Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | retinoid X receptor, alpha | Starlite/ChEMBL | References |
Mus musculus | retinoid X receptor gamma | Starlite/ChEMBL | References |
Homo sapiens | retinoic acid receptor, alpha | Starlite/ChEMBL | References |
Mus musculus | retinoid X receptor beta | Starlite/ChEMBL | References |
Homo sapiens | retinoic acid receptor, beta | Starlite/ChEMBL | References |
Homo sapiens | retinoic acid receptor, gamma | 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 % |
Brugia malayi | ecdysteroid receptor | retinoid X receptor gamma | 340 aa | 338 aa | 24.6 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Schistosoma mansoni | retinoic acid receptor RXR | 0.0507 | 0.1003 | 0.5 |
Brugia malayi | nuclear hormone receptor | 0.0802 | 0.8997 | 0.5 |
Loa Loa (eye worm) | nuclear receptor nhr-7B | 0.0802 | 0.8997 | 1 |
Echinococcus multilocularis | retinoic acid receptor rxr beta a retinoic acid receptor rxr alpha a retinoic acid receptor rxr alpha | 0.047 | 0 | 0.5 |
Echinococcus granulosus | retinoic acid receptor rxr beta a | 0.0507 | 0.1003 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
AC50 (binding) | = 22 nM | Transcriptional activation in CV-1 cells expressing Retinoid X receptor RXR-alpha | ChEMBL. | 10890152 |
AC50 (binding) | = 22 nM | Transcriptional activation in CV-1 cells expressing Retinoid X receptor RXR-alpha | ChEMBL. | 10890152 |
AC50 (binding) | > 1000 nM | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR alpha | ChEMBL. | 10890152 |
AC50 (binding) | > 1000 nM | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR beta | ChEMBL. | 10890152 |
AC50 (binding) | > 1000 nM | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR gamma | ChEMBL. | 10890152 |
AC50 (binding) | > 1000 nM | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR alpha | ChEMBL. | 10890152 |
AC50 (binding) | > 1000 nM | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR beta | ChEMBL. | 10890152 |
AC50 (binding) | > 1000 nM | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR gamma | ChEMBL. | 10890152 |
Activation (binding) | = -12 % | Percent transcriptional activation of Retinoic acid receptor RAR gamma receptor at 1 uM compared to 1 uM trans-retinoic acid | ChEMBL. | 10890152 |
Activation (binding) | = -12 % | Percent transcriptional activation of Retinoic acid receptor RAR gamma receptor at 1 uM compared to 1 uM trans-retinoic acid | ChEMBL. | 10890152 |
Activation (binding) | = -6 % | Percent transcriptional activation of Retinoic acid receptor beta at 1 uM compared to 1 uM trans-retinoic acid | ChEMBL. | 10890152 |
Activation (binding) | = -6 % | Percent transcriptional activation of Retinoic acid receptor beta at 1 uM compared to 1 uM trans-retinoic acid | ChEMBL. | 10890152 |
Activation (binding) | = 0 % | Percent transcriptional activation of Retinoic acid receptor RAR alpha at 1 uM compared to 1 uM trans-retinoic acid | ChEMBL. | 10890152 |
Activation (binding) | = 0 % | Percent transcriptional activation of Retinoic acid receptor RAR alpha at 1 uM compared to 1 uM trans-retinoic acid | ChEMBL. | 10890152 |
Activation (binding) | = 107 % | Percent transcriptional activation of Retinoic acid receptor RXR-alpha at 1 uM compared to 1 uM 9-cis-retinoic acid | ChEMBL. | 10890152 |
Activation (binding) | = 107 % | Percent transcriptional activation of Retinoic acid receptor RXR-alpha at 1 uM compared to 1 uM 9-cis-retinoic acid | ChEMBL. | 10890152 |
Activity (functional) | 0 | Effect on MDA-MB-231 cell proliferation; No inhibition | ChEMBL. | 10890152 |
Activity (functional) | 0 | Effect on MDA-MB-231 cell proliferation with trans-RA; No inhibition | ChEMBL. | 10890152 |
EC50 (binding) | = 130 nM | Ability to activate gene expression at Retinoic acid receptor RXR-beta was evaluated in a cotransfection assay. | ChEMBL. | 7636877 |
EC50 (binding) | = 130 nM | Ability to activate gene expression at Retinoic acid receptor RXR-beta was evaluated in a cotransfection assay. | ChEMBL. | 7636877 |
EC50 (binding) | = 240 nM | Ability to activate gene expression at Retinoic acid receptor RXR-gamma was evaluated in a cotransfection assay. | ChEMBL. | 7636877 |
EC50 (binding) | = 240 nM | Ability to activate gene expression at Retinoic acid receptor RXR-gamma was evaluated in a cotransfection assay. | ChEMBL. | 7636877 |
EC50 (binding) | = 300 nM | Ability to activate gene expression at Retinoic acid receptor RXR-alpha was evaluated in a cotransfection assay. | ChEMBL. | 7636877 |
EC50 (binding) | = 300 nM | Ability to activate gene expression at Retinoic acid receptor RXR-alpha was evaluated in a cotransfection assay. | ChEMBL. | 7636877 |
Kd (binding) | = 50 nM | Ability to bind directly to Retinoic acid receptor RXR-alpha was evaluated in a competitive binding assay. | ChEMBL. | 7636877 |
Kd (binding) | = 50 nM | Ability to bind directly to Retinoic acid receptor RXR-alpha was evaluated in a competitive binding assay. | ChEMBL. | 7636877 |
Kd (binding) | = 150 nM | Binding affinity to Retinoic acid receptor RXR-gamma was evaluated in a competitive binding assay. | ChEMBL. | 7636877 |
Kd (binding) | = 150 nM | Binding affinity to Retinoic acid receptor RXR-gamma was evaluated in a competitive binding assay. | ChEMBL. | 7636877 |
Kd (binding) | = 160 nM | Binding affinity to Retinoic acid receptor RXR-beta was determined in a competitive binding assay. | ChEMBL. | 7636877 |
Kd (binding) | = 160 nM | Binding affinity to Retinoic acid receptor RXR-beta was determined in a competitive binding assay. | ChEMBL. | 7636877 |
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.
2 literature references were collected for this gene.