Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | glucagon receptor | Starlite/ChEMBL | References |
Homo sapiens | gastric inhibitory polypeptide receptor | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Loa Loa (eye worm) | pigment dispersing factor receptor c | gastric inhibitory polypeptide receptor | 466 aa | 425 aa | 24.7 % |
Loa Loa (eye worm) | pigment dispersing factor receptor c | glucagon receptor | 477 aa | 457 aa | 25.4 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Brugia malayi | Low-density lipoprotein receptor repeat class B containing protein | 0.0179 | 0.1882 | 0.8351 |
Onchocerca volvulus | Arrow homolog | 0.0179 | 0.1882 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0179 | 0.1882 | 0.1882 |
Toxoplasma gondii | calcium binding egf domain-containing protein | 0.0199 | 0.2253 | 0.5 |
Loa Loa (eye worm) | low-density lipoprotein receptor repeat class B containing protein | 0.0179 | 0.1882 | 0.1882 |
Brugia malayi | Calcium binding EGF domain containing protein | 0.0199 | 0.2253 | 1 |
Loa Loa (eye worm) | multiple epidermal growth factor-like domains 6 | 0.0199 | 0.2253 | 0.2253 |
Schistosoma mansoni | subfamily M12A unassigned peptidase (M12 family) | 0.0618 | 1 | 1 |
Loa Loa (eye worm) | pigment dispersing factor receptor c | 0.012 | 0.0795 | 0.0795 |
Loa Loa (eye worm) | hypothetical protein | 0.0592 | 0.9535 | 0.9535 |
Loa Loa (eye worm) | hypothetical protein | 0.0252 | 0.3223 | 0.3223 |
Echinococcus multilocularis | Tolloid protein 1 | 0.0618 | 1 | 1 |
Brugia malayi | latrophilin 2 splice variant baaae | 0.0082 | 0.0089 | 0.0397 |
Brugia malayi | Calcitonin receptor-like protein seb-1 | 0.012 | 0.0795 | 0.3527 |
Brugia malayi | Corticotropin releasing factor receptor 2 precursor, putative | 0.012 | 0.0795 | 0.3527 |
Loa Loa (eye worm) | bone morphogenetic protein 1b | 0.0618 | 1 | 1 |
Toxoplasma gondii | calcium binding egf domain-containing protein | 0.0199 | 0.2253 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0179 | 0.1882 | 0.1882 |
Loa Loa (eye worm) | hypothetical protein | 0.0082 | 0.0089 | 0.0089 |
Brugia malayi | Fibulin-1 precursor | 0.0199 | 0.2253 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.012 | 0.0795 | 0.0795 |
Schistosoma mansoni | egf-like domain protein | 0.0179 | 0.1882 | 0.1808 |
Loa Loa (eye worm) | AStacin protease | 0.0386 | 0.5714 | 0.5714 |
Loa Loa (eye worm) | hypothetical protein | 0.0199 | 0.2253 | 0.2253 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
AUC (ADMET) | = 0.34 uM.hr | Normalized AUC in mouse at 2 mg/kg, po | ChEMBL. | 17126016 |
AUC (ADMET) | = 0.34 uM.hr | Normalized AUC in mouse at 2 mg/kg, po | ChEMBL. | 17126016 |
CL (ADMET) | = 13 ml/min.kg | Plasma clearance in mouse at 1 mg/kg, iv and 2 mg/kg, po | ChEMBL. | 17126016 |
CL (ADMET) | = 13 ml/min.kg | Plasma clearance in mouse at 1 mg/kg, iv and 2 mg/kg, po | ChEMBL. | 17126016 |
Cmax (ADMET) | = 0.06 uM | Cmax in mouse at 1 mg/kg, iv and 2 mg/kg, po | ChEMBL. | 17126016 |
Cmax (ADMET) | = 0.06 uM | Cmax in mouse at 1 mg/kg, iv and 2 mg/kg, po | ChEMBL. | 17126016 |
F (ADMET) | = 15 % | Bioavailability in mouse at 1 mg/kg, iv and 2 mg/kg, po | ChEMBL. | 17126016 |
F (ADMET) | = 15 % | Bioavailability in mouse at 1 mg/kg, iv and 2 mg/kg, po | ChEMBL. | 17126016 |
IC50 (binding) | = 4.8 nM | Displacement of [125]glucagon from human glucagon receptor expressed in CHO cells | ChEMBL. | 17126016 |
IC50 (binding) | = 4.8 nM | Displacement of [125]glucagon from human glucagon receptor expressed in CHO cells | ChEMBL. | 17126016 |
IC50 (functional) | = 44 nM | Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation | ChEMBL. | 17126016 |
IC50 (functional) | = 44 nM | Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation | ChEMBL. | 17126016 |
IC50 (functional) | = 217 nM | Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation | ChEMBL. | 17126016 |
IC50 (functional) | = 217 nM | Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation | ChEMBL. | 17126016 |
IC50 (binding) | = 218 nM | Displacement of [125]glucagon from human glucagon receptor expressed in CHO cells | ChEMBL. | 17126016 |
IC50 (binding) | = 218 nM | Displacement of [125]glucagon from human glucagon receptor expressed in CHO cells | ChEMBL. | 17126016 |
IC50 (functional) | = 1013 nM | Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation | ChEMBL. | 17126016 |
IC50 (functional) | = 1013 nM | Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation | ChEMBL. | 17126016 |
t1/2 (ADMET) | = 3.4 hr | Half life in mouse at 1 mg/kg, iv and 2 mg/kg, po | ChEMBL. | 17126016 |
T1/2 (ADMET) | = 3.4 hr | Half life in mouse at 1 mg/kg, iv and 2 mg/kg, po | ChEMBL. | 17126016 |
Vdss (ADMET) | = 1.4 L/Kg | Volume of distribution at steady state in mouse at 1 mg/kg, iv and 2 mg/kg, po | ChEMBL. | 17126016 |
Vdss (ADMET) | = 1.4 L/Kg | Volume of distribution at steady state in mouse at 1 mg/kg, iv and 2 mg/kg, po | ChEMBL. | 17126016 |
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.