Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Mus musculus | retinoid X receptor alpha | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Echinococcus granulosus | retinoic acid receptor rxr beta a | Get druggable targets OG5_130073 | All targets in OG5_130073 |
Schistosoma japonicum | ko:K08524 nuclear receptor, subfamily 2, group B, member 1, putative | Get druggable targets OG5_130073 | All targets in OG5_130073 |
Schistosoma mansoni | retinoic acid receptor RXR | Get druggable targets OG5_130073 | All targets in OG5_130073 |
Echinococcus multilocularis | retinoic acid receptor rxr beta a retinoic acid receptor rxr alpha a retinoic acid receptor rxr alpha | Get druggable targets OG5_130073 | All targets in OG5_130073 |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | ecdysteroid receptor | retinoid X receptor alpha | 439 aa | 352 aa | 23.9 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | GTP-binding regulatory protein Gs alpha-S chain | 0.0097 | 0.2681 | 0.5104 |
Mycobacterium ulcerans | fusion of enoyl-CoA hydratase, EchA21 and lipase, LipE | 0.004 | 0 | 0.5 |
Trypanosoma cruzi | hypothetical protein, conserved | 0.004 | 0 | 0.5 |
Brugia malayi | GTP-binding regulatory protein Gs alpha-S chain, putative | 0.0097 | 0.2681 | 0.5104 |
Echinococcus granulosus | retinoic acid receptor rxr beta a | 0.0139 | 0.463 | 0.7995 |
Schistosoma mansoni | hypothetical protein | 0.0164 | 0.5791 | 1 |
Mycobacterium ulcerans | beta-lactamase | 0.004 | 0 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0153 | 0.5254 | 1 |
Mycobacterium ulcerans | lipase LipD | 0.004 | 0 | 0.5 |
Onchocerca volvulus | 0.004 | 0 | 0.5 | |
Schistosoma mansoni | retinoic acid receptor RXR | 0.0139 | 0.463 | 0.7995 |
Mycobacterium ulcerans | esterase/lipase LipP | 0.004 | 0 | 0.5 |
Echinococcus granulosus | muscleblind protein | 0.0153 | 0.5254 | 0.9073 |
Plasmodium vivax | hypothetical protein, conserved | 0.004 | 0 | 0.5 |
Trichomonas vaginalis | penicillin-binding protein, putative | 0.004 | 0 | 0.5 |
Schistosoma mansoni | Guanine nucleotide-binding protein G(s) subunit alpha (Adenylate cyclase-stimulating G alpha protein) | 0.0097 | 0.2681 | 0.4631 |
Echinococcus multilocularis | muscleblind protein 1 | 0.0153 | 0.5254 | 0.9073 |
Trichomonas vaginalis | D-aminoacylase, putative | 0.004 | 0 | 0.5 |
Schistosoma mansoni | hypothetical protein | 0.0164 | 0.5791 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0153 | 0.5254 | 1 |
Echinococcus multilocularis | muscleblind protein | 0.0153 | 0.5254 | 0.9073 |
Brugia malayi | Muscleblind-like protein | 0.0153 | 0.5254 | 1 |
Echinococcus granulosus | geminin | 0.0164 | 0.5791 | 1 |
Toxoplasma gondii | ABC1 family protein | 0.004 | 0 | 0.5 |
Mycobacterium ulcerans | hypothetical protein | 0.004 | 0 | 0.5 |
Trichomonas vaginalis | penicillin-binding protein, putative | 0.004 | 0 | 0.5 |
Echinococcus multilocularis | retinoic acid receptor rxr beta a retinoic acid receptor rxr alpha a retinoic acid receptor rxr alpha | 0.0129 | 0.4134 | 0.7139 |
Onchocerca volvulus | 0.004 | 0 | 0.5 | |
Onchocerca volvulus | 0.004 | 0 | 0.5 | |
Mycobacterium leprae | Probable lipase LipE | 0.004 | 0 | 0.5 |
Trypanosoma brucei | hypothetical protein, conserved | 0.004 | 0 | 0.5 |
Echinococcus granulosus | guanine nucleotide binding protein Gs subunit | 0.0097 | 0.2681 | 0.4631 |
Echinococcus multilocularis | guanine nucleotide binding protein G(s) subunit | 0.0097 | 0.2681 | 0.4631 |
Schistosoma mansoni | Guanine nucleotide-binding protein G(s) subunit alpha (Adenylate cyclase-stimulating G alpha protein) | 0.0097 | 0.2681 | 0.4631 |
Leishmania major | hypothetical protein, conserved | 0.004 | 0 | 0.5 |
Mycobacterium leprae | conserved hypothetical protein | 0.004 | 0 | 0.5 |
Echinococcus granulosus | guanine nucleotide binding protein Gs subunit | 0.0097 | 0.2681 | 0.4631 |
Echinococcus multilocularis | geminin | 0.0164 | 0.5791 | 1 |
Echinococcus multilocularis | guanine nucleotide binding protein G(s) subunit | 0.0097 | 0.2681 | 0.4631 |
Trichomonas vaginalis | D-aminoacylase, putative | 0.004 | 0 | 0.5 |
Trypanosoma cruzi | hypothetical protein, conserved | 0.004 | 0 | 0.5 |
Trichomonas vaginalis | D-aminoacylase, putative | 0.004 | 0 | 0.5 |
Schistosoma mansoni | Guanine nucleotide-binding protein G(s) subunit alpha (Adenylate cyclase-stimulating G alpha protein) | 0.0097 | 0.2681 | 0.4631 |
Trichomonas vaginalis | esterase, putative | 0.004 | 0 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (binding) | Inhibition of transactivation activity of Gal4-LBD fused human RARbeta (169 to 448) transfected in atRA-stimulated african green monkey CV1 cells at 4 uM after 6 hrs by Dual-light chemiluminescent assay | ChEMBL. | 19216008 | |
Activity (binding) | Transactivation of Gal4-LBD fused mouse RXRalpha (218 to 467) transfected in african green monkey CV1 cells assessed as luciferase activity at 2 uM after 6 hrs by Dual-light chemiluminescent assay | ChEMBL. | 19216008 | |
Activity (binding) | Transactivation of Gal4-LBD fused human RARalpha (156 to 454) transfected in african green monkey CV1 cells assessed as luciferase activity at 2 uM after 6 hrs by Dual-light chemiluminescent assay | ChEMBL. | 19216008 | |
Activity (binding) | Inhibition of transactivation activity of Gal4-LBD fused human RARgamma (178 to 454) transfected in atRA-stimulated african green monkey CV1 cells at 4 uM after 6 hrs by Dual-light chemiluminescent assay | ChEMBL. | 19216008 | |
Activity (binding) | Transactivation of Gal4-LBD fused human RARgamma (178 to 454) transfected in african green monkey CV1 cells assessed as luciferase activity at 2 uM after 20 hrs by Dual-light chemiluminescent assay | ChEMBL. | 19216008 | |
Activity (binding) | Transactivation of Gal4-LBD fused human RARbeta (169 to 448) transfected in african green monkey CV1 cells assessed as luciferase activity at 2 uM after 6 hrs by Dual-light chemiluminescent assay | ChEMBL. | 19216008 | |
Activity (binding) | = 67.1 % | Antagonist activity at Gal4-fused RARalpha (unknown origin) transfected in HEK293 cells assessed as ATRA-induced transcriptional activity at 4 uM by luciferase/beta-galactosidase reporter gene assay relative to ATRA-treated control | ChEMBL. | 24457093 |
Activity (binding) | = 96.2 % | Antagonist activity at Gal4-fused RXRalpha (unknown origin) transfected in HEK293 cells assessed as CD3254-induced transcriptional activity at 4 uM by luciferase/beta-galactosidase reporter gene assay relative to CD3254-treated control | ChEMBL. | 24457093 |
Activity (binding) | = 373 % | Agonist activity at recombinant GST-tagged RXRalpha LBD (unknown origin) assessed as induction of biotinylated SRC-1-676-700 coactivator recruitment after 4 hrs by TR-FRET assay (Rvb = 148 +/- 7%) | ChEMBL. | 24457093 |
Activity (binding) | = 487 % | Agonist activity at recombinant GST-tagged RXRalpha LBD (unknown origin) assessed as induction of fluorescein labeled D22 coactivator recruitment after 4 hrs by TR-FRET assay relative to control | ChEMBL. | 24457093 |
EC50 (binding) | = 0.576 uM | Transactivation of Gal4-LBD fused mouse RXRalpha (218 to 467) transfected in african green monkey CV1 cells assessed as luciferase activity at after 6 hrs by Dual-light chemiluminescent assay | ChEMBL. | 19216008 |
IC50 (functional) | = 1.414 uM | Antiproliferative activity against human Jurkat T cells after 48 hrs by MTT assay | ChEMBL. | 19216008 |
Inhibition (binding) | Inhibition of transactivation activity of Gal4-LBD fused human RARalpha (156 to 454) transfected in atRA-stimulated african green monkey CV1 cells at 0.2 uM after 6 hrs by Dual-light chemiluminescent assay | ChEMBL. | 19216008 | |
Inhibition (binding) | = 4.9 % | Inhibition of recombinant IKKbeta (unknown origin) using ulight-IkappaomegaBalpha as substrate at 20 uM after 2 hrs by LANCE ultra TR-FRET assay relative to control | ChEMBL. | 24457093 |
Inhibition (binding) | = 11.9 % | Inhibition of recombinant IKKepsilon (unknown origin) using ulight-rpS6 as substrate at 20 uM after 1 hr by LANCE ultra TR-FRET assay relative to control | ChEMBL. | 24457093 |
Inhibition (binding) | = 23.7 % | Inhibition of recombinant IKKalpha (unknown origin) using ulight-IkappaomegaBalpha as substrate at 20 uM after 2 hrs by LANCE ultra TR-FRET assay relative to control | ChEMBL. | 24457093 |
Inhibition (functional) | = 23.7 % | Antiproliferative activity against human A549 cells at 4 uM after 72 hrs by MTT assay | ChEMBL. | 19216008 |
Inhibition (functional) | = 24.2 % | Antiproliferative activity against human T47D cells at 4 uM after 48 hrs by MTT assay | ChEMBL. | 19216008 |
Inhibition (functional) | = 24.9 % | Antiproliferative activity against human MDA-MB-468 cells at 4 uM after 48 hrs by MTT assay | ChEMBL. | 19216008 |
Inhibition (functional) | = 26.3 % | Antiproliferative activity against human MIAPaCa2 cells at 4 uM after 48 hrs by MTT assay | ChEMBL. | 19216008 |
Inhibition (functional) | = 36 % | Antiproliferative activity against human BxPC3 cells at 4 uM after 48 hrs by MTT assay | ChEMBL. | 19216008 |
Inhibition (functional) | = 65.1 % | Antiproliferative activity against human SKOV3 cells at 4 uM after 48 hrs by MTT assay | ChEMBL. | 19216008 |
Inhibition (functional) | = 68.7 % | Antiproliferative activity against human PC3 cells at 4 uM after 48 hrs by MTT assay | ChEMBL. | 19216008 |
Species name | Source | Reference | Is orphan |
---|---|---|---|
Homo sapiens | ChEMBL23 | 19216008 |
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.