-[5-[[5-[[5-[[2-[[(2S)-1-[[2-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentyl]amino]-5-oxopentyl]amino]-5-oxopentyl]-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]hexanamide	1901680: Agonist activity at human NPBWR1 expressed in CHO-RD-HGA16 cells measured by calcium mobilization assay	ec50	0.2250	uM
5-chloro-2-(3-ethylphenyl)-4-(4-methoxyphenoxy)pyridazin-3-one	719325: Antagonist activity at human NPBWR1 expressed in HEK293T cells co-expressing Galphaqi3 assessed as calcium release after 15 mins by FLIPR assay assay	ic50	0.2300	uM
5-chloro-4-(4-ethylphenoxy)-2-(9H-fluoren-9-yl)pyridazin-3-one	724071: Antagonist activity against human NPBWR1 expressed in HEK293 cells co-expressing Gqi3 assessed as inhibition of agonist-induced response by FLIPR assay	ic50	0.2400	uM
5-chloro-2-[(2,6-dimethylphenyl)methyl]-4-(4-methoxyphenoxy)pyridazin-3-one	724071: Antagonist activity against human NPBWR1 expressed in HEK293 cells co-expressing Gqi3 assessed as inhibition of agonist-induced response by FLIPR assay	ic50	0.2400	uM
5-chloro-4-(4-ethoxyphenoxy)-2-(9H-fluoren-9-yl)pyridazin-3-one	724071: Antagonist activity against human NPBWR1 expressed in HEK293 cells co-expressing Gqi3 assessed as inhibition of agonist-induced response by FLIPR assay	ic50	0.2500	uM
5-chloro-4-(4-ethylphenoxy)-2-(naphthalen-1-ylmethyl)pyridazin-3-one	724071: Antagonist activity against human NPBWR1 expressed in HEK293 cells co-expressing Gqi3 assessed as inhibition of agonist-induced response by FLIPR assay	ic50	0.2500	uM
5-chloro-2-[(2-ethylphenyl)methyl]-4-(4-methoxyphenoxy)pyridazin-3-one	724071: Antagonist activity against human NPBWR1 expressed in HEK293 cells co-expressing Gqi3 assessed as inhibition of agonist-induced response by FLIPR assay	ic50	0.2600	uM
5-chloro-2-(3,5-dimethylphenyl)-4-(4-methoxyphenoxy)pyridazin-3-one	719325: Antagonist activity at human NPBWR1 expressed in HEK293T cells co-expressing Galphaqi3 assessed as calcium release after 15 mins by FLIPR assay assay	ic50	0.2700	uM
5-chloro-4-(4-methoxyphenoxy)-2-(4-propan-2-ylphenyl)pyridazin-3-one	719325: Antagonist activity at human NPBWR1 expressed in HEK293T cells co-expressing Galphaqi3 assessed as calcium release after 15 mins by FLIPR assay assay	ic50	0.2700	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
bisphenol A	affects cotreatment, increases methylation	1
quercitrin	increases expression	1
arsenite	increases methylation	1
ferrous chloride	decreases expression	1
S-(1,2-dichlorovinyl)cysteine	affects response to substance, increases expression	1
jinfukang	increases expression	1
Fulvestrant	affects cotreatment, increases methylation	1
Air Pollutants	increases abundance, increases expression	1
Atrazine	increases expression	1
Benzo(a)pyrene	increases methylation	1
Lipopolysaccharides	affects response to substance, increases expression	1
Valproic Acid	increases methylation	1
Particulate Matter	increases abundance, increases expression	1
Endocannabinoids	affects binding, decreases reaction, increases activity	1

ChEMBL screening assays

24 unique, capped per target: 18 functional, 6 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1613980	Functional	PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7). (Class of assay: confirmatory) [Related pubchem assays: 1952 (Screening assay	PubChem BioAssay data set
CHEMBL1942829	Binding	Displacement of [125]-hNPW23 from human NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	The discovery of potent antagonists of NPBWR1 (GPR7). — Bioorg Med Chem Lett

Cellosaurus cell lines

3 cell lines: 3 spontaneously immortalized cell line

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

Cellosaurus	Name	Category	Sex
CVCL_H474	CHO-K1/NPBW1/Galpha15	Spontaneously immortalized cell line	Female
CVCL_KV55	cAMP Hunter CHO-K1 NPBWR1 Gi	Spontaneously immortalized cell line	Female
CVCL_KY60	PathHunter CHO-K1 NPBWR1 beta-arrestin	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

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

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