Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | solute carrier family 10 (sodium/bile acid cotransporter), member 2 | Starlite/ChEMBL | References |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus multilocularis | sodium bile acid cotransporter | 0.0247 | 0.2218 | 1 |
Schistosoma mansoni | sodium-bile acid cotransporter related | 0.0247 | 0.2218 | 0.4384 |
Brugia malayi | Sodium Bile acid symporter family protein | 0.0247 | 0.2218 | 0.558 |
Echinococcus granulosus | sodium bile acid cotransporter | 0.0247 | 0.2218 | 1 |
Loa Loa (eye worm) | beta-glucuronidase | 0.0221 | 0.1822 | 0.6331 |
Loa Loa (eye worm) | glycosyl hydrolase family 2 | 0.024 | 0.21 | 0.8909 |
Trichomonas vaginalis | conserved hypothetical protein | 0.0567 | 0.7042 | 0.6583 |
Schistosoma mansoni | beta-mannosidase | 0.0189 | 0.1343 | 0.2655 |
Echinococcus multilocularis | sodium bile acid cotransporter | 0.0247 | 0.2218 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0247 | 0.2218 | 1 |
Entamoeba histolytica | beta-galactosidase, putative | 0.0346 | 0.3707 | 0.5 |
Trichomonas vaginalis | beta-galactosidase, putative | 0.0567 | 0.7042 | 0.6583 |
Echinococcus granulosus | sodium bile acid cotransporter | 0.0247 | 0.2218 | 1 |
Schistosoma mansoni | hypothetical protein | 0.0436 | 0.5059 | 1 |
Schistosoma mansoni | alpha-glucosidase | 0.0151 | 0.0771 | 0.1523 |
Schistosoma mansoni | alpha-glucosidase | 0.0151 | 0.0771 | 0.1523 |
Brugia malayi | manba-prov protein | 0.0304 | 0.3072 | 1 |
Brugia malayi | Glycosyl hydrolases family 2, sugar binding domain containing protein | 0.024 | 0.21 | 0.4971 |
Echinococcus multilocularis | sodium bile acid cotransporter | 0.0247 | 0.2218 | 1 |
Echinococcus granulosus | sodium bile acid cotransporter | 0.0247 | 0.2218 | 1 |
Schistosoma mansoni | sodium-bile acid cotransporter | 0.0147 | 0.0705 | 0.1394 |
Onchocerca volvulus | 0.0247 | 0.2218 | 1 | |
Brugia malayi | Beta-glucuronidase precursor | 0.0221 | 0.1822 | 0.3532 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Efficacy (functional) | = 47 % | In vivo inhibition of ASBT in C57BL/6J mouse assessed as increase in fecal bile acid excretion measured for 24 hrs relative to 264W94 | ChEMBL. | 23678871 |
IC50 (binding) | Inhibition of rat ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis | ChEMBL. | 23678871 | |
IC50 (binding) | Inhibition of mouse ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis | ChEMBL. | 23678871 | |
IC50 (binding) | = 59 nM | Inhibition of human ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis | ChEMBL. | 23678871 |
IC50 (binding) | = 59 nM | BindingDB_Patents: Inhibition Assay. On the day of the uptake experiment, 10 mM HEPES was added to Hank's Balanced Salt Solution, and the pH was adjusted to 7.4 with TRIS (HBSSH). The assay buffer was prepared by adding 100 uM [3H]-taurocholate and 10 uM cold taurocholate to room temperature HBSSH. A separate washing buffer was prepared by adding 10 uM cold taurocholate to HBSSH (30 ml per assay plate) and placed on ice. Using 100% DMSO, 8 point, 3-fold dilution curves for each test compound was prepared starting at 200 uM. Similarly, an 8 point dose response curve was prepared of the control compound [(3R,5R)-3-butyl-3-ethyl-7,8-bis(methyloxy)-5-phenyl-2,3,4,5-tetrahydro-1,4-benzothiazepine 1,1-dioxide (Brieaddy, L. E. WO9605188, 1996)] starting at 1.8 mM. Drug plates were created by adding 3 uL of each concentration to a v-bottom 96-well plate then diluted 60-fold with 177 uL of assay buffer. Plates were removed from the incubator and allowed to cool to ambient temperature. | ChEMBL. | No reference |
IC50 (binding) | = 59 nM | BindingDB_Patents: Inhibition Assay. On the day of the uptake experiment, 10 mM HEPES was added to Hank's Balanced Salt Solution, and the pH was adjusted to 7.4 with TRIS (HBSSH). The assay buffer was prepared by adding 100 uM [3H]-taurocholate and 10 uM cold taurocholate to room temperature HBSSH. A separate washing buffer was prepared by adding 10 uM cold taurocholate to HBSSH (30 ml per assay plate) and placed on ice. Using 100% DMSO, 8 point, 3-fold dilution curves for each test compound was prepared starting at 200 uM. Similarly, an 8 point dose response curve was prepared of the control compound [(3R,5R)-3-butyl-3-ethyl-7,8-bis(methyloxy)-5-phenyl-2,3,4,5-tetrahydro-1,4-benzothiazepine 1,1-dioxide (Brieaddy, L. E. WO9605188, 1996)] starting at 1.8 mM. Drug plates were created by adding 3 uL of each concentration to a v-bottom 96-well plate then diluted 60-fold with 177 uL of assay buffer. Plates were removed from the incubator and allowed to cool to ambient temperature. | ChEMBL. | No reference |
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.