Table 1.
A schematic representation of GPR35 ligands.
| Name | Type | Potency (EC50) | Role in inflammation | References |
|---|---|---|---|---|
| Kynurenic acid | Metabolite of L-tryptophan |
Human: 217 μM Rat: 66 μM |
Anti-inflammatory | (52, 53) |
| LPA | Phospholipid derivative | Not reported | Pro-inflammatory | (54, 55) |
| 5-HIAA | Serotonin metabolite | Not reported | Pro-inflammatory in Neutrophils |
(26) |
| CXCL17 | Endogenous peptide | Not reported | Anti-inflammatory | (56, 57) |
| cGMP | Cyclic nucleotide derived from GTP | Human: 131 μM | No conclusion | (58) |
| DHICA | Intermediate in the biosynthesis of elanin |
Human: 22 μM | No conclusion | (40) |
| Reverse T3 | Hormone produced in the thyroid gland | Human: 100 μM | No conclusion | (40) |
| Zaprinast | Synthetic agonist | Human: 2-8 μM Mouse: 1 μM Rat: 100 nM |
No conclusion | (59) |
| Pamoic acid | Synthetic agonist | Human: 30-50 nM Mouse: Inactive Rat: >100 μM |
Anti-inflammatory | (60, 61) |
| YE120 | Synthetic agonist | Human: 30-35 nM | Anti-inflammatory | (62, 63) |
| Lodoxamide | Synthetic agonist | Human: 4 nM Rat: 13 nM |
Allergic inhibition | (51) |
| Bufrolin | Synthetic agonist | Human: 13 nM Rat: 10 nM |
Allergic inhibition | (51) |
| Compound 1 | Synthetic agonist | Human: 26 nM Mouse: 17 μM Rat: 8 μM |
No conclusion | (64) |
| PSB-13253 | Synthetic agonist | Human: 12 nM Mouse: Inactive Rat: 1.4 μM |
No conclusion | (65) |
| Amoxanox | Synthetic agonist | Human: 4 μM Rat: 23 nM |
Mast cell stabilizer,anti-asthma and anti-allergy medication | (51) |
| Cromolyn disodium | Synthetic agonist | Not reported | Mast cell stabilizer, mitigate asthma | (21) |
| Nedocromil | Synthetic agonist | Human: 0.13 μM Mouse: 7.3 μM Rat: 2.7 μM |
Mast cell stabilizer, mitigate asthma | (21) |
| Doxantrazole | Synthetic agonist | Human: 3.4 μM Rat: 300 nM |
Mast cell stabilizer | (51) |
| Pemirolast | Synthetic agonist | Human: Inactive Rat: 95 nM |
Mast cell stabilizer | (51) |
| Furosemide | Synthetic agonist | Human: 8.3 μM | Anti-inflammatory | (66) |
| Tyrphostin-51 | Synthetic agonist | Human: 8 μM (DMR 120 nM) | No conclusion | (67) |
| 2,3,5-THB | Synthetic agonist | Human: 8.4 μM (DMR 250 nM) |
No conclusion | (68) |
| Gallic acid | Synthetic agonist | Human: 11.4 μM (DMR 1.16 μM) | Anti-inflammatory | (69) |
| wedelolactone | Synthetic agonist | Human: 1.39 μM (DMR 2.73 μM) | Anti-inflammatory | (69) |
| Ellagic acid | Synthetic agonist | Human: 2.96 μM (DMR 110 nM) | Anti-inflammatory | (69) |
| Aminosalicylate | Synthetic agonist | Not reported | Anti-inflammatory | (70) |
| Compound 50 | Synthetic agonist | Human: 5.8 nM | No conclusion | (71) |
| CID2745687 | Synthetic antagonist | Human (Ki): 10-20 nM | No conclusion | (60) |
| ML-145 | Synthetic antagonist | Human (Ki): 25 nM | No conclusion | (72) |