Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | nuclear receptor nhr-7B | 0.1367 | 0.901 | 1 |
Echinococcus granulosus | retinoic acid receptor rxr beta a | 0.1331 | 0.8633 | 1 |
Echinococcus multilocularis | retinoic acid receptor rxr beta a retinoic acid receptor rxr alpha a retinoic acid receptor rxr alpha | 0.1236 | 0.7643 | 1 |
Brugia malayi | nuclear hormone receptor | 0.1367 | 0.901 | 0.5 |
Schistosoma mansoni | retinoic acid receptor RXR | 0.1331 | 0.8633 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activation (functional) | = 6.3 fold | Transcriptional activation in CV-1 cells expressing RXR and LXR at 1 uM | ChEMBL. | 12801232 |
Activity (functional) | = 152 mg dl-1 | Effect on triglyceride level in male Dawley rats at 24 hr r | ChEMBL. | 12801232 |
Activity (functional) | = 400 mg dl-1 | Hypoglycemic activity in db/db mouse model after 7 days at 10 mg/kg/day oral dose | ChEMBL. | 12954061 |
Activity (functional) | = 400 mg dl-1 | In vivo hypoglycemic activity, as reduced plasma glucose in db/db mouse type II diabetes model | ChEMBL. | 12801232 |
Activity (functional) | = 400 mg dl-1 | Hypoglycemic activity in db/db mouse model after 7 days at 10 mg/kg/day oral dose | ChEMBL. | 12954061 |
Activity (functional) | = 400 mg dl-1 | In vivo hypoglycemic activity, as reduced plasma glucose in db/db mouse type II diabetes model | ChEMBL. | 12801232 |
Activity (functional) | = 37 ng ml-1 | Effect on T4 levels in male Dawley rats at 24 hr r | ChEMBL. | 12801232 |
EC50 (functional) | 0 nM | Agonist activity for Retinoic X receptor alpha in CV1 cells | ChEMBL. | 15006411 |
EC50 (binding) | = 3 nM | Ability to activate gene expression at Retinoic acid receptor RXR-beta was evaluated in a cotransfection assay. | ChEMBL. | 7636877 |
EC50 (binding) | = 3 nM | Ability to activate gene expression at Retinoic acid receptor RXR-beta was evaluated in a cotransfection assay. | ChEMBL. | 7636877 |
EC50 (binding) | = 4 nM | Ability to activate gene expression at Retinoic acid receptor RXR-alpha was evaluated in a cotransfection assay. | ChEMBL. | 7636877 |
EC50 (binding) | = 4 nM | Ability to activate gene expression at Retinoic acid receptor RXR-gamma was evaluated in a cotransfection assay. | ChEMBL. | 7636877 |
EC50 (binding) | = 4 nM | Ability to activate gene expression at Retinoic acid receptor RXR-alpha was evaluated in a cotransfection assay. | ChEMBL. | 7636877 |
EC50 (binding) | = 4 nM | Ability to activate gene expression at Retinoic acid receptor RXR-gamma was evaluated in a cotransfection assay. | ChEMBL. | 7636877 |
EC50 (binding) | = 11 nM | In vitro transcriptional activation in CV-1 cells expressing RXR-alpha | ChEMBL. | 12954061 |
EC50 (functional) | = 11 nM | Inhibition of Retinoic acid receptor RXR-alpha agonist activity in vitro | ChEMBL. | 12801232 |
EC50 (binding) | = 11 nM | In vitro transcriptional activation in CV-1 cells expressing RXR-alpha | ChEMBL. | 12954061 |
EC50 (functional) | = 11 nM | Inhibition of Retinoic acid receptor RXR-alpha agonist activity in vitro | ChEMBL. | 12801232 |
EC50 (functional) | = 17 nM | In vitro agonistic activity against RXR alpha in CV-1 cells | ChEMBL. | 14592510 |
EC50 (functional) | = 17 nM | In vitro agonistic activity against RXR alpha in CV-1 cells | ChEMBL. | 14592510 |
EC50 (functional) | = 18.6 nM | In vitro agonistic activity against PPAR gamma along with 100 nM BRL49653 | ChEMBL. | 14592510 |
EC50 (functional) | = 18.6 nM | In vitro agonistic activity against PPAR gamma along with 100 nM BRL49653 | ChEMBL. | 14592510 |
EC50 (functional) | = 38 nM | Transcriptional activity against RXR:PPAR-gamma synergy was determined in vitro | ChEMBL. | 12801232 |
EC50 (functional) | = 38 nM | Transcriptional activity against RXR:PPAR-gamma synergy was determined in vitro | ChEMBL. | 12801232 |
EC50 (binding) | = 99 nM | In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay was determined | ChEMBL. | 12954061 |
EC50 (functional) | = 161 nM | In vitro agonist efficacy against PPAR gamma along with 100 nM BRL49653 | ChEMBL. | 14592510 |
EC50 (functional) | = 161 nM | In vitro agonist efficacy against PPAR gamma along with 100 nM BRL49653 | ChEMBL. | 14592510 |
EC50 (binding) | = 0.04 uM | Activation of human RXRalpha activity expressed in COS1 cells after 12 hrs by RXRE-luciferase reporter gene assay | ChEMBL. | 23472886 |
Efficacy (functional) | = 12 | Antagonistic efficacy against Retinoic acid receptor RXR-alpha was determined in vitro | ChEMBL. | 12801232 |
Efficacy (functional) | = 70 | Agonistic efficacy against Retinoic acid receptor RXR-alpha was determined in vitro | ChEMBL. | 12801232 |
Efficacy (functional) | = 166 | Synergistic efficacy against RXR:PPAR-gamma heterodimer was determined in vitro | ChEMBL. | 12801232 |
Efficacy (functional) | = 12 | Antagonistic efficacy against Retinoic acid receptor RXR-alpha was determined in vitro | ChEMBL. | 12801232 |
Efficacy (functional) | = 70 | Agonistic efficacy against Retinoic acid receptor RXR-alpha was determined in vitro | ChEMBL. | 12801232 |
Efficacy (functional) | = 166 | Synergistic efficacy against RXR:PPAR-gamma heterodimer was determined in vitro | ChEMBL. | 12801232 |
Efficacy (functional) | = 4 % | In vitro agonist efficacy at human Retinoic X receptor alpha expressed in CV1 cells. | ChEMBL. | 15006411 |
Efficacy (functional) | = 4 % | In vitro agonist efficacy at human Retinoic X receptor alpha expressed in CV1 cells. | ChEMBL. | 15006411 |
Efficacy (binding) | = 12 % | In vitro transcriptional activation in CV-1 cells expressing RXR-alpha | ChEMBL. | 12954061 |
Efficacy (binding) | = 12 % | In vitro transcriptional activation in CV-1 cells expressing RXR-alpha | ChEMBL. | 12954061 |
Efficacy (binding) | = 62 % | In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay. | ChEMBL. | 12954061 |
Efficacy (binding) | = 70 % | In vitro transcriptional activation in CV-1 cells expressing RXR-alpha | ChEMBL. | 12954061 |
Efficacy (binding) | = 70 % | In vitro transcriptional activation in CV-1 cells expressing RXR-alpha | ChEMBL. | 12954061 |
Efficacy (functional) | = 84 % | In vitro agonist efficacy at human Retinoic X receptor alpha expressed in CV1 cells. | ChEMBL. | 15006411 |
Efficacy (functional) | = 84 % | In vitro agonist efficacy at human Retinoic X receptor alpha expressed in CV1 cells. | ChEMBL. | 15006411 |
Efficacy (binding) | = 166 % | In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay. | ChEMBL. | 12954061 |
Efficacy (functional) | = 12 nM | In vitro anatagonist efficacy against RXR alpha in CV-1 cells | ChEMBL. | 14592510 |
Efficacy (functional) | = 12 nM | In vitro anatagonist efficacy against RXR alpha in CV-1 cells | ChEMBL. | 14592510 |
Efficacy (functional) | = 75 nM | In vitro agonist efficacy against RXR alpha in CV-1 cells | ChEMBL. | 14592510 |
Efficacy (functional) | = 75 nM | In vitro agonist efficacy against RXR alpha in CV-1 cells | ChEMBL. | 14592510 |
IC50 (binding) | = 0 nM | In vitro transcriptional activation in CV-1 cells expressing RXR-alpha | ChEMBL. | 12954061 |
IC50 (binding) | = 0 nM | In vitro transcriptional activation in CV-1 cells expressing RXR-alpha | ChEMBL. | 12954061 |
IC50 (functional) | = 8 nM | Antagonist activity for Retinoic X receptor alpha in CV1 cells | ChEMBL. | 15006411 |
IC50 (functional) | = 8 nM | Antagonist activity for Retinoic X receptor alpha in CV1 cells | ChEMBL. | 15006411 |
Kd (binding) | = 3 nM | Ability to bind directly to Retinoic acid receptor RXR-alpha was evaluated in a competitive binding assay. | ChEMBL. | 7636877 |
Kd (binding) | = 3 nM | Binding affinity to Retinoic acid receptor RXR-beta was determined in a competitive binding assay. | ChEMBL. | 7636877 |
Kd (binding) | = 3 nM | Binding affinity to Retinoic acid receptor RXR-gamma was evaluated in a competitive binding assay. | ChEMBL. | 7636877 |
Kd (binding) | = 3 nM | Ability to bind directly to Retinoic acid receptor RXR-alpha was evaluated in a competitive binding assay. | ChEMBL. | 7636877 |
Kd (binding) | = 3 nM | Binding affinity to Retinoic acid receptor RXR-beta was determined in a competitive binding assay. | ChEMBL. | 7636877 |
Kd (binding) | = 3 nM | Binding affinity to Retinoic acid receptor RXR-gamma was evaluated in a competitive binding assay. | ChEMBL. | 7636877 |
Ki (binding) | = 3 nM | Binding affinity against Retinoic acid receptor RXR-alpha by [3H]-9-cis-RA displacement. | ChEMBL. | 15006411 |
Ki (binding) | = 3 nM | Binding affinity against Retinoic acid receptor RXR-alpha by [3H]-9-cis-RA displacement. | ChEMBL. | 15006411 |
Ki (binding) | = 7.5 nM | Displacement of [3H]-9-cis-RA from Retinoic X receptor beta | ChEMBL. | 15006411 |
Ki (binding) | = 7.5 nM | Displacement of [3H]-9-cis-RA from Retinoic X receptor beta | ChEMBL. | 15006411 |
Ki (binding) | = 12 nM | Binding affinity against RXR gamma receptor using [3H]-9-cis-RA as radioligand in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | = 12 nM | Displacement of [3H]-9-cis-RA from retinoic X receptor gamma | ChEMBL. | 15006411 |
Ki (binding) | = 12 nM | Binding affinity against RXR gamma receptor using [3H]-9-cis-RA as radioligand in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | = 12 nM | Displacement of [3H]-9-cis-RA from retinoic X receptor gamma | ChEMBL. | 15006411 |
Ki (binding) | = 12.9 nM | Binding affinity against RXR alpha receptor using [3H]-9-cis-RA as radioligand in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | = 12.9 nM | Binding affinity against RXR alpha receptor using [3H]-9-cis-RA as radioligand in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | = 18 nM | Binding affinity for Retinoic acid receptor RXR-alpha was determined by competing with 3[H]-9-cis-RA | ChEMBL. | 12954061 |
Ki (binding) | = 18 nM | Binding affinity for Retinoic acid receptor RXR-gamma was determined by competing with 3[H]-9-cis-RA | ChEMBL. | 12954061 |
Ki (binding) | = 18 nM | Binding affinity against Retinoic acid receptor RXR-alpha was determined in vitro by using [3H]-9-cis-RA as radioligand | ChEMBL. | 12801232 |
Ki (binding) | = 18 nM | Binding affinity for Retinoic acid receptor RXR-alpha was determined by competing with 3[H]-9-cis-RA | ChEMBL. | 12954061 |
Ki (binding) | = 18 nM | Binding affinity for Retinoic acid receptor RXR-gamma was determined by competing with 3[H]-9-cis-RA | ChEMBL. | 12954061 |
Ki (binding) | = 18 nM | Binding affinity against Retinoic acid receptor RXR-alpha was determined in vitro by using [3H]-9-cis-RA as radioligand | ChEMBL. | 12801232 |
Ki (binding) | = 20 nM | Binding affinity for Retinoic acid receptor RXR-beta was determined by competing with 3[H]-9-cis-RA | ChEMBL. | 12954061 |
Ki (binding) | = 20 nM | Binding affinity for Retinoic acid receptor RXR-beta was determined by competing with 3[H]-9-cis-RA | ChEMBL. | 12954061 |
Ki (binding) | = 75 nM | Displacement of [3H]-9-cis-RA from RXR beta receptor in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | = 75 nM | Displacement of [3H]-9-cis-RA from RXR beta receptor in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | > 1000 nM | Binding affinity for Retinoic acid receptor alpha was determined by competing with 3[H]-ATRA | ChEMBL. | 12954061 |
Ki (binding) | > 1000 nM | Binding affinity for Retinoic acid receptor beta was determined by competing with 3[H]-ATRA | ChEMBL. | 12954061 |
Ki (binding) | > 1000 nM | Binding affinity for Retinoic acid receptor gamma was determined by competing with 3[H]-ATRA | ChEMBL. | 12954061 |
Ki (binding) | > 1000 nM | Binding affinity for peroxisome Peroxisome proliferator activated receptor alpha was determined | ChEMBL. | 12954061 |
Ki (binding) | > 1000 nM | Binding affinity for Peroxisome proliferator activated receptor gamma was determined | ChEMBL. | 12954061 |
Ki (binding) | > 1000 nM | Binding affinity for Retinoic acid receptor alpha was determined by competing with 3[H]-ATRA | ChEMBL. | 12954061 |
Ki (binding) | > 1000 nM | Binding affinity for Retinoic acid receptor beta was determined by competing with 3[H]-ATRA | ChEMBL. | 12954061 |
Ki (binding) | > 1000 nM | Binding affinity for Retinoic acid receptor gamma was determined by competing with 3[H]-ATRA | ChEMBL. | 12954061 |
Ki (binding) | > 1000 nM | Binding affinity for peroxisome Peroxisome proliferator activated receptor alpha was determined | ChEMBL. | 12954061 |
Ki (binding) | > 1000 nM | Binding affinity for Peroxisome proliferator activated receptor gamma was determined | ChEMBL. | 12954061 |
Ki (binding) | = 1550 nM | Binding affinity against RAR alpha receptor using [3H]-ATRA as radioligand in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | = 1550 nM | Binding affinity against RAR alpha receptor using [3H]-ATRA as radioligand in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | = 2745 nM | Binding affinity against retinoic acid receptor alpha by [3H]-ATRA displacement. | ChEMBL. | 15006411 |
Ki (binding) | = 2745 nM | Binding affinity against retinoic acid receptor alpha by [3H]-ATRA displacement. | ChEMBL. | 15006411 |
Ki (binding) | = 3515 nM | Binding affinity again retinoic acid receptor beta by [3H]-ATRA displacement. | ChEMBL. | 15006411 |
Ki (binding) | = 3515 nM | Binding affinity again retinoic acid receptor beta by [3H]-ATRA displacement. | ChEMBL. | 15006411 |
Ki (binding) | = 9901 nM | Binding affinity against RAR beta receptor using [3H]-ATRA as radioligand in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | = 9901 nM | Binding affinity against RAR gamma receptor using [3H]-ATRA as radioligand in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | = 9901 nM | Binding affinity against RAR beta receptor using [3H]-ATRA as radioligand in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | = 9901 nM | Binding affinity against RAR gamma receptor using [3H]-ATRA as radioligand in CV-1 cells | ChEMBL. | 14592510 |
Ki (binding) | > 10000 nM | Binding affinity against retinoic acid receptor gamma by [3H]-ATRA displacement. | ChEMBL. | 15006411 |
Ki (binding) | = 10000 nM | Binding affinity against Retinoic acid receptor gamma was determined in vitro by using [3H]-ATRA as radioligand | ChEMBL. | 12801232 |
Ki (binding) | > 10000 nM | Binding affinity against retinoic acid receptor gamma by [3H]-ATRA displacement. | ChEMBL. | 15006411 |
Ki (binding) | = 10000 nM | Binding affinity against Retinoic acid receptor gamma was determined in vitro by using [3H]-ATRA as radioligand | ChEMBL. | 12801232 |
NC (functional) | Inhibition of Retinoic acid receptor RXR-alpha antagonist activity in vitro; Not calculated | ChEMBL. | 12801232 | |
NC (functional) | 0 | Inhibition of Retinoic acid receptor RXR-alpha antagonist activity in vitro; Not calculated | ChEMBL. | 12801232 |
Normalization (functional) | = 101 % | In vivo hypoglycemic activity compared to BRL46953 as reduced plasma glucose in db/db mouse type II diabetes model | ChEMBL. | 12801232 |
Normalization (functional) | = 101 % | In vivo hypoglycemic activity compared to BRL46953 as reduced plasma glucose in db/db mouse type II diabetes model | ChEMBL. | 12801232 |
Potency (functional) | 61.3494 uM | PubChem BioAssay. qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen. (Class of assay: confirmatory) | ChEMBL. | No reference |
Ratio (binding) | = 3.15 | Activation of human RXRalpha activity expressed in COS1 cells assessed as induction ratio after 12 hrs by RXRE-luciferase reporter gene assay relative to untreated control | ChEMBL. | 23472886 |
Synergy (binding) | = 7 fold | In vitro snergistic elevation of transcriptional activation in CV-1 cells expressing RAR and RXR with 3 nm TTNBP | ChEMBL. | 12954061 |
Synergy (binding) | = 7 fold | RXR:RAR synergy expressed as fold induction | ChEMBL. | 12801232 |
Synergy (binding) | = 7 fold | In vitro snergistic elevation of transcriptional activation in CV-1 cells expressing RAR and RXR with 3 nm TTNBP | ChEMBL. | 12954061 |
Synergy (functional) | = 6.9 nM | Agonist synergy against RAR alpha was tested along with 3 nM TTNPB | ChEMBL. | 14592510 |
Synergy (functional) | = 6.9 nM | Agonist synergy against RAR alpha was tested along with 3 nM TTNPB | ChEMBL. | 14592510 |
Synergy EC50 (binding) | = 38 nM | In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay was determined | ChEMBL. | 12954061 |
T4 (functional) | = 37 ng ml-1 | T4 level in rats at 24 hr r after 30 mg/kg oral dose | ChEMBL. | 12954061 |
Triglycerides (functional) | = 152 mg dl-1 | Triglyceride level in rats 24 hr r after 30 mg/kg oral dose | ChEMBL. | 12954061 |
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.
6 literature references were collected for this gene.