GALR1

gene

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Summary

GALR1 (galanin receptor 1, HGNC:4132) is a protein-coding gene on chromosome 18q23, encoding Galanin receptor type 1 (P47211). Receptor for the hormone galanin.

The neuropeptide galanin elicits a range of biological effects by interaction with specific G-protein-coupled receptors. Galanin receptors are seven-transmembrane proteins shown to activate a variety of intracellular second-messenger pathways. GALR1 inhibits adenylyl cyclase via a G protein of the Gi/Go family. GALR1 is widely expressed in the brain and spinal cord, as well as in peripheral sites such as the small intestine and heart.

Source: NCBI Gene 2587 — RefSeq curated summary.

At a glance

GWAS associations: 10
Clinical variants (ClinVar): 75 total — 1 likely-pathogenic
Druggable target: yes
Dosage sensitivity (ClinGen): haploinsufficiency no evidence, triplosensitivity no evidence
MANE Select transcript: NM_001480

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:4132
Approved symbol	GALR1
Name	galanin receptor 1
Location	18q23
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000166573
Ensembl biotype	protein_coding
OMIM	600377
Entrez	2587

Gene structure

Transcript identifiers

Ensembl transcripts: 2 — 1 protein_coding, 1 protein_coding_CDS_not_defined

ENST00000299727, ENST00000582943

RefSeq mRNA: 1 — MANE Select: NM_001480 NM_001480

CCDS: CCDS12012

Canonical transcript exons

ENST00000299727 — 3 exons

Exon	Start	End
ENSE00001104298	77256158	77256223
ENSE00001156523	77268585	77277900
ENSE00001280747	77249848	77251214

Expression profiles

Bgee: expression breadth ubiquitous, 103 present calls, max score 64.25.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.0418 / max 20.4135, expressed in 13 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
170877	0.0219	6
170876	0.0138	5
170875	0.0061	3

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
pituitary gland	UBERON:0000007	64.25	gold quality
hair follicle	UBERON:0002073	62.78	gold quality
adenohypophysis	UBERON:0002196	60.95	gold quality
colonic epithelium	UBERON:0000397	57.41	gold quality
prefrontal cortex	UBERON:0000451	56.76	gold quality
decidua	UBERON:0002450	56.55	gold quality
buccal mucosa cell	CL:0002336	56.45	gold quality
endothelial cell	CL:0000115	55.40	gold quality
hypothalamus	UBERON:0001898	55.32	gold quality
pigmented layer of retina	UBERON:0001782	54.61	gold quality
corpus callosum	UBERON:0002336	54.04	gold quality
amygdala	UBERON:0001876	52.36	gold quality
right uterine tube	UBERON:0001302	52.24	gold quality
seminal vesicle	UBERON:0000998	51.57	gold quality
postcentral gyrus	UBERON:0002581	51.42	gold quality
frontal cortex	UBERON:0001870	51.36	gold quality
primary visual cortex	UBERON:0002436	51.32	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	51.05	gold quality
neocortex	UBERON:0001950	50.70	gold quality
rectum	UBERON:0001052	50.55	gold quality
lower esophagus mucosa	UBERON:0035834	50.50	gold quality
superior frontal gyrus	UBERON:0002661	50.17	gold quality
forebrain	UBERON:0001890	50.16	gold quality
anterior cingulate cortex	UBERON:0009835	50.14	gold quality
cranial nerve II	UBERON:0000941	50.05	gold quality
cerebral cortex	UBERON:0000956	49.78	gold quality
temporal lobe	UBERON:0001871	49.72	gold quality
parietal lobe	UBERON:0001872	49.45	gold quality
blood vessel layer	UBERON:0004797	49.29	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	49.23	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	6.38

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): CREB1

miRNA regulators (miRDB)

80 targeting GALR1, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-513A-5P	100.00	69.77	2465
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-30A-5P	100.00	76.31	3233
HSA-MIR-30B-5P	100.00	76.29	3248
HSA-MIR-30C-5P	100.00	76.29	3248
HSA-MIR-30D-5P	100.00	76.32	3233
HSA-MIR-30E-5P	100.00	76.32	3242
HSA-MIR-8485	100.00	77.57	4731
HSA-MIR-6873-3P	100.00	71.42	2626
HSA-MIR-7110-3P	100.00	73.18	2486
HSA-MIR-3646	100.00	73.56	5283
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-186-5P	99.99	70.83	3707
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-371B-5P	99.99	75.34	4759
HSA-MIR-373-5P	99.98	75.36	4753
HSA-MIR-616-5P	99.98	75.58	4775
HSA-MIR-8068	99.98	73.85	2376
HSA-MIR-7152-3P	99.97	67.47	849
HSA-MIR-3688-3P	99.97	72.02	2834
HSA-MIR-607	99.97	73.62	5593
HSA-MIR-302C-5P	99.97	72.56	3642
HSA-MIR-551B-5P	99.96	71.28	3493
HSA-MIR-9-3P	99.96	70.88	2068
HSA-MIR-3143	99.93	71.96	3104
HSA-MIR-552-5P	99.93	68.56	1583
HSA-MIR-3682-5P	99.93	67.97	1163
HSA-MIR-3119	99.92	71.34	2390
HSA-MIR-4753-3P	99.90	71.03	3786

Functional genomics

ClinGen dosage: haploinsufficiency 0 (no evidence), triplosensitivity 0 (no evidence). ClinGen Gene Dosage Map

Literature-anchored findings (GeneRIF, showing 22)

disregulation of galanin receptor 1 may lead to uncontrolled proliferation and neoplastic transformation (PMID:15767248)
The analyzed single nucleotide polymorphisms in GAL and GALR1 do not play major role in early onset obesity or dietary fat intake in obese children and adolescents. (PMID:15930442)
There was no effect of GALR1 on alcoholism risk. (PMID:17083333)
Data suggest that galanin stimulates cortisol secretion from human inner adrenocortical cells, acting through GAL-R1 coupled to the adenylate cyclase/PKA-dependent signaling cascade via a Ptx-sensitive Galpha protein. (PMID:17982695)
GalR1 is internalized via the clathrin-dependent, endocytic pathway and then, to a large extent, delivered to lysosomes for degradation through the lysosome-targeting signal YXXO (PMID:18385373)
GAL, coding for the neuropeptide galanin, and GALR1, a galanin receptor, were identified as candidate genes of oncogenesis in squamous cell carcinoma using a survey of parallel chromosomal alterations and gene expression studies in 10 SCC cell lines. (PMID:18973137)
GALR1 is a tumor suppressor gene in head and neck squamous cell carcinoma (PMID:19047085)
it has been demonstrated that GalR1-5-HT1A receptors heteromerize. (PMID:20171159)
The results of this study suggested an association between variation at the GALR1 locus and baseline craving for tobacco in smokers seeking cessation treatment. (PMID:21430647)
Genetic variants in the GALR1 gene are associated with a protective effect in nicotine dependence. (PMID:21796100)
Moreover, we have identified a novel role for the GalR1/galanin receptor-ligand axis in chemoresistance, providing evidence to support its further evaluation as a potential therapeutic target and biomarker in colorectal cancer . (PMID:22859720)
GALR1 methylation is associated with endometrial cancer. (PMID:23727823)
Variants in genes for galanin (GAL) and its receptors (GALR1, GALR2, GALR3), despite their disparate genomic loci, conferred increased risk of depression and anxiety in people who experienced childhood adversity or recent negative life events. (PMID:24706871)
GAL and its receptors, GALR1 and GALR2, play a role in head and neck squamous cell carcinoma tumorigenesis (PMID:26572146)
High methylation of GALR1 is associated with head and neck cancer. (PMID:27027429)
Study provides evidence that GAL and GALR1/2 genes were identified as aberrantly methylated in head and neck squamous cell carcinoma. (PMID:27685843)
The MOR-Gal1R heteromer can explain previous results showing antagonistic galanin-opioid interactions and offers a new therapeutic target for the treatment of opioid use disorder (PMID:28007761)
Low GALR1 expression is associated with gastric cancer. (PMID:30616468)
Further evidence for the association of GAL, GALR1 and NPY1R variants with opioid dependence. (PMID:32757697)
A Three Protein-Coding Gene Prognostic Model Predicts Overall Survival in Bladder Cancer Patients. (PMID:33150179)
Galanin Receptors (GalR1, GalR2, and GalR3) Expression in Colorectal Cancer Tissue and Correlations to the Overall Survival and Poor Prognosis of CRC Patients. (PMID:35409094)
Promoter hypermethylation of GALR1 acts as an early epigenetic susceptibility event in colorectal carcinogenesis. (PMID:35606503)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	galr1a	ENSDARG00000005522
mus_musculus	Galr1	ENSMUSG00000024553
rattus_norvegicus	Galr1	ENSRNOG00000016654

Paralogs (16): NPFFR2 (ENSG00000056291), GNRHR (ENSG00000109163), CCKBR (ENSG00000110148), HCRTR1 (ENSG00000121764), AVPR2 (ENSG00000126895), GALR3 (ENSG00000128310), HCRTR2 (ENSG00000137252), NPFFR1 (ENSG00000148734), CCKAR (ENSG00000163394), AVPR1A (ENSG00000166148), GPR22 (ENSG00000172209), GPR150 (ENSG00000178015), OXTR (ENSG00000180914), FFAR4 (ENSG00000186188), QRFPR (ENSG00000186867), AVPR1B (ENSG00000198049)

Protein

Protein identifiers

Galanin receptor type 1 — P47211 (reviewed: P47211)

All UniProt accessions (1): P47211

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for the hormone galanin. The activity of this receptor is mediated by G proteins that inhibit adenylate cyclase activity.

Subunit / interactions. Interacts with GRP39 AND HTR1A.

Subcellular location. Cell membrane.

Post-translational modifications. Palmitoylated on at least one of the three cysteine residues present in the C-terminal part.

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

RefSeq proteins (1): NP_001471* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000405	Galanin_rcpt	Family
IPR003906	GAL1_rcpt	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (41 total): helix 12, topological domain 8, transmembrane region 7, strand 4, glycosylation site 3, sequence variant 3, chain 1, lipid moiety-binding region 1, disulfide bond 1, turn 1

Structure

Experimental structures (PDB)

2 structures.

PDB	Method	Resolution (Å)
7WQ3	ELECTRON MICROSCOPY	2.7
7XJJ	ELECTRON MICROSCOPY	3.3

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P47211-F1	84.14	0.61

Antibody-complex structures (SAbDab): 2 — 7WQ3, 7XJJ

Functional residue map

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

Post-translational modifications (1): 320

Disulfide bonds (1): 108–187

Glycosylation sites (3): 7, 12, 183

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: 121 (showing top): GCANCTGNY_MYOD_Q6, GOBP_REGULATION_OF_HORMONE_LEVELS, GOBP_HORMONE_TRANSPORT, GOBP_POSITIVE_REGULATION_OF_LIPID_TRANSPORT, GOBP_CELL_CELL_SIGNALING, GOBP_ORGANIC_HYDROXY_COMPOUND_TRANSPORT, GOBP_ADENYLATE_CYCLASE_MODULATING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, GOBP_REGULATION_OF_ADENYLATE_CYCLASE_ACTIVITY, MARTINEZ_RB1_TARGETS_DN, GOBP_REGULATION_OF_ENDOCRINE_PROCESS, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, GOBP_NEGATIVE_REGULATION_OF_MOLECULAR_FUNCTION, GOBP_SECRETION, GOBP_POSITIVE_REGULATION_OF_HORMONE_SECRETION

GO Biological Process (8): adenylate cyclase-activating G protein-coupled receptor signaling pathway (GO:0007189), negative regulation of adenylate cyclase activity (GO:0007194), positive regulation of cytosolic calcium ion concentration (GO:0007204), neuropeptide signaling pathway (GO:0007218), positive regulation of transcription by RNA polymerase II (GO:0045944), positive regulation of cortisol secretion (GO:0051464), signal transduction (GO:0007165), G protein-coupled receptor signaling pathway (GO:0007186)

GO Molecular Function (5): galanin receptor activity (GO:0004966), peptide hormone binding (GO:0017046), 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

Rollup of top-2 pathways:

Category	Pathways
Class A/1 (Rhodopsin-like receptors)	1
GPCR downstream signalling	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
G protein-coupled receptor signaling pathway	2
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	1
adenylate cyclase activator activity	1
adenylate cyclase activity	1
negative regulation of catalytic activity	1
regulation of adenylate cyclase activity	1
regulation of biological quality	1
regulation of transcription by RNA polymerase II	1
transcription by RNA polymerase II	1
positive regulation of DNA-templated transcription	1
cortisol secretion	1
regulation of cortisol secretion	1
positive regulation of glucocorticoid secretion	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
G protein-coupled receptor activity	1
signal transduction	1
neuropeptide receptor activity	1
hormone binding	1
peptide binding	1
transmembrane signaling receptor activity	1
binding	1
membrane	1
cell periphery	1
cellular anatomical structure	1

Protein interactions and networks

STRING

862 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
GALR1	GAL	P22466	999
GALR1	GALP	Q9UBC7	968
GALR1	FFAR1	O14842	818
GALR1	GALR2	O43603	810
GALR1	HTR1A	P08908	800
GALR1	CD22	P20273	764
GALR1	SPX	Q9BT56	637
GALR1	NPY	P01303	621
GALR1	SERPINB4	P48594	513
GALR1	LGALS2	P05162	506
GALR1	QRFP	P83859	505
GALR1	MBP	P02686	497
GALR1	ZNF516	Q92618	473
GALR1	ACHE	P22303	468
GALR1	OPRM1	P35372	467

IntAct

18 interactions, top by confidence:

A	B	Type	Score
GALR1	HTR1A	psi-mi:“MI:0403”(colocalization)	0.590
GALR1	HTR1A	psi-mi:“MI:2364”(proximity)	0.590
HTR1A	GPR39	psi-mi:“MI:0914”(association)	0.570
SNAPC5	GALR1	psi-mi:“MI:0915”(physical association)	0.560
H2BC9	GALR1	psi-mi:“MI:0915”(physical association)	0.400
GALR1	PDIA3	psi-mi:“MI:0915”(physical association)	0.400
GALR1	PDZD8	psi-mi:“MI:0915”(physical association)	0.400
GALR1	GAL	psi-mi:“MI:0915”(physical association)	0.400
GAL	GALR1	psi-mi:“MI:0915”(physical association)	0.400
RAMP1	GALR1	psi-mi:“MI:0915”(physical association)	0.400
GALR1	RAMP2	psi-mi:“MI:0915”(physical association)	0.400
GALR1	RAMP3	psi-mi:“MI:0915”(physical association)	0.400
SNAPC5	GALR1	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (3): SNAPC5 (Two-hybrid), GALR1 (Proximity Label-MS), GALR1 (Cross-Linking-MS (XL-MS))

ESM2 similar proteins: A5A4L1, B2ZI34, O08725, O54799, O62709, P14600, P21450, P21451, P21729, P24053, P24530, P25101, P25103, P26684, P28088, P28336, P30547, P30548, P30550, P32304, P32305, P33534, P33535, P34975, P35372, P35463, P41144, P41145, P42866, P47211, P48302, P52500, P56479, P56497, P79350, Q29010, Q2KIP6, Q5DUB3, Q5IS39, Q5IS84

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

SIGNOR signaling

4 interactions.

A	Effect	B	Mechanism
GALR1	“up-regulates activity”	GNAI1	binding
GALR1	“up-regulates activity”	GNAI3	binding
GALR1	“up-regulates activity”	GNAO1	binding
Galanin	“up-regulates activity”	GALR1	“chemical activation”

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 10 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

GO biological processes:

GO term	Partners	Fold	FDR
G protein-coupled receptor signaling pathway	5	18.1×	7e-05

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	1
Uncertain significance	70
Likely benign	4
Benign	0

Top pathogenic / likely-pathogenic (1)

Variant ID	HGVS	Classification
394288	GRCh37/hg19 18q23(chr18:74347427-75077574)x3	Likely pathogenic

SpliceAI

1263 predictions. Top by Δscore:

Variant	Effect	Δscore
18:77256219:AAAAG:A	donor_loss	0.9900
18:77256220:AAAG:A	donor_loss	0.9900
18:77256221:AAG:A	donor_loss	0.9900
18:77256222:AGGT:A	donor_loss	0.9900
18:77256223:GG:G	donor_loss	0.9900
18:77256224:G:GA	donor_loss	0.9900
18:77256225:T:G	donor_loss	0.9900
18:77268850:A:T	donor_gain	0.9900
18:77272979:A:T	donor_gain	0.9900
18:77251143:GCC:G	donor_gain	0.9800
18:77253422:GCTGT:G	donor_gain	0.9800
18:77251248:G:GT	donor_gain	0.9700
18:77268748:A:G	donor_gain	0.9700
18:77251249:G:T	donor_gain	0.9600
18:77257781:GT:G	donor_gain	0.9600
18:77268785:G:GT	donor_gain	0.9600
18:77271000:G:GT	donor_gain	0.9600
18:77271230:A:AG	donor_gain	0.9600
18:77272969:GTGTC:G	donor_gain	0.9600
18:77272970:TGTCT:T	donor_gain	0.9600
18:77268583:A:AG	acceptor_gain	0.9500
18:77268584:G:GG	acceptor_gain	0.9500
18:77273011:G:GT	donor_gain	0.9500
18:77251226:T:TA	donor_gain	0.9400
18:77256149:GTCTT:G	acceptor_loss	0.9400
18:77256150:TCTTT:T	acceptor_loss	0.9400
18:77256151:CTTTC:C	acceptor_loss	0.9400
18:77256152:TTTCA:T	acceptor_loss	0.9400
18:77256153:TTCA:T	acceptor_loss	0.9400
18:77256154:TCAGG:T	acceptor_loss	0.9400

AlphaMissense

2277 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
18:77268618:T:C	F256L	1.000
18:77268620:T:A	F256L	1.000
18:77268620:T:G	F256L	1.000
18:77250687:G:C	G47R	0.999
18:77250778:T:C	L77P	0.999
18:77250790:A:C	D81A	0.999
18:77250851:G:C	W101C	0.999
18:77250851:G:T	W101C	0.999
18:77250912:A:C	S122R	0.999
18:77250914:C:A	S122R	0.999
18:77250914:C:G	S122R	0.999
18:77251121:G:C	W191C	0.999
18:77251121:G:T	W191C	0.999
18:77250701:C:A	N51K	0.998
18:77250701:C:G	N51K	0.998
18:77250776:C:A	N76K	0.998
18:77250776:C:G	N76K	0.998
18:77250780:A:C	S78R	0.998
18:77250782:C:A	S78R	0.998
18:77250782:C:G	S78R	0.998
18:77250789:G:C	D81H	0.998
18:77250790:A:G	D81G	0.998
18:77250790:A:T	D81V	0.998
18:77250791:C:A	D81E	0.998
18:77250791:C:G	D81E	0.998
18:77250871:G:A	C108Y	0.998
18:77250946:G:C	R133P	0.998
18:77251026:T:A	W160R	0.998
18:77251026:T:C	W160R	0.998
18:77251107:T:A	C187S	0.998

dbSNP variants (sampled 300 via entrez): RS1000033950 (18:77249962 C>T), RS1000085508 (18:77272351 G>A), RS1000118481 (18:77272695 G>A), RS1000252387 (18:77271263 A>C,G), RS1000297792 (18:77252473 A>C,T), RS1000582822 (18:77250423 G>A,T), RS1000748429 (18:77262237 T>G), RS1001086057 (18:77273805 G>A), RS1001091488 (18:77268570 C>G,T), RS1001118405 (18:77256706 C>T), RS1001338508 (18:77267872 G>A), RS1001394025 (18:77253131 G>T), RS1001409979 (18:77260742 T>C), RS1001426891 (18:77252772 C>G), RS1001549933 (18:77256514 T>A,C)

Disease associations

OMIM: gene MIM:600377 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

10 associations (top):

Study	Trait	p-value
GCST001762_914	Obesity-related traits	7.000000e-06
GCST004267_8	Blood osmolality (transformed sodium)	3.000000e-07
GCST008839_447	Height	1.000000e-09
GCST009399_2	Smoking initiation (ever regular vs never regular)	2.000000e-08
GCST009698_57	Metabolite levels	9.000000e-09
GCST90000025_663	Appendicular lean mass	2.000000e-17
GCST90020024_526	A body shape index	4.000000e-09
GCST90020025_1477	Waist-to-hip ratio adjusted for BMI	1.000000e-08
GCST90020027_187	Waist-hip index	6.000000e-09
GCST90093090_11	DHEAS levels	4.000000e-08

EFO canonical traits (5, from GWAS)

EFO ID	Trait name
EFO:0006527	smoking status measurement
EFO:0004980	appendicular lean mass
EFO:0007789	BMI-adjusted waist circumference
EFO:0007788	BMI-adjusted waist-hip ratio
EFO:0007001	dehydroepiandrosterone sulphate measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL4524008 (PROTEIN FAMILY), CHEMBL4894 (SINGLE PROTEIN)

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

PharmGKB clinical annotations

2 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs2717162	Efficacy	3	bupropion	Tobacco Use Disorder
rs2717162	Efficacy	3	nicotine	Tobacco Use Disorder

PharmGKB variants

1 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs2717162	GALR1	3	5.75	2	bupropion;nicotine

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Galanin receptors

Most potent curated ligand interactions (63 total), top 25:

Ligand	Action	Affinity	Parameter
galanin	Full agonist	10.6	pKi
M15	Antagonist	10.57	pKi
galanin	Full agonist	10.51	pKi
M35	Antagonist	10.4	pIC50
[¹²⁵I][Tyr²⁶]galanin (human)	Agonist	10.31	pKd
galanin	Full agonist	10.1	pKi
C7	Antagonist	10.09	pKi
[¹²⁵I][Tyr²⁶]galanin (rat/mouse)	Agonist	9.87	pKd
[¹²⁵I][Tyr²⁶]galanin (pig)	Agonist	9.82	pKd
M32	Antagonist	9.74	pKi
M617	Agonist	9.64	pKi
M242	Agonist	9.6	pKi
galanin(1-19) (human)	Agonist	9.47	pIC50
[Sar¹, D-Ala¹²]galanin(1-16)	Agonist	9.4	pIC50
Gal-(K)4	Agonist	9.4	pKi
M40	Antagonist	9.3	pIC50
Gal-B2-MPEG₄	Agonist	9.3	pKi
galanin(1-16) (rat/mouse/pig)	Agonist	9.22	pIC50
[¹⁹Lys,²⁶Leu]-galparan	Agonist	9.15	pKd
Gal-B2-C₈	Agonist	9.15	pKi
galanin(1-11)	Agonist	8.96	pIC50
Gal-B2-dPEG₂₄	Agonist	8.89	pKi
Gal-B2-C₁₀	Agonist	8.89	pKi
Gal-B2-C₁₂	Agonist	8.85	pKi
galanin(1-15)	Agonist	8.77	pIC50

Binding affinities (BindingDB)

13 measured of 13 human assays (14 total across all organisms); most potent 13 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
M35	KI	0.11 nM
Galanin, Porcine	KI	0.23 nM
CAS_3043476	KI	0.25 nM
M32	KI	0.26 nM
Galanin rat	KI	0.29 nM
Galanin, Human	KI	0.44 nM
Galanin (1-16), rat	KI	2.88 nM
Galanin Porcine 2-29	KI	26.3 nM
Galanin (1-16)	KI	106 nM
M40	KI	109 nM
Galanin (1-13)-SP-(5-11)	KI	256 nM
Galanin [D-Trp2], porcine	KI	631 nM
Galanin (3-29), porcine	KI	1000 nM

ChEMBL bioactivities

109 potent at pChembl≥5 of 117 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
11.00	Ki	0.01	nM	CHEMBL503473
10.52	Ki	0.03	nM	GALANIN
10.52	Ki	0.03	nM	GALANTIDE
10.10	IC50	0.079	nM	CHEMBL506553
10.10	Ki	0.08	nM	CHEMBL604373
10.00	Kd	0.1	nM	CHEMBL503473
10.00	Ki	0.1	nM	CHEMBL604990
9.80	IC50	0.16	nM	GALANIN
9.52	Kd	0.3	nM	GALANTIDE
9.52	Ki	0.3	nM	CHEMBL592413
9.46	Ki	0.35	nM	GALANIN
9.40	Ki	0.4	nM	CHEMBL508036
9.40	Ki	0.4	nM	CHEMBL525055
9.40	Kd	0.4	nM	CHEMBL499179
9.34	Ki	0.46	nM	GALANIN
9.30	Ki	0.5	nM	CHEMBL505299
9.30	Ki	0.5	nM	CHEMBL508083
9.15	Ki	0.7	nM	CHEMBL503900
9.11	IC50	0.77	nM	GALANIN
9.08	IC50	0.84	nM	GALANIN
9.05	Ki	0.9	nM	CHEMBL526500
8.89	Ki	1.3	nM	CHEMBL460706
8.85	Ki	1.4	nM	CHEMBL507733
8.77	Ki	1.7	nM	CHEMBL578317
8.72	Ki	1.9	nM	CHEMBL525755
8.59	Ki	2.6	nM	CHEMBL524678
8.55	Ki	2.8	nM	CHEMBL499807
8.49	Kd	3.2	nM	CHEMBL499980
8.48	Ki	3.3	nM	CHEMBL1790054
8.46	Ki	3.5	nM	CHEMBL507353
8.46	Ki	3.5	nM	CHEMBL525023
8.46	Ki	3.5	nM	CHEMBL578514
8.42	Ki	3.8	nM	CHEMBL2324950
8.40	Ki	4	nM	CHEMBL450827
8.28	Ki	5.3	nM	CHEMBL499807
8.22	Ki	6	nM	CHEMBL504914
7.96	Ki	11	nM	CHEMBL578910
7.67	Ki	21.5	nM	CHEMBL504758
7.59	Ki	25.5	nM	CHEMBL507373
7.59	Ki	25.5	nM	CHEMBL501306
7.43	Ki	37.5	nM	CHEMBL2324949
7.38	Ki	41.5	nM	CHEMBL526889
7.29	Ki	51	nM	CHEMBL592415
7.07	Ki	85	nM	CHEMBL526862
6.72	IC50	190	nM	CHEMBL3906195
6.58	IC50	260	nM	CHEMBL3941767
6.51	Ki	306.5	nM	CHEMBL524892
6.44	Ki	364.5	nM	CHEMBL604991
6.43	IC50	371	nM	CHEMBL3955764
6.41	Ki	387	nM	CHEMBL506495

PubChem BioAssay actives

70 with measured affinity, of 255 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,3R)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[(2S)-2-[(2S)-2-[[2-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-amino-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]butanediamide	459286: Binding affinity to human GalR1	ki	<0.0001	uM
(2S)-2-[[(2S)-1-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]propanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-N-[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1,5-dioxopentan-2-yl]pentanediamide	459286: Binding affinity to human GalR1	ki	<0.0001	uM
(3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]propanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]propanoyl]amino]-3-methylpentanoyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-[[(2S)-6-amino-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-oxobutanoic acid	459286: Binding affinity to human GalR1	ki	<0.0001	uM
(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[(2S)-2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]butanediamide	459286: Binding affinity to human GalR1	ki	0.0001	uM
(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-1-[(2R)-2-[[(2S)-1-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]propanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-N-[(2S)-5-amino-1-[[(2R)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]pentanediamide	459286: Binding affinity to human GalR1	ki	0.0001	uM
(3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]propanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]acetyl]amino]-4-oxobutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-4-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[2-[[(2S)-1-[[(2S,3R)-1-[[(1S)-1-carboxy-2-hydroxyethyl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-oxobutanoic acid	1336325: Displacement of [125I]galanin from human recombinant GAL1 receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method	ic50	0.0001	uM
(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]propanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-N-[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]pentanediamide	459286: Binding affinity to human GalR1	ki	0.0003	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S,3R)-3-hydroxy-2-[[(2S)-3-(1H-indol-3-yl)-2-[[2-(methylamino)acetyl]amino]propanoyl]amino]butanoyl]amino]-4-methylpentanoyl]amino]butanediamide	413945: Displacement of europium-labeled galanin from human GalR1 expressed in HEK293 EBNA cells	ki	0.0004	uM
[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl] 2-(methylamino)acetate	370752: Displacement of europium labeled galanin from human recombinant GalR1 receptor by time-resolved fluorescence binding assay	ki	0.0004	uM
(3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]propanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]acetyl]amino]-4-oxobutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-4-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[2-[[(2S)-1-[[(1S,2R)-1-carboxy-2-hydroxypropyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-oxobutanoic acid	413940: Binding affinity to human GalR1	kd	0.0004	uM
[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-6-[[2-[2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethoxy]acetyl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl] 2-(methylamino)acetate	370752: Displacement of europium labeled galanin from human recombinant GalR1 receptor by time-resolved fluorescence binding assay	ki	0.0005	uM
(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]butanediamide	413945: Displacement of europium-labeled galanin from human GalR1 expressed in HEK293 EBNA cells	ki	0.0005	uM
[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-6-(octanoylamino)-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl] 2-(methylamino)acetate	370752: Displacement of europium labeled galanin from human recombinant GalR1 receptor by time-resolved fluorescence binding assay	ki	0.0007	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2R)-2-[[(2R)-6-amino-1-[[(2S)-6-amino-1-[[(2R)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-6-(hexadecanoylamino)-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S,3R)-3-hydroxy-2-[[(2S)-3-(1H-indol-3-yl)-2-[[2-(methylamino)acetyl]amino]propanoyl]amino]butanoyl]amino]-4-methylpentanoyl]amino]butanediamide	413945: Displacement of europium-labeled galanin from human GalR1 expressed in HEK293 EBNA cells	ki	0.0009	uM
[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-6-(decanoylamino)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl] 2-(methylamino)acetate	370752: Displacement of europium labeled galanin from human recombinant GalR1 receptor by time-resolved fluorescence binding assay	ki	0.0013	uM
[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-6-(dodecanoylamino)-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl] 2-(methylamino)acetate	370752: Displacement of europium labeled galanin from human recombinant GalR1 receptor by time-resolved fluorescence binding assay	ki	0.0014	uM
(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-acetamido-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-6-(hexadecanoylamino)-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]butanediamide	459291: Displacement of Eu-labeled galanin from human GalR1 by DELFIA competitive assay	ki	0.0017	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-amino-6-(hexadecanoylamino)-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S,3R)-3-hydroxy-2-[[(2S)-3-(1H-indol-3-yl)-2-[[2-(methylamino)acetyl]amino]propanoyl]amino]butanoyl]amino]-4-methylpentanoyl]amino]butanediamide	413945: Displacement of europium-labeled galanin from human GalR1 expressed in HEK293 EBNA cells	ki	0.0019	uM
[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxo-6-(tetradecanoylamino)hexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl] 2-(methylamino)acetate	370752: Displacement of europium labeled galanin from human recombinant GalR1 receptor by time-resolved fluorescence binding assay	ki	0.0026	uM
(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-6-(hexadecanoylamino)-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]butanediamide	459291: Displacement of Eu-labeled galanin from human GalR1 by DELFIA competitive assay	ki	0.0028	uM
(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]propanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]propanoyl]amino]-3-methylpentanoic acid	413940: Binding affinity to human GalR1	kd	0.0032	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-5-carbamimidamido-1-oxopentan-2-yl]amino]-6-(hexadecanoylamino)-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S,3R)-3-hydroxy-2-[[(2S)-3-(1H-indol-3-yl)-2-[[2-(methylamino)acetyl]amino]propanoyl]amino]butanoyl]amino]-4-methylpentanoyl]amino]butanediamide	413945: Displacement of europium-labeled galanin from human GalR1 expressed in HEK293 EBNA cells	ki	0.0033	uM
(2S)-6-amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-1-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-3-hydroxy-2-[[(2S)-3-(1H-indol-3-yl)-2-[[2-(methylamino)acetyl]amino]propanoyl]amino]butanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]propanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]hexanoyl]amino]hexanoyl]amino]-6-(hexadecanoylamino)hexanoyl]amino]hexanoic acid	459286: Binding affinity to human GalR1	ki	0.0035	uM
[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-6-(hexadecanoylamino)-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl] 2-(methylamino)acetate	370752: Displacement of europium labeled galanin from human recombinant GalR1 receptor by time-resolved fluorescence binding assay	ki	0.0035	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-6-(hexadecanoylamino)-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S,3R)-3-hydroxy-2-[[(2S)-3-(1H-indol-3-yl)-2-[[2-(methylamino)acetyl]amino]propanoyl]amino]butanoyl]amino]-4-methylpentanoyl]amino]butanediamide	413945: Displacement of europium-labeled galanin from human GalR1 expressed in HEK293 EBNA cells	ki	0.0035	uM
(2S)-N-[(2S)-3-hydroxy-1-[[(2S)-1-[[2-[[(2S)-3-(4-hydroxyphenyl)-1-[[(2S)-4-methyl-1-[[(2S)-4-methyl-1-oxo-1-[[2-oxo-2-[(2S)-2-[[(3S,6S,9S,12S,16Z,21S)-3,6,9-tris(4-aminobutyl)-21-[[(2S)-1,6-diamino-1-oxohexan-2-yl]carbamoyl]-12,21-dimethyl-2,5,8,11-tetraoxo-1,4,7,10-tetrazacyclohenicos-16-en-12-yl]carbamoyl]pyrrolidin-1-yl]ethyl]amino]pentan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S,3R)-3-hydroxy-2-[[(2S)-3-(1H-indol-3-yl)-2-[[2-(methylamino)acetyl]amino]propanoyl]amino]butanoyl]amino]-4-methylpentanoyl]amino]butanediamide	726398: Displacement of euporium-galanin from human GalR1 after 1.5 hrs by DELFIA assay	ki	0.0038	uM
[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-6-(octadecanoylamino)-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl] 2-(methylamino)acetate	370752: Displacement of europium labeled galanin from human recombinant GalR1 receptor by time-resolved fluorescence binding assay	ki	0.0040	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-6-(hexadecanoylamino)-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S,3R)-3-hydroxy-2-[[(2S)-3-(1H-indol-3-yl)-2-[[2-(methylamino)acetyl]amino]propanoyl]amino]butanoyl]amino]-4-methylpentanoyl]amino]butanediamide	413945: Displacement of europium-labeled galanin from human GalR1 expressed in HEK293 EBNA cells	ki	0.0060	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-6-(hexadecanoylamino)-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]butanediamide	459291: Displacement of Eu-labeled galanin from human GalR1 by DELFIA competitive assay	ki	0.0110	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-6-(hexadecanoylamino)-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-(6-aminohexanoylamino)-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]butanediamide	413945: Displacement of europium-labeled galanin from human GalR1 expressed in HEK293 EBNA cells	ki	0.0215	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-6-(hexadecanoylamino)-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S,3R)-3-hydroxy-2-[[(2S)-3-(1H-indol-3-yl)-2-[[2-(methylamino)acetyl]amino]propanoyl]amino]butanoyl]amino]-4-methylpentanoyl]amino]butanediamide	413945: Displacement of europium-labeled galanin from human GalR1 expressed in HEK293 EBNA cells	ki	0.0255	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-6-(hexadecanoylamino)-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S,3R)-3-hydroxy-2-[[(2S)-3-(1H-indol-3-yl)-2-[[2-(methylamino)acetyl]amino]propanoyl]amino]butanoyl]amino]-4-methylpentanoyl]amino]butanediamide	413945: Displacement of europium-labeled galanin from human GalR1 expressed in HEK293 EBNA cells	ki	0.0255	uM
(2S)-N-[(2S)-1-[[(3S,6S,12S,16E,21S)-21-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]carbamoyl]-6-[(4-hydroxyphenyl)methyl]-12,21-dimethyl-3-(2-methylpropyl)-2,5,8,11-tetraoxo-1,4,7,10-tetrazacyclohenicos-16-en-12-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S,3R)-3-hydroxy-2-[[(2S)-3-(1H-indol-3-yl)-2-[[2-(methylamino)acetyl]amino]propanoyl]amino]butanoyl]amino]-4-methylpentanoyl]amino]butanediamide	726398: Displacement of euporium-galanin from human GalR1 after 1.5 hrs by DELFIA assay	ki	0.0375	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-6-(hexadecanoylamino)-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S,3R)-3-hydroxy-2-[[(2S)-3-(1H-indol-3-yl)-2-[[2-(methylamino)acetyl]amino]propanoyl]amino]butanoyl]amino]-4-methylpentanoyl]amino]butanediamide	413945: Displacement of europium-labeled galanin from human GalR1 expressed in HEK293 EBNA cells	ki	0.0415	uM
(3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]propanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]acetyl]amino]-4-oxobutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-4-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[2-[[(2S)-1-[[(2S,3R)-1-[[(1S)-1-carboxy-2-hydroxyethyl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-oxobutanoic acid	459286: Binding affinity to human GalR1	ki	0.0510	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-6-(hexadecanoylamino)-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S,3R)-3-hydroxy-2-[[(2S)-3-(1H-indol-3-yl)-2-[[2-(methylamino)acetyl]amino]propanoyl]amino]butanoyl]amino]-4-methylpentanoyl]amino]butanediamide	413945: Displacement of europium-labeled galanin from human GalR1 expressed in HEK293 EBNA cells	ki	0.0850	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-6-(hexadecanoylamino)-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S,3R)-3-hydroxy-2-[[(2S)-3-(1H-indol-3-yl)-2-[[2-(methylamino)acetyl]amino]propanoyl]amino]butanoyl]amino]-4-methylpentanoyl]amino]butanediamide	413945: Displacement of europium-labeled galanin from human GalR1 expressed in HEK293 EBNA cells	ki	0.3065	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-6-(hexadecanoylamino)-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S,3R)-3-hydroxy-2-[[(2S)-3-(1H-indol-3-yl)-2-(methylamino)propanoyl]amino]butanoyl]amino]-4-methylpentanoyl]amino]butanediamide	459291: Displacement of Eu-labeled galanin from human GalR1 by DELFIA competitive assay	ki	0.3645	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-6-(hexadecanoylamino)-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]butanediamide	413945: Displacement of europium-labeled galanin from human GalR1 expressed in HEK293 EBNA cells	ki	0.3870	uM
(3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]propanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]acetyl]amino]-4-oxobutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-4-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[2-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-oxobutanoic acid	459286: Binding affinity to human GalR1	ki	0.5450	uM
(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]butanediamide	459286: Binding affinity to human GalR1	ki	0.8700	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]propanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoic acid	413940: Binding affinity to human GalR1	kd	0.8790	uM
N-(3-fluoro-2-methylphenyl)-6-piperidin-1-yl-2-[4-[3-(trifluoromethyl)-2-pyridinyl]-1,4-diazepan-1-yl]pyrimidin-4-amine	631990: Displacement of [125I]galanin from GalR1 by gamma counting	ic50	1.3000	uM
tert-butyl 4-[6-(3-fluoro-4-methoxyanilino)-2-(4-methoxyanilino)pyrimidin-4-yl]-1,4-diazepane-1-carboxylate	631990: Displacement of [125I]galanin from GalR1 by gamma counting	ic50	2.8200	uM
N-(4-methoxyphenyl)-6-piperidin-1-yl-2-[4-[3-(trifluoromethyl)-2-pyridinyl]-1,4-diazepan-1-yl]pyrimidin-4-amine	631990: Displacement of [125I]galanin from GalR1 by gamma counting	ic50	3.3500	uM
4-N-(3-fluoro-4-methoxyphenyl)-2-N-(4-methoxyphenyl)-6-(4-pyrimidin-2-ylpiperazin-1-yl)pyrimidine-2,4-diamine	631990: Displacement of [125I]galanin from GalR1 by gamma counting	ic50	3.8400	uM
6-N-(cyclohexylmethyl)-4-N-(3-fluoro-4-methoxyphenyl)-2-N-(4-methoxyphenyl)pyrimidine-2,4,6-triamine	631990: Displacement of [125I]galanin from GalR1 by gamma counting	ic50	3.8400	uM
N-(2,5-dimethylphenyl)-6-piperidin-1-yl-2-[4-[3-(trifluoromethyl)-2-pyridinyl]-1,4-diazepan-1-yl]pyrimidin-4-amine	631990: Displacement of [125I]galanin from GalR1 by gamma counting	ic50	3.9000	uM
4-N-(3-methoxyphenyl)-6-N-(4-methoxyphenyl)-2-pyrrolidin-1-ylpyrimidine-4,6-diamine	631990: Displacement of [125I]galanin from GalR1 by gamma counting	ic50	4.6000	uM
2-N-cyclohexyl-4-N-[3-(difluoromethoxy)phenyl]-6-N-(4-methoxyphenyl)pyrimidine-2,4,6-triamine	631990: Displacement of [125I]galanin from GalR1 by gamma counting	ic50	5.0300	uM

CTD chemical–gene interactions

20 total (human), top 20 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
bisphenol A	decreases methylation, increases expression	2
Phenylmercuric Acetate	affects cotreatment, increases expression	2
ethyl-p-hydroxybenzoate	increases expression	1
terbufos	increases methylation	1
sodium arsenite	increases expression	1
CGP 52608	affects binding, increases reaction	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, increases expression	1
dorsomorphin	affects cotreatment, increases expression	1
bisphenol S	affects cotreatment, increases methylation	1
Resveratrol	affects cotreatment, decreases expression	1
Fulvestrant	affects cotreatment, increases methylation	1
Acetaminophen	decreases expression	1
Benzo(a)pyrene	affects methylation, decreases methylation	1
Fonofos	increases methylation	1
Parathion	increases methylation	1
Plant Extracts	affects cotreatment, decreases expression	1
Rotenone	decreases expression	1
8-Bromo Cyclic Adenosine Monophosphate	increases expression	1
1-Methyl-4-phenylpyridinium	decreases expression	1
Aflatoxin B1	decreases methylation	1

ChEMBL screening assays

41 unique, capped per target: 40 binding, 1 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4880266	Binding	Galanin receptor (h) CEREP ligand profiling	Data for DCP probe ABT-546
CHEMBL1072083	Functional	Agonist activity at human GalR1 expressed in CHO-K1 cells at 1.25 uM by calcium mobilization assay relative to Galanin (1-30)	Engineering galanin analogues that discriminate between GalR1 and GalR2 receptor subtypes and exhibit anticonvulsant activity following systemic delivery. — J Med Chem

Cellosaurus cell lines

4 cell lines: 3 spontaneously immortalized cell line, 1 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_H433	CHO-K1/GAL1/Galpha15	Spontaneously immortalized cell line	Female
CVCL_KV20	cAMP Hunter CHO-K1 GALR1 Gi	Spontaneously immortalized cell line	Female
CVCL_KX09	PathHunter CHO-K1 GALR1 beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_LA33	PathHunter U2OS GALR1 Total GPCR Internalization	Cancer cell line	Female

Clinical trials (associated diseases)

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

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