Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | prostaglandin D2 receptor (DP) | Starlite/ChEMBL | References |
Mus musculus | prostaglandin D2 receptor 2 | Starlite/ChEMBL | References |
Homo sapiens | thromboxane A2 receptor | Starlite/ChEMBL | References |
Homo sapiens | prostaglandin D2 receptor 2 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Echinococcus multilocularis | rhodopsin orphan GPCR | prostaglandin D2 receptor (DP) | 359 aa | 312 aa | 23.1 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Brugia malayi | LBP / BPI / CETP family, C-terminal domain containing protein | 0.0156 | 1 | 1 |
Onchocerca volvulus | 0.0156 | 1 | 1 | |
Onchocerca volvulus | 0.0156 | 1 | 1 | |
Onchocerca volvulus | 0.0156 | 1 | 1 | |
Onchocerca volvulus | 0.0156 | 1 | 1 | |
Onchocerca volvulus | 0.0156 | 1 | 1 | |
Onchocerca volvulus | 0.0156 | 1 | 1 | |
Onchocerca volvulus | 0.0156 | 1 | 1 | |
Loa Loa (eye worm) | hypothetical protein | 0.0156 | 1 | 1 |
Onchocerca volvulus | 0.0156 | 1 | 1 | |
Loa Loa (eye worm) | LBP/BPI/CETP family domain-containing protein | 0.0156 | 1 | 1 |
Brugia malayi | LBP / BPI / CETP family, N-terminal domain containing protein | 0.0156 | 1 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 1.2 nM | Inhibition of CRTH2 receptor-mediated chemotaxis in human basophils | ChEMBL. | 24512187 |
IC50 (binding) | = 1.4 nM | Binding affinity to human CRTH2 receptor | ChEMBL. | 24512187 |
IC50 (binding) | = 4 nM | Inhibition of mouse CRTH2 receptor | ChEMBL. | 24512187 |
IC50 (binding) | = 6 nM | Antagonist activity at human recombinant CRTh2 expressed in CHO-K1 cells by cAMP TR FRET assay | ChEMBL. | 24512187 |
IC50 (binding) | = 8 nM | Antagonist activity at CRTh2 in human peripheral blood assessed as inhibition of PGD2-induced eosinophil shape change at room temperature by flow cytometry | ChEMBL. | 24512187 |
IC50 (binding) | > 1000 nM | Antagonist activity at TXA2 receptor (unknown origin) by FRET assay | ChEMBL. | 24512187 |
IC50 (binding) | = 16000 nM | Binding affinity to DP1 receptor (unknown origin) by FRET assay | ChEMBL. | 24512187 |
IC50 (ADMET) | = 55 uM | Inhibition of CYP2C9 (unknown origin) | ChEMBL. | 24512187 |
IC50 (ADMET) | > 100 uM | Inhibition of CYP3A4 (unknown origin) | ChEMBL. | 24512187 |
IC50 (ADMET) | > 100 uM | Inhibition of CYP2D6 (unknown origin) | ChEMBL. | 24512187 |
IC50 (ADMET) | > 100 uM | Inhibition of CYP2C19 (unknown origin) | ChEMBL. | 24512187 |
IC50 (ADMET) | > 100 uM | Inhibition of CYP2B6 (unknown origin) | ChEMBL. | 24512187 |
IC50 (ADMET) | > 100 uM | Inhibition of CYP2A6 (unknown origin) | ChEMBL. | 24512187 |
IC50 (ADMET) | > 100 uM | Inhibition of CYP1A2 (unknown origin) | ChEMBL. | 24512187 |
Inhibition (functional) | = 50.45 % | Antiallergic inflammatory activity in oxazolone induced contact hypersensitivity mouse model assessed as reduction ear swelling at 3 mg/kg, po prior to oxazolone and 7 hrs post challenge measured after 24 hrs | ChEMBL. | 24512187 |
Papp (ADMET) | = 2.7 ucm/s | Permeability in human Caco2 cells at pH 6 | ChEMBL. | 24512187 |
Many chemical entities in TDR Targets come from high-throughput screenings with whole cells or tissue samples, and not all assayed compounds have been tested against a single a single target protein, probably because they get ruled out during screening process. Even if these compounds may have not been of interest in the original screening, they may come as interesting leads for other screening assays. Furthermore, we may be able to propose drug-target associations using chemical similarities and network patterns.
1 literature reference was collected for this gene.