GRPR

Summary

GRPR (gastrin releasing peptide receptor, HGNC:4609) is a protein-coding gene on chromosome Xp22.2, encoding Gastrin-releasing peptide receptor (P30550). Receptor for gastrin-releasing peptide (GRP).

Gastrin-releasing peptide (GRP) regulates numerous functions of the gastrointestinal and central nervous systems, including release of gastrointestinal hormones, smooth muscle cell contraction, and epithelial cell proliferation and is a potent mitogen for neoplastic tissues. The effects of GRP are mediated through the gastrin-releasing peptide receptor. This receptor is a glycosylated, 7-transmembrane G-protein coupled receptor that activates the phospholipase C signaling pathway. The receptor is aberrantly expressed in numerous cancers such as those of the lung, colon, and prostate. An individual with autism and multiple exostoses was found to have a balanced translocation between chromosome 8 and a chromosome X breakpoint located within the gastrin-releasing peptide receptor gene.

Source: NCBI Gene 2925 — RefSeq curated summary.

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 84 total — 1 pathogenic
• GTEx eGene: eQTL in 9 tissues, sQTL in 1 (q < 0.05)
• ChEMBL bioactivity: 1 clinical-phase molecule tested; no curated mechanism-of-action drug
• MANE Select transcript: NM_005314
• Notable: 84 clinical variants but no curated precision-oncology (CIViC) evidence yet

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:4609
Approved symbol	GRPR
Name	gastrin releasing peptide receptor
Location	Xp22.2
Locus type	gene with protein product
Status	Approved
Aliases	BB2, BB2R, BRS2
Ensembl gene	ENSG00000126010
Ensembl biotype	protein_coding
OMIM	305670
Entrez	2925

Gene structure

Transcript identifiers

Ensembl transcripts: 2 — 2 protein_coding

MANE Select: ENST00000380289

Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 1

ENST00000380289, ENST00001134327

RefSeq mRNA: 1 — MANE Select: NM_005314 NM_005314

CCDS: CCDS14174

Canonical transcript exons

ENST00000380289 — 3 exons

Exon	Start	End
ENSE00000893445	16150305	16150656
ENSE00001484475	16152256	16153518
ENSE00001484478	16123565	16124366

Expression profiles

Bgee: expression breadth broad, 86 present calls, max score 83.05.

FANTOM5 (CAGE): breadth broad, TPM avg 1.6967 / max 164.9504, expressed in 254 samples.

Highest expression (Bgee): primordial germ cell in gonad, male germ line stem cell (sensu Vertebrata) in testis, buccal mucosa cell, body of pancreas, pancreatic ductal cell.

Genetic regulation across tissues (GTEx eQTL / sQTL)

GRPR is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 9 tissues and its splicing (sQTL) in 1 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

10 significant tissue × QTL associations:

Tissue	QTL	q-value	Slope	Lead variant
Muscle Skeletal	eqtl	3.0e-11	+0.26	X:16121037:G:A
Cells Cultured fibroblasts	eqtl	2.5e-08	-0.24	X:16581710:A:G
Adipose Subcutaneous	eqtl	1.3e-04	+0.19	X:15860198:C:T
Pancreas	eqtl	6.2e-03	+0.12	X:16202128:TGTG:T
Thyroid	eqtl	1.1e-02	+0.99	X:15904654:G:T
Pancreas	sqtl	1.1e-02	-1.13	X:16124672:T:C
Colon Transverse	eqtl	2.0e-02	-0.26	X:15276521:G:T
Brain Frontal Cortex BA9	eqtl	3.0e-02	+0.40	X:15404987:C:G
Skin Sun Exposed Lower leg	eqtl	4.2e-02	+0.16	X:15871658:GCGCA:G
Nerve Tibial	eqtl	4.6e-02	+0.18	X:15862525:T:C

FANTOM5 promoters

4 alternative TSS:

Promoter ID	TPM avg	Samples expressed
195627	1.3287	225
195628	0.2811	92
195626	0.0665	30
195629	0.0204	10

Top tissues by expression

showing 100 of 249 tissues by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	83.05	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	82.67	gold quality
buccal mucosa cell	CL:0002336	79.06	silver quality
body of pancreas	UBERON:0001150	78.22	gold quality
pancreatic ductal cell	CL:0002079	75.48	silver quality
triceps brachii	UBERON:0001509	73.17	gold quality
ileal mucosa	UBERON:0000331	73.01	silver quality
gluteal muscle	UBERON:0002000	73.00	gold quality
diaphragm	UBERON:0001103	70.59	gold quality
stromal cell of endometrium	CL:0002255	70.51	gold quality
pancreas	UBERON:0001264	69.30	gold quality
deltoid	UBERON:0001476	67.93	silver quality
olfactory bulb	UBERON:0002264	67.79	gold quality
type B pancreatic cell	CL:0000169	67.51	gold quality
quadriceps femoris	UBERON:0001377	67.36	gold quality
mammary duct	UBERON:0001765	67.12	gold quality
endometrium epithelium	UBERON:0004811	66.82	gold quality
vastus lateralis	UBERON:0001379	66.06	gold quality
epithelium of mammary gland	UBERON:0003244	65.67	gold quality
esophagogastric junction muscularis propria	UBERON:0035841	65.20	gold quality
lower esophagus muscularis layer	UBERON:0035833	63.37	gold quality
lower esophagus	UBERON:0013473	63.08	gold quality
cranial nerve II	UBERON:0000941	62.05	silver quality
cerebellar vermis	UBERON:0004720	62.03	gold quality
colonic epithelium	UBERON:0000397	61.98	silver quality
tongue squamous epithelium	UBERON:0006919	61.71	gold quality
lower lobe of lung	UBERON:0008949	61.53	silver quality
CA1 field of hippocampus	UBERON:0003881	61.34	gold quality
vena cava	UBERON:0004087	61.17	gold quality
muscle tissue	UBERON:0002385	61.06	gold quality
mucosa of stomach	UBERON:0001199	61.00	gold quality
biceps brachii	UBERON:0001507	60.97	gold quality
heart right ventricle	UBERON:0002080	60.39	gold quality
smooth muscle tissue	UBERON:0001135	59.99	gold quality
skeletal muscle tissue of biceps brachii	UBERON:0004502	57.95	gold quality
mononuclear cell	CL:0000842	57.20	gold quality
nasal cavity epithelium	UBERON:0005384	57.15	gold quality
germinal epithelium of ovary	UBERON:0001304	56.98	gold quality
parotid gland	UBERON:0001831	56.93	gold quality
leukocyte	CL:0000738	56.86	gold quality
monocyte	CL:0000576	56.85	gold quality
decidua	UBERON:0002450	56.55	gold quality
myocardium	UBERON:0002349	56.42	gold quality
islet of Langerhans	UBERON:0000006	55.81	gold quality
jejunal mucosa	UBERON:0000399	55.66	gold quality
frontal pole	UBERON:0002795	55.60	gold quality
cardia of stomach	UBERON:0001162	55.42	gold quality
colonic mucosa	UBERON:0000317	54.98	gold quality
left ventricle myocardium	UBERON:0006566	54.94	gold quality
Brodmann (1909) area 46	UBERON:0006483	54.66	gold quality
trabecular bone tissue	UBERON:0002483	54.38	gold quality
skin of hip	UBERON:0001554	54.11	silver quality
cartilage tissue	UBERON:0002418	53.79	gold quality
mucosa of sigmoid colon	UBERON:0004993	53.19	gold quality
thoracic mammary gland	UBERON:0005200	53.11	gold quality
mammary gland	UBERON:0001911	52.94	gold quality
hair follicle	UBERON:0002073	52.90	gold quality
mucosa of paranasal sinus	UBERON:0005030	52.72	gold quality
entorhinal cortex	UBERON:0002728	52.71	gold quality
thymus	UBERON:0002370	52.06	gold quality
pigmented layer of retina	UBERON:0001782	52.02	gold quality
sigmoid colon	UBERON:0001159	51.82	gold quality
postcentral gyrus	UBERON:0002581	51.48	gold quality
muscle layer of sigmoid colon	UBERON:0035805	51.48	gold quality
bone marrow cell	CL:0002092	51.18	gold quality
endometrium	UBERON:0001295	51.13	gold quality
prefrontal cortex	UBERON:0000451	51.01	gold quality
jejunum	UBERON:0002115	50.98	gold quality
oocyte	CL:0000023	50.78	gold quality
lateral globus pallidus	UBERON:0002476	50.62	gold quality
tibia	UBERON:0000979	50.49	gold quality
muscle organ	UBERON:0001630	50.32	silver quality
middle frontal gyrus	UBERON:0002702	50.30	gold quality
paraflocculus	UBERON:0005351	50.18	gold quality
Brodmann (1909) area 10	UBERON:0013541	50.18	gold quality
epithelium of bronchus	UBERON:0002031	49.99	gold quality
parietal lobe	UBERON:0001872	49.74	gold quality
bronchus	UBERON:0002185	49.63	gold quality
blood vessel layer	UBERON:0004797	49.29	gold quality
cardiac muscle of right atrium	UBERON:0003379	49.28	gold quality
oviduct epithelium	UBERON:0004804	49.20	gold quality
cervix squamous epithelium	UBERON:0006922	49.20	gold quality
orbitofrontal cortex	UBERON:0004167	49.16	gold quality
caecum	UBERON:0001153	49.15	gold quality
cervix epithelium	UBERON:0004801	48.95	gold quality
lateral nuclear group of thalamus	UBERON:0002736	48.94	gold quality
choroid plexus epithelium	UBERON:0003911	48.89	gold quality
vermiform appendix	UBERON:0001154	48.85	gold quality
urinary bladder	UBERON:0001255	48.59	silver quality
colon	UBERON:0001155	48.44	gold quality
ventral tegmental area	UBERON:0002691	48.38	gold quality
ventricular zone	UBERON:0003053	48.29	silver quality
metanephric glomerulus	UBERON:0004736	48.29	gold quality
large intestine	UBERON:0000059	48.16	gold quality
bronchial epithelial cell	CL:0002328	48.12	gold quality
upper arm skin	UBERON:0004263	48.06	gold quality
renal glomerulus	UBERON:0000074	48.04	gold quality
nephron tubule	UBERON:0001231	48.00	gold quality
kidney epithelium	UBERON:0004819	47.92	gold quality
mucosa of urinary bladder	UBERON:0001259	47.80	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-GEOD-109979	no	175.93
E-ANND-3	no	2.82

HPA expression

RNA tissue specificity: Tissue enriched

showing 60 of 63 HPA tissues / cells by nTPM:

Tissue / cell	Axis	nTPM
Pancreas	tissue	19.1
Hippocampal formation	tissue	6.3
Hypothalamus	tissue	4.5
Thalamus	tissue	4.3
Prefrontal cortex	tissue	4.0
Cerebral cortex	tissue	4.0
Pons	tissue	3.8
Motor cortex	tissue	3.8
Superior colliculi	tissue	3.3
Retrosplenial and cingulate cortex	tissue	3.3
Retrosplenial cortex	tissue	3.3
Entorhinal cortex	tissue	3.0
Somatosensory cortex	tissue	2.9
Amygdala	tissue	2.8
Temporal cortex	tissue	2.8
Occipital cortex	tissue	2.8
Insular cortex	tissue	2.8
Medulla oblongata	tissue	2.7
Substantia nigra	tissue	2.6
Septum	tissue	2.6
Spinal cord	tissue	2.4
Cerebellum	tissue	2.3
Locus coeruleus	tissue	2.0
Corpus callosum	tissue	2.0
Ventral forebrain	tissue	1.9
Epididymis	tissue	1.8
Breast	tissue	1.7
Midbrain	tissue	1.7
Hippocampus	tissue	1.7
Periaqueductal gray	tissue	1.7
Olfactory bulb	tissue	1.5
Basal ganglia	tissue	1.4
Postcentral gyrus	tissue	1.3
Stomach 1	tissue	1.1
Choroid plexus	tissue	1.0
Putamen	tissue	0.9
Smooth muscle	tissue	0.7
Endometrium 1	tissue	0.5
Frontal cortex	tissue	0.5
Nucleus accumbens	tissue	0.5
Prostate	tissue	0.5
Cervix	tissue	0.3
Rectum	tissue	0.3
Caudate putamen	tissue	0.3
Heart muscle	tissue	0.2
Parathyroid gland	tissue	0.2
Skeletal muscle	tissue	0.2
Tongue	tissue	0.2
Appendix	tissue	0.2
Retina	tissue	0.1
Seminal vesicle	tissue	0.1
Adipose tissue	tissue	0.1
Colon	tissue	0.1
Urinary bladder	tissue	0.1
Placenta	tissue	0.1
Thyroid gland	tissue	0.1
Lung	tissue	0.1
Spleen	tissue	0.1
Small intestine	tissue	0.1
Gallbladder	tissue	0.1

Brain sub-regions (HPA Brain Atlas): detected in 188; highest nTPM — Ventral hippocampus (6.3), Mammillary body (4.6), Supraoptic nucleus (4.6), Dorsal hippocampus (3.8), Cervical spinal cord, dorsal horn (3.6).

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): CREB1, ETS1, ZNF699

miRNA regulators (miRDB)

Targeting GRPR by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).

showing 30 of 47 miRNAs:

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-574-5P	100.00	66.01	989
HSA-MIR-513B-5P	99.99	69.96	2150
HSA-MIR-335-3P	99.93	73.36	4958
HSA-MIR-497-5P	99.92	71.83	2674
HSA-MIR-1297	99.91	73.41	3162
HSA-MIR-8063	99.91	69.76	3146
HSA-MIR-15A-5P	99.90	72.80	2787
HSA-MIR-15B-5P	99.90	72.78	2798
HSA-MIR-16-5P	99.90	72.80	2780
HSA-MIR-195-5P	99.90	72.81	2805
HSA-MIR-424-5P	99.89	71.90	2641
HSA-MIR-6838-5P	99.89	71.94	2690
HSA-MIR-5003-3P	99.85	69.29	2517
HSA-MIR-4495	99.82	72.08	3080
HSA-MIR-4659A-3P	99.80	72.62	4248
HSA-MIR-4659B-3P	99.80	72.62	4248
HSA-MIR-204-5P	99.79	71.62	2439
HSA-MIR-211-5P	99.79	71.65	2440
HSA-MIR-26B-5P	99.78	73.51	2305
HSA-MIR-26A-5P	99.78	73.52	2303
HSA-MIR-6885-3P	99.75	70.36	3187
HSA-MIR-1179	99.71	68.70	1040
HSA-MIR-4465	99.71	72.56	2096
HSA-MIR-5003-5P	99.61	69.13	1624
HSA-MIR-7159-3P	99.51	70.17	1920
HSA-MIR-203A-3P	99.49	70.56	2806
HSA-MIR-223-5P	99.24	68.82	1206
HSA-MIR-3973	99.20	69.19	1990
HSA-MIR-10399-5P	99.17	69.87	2610
HSA-MIR-6504-3P	99.17	69.31	2891

Functional genomics

Regional missense constraint (gnomAD)

ENST00000380289 splits into 3 regions with different missense tolerance; 0 are missense-constrained. Missense variants in a constrained region (low observed/expected) are more likely to be pathogenic. gnomAD

Region (GRCh38)	Missense obs / exp	o/e	Constrained
X:16,123,954–16,150,375	115 / 128.8	0.89	no
X:16,150,376–16,150,577	22 / 51.9	0.42	no
X:16,150,578–16,152,642	133 / 123.4	1.08	no

Literature-anchored findings (GeneRIF, showing 40)

• GRP/GRP-R play a transient and non-critical role in intestinal development (PMID:11960700)
• hGRP-R activation stimulated sustained cyclic AMP response element binding protein (CREB) phosphorylation and transactivation in duodenal cancer cells through a protein kinase C and partially p38 mitogen-activated protein kinase-dependent pathway. (PMID:12220644)
• Bombesin-dependent activation (through GRP receptor) of the transcription factor Elk-1 and significant increase of cell proliferation in prostate cancer cell lines (PMID:12409226)
• mRNA transcripts are expressed in tumor cells of patients with small cell lung cancer (PMID:12474049)
• accumulation of mutations within the GRPR gene allows for the dedifferentiation of tumor cells within any particular colon cancer; poorly-differentiated tumor cells within any individual cancer may arise clonally from better-differentiated precursors (PMID:12720295)
• Increased gastrin-releasing peptide (GRP) receptor expression in small cell lung cancer cells confers sensitivity to [Arg6,D-Trp7,9,NmePhe8]-substance P (6-11)-induced growth inhibition (PMID:12771999)
• The expression of GRP-R in uterine tissue during specific phases of the cycle suggests a timely precise physiological action of GRP in these targets; in certain uterine neoplasms, the GRP-R overexpression may contribute to tumor development (PMID:15941862)
• Gastrin-releasing peptide receptor mediates activation of the epidermal growth factor receptor in lung cancer cells (PMID:15967120)
• GRP appears to rescue NSCLC cells exposed to gefitinib through release of amphiregulin and activation of the Akt pathway, suggesting GRPR and/or EGFR autocrine pathways in NSCLC cells may modulate therapeutic response to EGFR inhibitors. (PMID:17349623)
• The large amounts of GRP-receptors in ovarian tumor vessels suggest a role in tumoral vasculature and possibly angiogenesis. (PMID:17726264)
• There is a potential role of C6S and L181F mutations on GRPR function, and possibly in the pathogenesis of the autistic disorders. (PMID:18393381)
• genes encoding corticotropin releasing hormone receptor 1, tachykinin receptor 1, gastrin releasing peptide, and gastrin releasing peptide receptor were selected as candidates for PD based on their biology (PMID:18452185)
• CREB is a critical regulator of human GRP-R expression in gastrointestinal cancer and might be activated through different upstream intracellular pathways (PMID:18483184)
• Widespread GRPR expression in human cervical cancer. (PMID:18497507)
• These findings demonstrate that GRP and GRP-R have important oncogenic properties beyond their established mitogenic functions. (PMID:18753628)
• Gastrin-releasing peptide receptor is expressed in the vast majority of lymph node metastases and in 52.9% of bone metastases of prostate cancer. (PMID:19343734)
• High expression of gastrin-releasing peptide receptors is associated with the vascular bed of urinary tract cancers. (PMID:19478282)
• In MDA-MB-231 breast cancer cells, GRP-R and EGF-R synergize to regulate cell migration and IL-8 expression, but not cell proliferation. (PMID:19631337)
• The results suggest that brain-derived neurotrophic factor/TrkB and cAMP phosphodiesterase-4, but not the gastrin-releasing peptide receptor, regulate the viability of medulloblastoma cells. (PMID:19642024)
• This study is the first to confirm the presence of gastrin-releasing peptide receptor in human glioma specimens and normal human neurons. (PMID:20211708)
• GRP promotes the growth of HepG2 cells through interaction with GRPR co-expressed in tumor cells, and subsequently activates MAPK/ERK1/2 via EGFR-independent mechanisms. (PMID:20596631)
• Concomitant vascular GRP-receptor and VEGF-receptor expression in human tumors provides molecular basis for dual targeting of tumoral vasculature. (PMID:21605611)
• High GRPR is associated with prostate carcinoma. (PMID:22248281)
• Bronchial gastrin-releasing peptide receptor expression was significantly associated with lung cancer in a multivariable logistic regression model adjusted for age, sex, smoking status and pulmonary function. Lung cancer risk was not modified by sex. (PMID:22296774)
• Tonic stretch of human myometrium increases contractility and stimulates the expression of a known smooth muscle stimulatory agonist, GRP. GRP receptor antagonists attenuate the effect of stretch. (PMID:22411014)
• Elevated buccal GRPR espression was significantly associated with squamous cell carcinoma of the head and neck. (PMID:22431275)
• These findings highlight the role of GRPR signaling in sepsis outcome. (PMID:22735756)
• Protein kinase C is critically responsible for rapid VEGF secretion by gastrin-releasing peptide receptor signaling in neuroblastoma cells (PMID:23155231)
• integrin ss1 subunit critically regulates GRP-R-mediated neuroblastoma cell migration and invasion (PMID:23889963)
• GRPR is highly expressed in epidermoid carcinoma of the anal canal, suggesting this receptor might have a role in anal carcinogenesis. (PMID:23958544)
• GRPR expression was more pronounced in an advanced-stage lung cancer (PMID:24377816)
• BBS caused a significant increase in Shh gene transcription and protein secretion that was dependent on BBS-induced GPCR/Galphaq-//Rho mediated activation of nuclear factor kappaB (NFkappaB), which can stimulate a NF-kappaB response element in the Shh gene promoter (PMID:24747971)
• No association of 16 GRP and 7 GRPR variants were found with agoraphobia with/without panic disorder. (PMID:24912045)
• a key mechanism for GRPR-regulated colon cancer cell migration through the Galpha13-PRG-RhoA-ROCK pathway. (PMID:24958816)
• GRP-R regulates glucose metabolism in neuroblastoma by modulating HIF-1alpha, PDK4 and PDP2. (PMID:25630799)
• GRP/GRP-R signaling activation contributes to castration-resistant prostate cancer progression (PMID:27542219)
• Expression of Gastrin-Releasing Peptide Receptor in Breast Cancer and Its Association with Pathologic, Biologic, and Clinical Parameters (PMID:28280221)
• Our results suggest that, similar to what happens in neutrophils, gastrin-releasing peptide is a migratory, rather than a proliferative, stimulus, for non-small cell lung carcinoma cells, indicating a putative role for gastrin-releasing peptide and gastrin-releasing peptide receptor in metastasis (PMID:28351312)
• Novel Gastrin-Releasing Peptide Receptor Targeted Near-Infrared Fluorescence Dye for Image-Guided Surgery of Prostate Cancer. (PMID:31025163)
• Microglia-neuron interactions promote chronic itch via the NLRP3-IL-1beta-GRPR axis. (PMID:36876522)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	grpr	ENSDARG00000056620
mus_musculus	Grpr	ENSMUSG00000031364
rattus_norvegicus	Grpr	ENSRNOG00000004124
drosophila_melanogaster	CCHa2-R	FBGN0033058
drosophila_melanogaster	CCHa1-R	FBGN0050106

Paralogs (15): NTSR1 (ENSG00000101188), BRS3 (ENSG00000102239), MLNR (ENSG00000102539), GHSR (ENSG00000121853), NMUR2 (ENSG00000132911), NMBR (ENSG00000135577), EDNRB (ENSG00000136160), EDNRA (ENSG00000151617), NTSR2 (ENSG00000169006), GPR37L1 (ENSG00000170075), GPR37 (ENSG00000170775), NMUR1 (ENSG00000171596), GPR148 (ENSG00000173302), TRHR (ENSG00000174417), GPR39 (ENSG00000183840)

Mouse-model phenotypes

Observed phenotypes of the mouse ortholog (MGI:95836) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 4 distinct phenotype terms.

Mouse phenotype (MP)	Records
abnormal social investigation	1
abnormal response/metabolism to endogenous compounds	1
abnormal food intake	1
increased locomotor activity	1

Additional cross-species homologs

Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.

Organism	UniProt	Identity	Method
Pan troglodytes	Q5IS62	100.0%	Diamond
Bos taurus	P21450	99.1%	Diamond
Ovis aries	Q95L55	99.1%	Diamond
Macaca mulatta	Q9GK74	99.0%	Diamond
Macaca fascicularis	Q28468	98.0%	Diamond
Canis lupus familiaris	P56497	97.3%	Diamond
Sus scrofa	Q29010	95.8%	Diamond
Equus caballus	O62709	94.9%	Diamond
Cambarellus shufeldtii	O16018	94.0%	Diamond
Cavia porcellus	Q9Z2D5	93.8%	Diamond
Alloteuthis subulata	Q17094	93.5%	Diamond
Coturnix japonica	Q90328	93.4%	Diamond
Oryctolagus cuniculus	Q9N0W7	91.9%	Diamond
Bombina orientalis	P47751	68.5%	Diamond
Caenorhabditis elegans	O02300	45.9%	Diamond
Mizuhopecten yessoensis	O15974	38.5%	Diamond

Genomic neighbors (locus context)

Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).

Symbol	Type	Entrez
MAGEB17-AS1	ncRNA	128966703
MAGEB17	protein-coding	645864
AP1S2	protein-coding	8905
ZRSR2	protein-coding	8233

Protein

Protein identifiers

Gastrin-releasing peptide receptor — P30550 (reviewed: P30550)

Alternative names: GRP-preferring bombesin receptor

All UniProt accessions (2): P30550, X5D7H2

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for gastrin-releasing peptide (GRP). Signals via association with G proteins that activate a phosphatidylinositol-calcium second messenger system, resulting in Akt phosphorylation. Contributes to the regulation of food intake. Contributes to the perception of prurient stimuli and transmission of itch signals in the spinal cord that promote scratching behavior, but does not play a role in the perception of pain. Contributes primarily to nonhistaminergic itch sensation. In one study, shown to act in the amygdala as part of an inhibitory network which inhibits memory specifically related to learned fear. In another study, shown to contribute to disinhibition of glutamatergic cells in the auditory cortex via signaling on vasoactive intestinal peptide-expressing cells which leads to enhanced auditory fear memories. Contributes to the induction of sighing through signaling in the pre-Botzinger complex, a cluster of several thousand neurons in the ventrolateral medulla responsible for inspiration during respiratory activity.

Subcellular location. Cell membrane.

Tissue specificity. Highly expressed in pancreas. Also expressed in stomach, adrenal cortex and brain. In brain, expressed in cells throughout the cortex.

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

RefSeq proteins (1): NP_005305* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR001556	Bombsn_rcpt-like	Family
IPR001966	Gastrin_pep_rcpt	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (39 total): helix 13, topological domain 8, transmembrane region 7, strand 5, chain 1, modified residue 1, lipid moiety-binding region 1, glycosylation site 1, disulfide bond 1, turn 1

Structure

Experimental structures (PDB)

4 structures by resolution:

PDB	Title	Method	Resolution (Å)
7W41	Crystal Structure of Human Gastrin Releasing Peptide Receptor in complex with the …	X-RAY DIFFRACTION	2.95
7W3Z	Cryo-EM Structure of Human Gastrin Releasing Peptide Receptor in complex with the agonist …	ELECTRON MICROSCOPY	3
7W40	Cryo-EM Structure of Human Gastrin Releasing Peptide Receptor in complex with the agonist …	ELECTRON MICROSCOPY	3
8H0Q	Structure of the GRP14-27-GRPR-Gq complex	ELECTRON MICROSCOPY	3.3

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P30550-F1	78.78	0.52

Antibody-complex structures (SAbDab)

3 antibodies co-crystallized with this protein: 7W3Z, 7W40, 8H0Q

Human Protein Atlas

Protein class: G-protein coupled receptors, GPCRs excl olfactory receptors, Predicted membrane proteins, GPCRHMM predicted membrane proteins, UniProt - Evidence at transcript level

Protein evidence: Evidence at protein level

Subcellular location (HPA, imaging): plasma membrane

Antibody reliability (HPA): IF supported

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 (2)

Type	Positions
Phosphoserine	350
S-palmitoyl cysteine	339

Disulfide bonds (1)

Type	Positions
Disulfide bond	113–196

Glycosylation sites (1)

Type	Positions
N-linked (glcnac…) asparagine	20

Function

Pathways and Gene Ontology

Reactome pathways

2 curated (TAS) of 7; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

7 pathways:

ID	Pathway	Evidence
R-HSA-416476	G alpha (q) signalling events	curated
R-HSA-375276	Peptide ligand-binding receptors	curated
R-HSA-373076	Class A/1 (Rhodopsin-like receptors)	—
R-HSA-388396	GPCR downstream signalling	—
R-HSA-500792	GPCR ligand binding	—
R-HSA-162582	Signal Transduction	—
R-HSA-372790	Signaling by GPCR	—

MSigDB gene sets: 127 (showing top): GOBP_RESPIRATORY_GASEOUS_EXCHANGE_BY_RESPIRATORY_SYSTEM, GOBP_COGNITION, GOBP_BEHAVIOR, MODULE_64, GOBP_POSITIVE_REGULATION_OF_BEHAVIOR, LHX3_01, CAGCTG_AP4_Q5, GOBP_MULTICELLULAR_ORGANISMAL_RESPONSE_TO_STRESS, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, CCANNAGRKGGC_UNKNOWN, GOBP_REGULATION_OF_BEHAVIOR, GOBP_FEAR_RESPONSE, GOBP_BIOLOGICAL_PROCESS_INVOLVED_IN_INTRASPECIES_INTERACTION_BETWEEN_ORGANISMS, GOBP_REGULATION_OF_RESPONSE_TO_STRESS, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION

GO Biological Process (11): G protein-coupled receptor signaling pathway (GO:0007186), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), learning or memory (GO:0007611), social behavior (GO:0035176), psychomotor behavior (GO:0036343), response to external biotic stimulus (GO:0043207), motor behavior (GO:0061744), positive regulation of respiratory gaseous exchange (GO:1903942), positive regulation of behavioral fear response (GO:2000987), signal transduction (GO:0007165), neuropeptide signaling pathway (GO:0007218)

GO Molecular Function (5): neuropeptide receptor activity (GO:0008188), G protein-coupled peptide receptor activity (GO:0008528), neuropeptide binding (GO:0042923), G protein-coupled receptor activity (GO:0004930), protein binding (GO:0005515)

GO Cellular Component (2): plasma membrane (GO:0005886), membrane (GO:0016020)

Reactome top-level categories

5 top-level categories:

Category	Pathways
Signaling by GPCR	2
Class A/1 (Rhodopsin-like receptors)	1
GPCR downstream signalling	1
Signal Transduction	1
GPCR ligand binding	1

GO top-level categories

33 GO namespaces:

Category	Terms
G protein-coupled receptor signaling pathway	3
behavior	3
G protein-coupled receptor activity	2
signal transduction	1
phospholipase C activator activity	1
cognition	1
biological process involved in intraspecies interaction between organisms	1
motor behavior	1
response to external stimulus	1
response to biotic stimulus	1
respiratory gaseous exchange by respiratory system	1
regulation of respiratory gaseous exchange	1
positive regulation of multicellular organismal process	1
behavioral fear response	1
positive regulation of defense response	1
positive regulation of behavior	1
positive regulation of fear response	1
regulation of behavioral fear response	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
neuropeptide signaling pathway	1
G protein-coupled peptide receptor activity	1
neuropeptide binding	1
peptide receptor activity	1
peptide binding	1
transmembrane signaling receptor activity	1
binding	1
membrane	1
cell periphery	1
cellular anatomical structure	1

Experimentally-supported GO annotations

GO terms backed by direct experimental evidence (ECO experimental codes) — 2 of 18 annotations. The rest are phylogenetic / computational / electronic (IEA).

2 experimentally-supported GO terms:

GO term	NS	Evidence
plasma membrane	CC	direct assay
G protein-coupled peptide receptor activity	MF	direct assay

Protein interactions and networks

STRING

showing 15 of 808 interactions by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
GRPR	GRP	P07491	978
GRPR	NMB	P08949	817
GRPR	FOLH1	Q04609	719
GRPR	GLRA2	P23416	666
GRPR	GAST	P01350	655
GRPR	NTNG2	Q96CW9	650
GRPR	NTNG1	Q9Y2I2	646
GRPR	GPM6B	Q13491	630
GRPR	SDC2	P34741	602
GRPR	SST	P01166	599
GRPR	TRPV1	Q8NER1	597
GRPR	PROCA1	Q8NCQ7	587
GRPR	NPPB	P16860	584
GRPR	NTS	P30990	567
GRPR	BHLHE22	Q8NFJ8	566

IntAct

Human interaction partners of GRPR in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).

3 partners by confidence:

Partner	Interaction type	MIscore	Records
RAMP3	physical association	0.400	2
RAMP2	physical association	0.400	1
GPR89A	association	0.350	2

BioGRID (101 interactions; top human partners by supporting records): ABCB6 (Affinity Capture-MS; 2 records), ACVR2B (Affinity Capture-MS; 2 records), ADCK1 (Affinity Capture-MS; 2 records), ARF5 (Affinity Capture-MS; 2 records), ARL8B (Affinity Capture-MS; 2 records), ARV1 (Affinity Capture-MS; 2 records), ASPHD2 (Affinity Capture-MS; 2 records), ATL3 (Affinity Capture-MS; 2 records), ATP12A (Affinity Capture-MS; 2 records), ATP7B (Affinity Capture-MS; 2 records), BTAF1 (Affinity Capture-MS; 2 records), CBWD3 (Affinity Capture-MS; 2 records), CDC42BPB (Affinity Capture-MS; 2 records), CDS1 (Affinity Capture-MS; 2 records), DHRS7 (Affinity Capture-MS; 2 records)

SIGNOR signaling

12 signaling interactions:

A	Effect	B	Mechanism
GRP	up-regulates	GRPR	binding
GRPR	up-regulates	GNAQ	binding
GRPR	up-regulates	PLA2G1B	binding
GRPR	“up-regulates activity”	GNAS	binding
GRPR	“up-regulates activity”	GNAL	binding
GRPR	“up-regulates activity”	GNAI1	binding
GRPR	“up-regulates activity”	GNAI3	binding
GRPR	“up-regulates activity”	GNAO1	binding
GRPR	“up-regulates activity”	GNAZ	binding
GRPR	“up-regulates activity”	GNAQ	binding
GRPR	“up-regulates activity”	GNA14	binding
Bombesin	“up-regulates activity”	GRPR	“chemical activation”

Ligand–receptor pairs (CellPhoneDB) (2)

Curated ligand–receptor partners (cell-cell communication), distinct from the protein–protein interactions above.

2 ligand–receptor pairs:

Partner	This gene’s role	Signaling class
GRP	receptor	Signaling by Gastrin
NMB	receptor	Signaling by Neuromedin

Disease & clinical

Genetic variants

Variant evidence for GRPR: 84 ClinVar records (1 pathogenic / likely pathogenic); 1 GWAS association. Per-variant detail is on Sugi Variant.

ClinVar

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

Classification	Count (floor)
Pathogenic	1
Likely pathogenic	0
Uncertain significance	39
Likely benign	13
Benign	4

Top pathogenic / likely-pathogenic (1)

Showing all 1 pathogenic / likely-pathogenic ClinVar records, ranked by ClinVar review status (expert panel → multiple submitters → single submitter), then by number of submitting labs.

Variant ID	HGVS	Classification	Review	Submitters
816245	GRCh37/hg19 Xp22.33-22.13(chrX:168546-17502124)x1	Pathogenic	no assertion criteria provided	1

Per-variant reference — Sugi Variant

Explore GRPR’s pathogenic and likely-pathogenic variants individually — each with its ClinVar classification and conditions, applied ACMG criteria (ClinGen expert panel, where curated), the calibrated in-silico predictors (AlphaMissense, REVEL, SaProt, conservation), gnomAD frequency, and the predictor-disagreement QC signal — on Sugi Variant.

SpliceAI

Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 25 predictions of 233):

Position(s)	Effect	Δscore	Sites
X:16150451	donor_gain	1.0000
X:16152254	acceptor_loss	1.0000	2
X:16150657–16150658	donor_loss	0.9900	5
X:16152239	acceptor_gain	0.9900
X:16152255	acceptor_loss	0.9900
X:16150303–16150304	acceptor_loss	0.9800	6
X:16152254–16152255	acceptor_loss	0.9800	2
X:16124367–16124368	donor_loss	0.9700	5
X:16133284	donor_gain	0.9500
X:16150297	acceptor_gain	0.9400

AlphaMissense

944 missense substitutions predicted likely pathogenic (of 2,544 scored), across 234 residues. Top 20 hotspot residues, ranked by the number of likely-pathogenic substitutions (of those reachable by a single-nucleotide change), then by mean score:

Residue	Likely-pathogenic substitutions	Mean am_pathogenicity	Max am_pathogenicity
D86	8	0.997	0.999
N58	8	0.995	0.999
F273	8	0.987	0.999
N318	8	0.977	0.996
D97	8	0.958	0.985
F329	8	0.933	0.997
D137	8	0.917	0.967
H281	8	0.912	0.985
F129	8	0.903	0.973
F269	8	0.894	0.966
S326	8	0.886	0.989
F215	8	0.842	0.937
C113	7	0.996	0.999
C196	7	0.995	0.998
W106	7	0.990	0.998
W277	7	0.981	0.997
F108	7	0.973	0.982
F312	7	0.971	0.994
W165	7	0.969	0.999
N314	7	0.942	0.996

HPA cancer prognostics

RNA cancer specificity: Cancer enriched (Breast Invasive Carcinoma)

Disease associations

OMIM: gene MIM:305670 | disease phenotypes:

GWAS associations

1 associations:

Study	Trait	p-value
GCST008481_11	Lung function (FEV1/FVC)	4e-8

EFO canonical traits (from GWAS)

1 canonical traits:

EFO ID	Trait name
EFO:0004713	FEV/FVC ratio

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL4524010 (PROTEIN FAMILY), CHEMBL4959 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 3,460 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

1 molecules by phase:

Molecule	Name	Phase	Patents
CHEMBL437027	BOMBESIN	1	3,460

PharmGKB: 1 entry (CPIC guideline: no)

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Bombesin receptors

Most potent curated ligand interactions (40 total), top 25:

Ligand	Action	Affinity	Parameter
[D-Phe6,β-Ala11,Phe13,Nle14]bombesin-(6-14)	Full agonist	10.32	pIC50
bombesin	Agonist	10.15	pIC50
gastrin-releasing peptide	Full agonist	9.96	pIC50
neuromedin C	Full agonist	9.85	pIC50
gastrin releasing peptide(14-27) (human)	Full agonist	9.77	pIC50
[D-Tyr6,β-Ala11,N-Me-Ala13,Nle14]bombesin-(6-14)	Agonist	9.5	pKi
[D-Phe6]bombesin(6-13)propylamide	Antagonist	9.41	pIC50
JMV641	Antagonist	9.34	pIC50
[125I][D-Tyr6]bombesin-(6-13)-methyl ester	Antagonist	9.28	pKd
litorin	Agonist	9.27	pIC50
(D-Ala11]bombesin	Full agonist	9.27	pIC50
[(3-Ph-Pr6), His7,D-Ala11,D-Pro13,ψ13-14),Phe14]bombesin-(6-14)	Antagonist	9.2	pIC50
[D-Phe6, Leu13, Cpa14,ψ13-14]bombesin-(6-14)	Antagonist	8.91	pIC50
JMV594	Antagonist	8.9	pIC50
[Leu14]bombesin	Agonist	8.88	pIC50
[D-Tpi6, Leu13 ψ(CH2NH)-Leu14]bombesin-(6-14)	Antagonist	8.88	pIC50
[Phe13]bombesin	Full agonist	8.74	pKi
Ac-GRP-(20-26)-methylester	Antagonist	8.7	pIC50
ranatensin	Full agonist	8.65	pIC50
BAY86-7548	Antagonist	8.6	pIC50
[125I][Tyr4]bombesin	Full agonist	8.2	pKd
[Leu14, ψ 13-14)]bombesin	Antagonist	8.11	pIC50
[D-Phe6, Stat13, Leu14]Bn(6-14)	Antagonist	8.1	pIC50
neuromedin B (1-30) (human)	Full agonist	7.82	pIC50
neuromedin B	Full agonist	7.52	pIC50

Binding affinities (BindingDB)

62 measured of 89 human assays (89 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
Compound GRP	KI	0.04 nM
CHEMBL272335	EC50	0.373 nM
(2S)-N1-((5S,8S,11S,17S,20S,23S,26S,29S,35S,38S)-11-((1H-imidazol-5-yl)methyl)-23-((1H-indol-3-yl)methyl)-43-amino-29-(2-amino-2-oxoethyl)-26-(3-amino-3-oxopropyl)-5-carbamoyl-43-imino-8,35-diisobutyl-17-isopropyl-20-methyl-7,10,13,16,19,22,25,28,31,34,37-undecaoxo-2-thia-6,9,12,15,18,21,24,27,30,33,36,42-dodecaazatritetracontan-38-yl)-2-(6-(2-(2-(2-aminoacetamido)acetamido)-3-mercaptopropanamido)hexanamido)pentanediamide	IC50	0.59 nM
CHEMBL3401466	IC50	0.6 nM
AcBB(7-14)	KI	0.7 nM
Bombesin analogue	KI	0.7 nM
[Tyr4]Bombesin	IC50	0.85 nM
Universal ligand	IC50	1.1 nM
CHEMBL6102759	IC50	1.1 nM
(S)-N1-((5S,8S,11S,17S,20S,23S,26S,29S,35S,38S)-11-((1H-imidazol-5-yl)methyl)-23-((1H-indol-3-yl)methyl)-43-amino-29-(2-amino-2-oxoethyl)-26-(3-amino-3-oxopropyl)-5-carbamoyl-35-((R)-1-hydroxyethyl)-43-imino-8-isobutyl-17-isopropyl-20-methyl-7,10,13,16,19,22,25,28,31,34,37-undecaoxo-2-thia-6,9,12,15,18,21,24,27,30,33,36,42-dodecaazatritetracontan-38-yl)-2-((S)-5-oxopyrrolidine-2-carboxamido)pentanediamide	IC50	1.24 nM
(2S)-N1-((5S,8S,11S,17S,20S,23S)-11-((1H-imidazol-5-yl)methyl)-5-carbamoyl-24-(1H-indol-3-yl)-8-isobutyl-17-isopropyl-20-methyl-7,10,13,16,19,22-hexaoxo-2-thia-6,9,12,15,18,21-hexaazatetracosan-23-yl)-2-(6-(2-(2-(2-aminoacetamido)acetamido)-3-mercaptopropanamido)hexanamido)pentanediamide	IC50	1.45 nM
(S)-3-(1H-Indol-3-yl)-N-[1-(4-methoxy-phenyl)-cyclohexylmethyl]-2-methyl-2-[3-(4-nitro-phenyl)-ureido]-propionamide	KI	3.7 nM
D-Phe-Gln-Trp-Ala-Val-b-Ala-His-Phe-Nle-NH2	EC50	3.9 nM
CHEMBL2429987	IC50	5.3 nM
(S)-N-[1-(4-Ethoxy-phenyl)-cyclohexylmethyl]-3-(1H-indol-3-yl)-2-methyl-2-[3-(4-nitro-phenyl)-ureido]-propionamide	KI	5.8 nM
(S)-3-(1H-Indol-3-yl)-2-methyl-N-[1-(4-nitro-phenyl)-cyclohexylmethyl]-2-[3-(4-nitro-phenyl)-ureido]-propionamide	KI	6.4 nM
CHEMBL2429980	IC50	8.3 nM
(S)-N-[1-(4-Dimethylamino-phenyl)-cyclohexylmethyl]-3-(1H-indol-3-yl)-2-methyl-2-[3-(4-nitro-phenyl)-ureido]-propionamide	KI	9 nM
CHEMBL6078008	IC50	10 nM
(S)-3-(1H-Indol-3-yl)-N-[1-(5-methoxy-pyridin-2-yl)-cyclohexylmethyl]-2-methyl-2-[3-(4-nitro-phenyl)-ureido]-propionamide	IC50	16 nM
(S)-3-(1H-Indol-3-yl)-2-methyl-2-[3-(4-nitro-phenyl)-ureido]-N-(1-pyridin-2-yl-cyclohexylmethyl)-propionamide	KI	17 nM
CHEMBL2314835	IC50	18 nM
CHEMBL2429981	IC50	23 nM
CHEMBL2429964	IC50	23 nM
(S)-N-[1-(4-Hydroxy-phenyl)-cyclohexylmethyl]-3-(1H-indol-3-yl)-2-methyl-2-[3-(4-nitro-phenyl)-ureido]-propionamide	KI	32 nM
(S)-N-[1-(3,4-Dimethoxy-phenyl)-cyclohexylmethyl]-3-(1H-indol-3-yl)-2-methyl-2-[3-(4-nitro-phenyl)-ureido]-propionamide	KI	33 nM
(S)-3-(1H-Indol-3-yl)-N-[1-(4-isopropyl-phenyl)-cyclohexylmethyl]-2-methyl-2-[3-(4-nitro-phenyl)-ureido]-propionamide	KI	35 nM
(S)-2-[3-(4-Cyano-phenyl)-ureido]-3-(1H-indol-3-yl)-2-methyl-N-(1-pyridin-2-yl-cyclohexylmethyl)-propionamide	KI	37 nM
[(N4-Bzdig)0]BB(7-14)	IC50	37 nM
CHEMBL6163713	IC50	44 nM
CHEMBL6152438	IC50	46 nM
2-(4-(2-(4-(2,2-dimethylbutyl)-1H-imidazol-2-yl)ethyl)phenyl)pyridine	EC50	47 nM
CHEMBL6078215	IC50	58 nM
CHEMBL6102904	IC50	59 nM
1-[4-(2,2-dimethylpropyl)-1H-imidazol-2-yl]-2-[4-(5-fluoropyridin-2-yl)phenyl]propan-2-ol	EC50	67 nM
CHEMBL6074465	IC50	68 nM
CHEMBL6078058	IC50	71 nM
CHEMBL6083003	IC50	79 nM
CHEMBL6078293	IC50	81 nM
(S)-2-[3-(3,4-Dichloro-phenyl)-ureido]-3-(1H-indol-3-yl)-2-methyl-N-(1-pyridin-2-yl-cyclohexylmethyl)-propionamide	KI	85 nM
(S)-3-(1H-Indol-3-yl)-2-methyl-2-[3-(3-nitro-phenyl)-ureido]-N-(1-pyridin-2-yl-cyclohexylmethyl)-propionamide	KI	85 nM
(S)-3-(1H-Indol-3-yl)-2-methyl-2-[3-(4-nitro-phenyl)-ureido]-N-(1-phenyl-cyclohexylmethyl)-propionamide	KI	89 nM
CHEMBL6078261	IC50	101 nM
CHEMBL6108918	IC50	106 nM
(S)-3-(1H-Indol-3-yl)-2-methyl-N-(1-pyridin-2-yl-cyclohexylmethyl)-2-[3-(4-trifluoromethyl-phenyl)-ureido]-propionamide	KI	124 nM
(S)-2-[3-(4-Chloro-phenyl)-ureido]-3-(1H-indol-3-yl)-2-methyl-N-(1-pyridin-2-yl-cyclohexylmethyl)-propionamide	KI	149 nM
[D-Tyr6-, Beta-Ala11, Phe13, Nle14] Bn (6-14)(Bombesin Analogue)	EC50	151 nM
(S)-3-(1H-Indol-3-yl)-2-[3-(4-isopropyl-phenyl)-ureido]-2-methyl-N-(1-pyridin-2-yl-cyclohexylmethyl)-propionamide	KI	273 nM
(S)-3-(1H-Indol-3-yl)-N-[1-(2-methoxy-phenyl)-cyclohexylmethyl]-2-methyl-2-[3-(4-nitro-phenyl)-ureido]-propionamide	KI	404 nM
SR 147778	KI	1000 nM

ChEMBL bioactivities

221 potent at pChembl≥5 of 223 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.40	Ki	0.04	nM	CHEMBL413196
10.22	IC50	0.06	nM	Demobesin 3
10.22	EC50	0.06	nM	CHEMBL525577
10.10	IC50	0.08	nM	CHEMBL414307
9.82	Ki	0.15	nM	BOMBESIN
9.82	IC50	0.15	nM	CHEMBL2371724
9.59	EC50	0.258	nM	BOMBESIN
9.43	EC50	0.373	nM	CHEMBL272335
9.33	IC50	0.47	nM	Demobesin 3
9.30	Ki	0.5	nM	CHEMBL3401466
9.23	IC50	0.59	nM	CHEMBL2372319
9.22	IC50	0.6	nM	CHEMBL266079
9.22	IC50	0.6	nM	CHEMBL3401466
9.19	IC50	0.65	nM	CHEMBL414307
9.15	Ki	0.7	nM	CHEMBL314375
9.15	Ki	0.7	nM	CHEMBL269432
9.14	IC50	0.72	nM	UNIVERSAL LIGAND
9.07	IC50	0.85	nM	CHEMBL2371726
9.00	Ki	1	nM	CHEMBL405908
9.00	Ki	0.99	nM	CHEMBL525577
8.91	IC50	1.24	nM	CHEMBL525820
8.89	IC50	1.3	nM	CHEMBL266079
8.84	IC50	1.45	nM	CHEMBL2372320
8.82	IC50	1.5	nM	CHEMBL3953323
8.82	IC50	1.5	nM	CHEMBL3927340
8.72	IC50	1.9	nM	CHEMBL3907272
8.71	IC50	1.94	nM	CHEMBL2371724
8.70	IC50	2	nM	BOMBESIN
8.70	IC50	2	nM	CHEMBL3904512
8.66	IC50	2.2	nM	CHEMBL3967904
8.60	IC50	2.5	nM	CHEMBL3963362
8.60	IC50	2.5	nM	CHEMBL3927633
8.60	IC50	2.5	nM	CHEMBL3984233
8.52	IC50	3	nM	CHEMBL3954296
8.52	IC50	3	nM	CHEMBL3985283
8.50	IC50	3.14	nM	CHEMBL6102759
8.47	IC50	3.4	nM	CHEMBL3979188
8.46	IC50	3.5	nM	CHEMBL3950452
8.46	IC50	3.5	nM	CHEMBL3960359
8.43	Ki	3.7	nM	CHEMBL312926
8.42	IC50	3.8	nM	CHEMBL3902429
8.40	IC50	4	nM	CHEMBL3905562
8.40	IC50	4	nM	CHEMBL3924852
8.40	IC50	4	nM	CHEMBL3917368
8.40	IC50	4	nM	CHEMBL3948894
8.40	IC50	4	nM	CHEMBL3924581
8.40	IC50	4	nM	CHEMBL3967299
8.40	IC50	4	nM	CHEMBL3951222
8.35	IC50	4.5	nM	CHEMBL3978233
8.35	IC50	4.5	nM	CHEMBL3935535

PubChem BioAssay actives

77 with measured affinity, of 152 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[2-[[2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-1-[(2S)-2-amino-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]acetyl]amino]acetyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]hexanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]acetyl]amino]-4-oxobutanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]acetyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoic acid	42630: In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin.	ki	<0.0001	uM
(2S)-2-[[2-[2-[4-[3-(2-aminoethylamino)-2-[(2-aminoethylamino)methyl]propyl]anilino]-2-oxoethoxy]acetyl]amino]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]pentanediamide	242679: Displacement of [125 I-Tyr4]BB from human gastrin releasing peptide receptor expressed in PC-3 cell membranes	ic50	0.0001	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-4-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]-2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]pentanediamide	42630: In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin.	ki	0.0001	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxohexan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[(2R)-2-amino-3-phenylpropanoyl]amino]pentanediamide	348844: Agonist activity at recombinant gastrin releasing peptide receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay	ec50	0.0001	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-4-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-5-methylsulfanyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-2-oxoethyl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-[[(2S)-1-[3-(2-aminoethylamino)-2-[(2-aminoethylamino)methyl]propanoyl]pyrrolidine-2-carbonyl]amino]pentanediamide	242679: Displacement of [125 I-Tyr4]BB from human gastrin releasing peptide receptor expressed in PC-3 cell membranes	ic50	0.0001	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-4-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxoheptan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-2-oxoethyl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-[[(2S)-1-[3-(2-aminoethylamino)-2-[(2-aminoethylamino)methyl]propanoyl]pyrrolidine-2-carbonyl]amino]pentanediamide	242679: Displacement of [125 I-Tyr4]BB from human gastrin releasing peptide receptor expressed in PC-3 cell membranes	ic50	0.0001	uM
(2S)-2-[8-(6-aminohexanoylamino)octanoylamino]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]pentanediamide	322034: Displacement of 125I[Tyr4]-bombesin from GRPR expressed in human PC3 cells	ec50	0.0004	uM
[[1-[2-[[1-[2-[[(2R)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(3S,4S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]piperidin-4-yl]amino]-2-oxoethyl]triazol-4-yl]methyl-dimethylazaniumyl]methyl-trifluoroboranuide	1193752: Displacement of [125I-Tyr4]bombesin from GRPR (unknown origin) expressed in human PC3 cells after 45 mins by gamma counting analysis	ki	0.0005	uM
(2S)-2-[[2-[2-[4-[3-(2-aminoethylamino)-2-[(2-aminoethylamino)methyl]propyl]anilino]-2-oxoethoxy]acetyl]amino]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]pentanediamide	242679: Displacement of [125 I-Tyr4]BB from human gastrin releasing peptide receptor expressed in PC-3 cell membranes	ic50	0.0006	uM
(2S)-2-[6-[[(2R)-2-[[2-[(2-aminoacetyl)amino]acetyl]amino]-3-sulfanylpropanoyl]amino]hexanoylamino]-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-4-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]pentanediamide	397036: Displacement of [125I-Tyr4]BN form BB2 receptor in human PC3 cells	ic50	0.0006	uM
(2S)-2-acetamido-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]pentanediamide	42630: In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin.	ki	0.0007	uM
(2S)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxohexan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]pentanediamide	242208: Inhibition of gastrin releasing peptide receptor expressed in human prostate cancer cells	ic50	0.0007	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-4-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-2-oxoethyl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]pentanediamide	242679: Displacement of [125 I-Tyr4]BB from human gastrin releasing peptide receptor expressed in PC-3 cell membranes	ic50	0.0008	uM
(2S)-3-(1H-indol-3-yl)-N-[[1-(5-methoxy-2-pyridinyl)cyclohexyl]methyl]-2-methyl-2-[(4-nitrophenyl)carbamoylamino]propanamide	42631: Antagonistic activity against cloned human Bombesin receptor bb2 labeled with [125I]- [Tyr] bombesin stably expressed in CHO cells; 0.66-1.3	ki	0.0010	uM
(2S)-N-[(2S)-1-[[(2S,3R)-1-[[2-[[(2S)-4-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]-2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]pentanediamide	397036: Displacement of [125I-Tyr4]BN form BB2 receptor in human PC3 cells	ic50	0.0012	uM
(2S)-2-[6-[[(2R)-2-[[2-[(2-aminoacetyl)amino]acetyl]amino]-3-sulfanylpropanoyl]amino]hexanoylamino]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]pentanediamide	397036: Displacement of [125I-Tyr4]BN form BB2 receptor in human PC3 cells	ic50	0.0014	uM
(2S)-2-[[(2R)-2-acetamido-3-phenylpropanoyl]amino]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(3S,4S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]pentanediamide	2203373: Displacement of 125 I- [Tyr4] from bombesin receptor 2 (unknown origin) assessed as inhibition by radioligand competitive binding assay	ic50	0.0031	uM
(2S)-3-(1H-indol-3-yl)-N-[[1-(4-methoxyphenyl)cyclohexyl]methyl]-2-methyl-2-[(4-nitrophenyl)carbamoylamino]propanamide	42630: In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin.	ki	0.0037	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-4-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-6-[(4-fluorobenzoyl)amino]-1-oxohexan-2-yl]-2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]pentanediamide	772828: Displacement of [125I]-Tyr4-bombesin from GRP receptor in human PC3 cells	ic50	0.0053	uM
(2S)-N-[[1-(4-ethoxyphenyl)cyclohexyl]methyl]-3-(1H-indol-3-yl)-2-methyl-2-[(4-nitrophenyl)carbamoylamino]propanamide	42630: In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin.	ki	0.0058	uM
(2S)-3-(1H-indol-3-yl)-2-methyl-2-[(4-nitrophenyl)carbamoylamino]-N-[[1-(4-nitrophenyl)cyclohexyl]methyl]propanamide	42630: In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin.	ki	0.0064	uM
(2R)-3-[[(2R)-1-[[5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(3S,4S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]-methylamino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentyl]amino]-1-oxo-3-sulfopropan-2-yl]amino]-2-[[2-[4-[ditert-butyl(fluoro)silyl]phenyl]acetyl]amino]-3-oxopropane-1-sulfonic acid	772907: Displacement of [125I]-Tyr4-bombesin from GRP receptor in human PC3 cells after 1 hr by gamma-counting analysis	ic50	0.0083	uM
(2S)-N-[[1-[4-(dimethylamino)phenyl]cyclohexyl]methyl]-3-(1H-indol-3-yl)-2-methyl-2-[(4-nitrophenyl)carbamoylamino]propanamide	42630: In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin.	ki	0.0090	uM
(2S)-3-(1H-indol-3-yl)-2-methyl-2-[(4-nitrophenyl)carbamoylamino]-N-[(1-pyridin-2-ylcyclohexyl)methyl]propanamide	42630: In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin.	ki	0.0170	uM
2-[4-[2-[[(2S)-1-[2-[2-[2-[[(5S)-5-[[(2S)-1-[(2S)-4-amino-2-[[(2S,3S)-2-amino-3-methylpentanoyl]amino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]amino]-6-[[(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]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-6-[[2-[2-[2-[2-[2-[[2-[4-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]carbamoyl]anilino]-2-oxoethyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]acetyl]amino]-1-oxohexan-2-yl]amino]-2-oxoethyl]-7,10-bis(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetic acid	721182: Displacement of [125I]-Tyr4-BBN from human GRPR overexpressed in human T47D cells	ic50	0.0180	uM
(2S)-2-[[(2R)-2-[[(2R)-2-acetamido-3-sulfanylpropanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(3S,4S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]pentanediamide	2203373: Displacement of 125 I- [Tyr4] from bombesin receptor 2 (unknown origin) assessed as inhibition by radioligand competitive binding assay	ic50	0.0205	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(3S,4S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]-methylamino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[5-[[(2S)-5-(diaminomethylideneamino)-2-[[2-[4-[ditert-butyl(fluoro)silyl]phenyl]acetyl]amino]pentanoyl]amino]pentanoylamino]pentanediamide	772829: Binding affinity to GRP receptor (unknown origin)	ic50	0.0229	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(3S,4S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]-methylamino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[5-[[(2S)-5-(diaminomethylideneamino)-2-[[4-[2-[4-[ditert-butyl(fluoro)silyl]phenyl]ethylamino]-2,3-dihydroxy-4-oxobutanoyl]amino]pentanoyl]amino]pentanoylamino]pentanediamide	772907: Displacement of [125I]-Tyr4-bombesin from GRP receptor in human PC3 cells after 1 hr by gamma-counting analysis	ic50	0.0230	uM
(2S)-N-[[1-(4-hydroxyphenyl)cyclohexyl]methyl]-3-(1H-indol-3-yl)-2-methyl-2-[(4-nitrophenyl)carbamoylamino]propanamide	42630: In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin.	ki	0.0320	uM
(2S)-N-[[1-(3,4-dimethoxyphenyl)cyclohexyl]methyl]-3-(1H-indol-3-yl)-2-methyl-2-[(4-nitrophenyl)carbamoylamino]propanamide	42630: In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin.	ki	0.0330	uM
(2S)-2-[[2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[2-[[2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-1-[(2S)-2-amino-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]acetyl]amino]acetyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]hexanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]acetyl]amino]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]butanediamide	73201: Effective concentration required against gastrin releasing peptide receptor (GRP-R) in CHO cells by using FLIPR assay	ec50	0.0340	uM
(2S)-3-(1H-indol-3-yl)-2-methyl-2-[(4-nitrophenyl)carbamoylamino]-N-[[1-(4-propan-2-ylphenyl)cyclohexyl]methyl]propanamide	42630: In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin.	ki	0.0350	uM
(2S)-2-[[(2R)-2-[[(2R)-2-acetamido-3-sulfanylpropanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(3S,4S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]-methylamino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]pentanediamide	2203373: Displacement of 125 I- [Tyr4] from bombesin receptor 2 (unknown origin) assessed as inhibition by radioligand competitive binding assay	ic50	0.0363	uM
(2S)-2-[(4-cyanophenyl)carbamoylamino]-3-(1H-indol-3-yl)-2-methyl-N-[(1-pyridin-2-ylcyclohexyl)methyl]propanamide	42630: In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin.	ki	0.0370	uM
(2S)-2-[(2-aminoacetyl)amino]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]butanediamide	73201: Effective concentration required against gastrin releasing peptide receptor (GRP-R) in CHO cells by using FLIPR assay	ec50	0.0410	uM
(2S)-2-[[(1S)-5-[[(2S)-2-[[4-[[[6-[4-[3-[[1-[2-[[(2R)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(4S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]piperidin-4-yl]amino]-3-oxopropyl]triazol-1-yl]-2-[[2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetyl]amino]hexanoyl]amino]methyl]cyclohexanecarbonyl]amino]-3-naphthalen-2-ylpropanoyl]amino]-1-carboxypentyl]carbamoylamino]pentanedioic acid	2258414: Displacement of 125I- bombesin from GRPR in human PC-3 cells incubated for 45 mins by competitive binding based gamma counter analysis	ic50	0.0439	uM
2-[4-[2-[[1-[2-[[(2R)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(4S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]piperidin-4-yl]amino]-2-oxoethyl]-7,10-bis(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetic acid	2258414: Displacement of 125I- bombesin from GRPR in human PC-3 cells incubated for 45 mins by competitive binding based gamma counter analysis	ic50	0.0456	uM
(4S)-4-[6-[3-[(2R)-3-[2-[2-[2-[2-[3-[[(2R)-1-[[(2S)-1-[[(2S)-3-(3a,7a-dihydro-1-benzothiophen-3-yl)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(3S,4S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-amino-1,5-dioxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethylamino]-2-acetamido-3-oxopropyl]sulfanyl-2,5-dioxopyrrolidin-1-yl]hexanoylamino]-5-[[(2S)-1-[[(2S)-5-(carbamoylamino)-1-[4-[[[(2S)-1-[[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-methylcarbamoyl]oxymethyl]anilino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-oxopentanoic acid	2203381: Displacement of 125 I- [Tyr4] from bombesin receptor 2 in human PC-3 cells assessed as inhibition by radioligand displacement assay	ic50	0.0582	uM
(4S)-4-[6-[3-[(2R)-3-[2-[2-[2-[2-[3-[[(2R)-1-[[(2S)-1-[[(2S)-3-(3a,7a-dihydro-1H-indol-3-yl)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(3S,4S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-amino-1,5-dioxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethylamino]-2-acetamido-3-oxopropyl]sulfanyl-2,5-dioxopyrrolidin-1-yl]hexanoylamino]-5-[[(2S)-1-[[(2S)-5-(carbamoylamino)-1-[4-[[[(2S)-1-[[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-methylcarbamoyl]oxymethyl]anilino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-oxopentanoic acid	2203381: Displacement of 125 I- [Tyr4] from bombesin receptor 2 in human PC-3 cells assessed as inhibition by radioligand displacement assay	ic50	0.0594	uM
(4R)-4-[6-[3-[(2R)-3-[2-[2-[2-[2-[3-[[(2R)-1-[[(2S)-1-[[(2S)-3-(3a,7a-dihydro-1H-indol-3-yl)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(3S,4S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-amino-1,5-dioxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethylamino]-2-acetamido-3-oxopropyl]sulfanyl-2,5-dioxopyrrolidin-1-yl]hexanoylamino]-5-[[2-[[(2S)-5-(carbamoylamino)-1-[4-[[[(2S)-1-[[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-methylcarbamoyl]oxymethyl]anilino]-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentanoic acid	2203381: Displacement of 125 I- [Tyr4] from bombesin receptor 2 in human PC-3 cells assessed as inhibition by radioligand displacement assay	ic50	0.0683	uM
(4S)-4-[6-[3-[(2R)-3-[2-[2-[2-[2-[3-[[(2R)-1-[[(2S)-1-[[(2S)-3-(3a,7a-dihydro-1-benzothiophen-3-yl)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(3S,4S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-amino-1,5-dioxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethylamino]-2-acetamido-3-oxopropyl]sulfanyl-2,5-dioxopyrrolidin-1-yl]hexanoylamino]-5-[[2-[[(2S)-5-(carbamoylamino)-1-[4-[[[(2S)-1-[[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-methylcarbamoyl]oxymethyl]anilino]-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentanoic acid	2203381: Displacement of 125 I- [Tyr4] from bombesin receptor 2 in human PC-3 cells assessed as inhibition by radioligand displacement assay	ic50	0.0711	uM
(4S)-4-[6-[3-[(2R)-3-[2-[2-[2-[2-[3-[[(2S)-1-[[(2S)-1-[[(2S)-3-(3a,7a-dihydro-1H-indol-3-yl)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-amino-1,5-dioxopentan-2-yl]amino]-4-amino-1,4-dioxobutan-2-yl]amino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethylamino]-2-acetamido-3-oxopropyl]sulfanyl-2,5-dioxopyrrolidin-1-yl]hexanoylamino]-5-[[2-[[(2S)-5-(carbamoylamino)-1-[4-[[[(2S)-1-[[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-methylcarbamoyl]oxymethyl]anilino]-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentanoic acid	2203382: Displacement of 125 I- [Tyr4] from bombesin receptor 2 in human MDA-MB-231 cells assessed as inhibition by radioligand displacement assay	ic50	0.0793	uM
(4S)-4-[6-[3-[(2R)-3-[2-[2-[2-[2-[3-[[(2S)-1-[[(2S)-1-[[(2S)-3-(3a,7a-dihydro-1-benzothiophen-3-yl)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-amino-1,5-dioxopentan-2-yl]amino]-4-amino-1,4-dioxobutan-2-yl]amino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethylamino]-2-acetamido-3-oxopropyl]sulfanyl-2,5-dioxopyrrolidin-1-yl]hexanoylamino]-5-[[2-[[(2S)-5-(carbamoylamino)-1-[4-[[[(2S)-1-[[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-methylcarbamoyl]oxymethyl]anilino]-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentanoic acid	2203381: Displacement of 125 I- [Tyr4] from bombesin receptor 2 in human PC-3 cells assessed as inhibition by radioligand displacement assay	ic50	0.0807	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]propanoylamino]-3-methylbutanoyl]amino]-3-phenylpropanoyl]amino]hexanoic acid	73201: Effective concentration required against gastrin releasing peptide receptor (GRP-R) in CHO cells by using FLIPR assay	ec50	0.0840	uM
(2S)-2-[(3,4-dichlorophenyl)carbamoylamino]-3-(1H-indol-3-yl)-2-methyl-N-[(1-pyridin-2-ylcyclohexyl)methyl]propanamide	42630: In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin.	ki	0.0850	uM
(2S)-3-(1H-indol-3-yl)-2-methyl-2-[(3-nitrophenyl)carbamoylamino]-N-[(1-pyridin-2-ylcyclohexyl)methyl]propanamide	42630: In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin.	ki	0.0850	uM
(2S)-3-(1H-indol-3-yl)-2-methyl-2-[(4-nitrophenyl)carbamoylamino]-N-[(1-phenylcyclohexyl)methyl]propanamide	42630: In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin.	ki	0.0890	uM
(4S)-4-[6-[3-[(2R)-3-[2-[2-[2-[2-[3-[[(2S)-1-[[(2S)-1-[[(2S)-3-(3a,7a-dihydro-1-benzothiophen-3-yl)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-amino-1,5-dioxopentan-2-yl]amino]-4-amino-1,4-dioxobutan-2-yl]amino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethylamino]-2-acetamido-3-oxopropyl]sulfanyl-2,5-dioxopyrrolidin-1-yl]hexanoylamino]-5-[[(2S)-1-[[(2S)-5-(carbamoylamino)-1-[4-[[[(2S)-1-[[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-methylcarbamoyl]oxymethyl]anilino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-oxopentanoic acid	2203381: Displacement of 125 I- [Tyr4] from bombesin receptor 2 in human PC-3 cells assessed as inhibition by radioligand displacement assay	ic50	0.0936	uM
(4S)-4-[6-[3-[(2R)-3-[2-[2-[2-[2-[3-[[(2S)-1-[[(2S)-1-[[(2S)-3-(3a,7a-dihydro-1H-indol-3-yl)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-amino-1,5-dioxopentan-2-yl]amino]-4-amino-1,4-dioxobutan-2-yl]amino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethylamino]-2-acetamido-3-oxopropyl]sulfanyl-2,5-dioxopyrrolidin-1-yl]hexanoylamino]-5-[[(2S)-1-[[(2S)-5-(carbamoylamino)-1-[4-[[[(2S)-1-[[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-methylcarbamoyl]oxymethyl]anilino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-oxopentanoic acid	2203382: Displacement of 125 I- [Tyr4] from bombesin receptor 2 in human MDA-MB-231 cells assessed as inhibition by radioligand displacement assay	ic50	0.0974	uM
(2S)-3-(1H-indol-3-yl)-2-methyl-N-[(1-pyridin-2-ylcyclohexyl)methyl]-2-[[4-(trifluoromethyl)phenyl]carbamoylamino]propanamide	42630: In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin.	ki	0.1240	uM

CTD chemical–gene interactions

25 total (human), top 25 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	affects methylation	2
methylmercuric chloride	increases expression	1
pirinixic acid	affects binding, decreases expression, increases activity	1
sodium arsenite	affects methylation	1
bombesin, Tyr(4)-	affects binding, decreases reaction	1
bisindolylmaleimide	decreases reaction, increases phosphorylation	1
bombesin (7-14)	affects binding, decreases reaction	1
abrine	increases expression	1
2-(3-(1,3-dicarboxypropyl)ureido)pentanedioic acid	affects binding, decreases reaction	1
(+)-JQ1 compound	decreases expression	1
1-(1,3-carboxypropyl)-4,7-carboxymethyl-1,4,7-triazacyclononane	affects binding, decreases reaction	1
Temozolomide	increases expression	1
Sunitinib	increases expression	1
Androgens	affects expression	1
Copper	affects binding, decreases reaction	1
Cytarabine	decreases expression	1
Dichloroacetic Acid	increases response to substance	1
Drugs, Chinese Herbal	decreases expression	1
Silicon Dioxide	decreases expression	1
Tetradecanoylphorbol Acetate	increases phosphorylation	1
Valerates	affects binding, decreases reaction	1
Valproic Acid	increases expression	1
Aminocaproic Acid	affects binding, decreases reaction	1
Aflatoxin B1	decreases methylation	1
3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer	increases phosphorylation, decreases reaction	1

ChEMBL screening assays

44 unique, capped per target: 38 binding, 6 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4880123	Binding	BB (non-select) CEREP ligand profiling	Data for DCP probe A-079
CHEMBL5665247	Functional	Agonist activity at GRPR (unknown origin)	In silico design of novel probes for the atypical opioid receptor MRGPRX2. — *Nat Chem Biol*

Cellosaurus cell lines

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

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

Cellosaurus	Name	Category	Sex
CVCL_DA12	Ace-1(huGRPr)	Cancer cell line	Male
CVCL_H405	CHO-K1/BB2	Spontaneously immortalized cell line	Female
CVCL_KZ57	PathHunter HEK 293 GRPR beta-arrestin	Transformed cell line	Female
CVCL_LA47	PathHunter U2OS GRPR Activated GPCR Internalization	Cancer cell line	Female
CVCL_LA48	PathHunter U2OS GRPR beta-arrestin	Cancer cell line	Female
CVCL_YK47	U2OS GRPR calcium-Nomad	Cancer cell line	Female
CVCL_YK48	U2OS GRPR HiTSeeker	Cancer cell line	Female
CVCL_ZK86	GeneBLAzer GRPR-NFAT-bla CHO-K1	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

Via MONDO — disease-level, not drug-specific.

Predicted chemistry — Sugi Predict

The predicted patent-compound landscape for GRPR across ~30M SureChEMBL compounds — explore on Sugi Predict.