GALR3

Summary

GALR3 (galanin receptor 3, HGNC:4134) is a protein-coding gene on chromosome 22q13.1, encoding Galanin receptor type 3 (O60755). Receptor for the hormone galanin.

The neuropeptide galanin modulates a variety of physiologic processes including cognition/memory, sensory/pain processing, hormone secretion, and feeding behavior. The human galanin receptors are G protein-coupled receptors that functionally couple to their intracellular effector through distinct signaling pathways. GALR3 is found in many tissues and may be expressed as 1.4-, 2.4-, and 5-kb transcripts

Source: NCBI Gene 8484 — RefSeq curated summary.

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 69 total
• Druggable target: yes — 5 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_003614

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:4134
Approved symbol	GALR3
Name	galanin receptor 3
Location	22q13.1
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000128310
Ensembl biotype	protein_coding
OMIM	603692
Entrez	8484

Gene structure

Transcript identifiers

Ensembl transcripts: 2 — 2 protein_coding

ENST00000249041, ENST00000910168

RefSeq mRNA: 1 — MANE Select: NM_003614 NM_003614

CCDS: CCDS13958

Canonical transcript exons

ENST00000249041 — 2 exons

Exon	Start	End
ENSE00000880225	37823382	37823765
ENSE00001286812	37824723	37825485

Expression profiles

Bgee: expression breadth broad, 34 present calls, max score 49.29.

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
blood vessel layer	UBERON:0004797	49.29	gold quality
choroid plexus epithelium	UBERON:0003911	48.89	gold quality
skin of hip	UBERON:0001554	48.57	silver quality
oocyte	CL:0000023	47.14	gold quality
periodontal ligament	UBERON:0008266	47.14	gold quality
cerebellar hemisphere	UBERON:0002245	46.92	silver quality
cerebellar cortex	UBERON:0002129	46.87	silver quality
renal glomerulus	UBERON:0000074	46.86	gold quality
metanephric glomerulus	UBERON:0004736	46.77	gold quality
nephron tubule	UBERON:0001231	46.71	gold quality
cerebellum	UBERON:0002037	46.70	silver quality
right hemisphere of cerebellum	UBERON:0014890	46.65	silver quality
gingiva	UBERON:0001828	45.40	gold quality
dorsal motor nucleus of vagus nerve	UBERON:0002870	45.35	gold quality
inferior olivary complex	UBERON:0002127	45.14	gold quality
nasal cavity epithelium	UBERON:0005384	44.87	gold quality
sural nerve	UBERON:0015488	43.92	gold quality
nucleus accumbens	UBERON:0001882	43.87	silver quality
esophagus squamous epithelium	UBERON:0006920	43.61	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	43.37	gold quality
skeletal muscle tissue	UBERON:0001134	42.78	gold quality
secondary oocyte	CL:0000655	42.57	gold quality
right lobe of liver	UBERON:0001114	42.34	silver quality
gingival epithelium	UBERON:0001949	42.33	gold quality
bone marrow cell	CL:0002092	42.16	gold quality
body of pancreas	UBERON:0001150	41.88	gold quality
medulla oblongata	UBERON:0001896	41.74	gold quality
oral cavity	UBERON:0000167	41.45	gold quality
vastus lateralis	UBERON:0001379	41.41	gold quality
quadriceps femoris	UBERON:0001377	41.37	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	no	0.42

Regulation

Is transcription factor: no

Literature-anchored findings (GeneRIF, showing 10)

• Elevated expression of galanin receptors in childhood neuroblastic tumors. (PMID:11867941)
• GALR3 showed a significant association with alcoholism that was driven by one SNP (rs3,091,367). (PMID:17083333)
• Mutated human GalR3 receptors are tested with competitive binding analysis in vitro, identifying six different sites in GalR3 that determine binding to galanin. (PMID:20817064)
• The results suggest that GalR3, a receptor for the neuroendocrine peptide galanin, is a potential marker for relapsing pituitary tumors. (PMID:22889491)
• 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)
• 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 receptor GALR3 are differentially methylated and expressed in brains of major depressive disorder subjects in a region- and sex-specific manner. (PMID:27940914)
• Study showed that galanin receptor 3 is present in endothelial cells in human and murine dermal vessels and is co-expressed with nestin in neo-vessels of psoriatic patients. (PMID:28844939)
• 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)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	galr2b	ENSDARG00000105113
mus_musculus	Galr3	ENSMUSG00000114755
rattus_norvegicus	Galr3	ENSRNOG00000027060

Paralogs (16): NPFFR2 (ENSG00000056291), GNRHR (ENSG00000109163), CCKBR (ENSG00000110148), HCRTR1 (ENSG00000121764), AVPR2 (ENSG00000126895), HCRTR2 (ENSG00000137252), NPFFR1 (ENSG00000148734), CCKAR (ENSG00000163394), AVPR1A (ENSG00000166148), GALR1 (ENSG00000166573), GPR22 (ENSG00000172209), GPR150 (ENSG00000178015), OXTR (ENSG00000180914), FFAR4 (ENSG00000186188), QRFPR (ENSG00000186867), AVPR1B (ENSG00000198049)

Protein

Protein identifiers

Galanin receptor type 3 — O60755 (reviewed: O60755)

All UniProt accessions (1): O60755

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for the hormone galanin. Receptor for the hormone spexin-1.

Subcellular location. Cell membrane.

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

RefSeq proteins (1): NP_003605* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000405	Galanin_rcpt	Family
IPR003908	Galnin_3_rcpt	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (22 total): topological domain 8, transmembrane region 7, sequence variant 2, chain 1, region of interest 1, lipid moiety-binding region 1, glycosylation site 1, disulfide bond 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-O60755-F1	81.83	0.55

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): 308

Disulfide bonds (1): 95–172

Glycosylation sites (1): 6

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: 105 (showing top): GOBP_COGNITION, MODULE_274, GOBP_BEHAVIOR, MODULE_64, MODULE_16, GOBP_CELL_CELL_SIGNALING, MODULE_66, MODULE_118, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, MODULE_75, MODULE_289, MODULE_379, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, MYOD_Q6, GOBP_SYNAPTIC_SIGNALING

GO Biological Process (10): G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger (GO:0007187), neuropeptide signaling pathway (GO:0007218), chemical synaptic transmission (GO:0007268), learning or memory (GO:0007611), feeding behavior (GO:0007631), positive regulation of transcription by RNA polymerase II (GO:0045944), 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 (3): galanin receptor activity (GO:0004966), peptide hormone binding (GO:0017046), G protein-coupled receptor activity (GO:0004930)

GO Cellular Component (5): plasma membrane (GO:0005886), cilium (GO:0005929), membrane (GO:0016020), synapse (GO:0045202), non-motile cilium (GO:0097730)

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
behavior	2
anterograde trans-synaptic signaling	1
cognition	1
regulation of transcription by RNA polymerase II	1
transcription by RNA polymerase II	1
positive regulation of DNA-templated transcription	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
adenylate cyclase activity	1
negative regulation of catalytic activity	1
regulation of adenylate cyclase activity	1
neuropeptide receptor activity	1
hormone binding	1
transmembrane signaling receptor activity	1
membrane	1
cell periphery	1
intraciliary transport particle	1
membrane-bounded organelle	1
plasma membrane bounded cell projection	1
cellular anatomical structure	1
cell junction	1
cilium	1

Protein interactions and networks

STRING

508 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
GALR3	GAL	P22466	999
GALR3	GCAT	O75600	900
GALR3	SPX	Q9BT56	879
GALR3	GALP	Q9UBC7	815
GALR3	LGALS2	P05162	580
GALR3	H1-0	P07305	527
GALR3	MC4R	P32245	473
GALR3	NPY2R	P49146	430
GALR3	DRD2	P14416	417
GALR3	NPY5R	Q15761	416
GALR3	SMO	Q99835	411
GALR3	SSTR3	P32745	408
GALR3	MCHR1	Q99705	405
GALR3	LIPE	Q05469	402
GALR3	GALR2	O43603	402

IntAct

9 interactions, top by confidence:

A	B	Type	Score
RAMP1	GALR3	psi-mi:“MI:0915”(physical association)	0.400
GALR3	RAMP2	psi-mi:“MI:0915”(physical association)	0.400
RAMP3	GALR3	psi-mi:“MI:0915”(physical association)	0.400
RAMP2	GALR3	psi-mi:“MI:0915”(physical association)	0.400
GALR3	IGHA2	psi-mi:“MI:0914”(association)	0.350

BioGRID (5): TMED8 (Affinity Capture-MS), IGHA2 (Affinity Capture-MS), LTF (Affinity Capture-MS), GOLPH3L (Affinity Capture-MS), GALR3 (Affinity Capture-MS)

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

7 interactions.

A	Effect	B	Mechanism
GALR3	“up-regulates activity”	GNAI1	binding
GALR3	“up-regulates activity”	GNAI3	binding
GALR3	“up-regulates activity”	GNAO1	binding
GALR3	“up-regulates activity”	GNAZ	binding
GALR3	“up-regulates activity”	GNA14	binding
Galanin	“up-regulates activity”	GALR3	“chemical activation”
SPX	“up-regulates activity”	GALR3	binding

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	65
Likely benign	3
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

154 predictions. Top by Δscore:

Variant	Effect	Δscore
22:37823762:ACAGG:A	donor_loss	1.0000
22:37823763:CAG:C	donor_loss	1.0000
22:37823764:AG:A	donor_loss	1.0000
22:37823765:GGTG:G	donor_loss	1.0000
22:37823766:G:C	donor_loss	1.0000
22:37823766:G:GG	donor_gain	0.9800
22:37824717:CCGCA:C	acceptor_loss	0.9700
22:37824718:CGCA:C	acceptor_loss	0.9700
22:37824719:GCA:G	acceptor_loss	0.9700
22:37824720:CAGG:C	acceptor_loss	0.9700
22:37824721:A:AC	acceptor_loss	0.9700
22:37824712:GCCCT:G	acceptor_loss	0.9300
22:37824713:CCCTC:C	acceptor_loss	0.9300
22:37824714:CCTCC:C	acceptor_loss	0.9300
22:37824715:CTCCG:C	acceptor_loss	0.9300
22:37824721:A:AG	acceptor_gain	0.9000
22:37824722:G:GG	acceptor_gain	0.9000
22:37825138:T:TA	acceptor_gain	0.9000
22:37824716:TCCGC:T	acceptor_loss	0.8700
22:37823723:T:G	donor_gain	0.8600
22:37823726:ACGCC:A	donor_gain	0.8500
22:37823766:GTGC:G	donor_gain	0.8400
22:37823761:GACA:G	donor_gain	0.8300
22:37823761:GACAG:G	donor_gain	0.8300
22:37823762:ACAG:A	donor_gain	0.8300
22:37823765:GGTGC:G	donor_gain	0.8300
22:37824702:CTGA:C	acceptor_loss	0.8300
22:37823763:CAGG:C	donor_gain	0.8200
22:37823764:AGG:A	donor_gain	0.8200
22:37823767:T:G	donor_gain	0.8200

AlphaMissense

2296 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
22:37823609:A:T	D68V	0.999
22:37823734:A:C	S110R	0.999
22:37823736:C:A	S110R	0.999
22:37823736:C:G	S110R	0.999
22:37823595:C:A	N63K	0.998
22:37823595:C:G	N63K	0.998
22:37823609:A:C	D68A	0.998
22:37823731:A:C	S109R	0.998
22:37823733:C:A	S109R	0.998
22:37823733:C:G	S109R	0.998
22:37823511:T:A	N35K	0.997
22:37823511:T:G	N35K	0.997
22:37823609:A:G	D68G	0.997
22:37823610:C:A	D68E	0.997
22:37823610:C:G	D68E	0.997
22:37823617:T:C	F71L	0.997
22:37823619:C:A	F71L	0.997
22:37823619:C:G	F71L	0.997
22:37823689:T:A	C95S	0.997
22:37823690:G:A	C95Y	0.997
22:37823690:G:C	C95S	0.997
22:37823741:C:A	T112K	0.997
22:37823765:G:T	R120M	0.997
22:37824950:C:A	P196H	0.997
22:37825212:C:A	N283K	0.997
22:37825212:C:G	N283K	0.997
22:37823497:G:C	G31R	0.996
22:37823608:G:C	D68H	0.996
22:37823636:C:A	P77H	0.996
22:37823670:G:C	W88C	0.996

dbSNP variants (sampled 300 via entrez): RS1000814605 (22:37821843 C>G), RS1001101359 (22:37822131 T>C), RS1002268151 (22:37822432 G>A), RS1003295047 (22:37823933 C>T), RS1004727704 (22:37824387 C>T), RS1005033285 (22:37821549 C>G,T), RS1005556194 (22:37821936 C>CA), RS1005598981 (22:37824672 G>T), RS1007315255 (22:37823453 G>A), RS1007841925 (22:37823601 G>A,C,T), RS1008486451 (22:37821519 C>A,T), RS1008945235 (22:37822653 G>A), RS1009077524 (22:37823111 G>A,C), RS1009193845 (22:37822170 G>A), RS1009413461 (22:37822388 G>A)

Disease associations

OMIM: gene MIM:603692 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

1 associations (top):

Study	Trait	p-value
GCST010703_11	Brain morphology (MOSTest)	9.000000e-10

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0004346	neuroimaging measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL2731 (SINGLE PROTEIN), CHEMBL4524008 (PROTEIN FAMILY)

Molecules with ChEMBL bioactivity

5 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 29,091 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1200764	METHACHOLINE CHLORIDE	4	12,253
CHEMBL83063	RITODRINE	4	38
CHEMBL95431	CARBOXYAMIDOTRIAZOLE	3	12,804
CHEMBL152649	CHLORMIDAZOLE	2	1,775
CHEMBL86882	ETILEFRINE	2	2,221

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 (37 total), top 25:

Ligand	Action	Affinity	Parameter
galanin-like peptide	Agonist	8.82	pIC50
[125I][Tyr26]galanin (pig)	Agonist	8.65	pKd
galanin	Full agonist	8.35	pKi
SNAP 398299	Antagonist	8.27	pKi
M32	Antagonist	8.22	pKi
galanin(1-19) (rat/mouse)	Agonist	8.2	pKi
C7	Antagonist	8.08	pKi
galanin-like peptide	Agonist	8.0	pIC50
galanin	Full agonist	7.92	pIC50
galanin(2-29) (rat/mouse)	Agonist	7.9	pKi
J20 (galanin analogue)	Agonist	7.89	pKi
M35	Antagonist	7.84	pKi
GalR3ant	Antagonist	7.82	pKi
SNAP 37889	Antagonist	7.77	pKi
[Ala6, D-Trp8]galanin-(1-15)-ol	Antagonist	7.75	pKi
galanin(7-29) (pig)	Agonist	7.45	pKi
M15	Antagonist	7.4	pKi
M617	Agonist	7.31	pKi
M40	Antagonist	7.28	pKi
galanin(2-29) (pig)	Agonist	7.22	pKi
galanin	Full agonist	7.12	pIC50
J18 (galanin analogue)	Agonist	6.95	pKi
galanin(2-11)	Agonist	6.7	pKi
M1153	Agonist	6.64	pKi
galanin(1-16) (rat/mouse/pig)	Agonist	6.5	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

197 potent at pChembl≥5 of 202 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.30	Ki	5	nM	CHEMBL209497
8.18	IC50	6.57	nM	PYRIDABEN
8.10	Ki	8	nM	CHEMBL209498
7.82	Ki	15	nM	CHEMBL378991
7.82	Kd	15	nM	CHEMBL503473
7.81	IC50	15.41	nM	CHEMBL267630
7.77	IC50	17.14	nM	CHEMBL1873644
7.77	Ki	17	nM	CHEMBL210288
7.68	Ki	21	nM	CHEMBL378825
7.58	Ki	26	nM	CHEMBL211398
7.57	Ki	27	nM	CHEMBL209642
7.54	Ki	29	nM	CHEMBL377468
7.47	Ki	34	nM	CHEMBL213893
7.42	Ki	38	nM	CHEMBL383941
7.41	IC50	38.65	nM	CHEMBL1721226
7.40	Kd	40	nM	GALANTIDE
7.35	Ki	45	nM	CHEMBL209476
7.31	Ki	49	nM	CHEMBL211031
7.28	Ki	52	nM	CHEMBL211169
7.16	Ki	70	nM	CHEMBL377328
7.16	Kd	69	nM	CHEMBL499179
7.11	Ki	78	nM	CHEMBL211467
7.06	IC50	86.87	nM	CHEMBL1423004
7.06	Ki	87	nM	CHEMBL209481
7.05	Ki	89	nM	CHEMBL387401
7.05	Ki	89	nM	CHEMBL209730
6.90	IC50	126.3	nM	CHEMBL1878609
6.89	IC50	128.3	nM	CHEMBL1323872
6.89	IC50	128.4	nM	CHEMBL1550278
6.85	IC50	142.1	nM	CHEMBL1386344
6.85	IC50	140.2	nM	CHEMBL1725453
6.84	IC50	143	nM	CHEMBL1461631
6.83	IC50	147.9	nM	CHEMBL1319304
6.82	Ki	150	nM	CHEMBL212729
6.81	IC50	154.7	nM	CHEMBL1499354
6.80	IC50	157.6	nM	CHEMBL1340112
6.80	IC50	158.4	nM	CHEMBL1705098
6.69	IC50	203.2	nM	CHLORMIDAZOLE
6.62	IC50	240	nM	CHEMBL1492752
6.61	IC50	246.4	nM	CHEMBL1422429
6.58	IC50	260.5	nM	CHEMBL1546066
6.54	Ki	290	nM	CHEMBL211522
6.52	IC50	303.1	nM	CARBOXYAMIDOTRIAZOLE
6.50	Kd	315	nM	CHEMBL499980
6.49	IC50	322.1	nM	CHEMBL1425552
6.48	IC50	330.6	nM	CHEMBL1604200
6.46	IC50	348.5	nM	CHEMBL1903414
6.45	IC50	358.4	nM	CHEMBL1981589
6.44	IC50	362.6	nM	CHEMBL1711360
6.43	IC50	367.2	nM	CHEMBL1569489

PubChem BioAssay actives

30 with measured affinity, of 60 total; 29 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
1-[3-(2-pyrrolidin-1-ylethoxy)phenyl]-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one	269267: Displacement of [125I]galanin from human galanin Gal3 receptor	ki	0.0050	uM
1-[3-(2-piperidin-1-ylethoxy)phenyl]-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one	269267: Displacement of [125I]galanin from human galanin Gal3 receptor	ki	0.0080	uM
1-[3-[3-(diethylamino)-2-hydroxypropoxy]phenyl]-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one	269267: Displacement of [125I]galanin from human galanin Gal3 receptor	ki	0.0150	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	413942: Binding affinity to human GalR3	kd	0.0150	uM
1-phenyl-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one	267249: Displacement of [125I]galanin from human GAL3	ki	0.0170	uM
1-[3-[3-(diethylamino)propoxy]phenyl]-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one	269267: Displacement of [125I]galanin from human galanin Gal3 receptor	ki	0.0210	uM
1-[3-[2-(dimethylamino)ethoxy]phenyl]-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one	269267: Displacement of [125I]galanin from human galanin Gal3 receptor	ki	0.0260	uM
1-[3-[(2S)-3-(diethylamino)-2-hydroxypropoxy]phenyl]-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one	269267: Displacement of [125I]galanin from human galanin Gal3 receptor	ki	0.0270	uM
1-[3-[3-(dimethylamino)propoxy]phenyl]-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one	269267: Displacement of [125I]galanin from human galanin Gal3 receptor	ki	0.0290	uM
1-[4-[3-(diethylamino)propoxy]phenyl]-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one	269267: Displacement of [125I]galanin from human galanin Gal3 receptor	ki	0.0340	uM
1-[3-(diethylaminomethoxy)phenyl]-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one	269267: Displacement of [125I]galanin from human galanin Gal3 receptor	ki	0.0380	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	413942: Binding affinity to human GalR3	kd	0.0400	uM
1-[3-[4-(diethylamino)butoxy]phenyl]-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one	269267: Displacement of [125I]galanin from human galanin Gal3 receptor	ki	0.0450	uM
1-[3-(3-pyrrolidin-1-ylpropoxy)phenyl]-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one	269267: Displacement of [125I]galanin from human galanin Gal3 receptor	ki	0.0490	uM
1-pentan-3-yl-3-[4-(trifluoromethyl)phenyl]iminoindol-2-one	267249: Displacement of [125I]galanin from human GAL3	ki	0.0520	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	413942: Binding affinity to human GalR3	kd	0.0690	uM
1-[4-[4-(diethylamino)butoxy]phenyl]-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one	269267: Displacement of [125I]galanin from human galanin Gal3 receptor	ki	0.0700	uM
1-[4-[2-(diethylamino)ethoxy]phenyl]-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one	269267: Displacement of [125I]galanin from human galanin Gal3 receptor	ki	0.0780	uM
1-[3-[2-(diethylamino)ethoxy]phenyl]-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one	269267: Displacement of [125I]galanin from human galanin Gal3 receptor	ki	0.0870	uM
1-prop-2-ynyl-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one	267249: Displacement of [125I]galanin from human GAL3	ki	0.0890	uM
1-[4-[2-(dimethylamino)ethoxy]phenyl]-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one	269267: Displacement of [125I]galanin from human galanin Gal3 receptor	ki	0.0890	uM
3-(3,4-dichlorophenyl)imino-1-prop-2-enylindol-2-one	267249: Displacement of [125I]galanin from human GAL3	ki	0.1500	uM
1-[3-[(2R)-3-(diethylamino)-2-hydroxypropoxy]phenyl]-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one	269267: Displacement of [125I]galanin from human galanin Gal3 receptor	ki	0.2900	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	413942: Binding affinity to human GalR3	kd	0.3150	uM
3-(2,3-dichlorophenyl)imino-1H-indol-2-one	267249: Displacement of [125I]galanin from human GAL3	ki	0.4370	uM
3-[3-(trifluoromethyl)phenyl]imino-1H-indol-2-one	267249: Displacement of [125I]galanin from human GAL3	ki	0.5960	uM
1-[2-(2-pyrrolidin-1-ylethoxy)phenyl]-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one	269267: Displacement of [125I]galanin from human galanin Gal3 receptor	ki	0.7900	uM
3-(4-chlorophenyl)imino-1H-indol-2-one	267249: Displacement of [125I]galanin from human GAL3	ki	0.8500	uM
1-[2-[2-(diethylamino)ethoxy]phenyl]-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one	269267: Displacement of [125I]galanin from human galanin Gal3 receptor	ki	1.0000	uM

CTD chemical–gene interactions

10 total (human), top 10 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	affects methylation, decreases expression, decreases methylation, increases methylation	2
quercitrin	increases expression	1
Resveratrol	affects cotreatment, decreases expression	1
Amphotericin B	increases expression	1
Lead	decreases expression	1
Plant Extracts	affects cotreatment, decreases expression	1
Valproic Acid	increases methylation	1
Vitamin E	increases expression	1
Aflatoxin B1	decreases expression	1
Sodium Selenite	increases expression	1

ChEMBL screening assays

8 unique, capped per target: 7 binding, 1 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1010034	Binding	Binding affinity to human GalR3	Design, synthesis, and characterization of high-affinity, systemically-active galanin analogues with potent anticonvulsant activities. — J Med Chem
CHEMBL2354227	Functional	PubChem BioAssay. Fluorescence-based cell-based primary high throughput dose response assay to identify antagonists of the Galanin Receptor 3 (GalR3). (Class of assay: confirmatory)	PubChem BioAssay data set

Clinical trials (associated diseases)

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