GALR2

gene

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Also known as GALNR2

Summary

GALR2 (galanin receptor 2, HGNC:4133) is a protein-coding gene on chromosome 17q25.1, encoding Galanin receptor type 2 (O43603). Receptor for the hormone galanin and GALP.

Galanin is an important neuromodulator present in the brain, gastrointestinal system, and hypothalamopituitary axis. It is a 30-amino acid non-C-terminally amidated peptide that potently stimulates growth hormone secretion, inhibits cardiac vagal slowing of heart rate, abolishes sinus arrhythmia, and inhibits postprandial gastrointestinal motility. The actions of galanin are mediated through interaction with specific membrane receptors that are members of the 7-transmembrane family of G protein-coupled receptors. GALR2 interacts with the N-terminal residues of the galanin peptide. The primary signaling mechanism for GALR2 is through the phospholipase C/protein kinase C pathway (via Gq), in contrast to GALR1, which communicates its intracellular signal by inhibition of adenylyl cyclase through Gi. However, it has been demonstrated that GALR2 couples efficiently to both the Gq and Gi proteins to simultaneously activate 2 independent signal transduction pathways.

Source: NCBI Gene 8811 — RefSeq curated summary.

At a glance

Clinical variants (ClinVar): 87 total — 2 pathogenic
Druggable target: yes
MANE Select transcript: NM_003857

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:4133
Approved symbol	GALR2
Name	galanin receptor 2
Location	17q25.1
Locus type	gene with protein product
Status	Approved
Aliases	GALNR2
Ensembl gene	ENSG00000182687
Ensembl biotype	protein_coding
OMIM	603691
Entrez	8811

Gene structure

Transcript identifiers

Ensembl transcripts: 1 — 1 protein_coding

ENST00000329003

RefSeq mRNA: 1 — MANE Select: NM_003857 NM_003857

CCDS: CCDS11739

Canonical transcript exons

ENST00000329003 — 2 exons

Exon	Start	End
ENSE00001297642	76076636	76077537
ENSE00001324448	76074781	76075251

Expression profiles

Bgee: expression breadth broad, 84 present calls, max score 70.93.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.2048 / max 26.1329, expressed in 84 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
162817	0.2048	84

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
muscle layer of sigmoid colon	UBERON:0035805	70.93	gold quality
sigmoid colon	UBERON:0001159	65.27	gold quality
lower esophagus mucosa	UBERON:0035834	62.63	gold quality
colon	UBERON:0001155	57.91	gold quality
buccal mucosa cell	CL:0002336	57.74	gold quality
large intestine	UBERON:0000059	56.98	gold quality
transverse colon	UBERON:0001157	56.23	gold quality
oviduct epithelium	UBERON:0004804	55.50	gold quality
esophagus mucosa	UBERON:0002469	54.41	gold quality
bone marrow cell	CL:0002092	54.21	gold quality
intestine	UBERON:0000160	54.21	gold quality
tendon of biceps brachii	UBERON:0008188	51.88	gold quality
smooth muscle tissue	UBERON:0001135	51.31	gold quality
medial globus pallidus	UBERON:0002477	50.81	gold quality
frontal pole	UBERON:0002795	50.41	gold 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
quadriceps femoris	UBERON:0001377	49.89	gold quality
granulocyte	CL:0000094	49.75	silver quality
monocyte	CL:0000576	49.59	silver quality
mononuclear cell	CL:0000842	49.58	silver quality
Brodmann (1909) area 46	UBERON:0006483	49.30	gold quality
blood vessel layer	UBERON:0004797	49.29	gold quality
cerebellar vermis	UBERON:0004720	49.25	gold quality
cervix squamous epithelium	UBERON:0006922	49.20	gold quality
leukocyte	CL:0000738	49.19	silver quality
hair follicle	UBERON:0002073	49.18	gold quality
vastus lateralis	UBERON:0001379	49.11	gold quality
thymus	UBERON:0002370	48.95	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	no	1.22

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

6 targeting GALR2, 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-6867-5P	100.00	82.21	3464
HSA-MIR-224-3P	98.91	68.42	1815
HSA-MIR-522-3P	98.91	68.56	1817
HSA-MIR-5087	98.01	69.09	965
HSA-MIR-6818-5P	97.50	67.10	1167
HSA-MIR-210-3P	92.54	65.16	165

Literature-anchored findings (GeneRIF, showing 17)

Elevated expression of galanin receptors in childhood neuroblastic tumors (PMID:11867941)
study indicates that a high level of GalR2 galanin receptor expression is able to inhibit cell proliferation and induce apoptosis in neuroblastoma cells (PMID:14592962)
There was no effect of GALR2 on alcoholism risk. (PMID:17083333)
point to GalR2 as a possible target for therapeuthic interventions in pheochromocytoma (PMID:18272487)
galanin receptor 2 promotes cell proliferation and survival, and promotes tumor growth, consistent with an oncogenic role for GALR2 in squamous cell carcinoma of the head and neck (PMID:21345369)
The expression of GALR2 mRNA is lost in head and neck squamous cell carcinoma as a consequence of DNA methylation.Silencing of the GALR2 gene by methylation may be a critical event in head and neck squamous cell carcinoma. (PMID:24122450)
In HEp-2 cells, GALR2-mediated apoptosis was caspase-independent. (PMID:24168112)
Data from ligand-receptor interaction studies suggest that human spexin-1 and zebrafish spexin-2 activate galanin receptors GALR2/GALR3 (but not GALR1); thus spexins appear to be natural ligands for human/Xenopus/zebrafish GALR2/GALR3. (PMID:24517231)
The G protein-coupled receptor GALR2 promotes angiogenesis in head and neck cancer (PMID:24568968)
Activation of GalR2 leads to elevation of intracellular Ca(2+) due to Ca(2+) efflux from endoplasmic reticulum through IP3R sequentially opening BK alpha channels. (PMID:24602615)
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)
Study provides evidence that GAL and GALR1/2 genes were identified as aberrantly methylated in head and neck squamous cell carcinoma. (PMID:27685843)
Low GALR2 expression is associated with gastric cancer. (PMID:30616468)
molecular structures that confer ligand selectivity for galanin type II and III receptors (PMID:32231393)
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)
Structure of the human galanin receptor 2 bound to galanin and Gq reveals the basis of ligand specificity and how binding affects the G-protein interface. (PMID:35913979)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	galr2a	ENSDARG00000020853
mus_musculus	Galr2	ENSMUSG00000020793
rattus_norvegicus	Galr2	ENSRNOG00000061733
drosophila_melanogaster	AstA-R2	FBGN0039595
drosophila_melanogaster	AstA-R1	FBGN0266429

Paralogs (23): CCR6 (ENSG00000112486), CCRL2 (ENSG00000121797), CCR2 (ENSG00000121807), CXCR4 (ENSG00000121966), CCR7 (ENSG00000126353), ACKR4 (ENSG00000129048), ACKR3 (ENSG00000144476), ACKR2 (ENSG00000144648), RGR (ENSG00000148604), CXCR5 (ENSG00000160683), CCR5 (ENSG00000160791), CXCR1 (ENSG00000163464), CCR1 (ENSG00000163823), CX3CR1 (ENSG00000168329), CXCR6 (ENSG00000172215), XCR1 (ENSG00000173578), CCR9 (ENSG00000173585), CCR8 (ENSG00000179934), CXCR2 (ENSG00000180871), CCR3 (ENSG00000183625), CCR4 (ENSG00000183813), CCR10 (ENSG00000184451), CXCR3 (ENSG00000186810)

Protein

Protein identifiers

Galanin receptor type 2 — O43603 (reviewed: O43603)

All UniProt accessions (1): O43603

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for the hormone galanin and GALP. Receptor for the hormone spexin-1. The activity of this receptor is mediated by G proteins that activate the phospholipase C/protein kinase C pathway (via G(q)) and that inhibit adenylyl cyclase (via G(i)).

Subcellular location. Cell membrane.

Tissue specificity. Expressed abundantly within the central nervous system in both hypothalamus and hippocampus. In peripheral tissues, the strongest expression was observed in heart, kidney, liver, and small intestine.

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

RefSeq proteins (1): NP_003848* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000405	Galanin_rcpt	Family
IPR003907	GAL2_rcpt	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (39 total): helix 13, topological domain 8, transmembrane region 7, strand 4, turn 3, glycosylation site 2, chain 1, disulfide bond 1

Structure

Experimental structures (PDB)

4 structures.

PDB	Method	Resolution (Å)
7WQ4	ELECTRON MICROSCOPY	2.6
7XBD	ELECTRON MICROSCOPY	3.11
7XJK	ELECTRON MICROSCOPY	3.3
7XJL	ELECTRON MICROSCOPY	3.5

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-O43603-F1	79.47	0.55

Antibody-complex structures (SAbDab): 4 — 7WQ4, 7XBD, 7XJK, 7XJL

Functional residue map

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

Disulfide bonds (1): 98–175

Glycosylation sites (2): 2, 11

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: 109 (showing top): GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, BENPORATH_ES_WITH_H3K27ME3, GOBP_COGNITION, GOBP_PHOSPHATIDYLINOSITOL_METABOLIC_PROCESS, GOBP_BEHAVIOR, PEREZ_TP63_TARGETS, GOBP_INOSITOL_PHOSPHATE_METABOLIC_PROCESS, GOBP_POLYOL_METABOLIC_PROCESS, GOBP_NEUROGENESIS, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, GOBP_GLYCEROLIPID_METABOLIC_PROCESS, GOBP_ADENYLATE_CYCLASE_MODULATING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, GOBP_MUSCLE_CONTRACTION, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION

GO Biological Process (15): muscle contraction (GO:0006936), adenylate cyclase-modulating G protein-coupled receptor signaling pathway (GO:0007188), adenylate cyclase-activating G protein-coupled receptor signaling pathway (GO:0007189), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), positive regulation of cytosolic calcium ion concentration (GO:0007204), learning or memory (GO:0007611), feeding behavior (GO:0007631), neuron projection development (GO:0031175), inositol phosphate metabolic process (GO:0043647), positive regulation of transcription by RNA polymerase II (GO:0045944), phosphatidylinositol metabolic process (GO:0046488), galanin-activated signaling pathway (GO:0090663), signal transduction (GO:0007165), G protein-coupled receptor signaling pathway (GO:0007186), negative regulation of adenylate cyclase activity (GO:0007194)

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 (3): plasma membrane (GO:0005886), cilium (GO:0005929), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-2 pathways:

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

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
G protein-coupled receptor signaling pathway	3
adenylate cyclase activity	2
behavior	2
muscle system process	1
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	1
adenylate cyclase activator activity	1
phospholipase C activator activity	1
regulation of biological quality	1
cognition	1
neuron development	1
plasma membrane bounded cell projection organization	1
organophosphate metabolic process	1
polyol metabolic process	1
regulation of transcription by RNA polymerase II	1
transcription by RNA polymerase II	1
positive regulation of DNA-templated transcription	1
phosphorus metabolic process	1
neuropeptide signaling pathway	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
negative regulation of catalytic activity	1
regulation of adenylate cyclase activity	1
neuropeptide receptor activity	1
hormone binding	1
peptide binding	1
transmembrane signaling receptor activity	1
binding	1
membrane	1
cell periphery	1
intraciliary transport particle	1
membrane-bounded organelle	1
plasma membrane bounded cell projection	1
cellular anatomical structure	1

Protein interactions and networks

STRING

560 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
GALR2	GAL	P22466	999
GALR2	GALP	Q9UBC7	970
GALR2	SPX	Q9BT56	926
GALR2	FFAR1	O14842	829
GALR2	ZACN	Q401N2	819
GALR2	GALR1	P47211	810
GALR2	CD22	P20273	769
GALR2	NPY	P01303	685
GALR2	LGALS2	P05162	604
GALR2	EXOC7	Q9UPT5	542
GALR2	TAC1	P20366	538
GALR2	HTR1A	P08908	482
GALR2	CRHR2	Q13324	452
GALR2	DRD2	P14416	445
GALR2	NPY5R	Q15761	442

IntAct

4 interactions, top by confidence:

A	B	Type	Score
GALR2	GAL	psi-mi:“MI:0915”(physical association)	0.400
GAL	GALR2	psi-mi:“MI:0915”(physical association)	0.400
NPY1R	GALR2	psi-mi:“MI:2364”(proximity)	0.270

BioGRID (1): GALR2 (Positive Genetic)

ESM2 similar proteins: A0A6I8PUB9, O00155, O00270, O14842, O14843, O15529, O43603, O46685, O60755, O88626, O88634, O88853, O88854, O88855, P0C5I1, P46092, P46093, P50132, Q149R9, Q15722, Q15743, Q1JQB3, Q3T181, Q3UFD7, Q3ZC80, Q4KLH9, Q6XKD3, Q76JU8, Q76JU9, Q76JV1, Q86VZ1, Q8BUD0, Q8BYC4, Q8HYC3, Q8K3T4, Q8TDS5, Q8TDU9, Q920E0, Q924U0, Q96G91

Diamond homologs: A0A4W3GG95, A0A6I8PUB9, B2GV46, B5X337, D4A7K7, E7FEL0, E9QJ73, F8VQN3, O00270, O08726, O08858, O14842, O14843, O15529, O42179, O43603, O46685, O60755, O77408, O88410, O88626, O88634, O88853, P21109, P23944, P25024, P25025, P35344, P35383, P35414, P41231, P41232, P46092, P46093, P49652, P49682, P49683, P50132, P51675, P51679

SIGNOR signaling

11 interactions.

A	Effect	B	Mechanism
GALR2	“up-regulates activity”	GNAI1	binding
GALR2	“up-regulates activity”	GNAI3	binding
GALR2	“up-regulates activity”	GNAQ	binding
GALR2	“up-regulates activity”	GNA14	binding
GALR2	“up-regulates activity”	GNA15	binding
GALR2	“up-regulates activity”	GNA12	binding
GALR2	“up-regulates activity”	GNA13	binding
Galanin	“up-regulates activity”	GALR2	“chemical activation”
SPX	“up-regulates activity”	GALR2	binding
GAL	up-regulates	GALR2	binding
GALP	up-regulates	GALR2	binding

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	2
Likely pathogenic	0
Uncertain significance	72
Likely benign	7
Benign	2

Top pathogenic / likely-pathogenic (2)

Variant ID	HGVS	Classification
2582671	NM_014230.4(SRP68):c.184+2T>C	Pathogenic
2582672	NC_000017.11:g.(76070445_76072307)(76072518?)del	Pathogenic

SpliceAI

134 predictions. Top by Δscore:

Variant	Effect	Δscore
17:76075250:AGG:A	donor_loss	1.0000
17:76075251:GGT:G	donor_loss	1.0000
17:76075252:G:GG	donor_gain	1.0000
17:76075252:GTG:G	donor_loss	1.0000
17:76075253:T:A	donor_loss	1.0000
17:76075247:GACAG:G	donor_gain	0.9900
17:76076622:C:CA	acceptor_gain	0.9900
17:76075248:ACAG:A	donor_gain	0.9600
17:76076630:CCGCA:C	acceptor_loss	0.9600
17:76076631:CGCAG:C	acceptor_loss	0.9600
17:76076632:GCA:G	acceptor_loss	0.9600
17:76076633:CA:C	acceptor_loss	0.9600
17:76076634:AGGT:A	acceptor_loss	0.9600
17:76076635:G:A	acceptor_loss	0.9600
17:76075250:AG:A	donor_gain	0.9500
17:76075251:GG:G	donor_gain	0.9500
17:76076627:T:TA	acceptor_gain	0.9500
17:76076271:T:TA	donor_gain	0.9400
17:76076272:A:AA	donor_gain	0.9400
17:76076635:GGT:G	acceptor_gain	0.9400
17:76076623:G:A	acceptor_gain	0.9300
17:76075249:CAG:C	donor_gain	0.9200
17:76076622:C:A	acceptor_loss	0.9000
17:76075054:C:A	donor_gain	0.8800
17:76076266:G:GG	donor_gain	0.8800
17:76076265:A:AG	donor_gain	0.8500
17:76076631:C:A	acceptor_gain	0.8200
17:76076634:A:AG	acceptor_gain	0.8000
17:76076635:G:GG	acceptor_gain	0.8000
17:76076269:G:A	donor_gain	0.7700

AlphaMissense

2462 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
17:76075156:G:C	W91C	0.998
17:76075156:G:T	W91C	0.998
17:76075081:C:A	N66K	0.997
17:76075081:C:G	N66K	0.997
17:76075217:A:C	S112R	0.997
17:76075219:C:A	S112R	0.997
17:76075219:C:G	S112R	0.997
17:76075176:G:A	C98Y	0.996
17:76075251:G:T	R123M	0.996
17:76077000:T:C	F245L	0.996
17:76077002:C:A	F245L	0.996
17:76077002:C:G	F245L	0.996
17:76075095:A:C	D71A	0.995
17:76075095:A:T	D71V	0.995
17:76075175:T:A	C98S	0.995
17:76075176:G:C	C98S	0.995
17:76075220:A:C	S113R	0.995
17:76075222:C:A	S113R	0.995
17:76075222:C:G	S113R	0.995
17:76077131:C:A	N288K	0.995
17:76077131:C:G	N288K	0.995
17:76075095:A:G	D71G	0.994
17:76075096:C:A	D71E	0.994
17:76075096:C:G	D71E	0.994
17:76075227:C:A	T115K	0.994
17:76076715:T:A	W150R	0.994
17:76076715:T:C	W150R	0.994
17:76076790:T:A	C175S	0.994
17:76076790:T:C	C175R	0.994
17:76076791:G:C	C175S	0.994

dbSNP variants (sampled 300 via entrez): RS1000061016 (17:76075776 T>C), RS1000512849 (17:76074359 A>T), RS1000929308 (17:76072066 C>A,T), RS1001156691 (17:76077516 C>A,G,T), RS1001201583 (17:76077970 G>GA,GC,GCGGAT,GT), RS1001351674 (17:76072695 G>A,C,T), RS1002359297 (17:76071245 G>C), RS1003071581 (17:76073899 A>G), RS1003202634 (17:76075587 T>A), RS1003482215 (17:76071563 T>C), RS1003554812 (17:76073174 C>T), RS1003814784 (17:76071892 A>G), RS1004247584 (17:76073002 G>A,C), RS1004636931 (17:76071139 A>G), RS1004703699 (17:76075486 GC>G)

Disease associations

OMIM: gene MIM:603691 | disease phenotypes: MIM:620534

GenCC curated gene-disease

Mondo (1): neutropenia, severe congenital, 10, autosomal recessive (MONDO:0957809)

Orphanet (0):

HPO phenotypes

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

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL3176 (SINGLE PROTEIN), CHEMBL4524008 (PROTEIN FAMILY)

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Galanin receptors

Most potent curated ligand interactions (73 total), top 25:

Ligand	Action	Affinity	Parameter
[¹²⁵I][Tyr²⁶]galanin (human)	Agonist	9.62	pKd
[¹²⁵I][Tyr²⁶]galanin (pig)	Agonist	9.51	pKd
CYM2503	Positive	9.16	pEC50
galanin(1-20) (human)	Agonist	9.11	pKi
galanin	Full agonist	9.07	pKi
galanin(2-29) (rat/mouse)	Full agonist	9.04	pKi
M15	Antagonist	8.97	pKi
galanin	Full agonist	8.81	pKi
galanin(1-11)	Agonist	8.78	pIC50
[Sar¹, D-Ala¹²]galanin(1-16)	Agonist	8.76	pIC50
M35	Antagonist	8.74	pKi
galanin(2-30) (human)	Full agonist	8.74	pKi
galanin(1-16) (rat/mouse/pig)	Agonist	8.66	pIC50
galanin-like peptide	Agonist	8.62	pEC50
galanin(2-29) (pig)	Full agonist	8.54	pKi
galanin(1-15)	Agonist	8.46	pKi
M32	Antagonist	8.37	pEC50
galanin(1-19) (rat/mouse)	Agonist	8.33	pKi
J20 (galanin analogue)	Agonist	8.31	pKi
M1153	Agonist	8.3	pKi
M617	Agonist	8.24	pKi
M242	Agonist	8.23	pKi
galanin(1-12)	Agonist	8.19	pKi
M1145	Full agonist	8.18	pKi
[D-Trp²]galanin-(1-29)	Full agonist	8.15	pKi

Binding affinities (BindingDB)

11 measured of 11 human assays (12 total across all organisms); most potent 11 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
M40	KI	109 nM
Galanin [D-Trp2], porcine	KI	631 nM
Galanin (3-29), porcine	KI	1000 nM

ChEMBL bioactivities

95 potent at pChembl≥5 of 110 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.72	IC50	0.19	nM	CHEMBL4128926
9.22	Ki	0.6	nM	CHEMBL604373
9.10	IC50	0.8	nM	GALANIN
9.05	Ki	0.9	nM	GALANIN
9.00	Kd	1	nM	GALANTIDE
8.96	Ki	1.1	nM	GALANTIDE
8.85	Ki	1.4	nM	CHEMBL592413
8.82	Ki	1.5	nM	CHEMBL604990
8.76	Ki	1.74	nM	CHEMBL578710
8.74	Kd	1.8	nM	WTLNSAGYLL
8.74	Ki	1.8	nM	CHEMBL503473
8.70	Kd	2	nM	CHEMBL503473
8.64	Kd	2.3	nM	CHEMBL499179
8.62	Ki	2.4	nM	GALANIN
8.59	IC50	2.6	nM	GALANIN
8.59	IC50	2.6	nM	CHEMBL506553
8.49	Ki	3.2	nM	GALANIN
8.46	IC50	3.5	nM	GALANIN
8.30	Kd	5	nM	CHEMBL499980
8.01	Ki	9.8	nM	CHEMBL592415
7.89	Ki	13	nM	CHEMBL508083
7.84	Ki	14.4	nM	CHEMBL460706
7.83	Ki	14.9	nM	CHEMBL503900
7.82	Ki	15	nM	CHEMBL450827
7.82	Ki	15	nM	CHEMBL526500
7.81	Ki	15.6	nM	CHEMBL2324950
7.80	Ki	15.9	nM	CHEMBL578317
7.79	Ki	16.1	nM	CHEMBL507733
7.76	Ki	17.5	nM	CHEMBL499807
7.74	Ki	18.2	nM	CHEMBL524678
7.70	Ki	20.2	nM	CHEMBL604991
7.69	Ki	20.5	nM	CHEMBL505299
7.66	Ki	22	nM	CHEMBL525755
7.65	Ki	22.5	nM	CHEMBL499807
7.62	Ki	24	nM	CHEMBL508036
7.62	Ki	24	nM	CHEMBL525055
7.55	Ki	28	nM	CHEMBL504914
7.46	Ki	35	nM	CHEMBL578910
7.32	Ki	48	nM	CHEMBL506495
7.29	Ki	51.5	nM	CHEMBL507353
7.29	Ki	51.5	nM	CHEMBL525023
7.29	Ki	51	nM	CHEMBL504758
7.29	Ki	51.5	nM	CHEMBL578514
7.28	Ki	52	nM	CHEMBL578514
7.18	Ki	65.5	nM	CHEMBL1790054
7.12	Ki	75	nM	CHEMBL507373
6.97	Ki	108	nM	CHEMBL501306
6.92	Ki	119	nM	CHEMBL2324949
6.80	Ki	160	nM	CHEMBL526862
6.67	Ki	214.5	nM	CHEMBL526889

PubChem BioAssay actives

87 with measured affinity, of 240 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
3-[[5-[4-(tert-butylsulfamoyl)naphthalen-1-yl]-4-(cyclohexylmethyl)-1,3-thiazole-2-carbonyl]amino]cyclobutane-1-carboxylic acid	1494744: Displacement of [125I]-endothelin-1 from human recombinant GAL2 receptor after 120 mins by scintillation counting analysis	ic50	0.0002	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	459287: Binding affinity to human GalR2	ki	0.0006	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	752243: Binding affinity to human GAL2 receptor by radioligand displacement assay	ic50	0.0008	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	413941: Binding affinity to human GalR2	kd	0.0010	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	459287: Binding affinity to human GalR2	ki	0.0014	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	459287: Binding affinity to human GalR2	ki	0.0015	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	459287: Binding affinity to human GalR2	ki	0.0017	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	413941: Binding affinity to human GalR2	kd	0.0018	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-[[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	459287: Binding affinity to human GalR2	ki	0.0018	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	413941: Binding affinity to human GalR2	kd	0.0023	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	1336326: Displacement of [125I]galanin from human recombinant GAL2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ic50	0.0026	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	413941: Binding affinity to human GalR2	kd	0.0050	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	459287: Binding affinity to human GalR2	ki	0.0098	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	413946: Displacement of europium-labeled galanin from human GalR2 expressed in CHO-K1 cells	ki	0.0130	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	370753: Displacement of europium labeled galanin from human recombinant GalR2 receptor by time-resolved fluorescence binding assay	ki	0.0144	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	370753: Displacement of europium labeled galanin from human recombinant GalR2 receptor by time-resolved fluorescence binding assay	ki	0.0149	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	413946: Displacement of europium-labeled galanin from human GalR2 expressed in CHO-K1 cells	ki	0.0150	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	370753: Displacement of europium labeled galanin from human recombinant GalR2 receptor by time-resolved fluorescence binding assay	ki	0.0150	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	726397: Displacement of euporium-galanin from human GalR2 after 1.5 hrs by DELFIA assay	ki	0.0156	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	459292: Displacement of Eu-labeled galanin from human GalR2 by DELFIA competitive assay	ki	0.0159	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	370753: Displacement of europium labeled galanin from human recombinant GalR2 receptor by time-resolved fluorescence binding assay	ki	0.0161	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	459292: Displacement of Eu-labeled galanin from human GalR2 by DELFIA competitive assay	ki	0.0175	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	370753: Displacement of europium labeled galanin from human recombinant GalR2 receptor by time-resolved fluorescence binding assay	ki	0.0182	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	459292: Displacement of Eu-labeled galanin from human GalR2 by DELFIA competitive assay	ki	0.0202	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	370753: Displacement of europium labeled galanin from human recombinant GalR2 receptor by time-resolved fluorescence binding assay	ki	0.0205	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	413946: Displacement of europium-labeled galanin from human GalR2 expressed in CHO-K1 cells	ki	0.0220	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	413946: Displacement of europium-labeled galanin from human GalR2 expressed in CHO-K1 cells	ki	0.0240	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	370753: Displacement of europium labeled galanin from human recombinant GalR2 receptor by time-resolved fluorescence binding assay	ki	0.0240	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	413946: Displacement of europium-labeled galanin from human GalR2 expressed in CHO-K1 cells	ki	0.0280	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	459292: Displacement of Eu-labeled galanin from human GalR2 by DELFIA competitive assay	ki	0.0350	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	413946: Displacement of europium-labeled galanin from human GalR2 expressed in CHO-K1 cells	ki	0.0480	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	413946: Displacement of europium-labeled galanin from human GalR2 expressed in CHO-K1 cells	ki	0.0510	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	459292: Displacement of Eu-labeled galanin from human GalR2 by DELFIA competitive assay	ki	0.0515	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	370753: Displacement of europium labeled galanin from human recombinant GalR2 receptor by time-resolved fluorescence binding assay	ki	0.0515	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	413946: Displacement of europium-labeled galanin from human GalR2 expressed in CHO-K1 cells	ki	0.0515	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	413946: Displacement of europium-labeled galanin from human GalR2 expressed in CHO-K1 cells	ki	0.0655	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	413946: Displacement of europium-labeled galanin from human GalR2 expressed in CHO-K1 cells	ki	0.0750	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	413946: Displacement of europium-labeled galanin from human GalR2 expressed in CHO-K1 cells	ki	0.1080	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	726397: Displacement of euporium-galanin from human GalR2 after 1.5 hrs by DELFIA assay	ki	0.1190	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	413946: Displacement of europium-labeled galanin from human GalR2 expressed in CHO-K1 cells	ki	0.1600	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	413946: Displacement of europium-labeled galanin from human GalR2 expressed in CHO-K1 cells	ki	0.2145	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	459287: Binding affinity to human GalR2	ki	0.2180	uM
2-N-(4-methoxyphenyl)-6-piperidin-1-yl-4-N-[4-(trifluoromethoxy)phenyl]pyrimidine-2,4-diamine	631991: Displacement of [125I]galanin from GalR2 by gamma counting	ic50	0.3300	uM
2-N-(4-methoxyphenyl)-6-piperidin-1-yl-4-N-[3-(trifluoromethoxy)phenyl]pyrimidine-2,4-diamine	631991: Displacement of [125I]galanin from GalR2 by gamma counting	ic50	0.3800	uM
4-N-(3-fluoro-2-methylphenyl)-2-N-(4-methoxyphenyl)-6-piperidin-1-ylpyrimidine-2,4-diamine	631991: Displacement of [125I]galanin from GalR2 by gamma counting	ic50	0.3800	uM
4-N-(3-fluoro-4-methoxyphenyl)-2-N-(4-methoxyphenyl)-6-piperidin-1-ylpyrimidine-2,4-diamine	631991: Displacement of [125I]galanin from GalR2 by gamma counting	ic50	0.4300	uM
4-N-(2,5-dimethylphenyl)-2-N-(4-methoxyphenyl)-6-piperidin-1-ylpyrimidine-2,4-diamine	631991: Displacement of [125I]galanin from GalR2 by gamma counting	ic50	0.4400	uM
4-N-[3-(difluoromethoxy)phenyl]-2-N-(4-methoxyphenyl)-6-piperidin-1-ylpyrimidine-2,4-diamine	631991: Displacement of [125I]galanin from GalR2 by gamma counting	ic50	0.5400	uM
2-N-cyclohexyl-6-N-(4-methoxyphenyl)-4-N-[3-(trifluoromethoxy)phenyl]pyrimidine-2,4,6-triamine	631991: Displacement of [125I]galanin from GalR2 by gamma counting	ic50	0.5500	uM
N-(3-fluoro-2-methylphenyl)-6-piperidin-1-yl-2-[4-[3-(trifluoromethyl)-2-pyridinyl]-1,4-diazepan-1-yl]pyrimidin-4-amine	631991: Displacement of [125I]galanin from GalR2 by gamma counting	ic50	0.5600	uM

CTD chemical–gene interactions

26 total (human), top 26 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Tetrachlorodibenzodioxin	affects cotreatment, increases expression	3
sodium arsenite	increases expression	2
Benzo(a)pyrene	affects methylation, increases expression, increases methylation	2
Estradiol	affects cotreatment, increases expression	2
aristolochic acid I	increases expression	1
bisphenol A	decreases expression	1
o,p’-DDT	decreases expression	1
tris(1,3-dichloro-2-propyl)phosphate	decreases expression	1
butyraldehyde	increases expression	1
abrine	increases expression	1
licochalcone B	increases expression	1
jinfukang	decreases expression	1
Air Pollutants	increases abundance, increases expression	1
Diethylstilbestrol	decreases expression	1
Formaldehyde	increases expression	1
Quercetin	increases expression	1
Tunicamycin	increases expression	1
Urethane	increases expression	1
Valproic Acid	decreases methylation	1
Zearalenone	decreases expression	1
Thapsigargin	increases expression	1
Okadaic Acid	increases expression	1
beta-Naphthoflavone	increases expression	1
Lactic Acid	decreases expression	1
Genistein	decreases expression	1
Particulate Matter	increases abundance, increases expression	1

ChEMBL screening assays

67 unique, capped per target: 62 binding, 5 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1000170	Binding	Binding affinity to GAL2 receptor	Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists. — J Med Chem
CHEMBL1072084	Functional	Agonist activity at human GalR2 expressed in CHO-K1 cells at 1.25 uM by calcium mobilization assay relative to Galanin (2-29)	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_H434	CHO-K1/GAL2	Spontaneously immortalized cell line	Female
CVCL_KU58	CHO-K1 GALR2 Gq	Spontaneously immortalized cell line	Female
CVCL_KX10	PathHunter CHO-K1 GALR2 beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_ZL03	Tango GALR2-bla U2OS	Cancer cell line	Female

Clinical trials (associated diseases)

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

Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): neutropenia, severe congenital, 10, autosomal recessive