Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | endothelin receptor type B | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
AUC (ADMET) | = 41.5 uM hr | Area under curve at oral dose of 25 umol/kg in monkey | ChEMBL. | 12502366 |
AUC (ADMET) | = 161 uM hr | Area under curve at intravenous dose of 25 umol/kg in monkey | ChEMBL. | 12502366 |
Cl (ADMET) | = 2.7 ml min-1 kg-1 | Tested for plasma clearance at intravenous dose of 25 umol/kg in monkey | ChEMBL. | 12502366 |
Cl (ADMET) | = 5.4 ml min-1 kg-1 | Tested for plasma clearance at intravenous dose of 10 micromol/kg in rat | ChEMBL. | 12502366 |
Cmax (ADMET) | = 16.1 uM | Cmax value of the compound at oral dose of 25 umol/kg in monkey | ChEMBL. | 12502366 |
Cmax (ADMET) | = 28 uM | C max value of the compound at oral dose of 10 umol/kg in rat | ChEMBL. | 12502366 |
F (ADMET) | = 26 % | Percent oral bioavailability of the compound at dose of 25 umol/kg in monkey | ChEMBL. | 12502366 |
F (ADMET) | = 100 % | Oral bioavailability in rat (dose 10 microM/kg) | ChEMBL. | 12502366 |
KB (functional) | = 1 nM | In vitro inhibition of ET-1 induced contractions in rabbit carotid artery rings | ChEMBL. | 12502366 |
Ki (binding) | = 0.01 nM | Inhibitory activity against human endothelin A receptor expressed in CHO cells | ChEMBL. | 12502366 |
Ki (binding) | = 0.01 nM | Inhibitory activity against human endothelin A receptor expressed in CHO cells | ChEMBL. | 12502366 |
Ki (binding) | = 810 nM | Inhibitory activity against human endothelin B receptor expressed in CHO cells | ChEMBL. | 12502366 |
Ki (binding) | = 810 nM | Inhibitory activity against human endothelin B receptor expressed in CHO cells | ChEMBL. | 12502366 |
MRT (ADMET) | = 1.6 hr | MRT value of the compound was calculated in monkey | ChEMBL. | 12502366 |
T max (ADMET) | = 0.4 hr | T max value of the compound at oral dose of 10 umol/kg in rat | ChEMBL. | 12502366 |
T max (ADMET) | = 1.2 hr | T max value of the compound at oral dose of 25 umol/kg in monkey | ChEMBL. | 12502366 |
T1/2 (ADMET) | = 3.4 hr | Half life of the compound was determined in rat | ChEMBL. | 12502366 |
T1/2 (ADMET) | = 14 hr | Half life of the compound was determined in monkey at intravenous dose of 25 umol/kg | ChEMBL. | 12502366 |
T1/2 (ADMET) | = 17 hr | Half life of the compound was determined in monkey at oral dose of 25 umol/kg | ChEMBL. | 12502366 |
Vss (ADMET) | = 0.25 l kg-1 | Tested for volume distribution at intravenous dose of 25 umol/kg in monkey | ChEMBL. | 12502366 |
Vss (ADMET) | = 1.1 l kg-1 | Tested for volume distribution at intravenous dose of 10 micromol/kg in rat | ChEMBL. | 12502366 |
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.