Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | retinoic acid receptor, alpha | Starlite/ChEMBL | References |
Homo sapiens | retinoid X receptor, alpha | Starlite/ChEMBL | References |
Homo sapiens | retinoic acid receptor, gamma | Starlite/ChEMBL | References |
Homo sapiens | retinoic acid receptor, beta | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | ecdysteroid receptor | retinoid X receptor, alpha | 435 aa | 352 aa | 23.9 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Schistosoma mansoni | retinoic acid receptor RXR | 0.0165 | 0.0359 | 0.5 |
Brugia malayi | nuclear hormone receptor | 0.0791 | 0.9641 | 0.5 |
Echinococcus granulosus | retinoic acid receptor rxr beta a | 0.0165 | 0.0359 | 0.5 |
Loa Loa (eye worm) | nuclear receptor nhr-7B | 0.0791 | 0.9641 | 1 |
Echinococcus multilocularis | retinoic acid receptor rxr beta a retinoic acid receptor rxr alpha a retinoic acid receptor rxr alpha | 0.0141 | 0 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
AC50 (binding) | < 1 nM | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor beta | ChEMBL. | 10890153 |
AC50 (binding) | < 1 nM | Transcriptional activation in CV-1 cells expressing retinoic acid gamma receptor | ChEMBL. | 10890153 |
AC50 (binding) | < 1 nM | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor beta | ChEMBL. | 10890153 |
AC50 (binding) | < 1 nM | Transcriptional activation in CV-1 cells expressing retinoic acid gamma receptor | ChEMBL. | 10890153 |
AC50 (binding) | = 14 nM | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor alpha | ChEMBL. | 10890153 |
AC50 (binding) | = 14 nM | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor alpha | ChEMBL. | 10890153 |
AC50 (binding) | = 100 nM | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RXR-alpha | ChEMBL. | 10890153 |
AC50 (binding) | = 100 nM | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RXR-alpha | ChEMBL. | 10890153 |
Activation (binding) | = 65 % | Percent activation of Retinoic acid receptor RXR-alpha at 1 uM relative to 1 uM 9-cis-retinoic acid | ChEMBL. | 10890153 |
Activation (binding) | = 65 % | Percent activation of Retinoic acid receptor RXR-alpha at 1 uM relative to 1 uM 9-cis-retinoic acid | ChEMBL. | 10890153 |
Activation (binding) | = 86 % | Percent activation of Retinoic acid receptor alpha at 1 uM relative to 1 uM trans-retinoic acid | ChEMBL. | 10890153 |
Activation (binding) | = 86 % | Percent activation of Retinoic acid receptor alpha at 1 uM relative to 1 uM trans-retinoic acid | ChEMBL. | 10890153 |
Activation (binding) | = 88 % | Percent activation of Retinoic acid receptor gamma receptor at 1 uM relative to 1 uM trans-retinoic acid | ChEMBL. | 10890153 |
Activation (binding) | = 88 % | Percent activation of Retinoic acid receptor gamma receptor at 1 uM relative to 1 uM trans-retinoic acid | ChEMBL. | 10890153 |
Activation (binding) | = 94 % | Percent activation of Retinoic acid receptor beta at 1 uM relative to 1 uM trans-retinoic acid | ChEMBL. | 10890153 |
Activation (binding) | = 94 % | Percent activation of Retinoic acid receptor beta at 1 uM relative to 1 uM trans-retinoic acid | ChEMBL. | 10890153 |
Inhibition (functional) | = 23 % | Inhibition of T47D retinoid sensitive breast carcinoma cell proliferation at 1 uM | ChEMBL. | 10890153 |
Inhibition (functional) | = 23 % | Inhibition of T47D retinoid sensitive breast carcinoma cell proliferation at 1 uM | ChEMBL. | 10890153 |
Inhibition (functional) | = 42 % | Inhibition of ZR-75-1 retinoid sensitive breast carcinoma cell proliferation at 1 uM | ChEMBL. | 10890153 |
Inhibition (functional) | = 42 % | Inhibition of ZR-75-1 retinoid sensitive breast carcinoma cell proliferation at 1 uM | ChEMBL. | 10890153 |
Inhibition (functional) | = 65 % | Inhibition of MDA-MB-231 retinoid resistant breast carcinoma cell proliferation at 1 uM | ChEMBL. | 10890153 |
Inhibition (functional) | = 65 % | Inhibition of MDA-MB-231 retinoid resistant breast carcinoma cell proliferation at 1 uM | ChEMBL. | 10890153 |
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.