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GAL2 receptor

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Target not currently curated in GtoImmuPdb

Target id: 244

Nomenclature: GAL2 receptor

Family: Galanin receptors

Contents:

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 387 17q25.1 GALR2 galanin receptor 2
Mouse 7 371 11 81.1 cM Galr2 galanin receptor 2
Rat 7 372 10q32.1 Galr2 galanin receptor 2
Previous and Unofficial Names Click here for help
GALNR2
Database Links Click here for help
Specialist databases
GPCRdb galr2_human (Hs), galr2_mouse (Mm), galr2_rat (Rn)
Other databases
Alphafold O43603 (Hs), O88854 (Mm), O08726 (Rn)
ChEMBL Target CHEMBL3176 (Hs), CHEMBL5577 (Rn)
Ensembl Gene ENSG00000182687 (Hs), ENSMUSG00000020793 (Mm), ENSRNOG00000061733 (Rn)
Entrez Gene 8811 (Hs), 14428 (Mm), 29234 (Rn)
Human Protein Atlas ENSG00000182687 (Hs)
KEGG Gene hsa:8811 (Hs), mmu:14428 (Mm), rno:29234 (Rn)
OMIM 603691 (Hs)
Pharos O43603 (Hs)
RefSeq Nucleotide NM_003857 (Hs), NM_010254 (Mm), NM_019172 (Rn)
RefSeq Protein NP_003848 (Hs), NP_034384 (Mm), NP_062045 (Rn)
UniProtKB O43603 (Hs), O88854 (Mm), O08726 (Rn)
Wikipedia GALR2 (Hs)
Natural/Endogenous Ligands Click here for help
galanin {Sp: Human} , galanin {Sp: Mouse, Rat}
galanin-like peptide {Sp: Human} , galanin-like peptide {Sp: Mouse} , galanin-like peptide {Sp: Rat}
spexin-1 {Sp: Human}
Potency order of endogenous ligands (Human)
galanin-like peptide (GALP, Q9UBC7) ≥ galanin (GAL, P22466)  [41]

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[125I][Tyr26]galanin (pig) Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Agonist 9.5 – 9.9 pKd 6,17
⤷ pKd 9.9 (Kd 1.2x10-10 M) [17]
pKd 9.5 (Kd 3.1x10-10 M) [6]
[125I][Tyr26]galanin (human) Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Agonist 9.5 – 9.6 pKd 5,26
⤷ pKd 9.5 – 9.6 (Kd 3.1x10-10 – 2.4x10-10 M) [5,26]
[125I][Tyr26]galanin (human) Peptide Ligand is labelled Ligand is radioactive Mm Agonist 9.3 pKd 42
⤷ pKd 9.3 (Kd 4.7x10-10 M) [42]
[125I][Tyr26]galanin (human) Peptide Ligand is labelled Ligand is radioactive Rn Agonist 9.2 pKd 61
⤷ pKd 9.2 (Kd 5.9x10-10 M) [61]
[125I][Tyr26]galanin (pig) Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Rn Agonist 8.4 – 9.9 pKd 12,18,54,61
⤷ pKd 8.4 – 9.9 (Kd 4x10-9 – 1.3x10-10 M) [12,18,54,61]
galmic Small molecule or natural product Rn Agonist <5.0 pKd 3,33
⤷ pKd <5.0 (Kd >1x10-5 M) [3,33]
galanin(1-15) Peptide Click here for species-specific activity table Rn Agonist 9.1 pKi 53
⤷ pKi 9.1 (Ki 7x10-10 M) [53]
galanin {Sp: Pig} Peptide Click here for species-specific activity table Rn Full agonist 9.0 – 9.3 pKi 53-54
⤷ pKi 9.0 – 9.3 (Ki 1.05x10-9 – 5x10-10 M) [53-54]
galanin(1-20) (human) Peptide Hs Agonist 9.1 pKi 5
⤷ pKi 9.1 (Ki 7.8x10-10 M) [5]
galanin(2-29) (rat/mouse) Peptide Click here for species-specific activity table Hs Full agonist 9.0 pKi 5
⤷ pKi 9.0 (Ki 9.1x10-10 M) [5]
galanin {Sp: Pig} Peptide Click here for species-specific activity table Hs Full agonist 9.0 pKi 6
⤷ pKi 9.0 (Ki 9.5x10-10 M) [6]
galanin {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 8.6 – 9.1 pKi 5-6,48
⤷ pKi 8.6 – 9.1 (Ki 2.34x10-9 – 8.6x10-10 M) [5-6,48]
galanin {Sp: Mouse, Rat} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Rn Full agonist 8.3 – 9.3 pKi 33,42,54,60-62
⤷ pKi 8.3 – 9.3 (Ki 5.6x10-9 – 5.6x10-10 M) [33,42,54,60-62]
galanin {Sp: Mouse, Rat} Peptide Click here for species-specific activity table Hs Full agonist 8.5 – 8.8 pKi 5-6,36,44,47,55
⤷ pKi 8.5 – 8.8 (Ki 2.98x10-9 – 1.54x10-9 M) [5-6,36,44,47,55]
galanin {Sp: Human} Peptide Click here for species-specific activity table Rn Full agonist 8.6 pKi 54
⤷ pKi 8.6 (Ki 2.51x10-9 M) [54]
galanin(7-29) (pig) Peptide Click here for species-specific activity table Rn Agonist 8.6 pKi 5
⤷ pKi 8.6 (Ki 2.51x10-9 M) [5]
galanin(2-29) (pig) Peptide Click here for species-specific activity table Hs Full agonist 8.5 pKi 6
⤷ pKi 8.5 (Ki 2.88x10-9 M) [6]
galanin(1-15) Peptide Click here for species-specific activity table Hs Agonist 8.5 pKi 5
⤷ pKi 8.5 (Ki 3.5x10-9 M) [5]
galanin {Sp: Mouse, Rat} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Mm Full agonist 8.4 pKi 42
⤷ pKi 8.4 (Ki 3.9x10-9 M) [42]
galanin(2-30) (human) Peptide Click here for species-specific activity table Hs Full agonist 8.0 – 8.7 pKi 5,11
⤷ pKi 8.0 – 8.7 (Ki 1x10-8 – 1.8x10-9 M) [5,11]
galanin(1-16) (rat/mouse/pig) Peptide Click here for species-specific activity table Hs Agonist 7.9 – 8.8 pKi 5-6,8
⤷ pKi 7.9 – 8.8 (Ki 1.3x10-8 – 1.6x10-9 M) [5-6,8]
galanin(1-19) (rat/mouse) Peptide Click here for species-specific activity table Rn Agonist 8.3 pKi 62
⤷ pKi 8.3 (Ki 4.7x10-9 M) [62]
galanin(1-16) (rat/mouse/pig) Peptide Click here for species-specific activity table Rn Agonist 7.9 – 8.7 pKi 42,53-54,60-62
⤷ pKi 7.9 – 8.7 (Ki 1.3x10-8 – 1.8x10-9 M) [42,53-54,60-62]
J20 (galanin analogue) Peptide Click here for species-specific activity table Hs Agonist 8.3 pKi 45
⤷ pKi 8.3 (Ki 4.9x10-9 M) [45]
galanin(7-29) (pig) Peptide Click here for species-specific activity table Hs Full agonist 8.3 pKi 6
⤷ pKi 8.3 (Ki 4.9x10-9 M) [6]
M1153 Peptide Click here for species-specific activity table Hs Agonist 8.3 pKi 47
⤷ pKi 8.3 (Ki 4.98x10-9 M) [47]
M617 Peptide Click here for species-specific activity table Hs Agonist 8.2 pKi 36
⤷ pKi 8.2 (Ki 5.71x10-9 M) [36]
M242 Peptide Click here for species-specific activity table Hs Agonist 8.2 pKi 48
⤷ pKi 8.2 (Ki 5.84x10-9 M) [48]
galanin(1-12) Peptide Hs Agonist 8.2 pKi 5
⤷ pKi 8.2 (Ki 6.4x10-9 M) [5]
M1145 Peptide Click here for species-specific activity table Hs Full agonist 8.2 pKi 44
⤷ pKi 8.2 (Ki 6.55x10-9 M) [44]
galanin(2-29) (rat/mouse) Peptide Click here for species-specific activity table Mm Full agonist 8.2 pKi 42
⤷ pKi 8.2 (Ki 6.8x10-9 M) [42]
[D-Trp2]galanin-(1-29) Peptide Rn Full agonist 8.1 pKi 53
⤷ pKi 8.1 (Ki 7x10-9 M) [53]
galanin(2-29) (rat/mouse) Peptide Click here for species-specific activity table Rn Full agonist 7.3 – 8.7 pKi 42,60-62
⤷ pKi 7.3 – 8.7 (Ki 5.6x10-8 – 1.9x10-9 M) [42,60-62]
galanin(1-16) (rat/mouse/pig) Peptide Click here for species-specific activity table Mm Agonist 7.9 pKi 42
⤷ pKi 7.9 (Ki 1.18x10-8 M) [42]
Gal-B2-dPEG24 Peptide Click here for species-specific activity table Hs Agonist 7.9 pKi 69
⤷ pKi 7.9 (Ki 1.35x10-8 M) [69]
galanin(D-Trp2) (pig) Peptide Click here for species-specific activity table Rn Agonist 7.6 – 8.1 pKi 53-54
⤷ pKi 7.6 – 8.1 (Ki 2.754x10-8 – 7x10-9 M) [53-54]
Gal-B2-C10 Peptide Click here for species-specific activity table Hs Agonist 7.8 pKi 70
⤷ pKi 7.8 (Ki 1.44x10-8 M) [70]
Gal-B2-C8 Peptide Click here for species-specific activity table Hs Agonist 7.8 pKi 70
⤷ pKi 7.8 (Ki 1.49x10-8 M) [70]
Gal-B2-C18 Peptide Click here for species-specific activity table Hs Agonist 7.8 pKi 70
⤷ pKi 7.8 (Ki 1.5x10-8 M) [70]
Gal-B2-C12 Peptide Click here for species-specific activity table Hs Agonist 7.8 pKi 70
⤷ pKi 7.8 (Ki 1.61x10-8 M) [70]
galanin(2-11) Peptide Click here for species-specific activity table Hs Agonist 7.8 pKi 44
⤷ pKi 7.8 (Ki 1.66x10-8 M) [44]
Gal-B2-C14 Peptide Click here for species-specific activity table Hs Agonist 7.7 pKi 70
⤷ pKi 7.7 (Ki 1.82x10-8 M) [70]
J18 (galanin analogue) Peptide Click here for species-specific activity table Hs Agonist 7.7 pKi 45
⤷ pKi 7.7 (Ki 2x10-8 M) [45]
[N-Me,des-Sar]Gal-B2 Peptide Click here for species-specific activity table Hs Agonist 7.7 pKi 43
⤷ pKi 7.7 (Ki 2.02x10-8 M) [43]
Gal-B2-MPEG4 Peptide Click here for species-specific activity table Hs Agonist 7.7 pKi 70
⤷ pKi 7.7 (Ki 2.05x10-8 M) [70]
Gal-(K)4 Peptide Click here for species-specific activity table Hs Agonist 7.6 pKi 70
⤷ pKi 7.6 (Ki 2.4x10-8 M) [70]
M1151 Peptide Click here for species-specific activity table Hs Agonist 7.5 pKi 47
⤷ pKi 7.5 (Ki 2.89x10-8 M) [47]
M1160 Peptide Click here for species-specific activity table Hs Agonist 7.5 pKi 46
⤷ pKi 7.5 (Ki 3.33x10-8 M) [46]
M1152 Peptide Click here for species-specific activity table Hs Agonist 7.4 pKi 47
⤷ pKi 7.4 (Ki 3.64x10-8 M) [47]
Gal-B5 Peptide Click here for species-specific activity table Hs Agonist 7.3 pKi 8
⤷ pKi 7.3 (Ki 4.8x10-8 M) [8]
Gal-B2 Peptide Click here for species-specific activity table Hs Agonist 7.3 pKi 8
⤷ pKi 7.3 (Ki 5.15x10-8 M) [8]
Gal-R2-dPEG24 Peptide Hs Agonist 7.2 pKi 69
⤷ pKi 7.2 (Ki 6.04x10-8 M) [69]
galanin(2-11) Peptide Click here for species-specific activity table Rn Agonist 7.1 pKi 32
⤷ pKi 7.1 (Ki 8.8x10-8 M) [32]
galanin(D-Trp2) (pig) Peptide Click here for species-specific activity table Hs Agonist 6.7 pKi 6
⤷ pKi 6.7 (Ki 1.995x10-7 M) [6]
galanin(3-29) (rat/mouse) Peptide Click here for species-specific activity table Hs Agonist <6.2 pKi 5
⤷ pKi <6.2 (Ki >7x10-7 M) [5]
galanin(10-29) (rat/mouse) Peptide Hs Agonist <6.2 pKi 5
⤷ pKi <6.2 (Ki >7x10-7 M) [5]
galanin(5-29) (rat/mouse) Peptide Hs Agonist <6.2 pKi 5
⤷ pKi <6.2 (Ki >7x10-7 M) [5]
galanin(9-29) (rat/mouse) Peptide Hs Agonist <6.2 pKi 5
⤷ pKi <6.2 (Ki >7x10-7 M) [5]
galanin(9-25) (rat/mouse) Peptide Hs Agonist <6.2 pKi 5
⤷ pKi <6.2 (Ki >7x10-7 M) [5]
galanin(3-30) (human) Peptide Hs Agonist <6.2 pKi 5
⤷ pKi <6.2 (Ki >7x10-7 M) [5]
galanin(1-10) Peptide Hs Agonist <6.2 pKi 5
⤷ pKi <6.2 (Ki >7x10-7 M) [5]
GMAP(1-41) {Sp: Pig} Peptide Rn Agonist <6.1 pKi 61
⤷ pKi <6.1 (Ki >8.4x10-7 M) [61]
galanin(3-29) (pig) Peptide Click here for species-specific activity table Hs Agonist <6.0 pKi 6
⤷ pKi <6.0 (Ki >1x10-6 M) [6]
galanin(3-29) (pig) Peptide Click here for species-specific activity table Rn Agonist <6.0 pKi 53-54
⤷ pKi <6.0 (Ki >1x10-6 M) [53-54]
GMAP(44-59) {Sp: Pig} Peptide Rn Agonist <6.0 pKi 62
⤷ pKi <6.0 (Ki >1x10-6 M) [62]
(D-Thr6, D-Trp8,9)galanin(1-15)ol Peptide Click here for species-specific activity table Rn Agonist <5.9 pKi 61
⤷ pKi <5.9 (Ki >1.25x10-6 M) [61]
galanin(3-29) (rat/mouse) Peptide Click here for species-specific activity table Rn Agonist 5.5 – 6.0 pKi 42,60,62
⤷ pKi 5.5 – 6.0 (Ki 3.125x10-6 – 1x10-6 M) [42,60,62]
galanin(10-29) (rat/mouse) Peptide Click here for species-specific activity table Mm Agonist <5.7 pKi 42
⤷ pKi <5.7 (Ki >1.86x10-6 M) [42]
galanin(3-29) (rat/mouse) Peptide Click here for species-specific activity table Mm Agonist <5.7 pKi 42
⤷ pKi <5.7 (Ki >2.2x10-6 M) [42]
galnon Small molecule or natural product Rn Agonist 4.5 pKi 3,33
⤷ pKi 4.5 (Ki 3.41x10-5 M) [3,33]
galanin(1-15) Peptide Click here for species-specific activity table Hs Agonist 9.1 pEC50 17
⤷ pEC50 9.1 (EC50 7.2x10-10 M) [17]
galanin-like peptide {Sp: Pig} Peptide Click here for species-specific activity table Rn Agonist 8.6 pEC50 41
⤷ pEC50 8.6 (EC50 2.4x10-9 M) [41]
galanin {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 7.9 – 9.1 pEC50 6,17
⤷ pEC50 7.9 – 9.1 (EC50 1.23x10-8 – 7.1x10-10 M) [6,17]
galanin(1-16) (rat/mouse/pig) Peptide Click here for species-specific activity table Hs Agonist 7.3 – 9.4 pEC50 6,17
⤷ pEC50 7.3 – 9.4 (EC50 5.495x10-8 – 4.2x10-10 M) [6,17]
galanin {Sp: Mouse, Rat} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Rn Full agonist 8.3 pEC50 41
⤷ pEC50 8.3 (EC50 5.2x10-9 M) [41]
galanin(2-29) (pig) Peptide Click here for species-specific activity table Hs Full agonist 7.6 – 8.9 pEC50 6,17
⤷ pEC50 7.6 – 8.9 (EC50 2.399x10-8 – 1.17x10-9 M) [6,17]
galanin {Sp: Pig} Peptide Click here for species-specific activity table Hs Full agonist 8.1 pEC50 6
⤷ pEC50 8.1 (EC50 8.12x10-9 M) [6]
galanin {Sp: Pig} Peptide Click here for species-specific activity table Rn Full agonist 7.7 pEC50 53
⤷ pEC50 7.7 (EC50 1.8x10-8 M) [53]
galanin(7-29) (pig) Peptide Click here for species-specific activity table Hs Agonist 7.5 pEC50 6
⤷ pEC50 7.5 (EC50 3.467x10-8 M) [6]
galanin(1-15) Peptide Click here for species-specific activity table Rn Agonist 7.2 pEC50 53
⤷ pEC50 7.2 (EC50 6.5x10-8 M) [53]
Qu-SPX Peptide Hs Agonist 7.1 pEC50 30
⤷ pEC50 7.1 (EC50 8.71x10-8 M) [30]
Description: SRE-luc reporter activation in HEK293 Gqi cells expressing hGAL3 receptor.
galanin(1-16) (rat/mouse/pig) Peptide Click here for species-specific activity table Rn Agonist 7.0 pEC50 53
⤷ pEC50 7.0 (EC50 9.4x10-8 M) [53]
galanin(D-Trp2) (pig) Peptide Click here for species-specific activity table Rn Agonist 6.8 pEC50 53
⤷ pEC50 6.8 (EC50 1.5x10-7 M) [53]
spexin-1 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Agonist 6.8 pEC50 25
⤷ pEC50 6.8 (EC50 1.61x10-7 M) [25]
Description: Determined by measuring SRE-luc activity in HEK293-Gqi cells expressing hGALR2.
galanin(D-Trp2) (pig) Peptide Click here for species-specific activity table Hs Agonist 6.5 pEC50 6
⤷ pEC50 6.5 (EC50 3.388x10-7 M) [6]
galanin(3-29) (pig) Peptide Click here for species-specific activity table Hs Agonist <6.0 pEC50 6
⤷ pEC50 <6.0 (EC50 >1x10-6 M) [6]
galanin(3-29) (pig) Peptide Click here for species-specific activity table Rn Agonist <6.0 pEC50 53
⤷ pEC50 <6.0 (EC50 >1x10-6 M) [53]
galanin(10-29) (pig) Peptide Hs Agonist <6.0 pEC50 17
⤷ pEC50 <6.0 (EC50 >1x10-6 M) [17]
galanin-like peptide {Sp: Pig} Peptide Click here for species-specific activity table Rn Agonist 9.6 pIC50 41
⤷ pIC50 9.6 (IC50 2.4x10-10 M) [41]
galanin {Sp: Pig} Peptide Click here for species-specific activity table Hs Full agonist 9.5 pIC50 17
⤷ pIC50 9.5 (IC50 3.5x10-10 M) [17]
galanin {Sp: Pig} Peptide Click here for species-specific activity table Rn Full agonist 9.3 – 9.4 pIC50 18,22
⤷ pIC50 9.3 – 9.4 (IC50 4.6x10-10 – 3.7x10-10 M) [18,22]
galanin {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 9.3 pIC50 17
⤷ pIC50 9.3 (IC50 5.1x10-10 M) [17]
galanin {Sp: Mouse, Rat} Peptide Click here for species-specific activity table Rn Full agonist 8.7 – 9.3 pIC50 7,18,41
⤷ pIC50 8.7 – 9.3 (IC50 1.9x10-9 – 4.8x10-10 M) [7,18,41]
galanin {Sp: Human} Peptide Click here for species-specific activity table Rn Full agonist 8.6 – 9.0 pIC50 18,22,31
⤷ pIC50 8.6 – 9.0 (IC50 2.5x10-9 – 1x10-9 M) [18,22,31]
galanin(1-11) Peptide Rn Agonist 8.8 pIC50 31
⤷ pIC50 8.8 (IC50 1.65x10-9 M) [31]
[Sar1, D-Ala12]galanin(1-16) Peptide Rn Agonist 8.8 pIC50 31
⤷ pIC50 8.8 (IC50 1.74x10-9 M) [31]
galanin(2-11) Peptide Click here for species-specific activity table Rn Agonist 8.8 pIC50 31
⤷ pIC50 8.8 (IC50 1.76x10-9 M) [31]
galanin(2-29) (pig) Peptide Click here for species-specific activity table Hs Full agonist 8.7 – 8.7 pIC50 17-18
⤷ pIC50 8.7 – 8.7 (IC50 1.87x10-9 – 1.8x10-9 M) [17-18]
galanin {Sp: Mouse, Rat} Peptide Click here for species-specific activity table Hs Full agonist 7.9 – 9.5 pIC50 6,17
⤷ pIC50 9.5 (IC50 3.4x10-10 M) [17]
pIC50 7.9 – 9.1 (IC50 1.175x10-8 – 7.6x10-10 M) [6,17]
galanin(1-16) (rat/mouse/pig) Peptide Click here for species-specific activity table Hs Agonist 8.7 pIC50 17
⤷ pIC50 8.7 (IC50 2.17x10-9 M) [17]
galanin(1-15) Peptide Click here for species-specific activity table Hs Agonist 8.6 pIC50 17
⤷ pIC50 8.6 (IC50 2.47x10-9 M) [17]
galanin(2-29) (rat/mouse) Peptide Click here for species-specific activity table Rn Full agonist 8.5 pIC50 22
⤷ pIC50 8.5 (IC50 2.9x10-9 M) [22]
galanin(1-16) (rat/mouse/pig) Peptide Click here for species-specific activity table Rn Agonist 7.9 – 8.5 pIC50 18,22
⤷ pIC50 7.9 – 8.5 (IC50 1.32x10-8 – 3x10-9 M) [18,22]
galanin(1-15) Peptide Click here for species-specific activity table Rn Agonist 8.1 pIC50 18
⤷ pIC50 8.1 (IC50 7.4x10-9 M) [18]
GALP(3-32) (human) Peptide Click here for species-specific activity table Hs Agonist 7.8 pIC50 27
⤷ pIC50 7.8 (IC50 1.5x10-8 M) [27]
galanin-like peptide {Sp: Human} Peptide Click here for species-specific activity table Hs Agonist 7.6 – 7.7 pIC50 7,27
⤷ pIC50 7.6 – 7.7 (IC50 2.8x10-8 – 1.87x10-8 M) [7,27]
GALP(1-32) (human) Peptide Click here for species-specific activity table Hs Agonist 7.2 pIC50 27
⤷ pIC50 7.2 (IC50 6.9x10-8 M) [27]
galanin(5-29) (pig) Peptide Rn Agonist 6.7 pIC50 65
⤷ pIC50 6.7 (IC50 2x10-7 M) [65]
galanin(3-29) (pig) Peptide Click here for species-specific activity table Hs Agonist <6.0 pIC50 17-18
⤷ pIC50 <6.0 (IC50 >1x10-6 M) [17-18]
galanin(3-29) (rat/mouse) Peptide Click here for species-specific activity table Rn Agonist <6.0 pIC50 22
⤷ pIC50 <6.0 (IC50 >1x10-6 M) [22]
galanin(10-29) (pig) Peptide Click here for species-specific activity table Rn Agonist 6.0 pIC50 18
⤷ pIC50 6.0 (IC50 1x10-6 M) [18]
alarin {Sp: Rat} Peptide Click here for species-specific activity table Rn Agonist <6.0 pIC50 7
⤷ pIC50 <6.0 (IC50 >1x10-6 M) [7]
[125I]spexin-1 Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Agonist - - 25
⤷ [25]
View species-specific agonist tables
Agonist Comments
Binding affinity is lost with removal of amino acids 1 and 2 of galanin [6]. Galanin(D-Trp2) has a higher binding affinity for GAL2 receptor than GAL1 receptor.
In [60], affinities are given for both membrane binding assays and whole cell binding assays. Two populations of binding sites (larger population of low affinity/ smaller population of higher affinity) are identified in [18].

In [8] and [43] many different galanin analogues were trialled. The most active compounds are reported here. The Ki values of other analogues are listed in these publications. In [49] a series of 2,4,6-triaminopyridimines analogs were tested and found to have IC50 values in the range 300-100nM.

NOTE that compounds with -ve log10 affinities <6 have no appreciable agonist function.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
M15 Peptide Am Antagonist 9.0 pKi 6
⤷ pKi 9.0 (Ki 1.07x10-9 M) [6]
C7 Peptide Click here for species-specific activity table Hs Antagonist 8.7 – 9.2 pKi 5-6
⤷ pKi 8.7 – 9.2 (Ki 2x10-9 – 6.3x10-10 M) [5-6]
M15 Peptide Click here for species-specific activity table Mm Antagonist 8.9 pKi