bexarotene [Ligand Id: 2807] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1023 (Bexarotene, LG-100069, LG100069, LGD-1069, LGD1069, NSC-747528, Targretin, Targretine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CYP26A1/Cytochrome P450 26A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5141] [GtoPdb: 1366] [UniProtKB: O43174] | ||||||||
| ChEMBL | Inhibition of microsomal fraction of human CYP26A1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 1 min by HPLC analysis in presence of rat P450 reductase | B | 4.87 | pIC50 | 13500 | nM | IC50 | J Med Chem (2016) 59: 2579-2595 [PMID:26918322] |
| CYP26B1/Cytochrome P450 26B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3713687] [GtoPdb: 1367] [UniProtKB: Q9NR63] | ||||||||
| ChEMBL | Inhibition of microsomal fraction of human CYP26B1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 5 mins by HPLC analysis in presence of rat P450 reductase | B | 5.23 | pIC50 | 5900 | nM | IC50 | J Med Chem (2016) 59: 2579-2595 [PMID:26918322] |
| Liver X receptor-α/LXR-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133] | ||||||||
| ChEMBL | Partial agonist activity at recombinant human GAL4-DBD-fused LXRalpha-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay | B | 6.71 | pEC50 | 196 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 1193-1198 [PMID:28169169] |
| Liver X receptor-β/LXR-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4093] [GtoPdb: 601] [UniProtKB: P55055] | ||||||||
| ChEMBL | Partial agonist activity at recombinant human GAL4-DBD-fused LXRbeta-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay | B | 6.36 | pEC50 | 434 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 1193-1198 [PMID:28169169] |
| Retinoid X receptor-α/Nuclear receptor related 1/Nuclear receptor subfamily 4 group A member 2/Retinoic acid receptor RXR-alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885613] [GtoPdb: 610, 630] [UniProtKB: P19793, P43354] | ||||||||
| GtoPdb | - | - | 7.4 | pIC50 | - | - | - |
Curr Pharm Des (2000) 6: 25-58 [PMID:10637371]; J Med Chem (1999) 42: 742-50 [PMID:10052980]; J Med Chem (1994) 37: 2930-41 [PMID:8071941] |
| ChEMBL | Agonist activity at Renilla luciferase/GFP2-tagged RXRalpha/Nurr1 (unknown origin) expressed in HEK293T cells by BRET2 assay | B | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (2016) 59: 1232-1238 [PMID:26820900] |
| Retinoic acid receptor-α/Retinoic acid receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2055] [GtoPdb: 590] [UniProtKB: P10276] | ||||||||
| ChEMBL | Inhibition of [3H]-ATRA binding to baculovirus expressed retinoid receptor RAR alpha | B | 6 | pKd | >1000 | nM | Kd | J Med Chem (1994) 37: 2930-2941 [PMID:8071941] |
| ChEMBL | Inhibition of [3H]ATRA binding to baculovirus expressed Retinoic acid receptor RAR alpha | B | 5.26 | pKi | 5453 | nM | Ki | J Med Chem (1999) 42: 742-750 [PMID:10052980] |
| ChEMBL | Inhibition of [3H]ATRA binding to RAR alpha receptor | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2747-2752 |
| ChEMBL | Inhibition of [3H]ATRA binding to retinoic acid receptor RAR alpha | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2393-2398 |
| ChEMBL | Selective activity towards retinoic acid receptor-alpha | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (1997) 40: 4222-4234 [PMID:9435893] |
| ChEMBL | Effective concentration against retinoid receptor isoform (RAR alpha) expressed in CV-1 cells | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (1994) 37: 2930-2941 [PMID:8071941] |
| ChEMBL | Agonist activity at RARaplha (unknown origin) | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2018) 61: 2166-2210 [PMID:28850227] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR alpha | F | 8.22 | pEC50 | 6 | nM | EC50 | J Med Chem (1999) 42: 742-750 [PMID:10052980] |
| Retinoic acid receptor-β/Retinoic acid receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826] | ||||||||
| ChEMBL | Inhibition of [3H]ATRA binding to baculovirus expressed retinoid receptor RAR beta | B | 6 | pKd | >1000 | nM | Kd | J Med Chem (1994) 37: 2930-2941 [PMID:8071941] |
| ChEMBL | Inhibition of [3H]ATRA binding to baculovirus expressed Retinoic acid receptor RAR beta | B | 5.27 | pKi | 5353 | nM | Ki | J Med Chem (1999) 42: 742-750 [PMID:10052980] |
| ChEMBL | Inhibition of [3H]ATRA binding to RAR beta receptor | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2747-2752 |
| ChEMBL | Inhibition of [3H]ATRA binding to retinoic acid receptor RAR beta | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2393-2398 |
| ChEMBL | Binding affinity towards cRAR-beta-2 receptor by displacing 1.1 nM 3[H]-9-cis-RA | B | 6.1 | pKi | >800 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2313-2318 |
| ChEMBL | Binding affinity towards cRAR-beta-2 receptor by displacing 0.82 nM 3[H]all-trans-RA | B | 6.26 | pKi | >550 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2313-2318 |
| ChEMBL | Selective activity towards retinoic acid receptor-beta | B | 7.3 | pKi | 50 | nM | Ki | J Med Chem (1997) 40: 4222-4234 [PMID:9435893] |
| ChEMBL | Effective concentration against retinoid receptor isoform (RAR beta) expressed in CV-1 cells | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (1994) 37: 2930-2941 [PMID:8071941] |
| ChEMBL | Agonist activity at RARbeta (unknown origin) | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2018) 61: 2166-2210 [PMID:28850227] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR beta | F | 6.55 | pEC50 | 282 | nM | EC50 | J Med Chem (1999) 42: 742-750 [PMID:10052980] |
| Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631] | ||||||||
| ChEMBL | Tested for binding affinity against [3H]-ATRA binding to retinoid receptor isoform (RAR gamma) expressed in baculovirus | B | 6 | pKd | >1000 | nM | Kd | J Med Chem (1994) 37: 2930-2941 [PMID:8071941] |
| ChEMBL | Inhibition of [3H]-ATRA binding to baculovirus expressed Retinoic acid receptor RAR gamma | B | 5.49 | pKi | 3206 | nM | Ki | J Med Chem (1999) 42: 742-750 [PMID:10052980] |
| ChEMBL | Inhibition of [3H]ATRA binding to RAR gamma receptor | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2747-2752 |
| ChEMBL | Inhibition of [3H]-ATRA binding to Retinoic acid receptor RAR gamma | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2393-2398 |
| ChEMBL | Selective activity towards retinoic acid receptor-gamma | B | 6.89 | pKi | 130 | nM | Ki | J Med Chem (1997) 40: 4222-4234 [PMID:9435893] |
| ChEMBL | Effective concentration against retinoid receptor isoform (RAR gamma) expressed in CV-1 cells | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (1994) 37: 2930-2941 [PMID:8071941] |
| ChEMBL | Agonist activity at RARgamma (unknown origin) | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2018) 61: 2166-2210 [PMID:28850227] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR gamma | F | 6.19 | pEC50 | 648 | nM | EC50 | J Med Chem (1999) 42: 742-750 [PMID:10052980] |
| Retinoid X receptor-α/Retinoid X receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793] | ||||||||
| ChEMBL | Agonist activity at human RXR-alpha-ligand binding domain homodimers assessed as coactivator recruitment by measuring GRIP1 binding to receptor by isothermal titration calorimetry | B | 5.72 | pKd | 1890 | nM | Kd | J Med Chem (2014) 57: 5370-5380 [PMID:24801499] |
| ChEMBL | Binding affinity to human RXRalpha LBD after 15 mins by isothermal titration calorimetry assay | B | 5.8 | pKd | 1590 | nM | Kd | J Med Chem (2015) 58: 7763-7774 [PMID:26331194] |
| ChEMBL | Binding affinity to recombinant RXRalpha (unknown origin) by isothermal titration calorimetry | B | 6.68 | pKd | 210 | nM | Kd | J Med Chem (2019) 62: 2112-2126 [PMID:30702885] |
| ChEMBL | Dissociation constant for binding to Retinoic acid receptor RXR-alpha | B | 7.44 | pKd | 36 | nM | Kd | Bioorg Med Chem Lett (2002) 12: 2607-2609 [PMID:12182871] |
| ChEMBL | Ability to bind directly to Retinoic acid receptor RXR-alpha was evaluated in a competitive binding assay. | B | 7.44 | pKd | 36 | nM | Kd | J Med Chem (1995) 38: 3146-3155 [PMID:7636877] |
| ChEMBL | Binding affinity to human RXRalpha ligand binding domain by fluorescence assay | B | 7.59 | pKd | 26 | nM | Kd | Bioorg Med Chem (2014) 22: 178-185 [PMID:24359708] |
| ChEMBL | Binding affinity to human RXR-alpha-ligand binding domain homodimers by fluorescence quenching method | B | 7.59 | pKd | 26 | nM | Kd | J Med Chem (2014) 57: 5370-5380 [PMID:24801499] |
| ChEMBL | Inhibition of [3H]9-cis-RA binding to baculovirus expressed retinoid receptor RXR alpha | B | 7.85 | pKd | 14 | nM | Kd | J Med Chem (1994) 37: 2930-2941 [PMID:8071941] |
| ChEMBL | Displacement of CU-6PMN from human RXRalpha LBD incubated for 2 hrs by fluorescence based assay | B | 6.42 | pKi | 379 | nM | Ki | J Med Chem (2019) 62: 8809-8818 [PMID:31483660] |
| ChEMBL | Binding affinity to human RXRalpha-LBD (224 to 462 residues) expressed in Escherichia coli BL21(DE3) incubated for 1 hr in presence of compound by fluorescence polarization assay | B | 6.46 | pKi | 350 | nM | Ki | ACS Med Chem Lett (2021) 12: 1024-1029 [PMID:34141088] |
| ChEMBL | Binding affinity to human RXRalpha-LBD (224 to 462 residues) expressed in Escherichia coli BL21(DE3) incubated for 1 hr in presence of compound by [3H]9-Cis retinoic acid assay | B | 6.7 | pKi | 201 | nM | Ki | ACS Med Chem Lett (2021) 12: 1024-1029 [PMID:34141088] |
| ChEMBL | Displacement of 9-cis-[11,12-3H]-retinoic acid from human RXRalpha LBD incubated for overnight by scintillation counting method | B | 6.82 | pKi | 150 | nM | Ki | J Med Chem (2019) 62: 8809-8818 [PMID:31483660] |
| ChEMBL | Binding affinity towards recombinantly expressed Retinoic acid receptor RXR-alpha in baculoviral system, by using 5 nM [3H]targretin in a competitive binding assay | B | 7.44 | pKi | 36 | nM | Ki | J Med Chem (1999) 42: 742-750 [PMID:10052980] |
| ChEMBL | Inhibition of [3H]9-cis-RA binding to Retinoid X receptor RXR alpha | B | 7.44 | pKi | 36 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2393-2398 |
| ChEMBL | Displacement of [3H]9-cis-retinoic acid form human RXRalpha expressed in human Caco-2 cells after 16 hrs | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2009) 52: 5950-5966 [PMID:19791803] |
| ChEMBL | Selective activity towards retinoid X receptor-alpha | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (1997) 40: 4222-4234 [PMID:9435893] |
| ChEMBL | Inhibition of [3H]9-cis-RA binding to RXR alpha receptor | B | 7.85 | pKi | 14 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2747-2752 |
| ChEMBL | Binding affinity to human RXRalpha-LBD (224 to 462 residues) expressed in Escherichia coli BL21(DE3) incubated for 1 hr in presence of compound by fluorescence polarization assay | B | 6.2 | pIC50 | 632 | nM | IC50 | ACS Med Chem Lett (2021) 12: 1024-1029 [PMID:34141088] |
| GtoPdb | - | - | 7.4 | pIC50 | - | - | - |
Curr Pharm Des (2000) 6: 25-58 [PMID:10637371]; J Med Chem (1999) 42: 742-50 [PMID:10052980]; J Med Chem (1994) 37: 2930-41 [PMID:8071941] |
| ChEMBL | Transactivation of human RXRalpha transfected in human 293 cells after 48 hrs by dual-luciferase reporter gene assay | B | 6.83 | pEC50 | 149 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 3891-3895 [PMID:23707260] |
| ChEMBL | Agonist activity at RXRalpha LBD (unknown origin) expressed in CV1 cells | B | 6.93 | pEC50 | 118 | nM | EC50 | J Med Chem (2015) 58: 7763-7774 [PMID:26331194] |
| ChEMBL | Agonist activity at human recombinant Gal4-tagged RXRalpha expressed in human Caco-2 cells assessed as receptor homodimerization after 24 hrs by mammalian two hybrid assay | F | 7.28 | pEC50 | 52 | nM | EC50 | J Med Chem (2009) 52: 5950-5966 [PMID:19791803] |
| ChEMBL | Effective concentration against Retinoic acid receptor RXR-alpha | B | 7.38 | pEC50 | 42 | nM | EC50 | J Med Chem (1995) 38: 3368-3383 [PMID:7650690] |
| ChEMBL | Agonist activity at Gal4-fused human RXR-alpha expressed in HEK293 cells assessed as receptor-mediated transcriptional activity treated 24 hrs after transfection measured 48 hrs post-transfection by dual luciferase reporter assay | B | 7.4 | pEC50 | 40 | nM | EC50 | J Med Chem (2014) 57: 5370-5380 [PMID:24801499] |
| ChEMBL | Agonist activity at human RXRalpha expressed in African green monkey CV1 cells | B | 7.48 | pEC50 | 33 | nM | EC50 | Medchemcomm (2018) 9: 1289-1292 [PMID:30151082] |
| ChEMBL | Agonist activity RXRalpha (unknown origin) | B | 7.48 | pEC50 | 33 | nM | EC50 | J Med Chem (2019) 62: 2112-2126 [PMID:30702885] |
| ChEMBL | Agonist activity at RXRaplha (unknown origin) | B | 7.48 | pEC50 | 33 | nM | EC50 | J Med Chem (2018) 61: 2166-2210 [PMID:28850227] |
| ChEMBL | Effective concentration against retinoid receptor isoform (RXR alpha) expressed in CV-1 cells | B | 7.48 | pEC50 | 33 | nM | EC50 | J Med Chem (1994) 37: 2930-2941 [PMID:8071941] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR alpha | F | 7.48 | pEC50 | 33 | nM | EC50 | Bioorg Med Chem Lett (1997) 7: 2747-2752 |
| ChEMBL | Agonist activity at histidine-tagged ligand binding domain of human RXRalpha expressed in Escherichia coli BL21 (DE3) by luciferase reporter gene assay | B | 7.5 | pEC50 | 31.62 | nM | EC50 | J Med Chem (2016) 59: 1232-1238 [PMID:26820900] |
| ChEMBL | Agonist activity at Renilla luciferase/GFP2-tagged RXRalpha homodimer (unknown origin) expressed in HEK293T cells by BRET2 assay | B | 7.5 | pEC50 | 31.62 | nM | EC50 | J Med Chem (2016) 59: 1232-1238 [PMID:26820900] |
| ChEMBL | Transcriptional activity was evaluated in CV-1 cells transfected with expression vector for Retinoic acid receptor RXR-alpha | F | 7.55 | pEC50 | 28 | nM | EC50 | J Med Chem (1999) 42: 742-750 [PMID:10052980] |
| ChEMBL | Ability to activate gene expression at Retinoic acid receptor RXR-alpha was evaluated in a cotransfection assay. | B | 7.55 | pEC50 | 28 | nM | EC50 | J Med Chem (1995) 38: 3146-3155 [PMID:7636877] |
| ChEMBL | Effective potency in transcriptional activation assay in CV-1 cells expressing Retinoid X receptor RXR alpha | F | 7.55 | pEC50 | 28 | nM | EC50 | Bioorg Med Chem Lett (1997) 7: 2393-2398 |
| ChEMBL | Agonist activity at human RXRalpha LBD expressed in African green monkey COS1 cells incubated for 24 hrs by luciferase reporter gene assay | B | 7.66 | pEC50 | 22 | nM | EC50 | J Med Chem (2019) 62: 8809-8818 [PMID:31483660] |
| ChEMBL | Agonist activity at human RXRalpha expressed in African green monkey COS1 cells harboring CRBP2-tk-luc reporter incubated for 18 hrs by steady-glo luciferase reporter gene assay | B | 7.7 | pEC50 | 20 | nM | EC50 | Bioorg Med Chem Lett (2019) 29: 1891-1894 [PMID:31160175] |
| ChEMBL | Agonist activity at RXRalpha transfected in human COS1 cells after 18 hrs by luciferase reporter gene transactivation assay | F | 7.7 | pEC50 | 20 | nM | EC50 | ACS Med Chem Lett (2010) 1: 521-525 [PMID:24900241] |
| ChEMBL | Agonist activity at RXRalpha (unknown origin) expressed in COS1 cells incubated for 18 hrs by luciferase reporter gene assay | B | 7.7 | pEC50 | 20 | nM | EC50 | ACS Med Chem Lett (2015) 6: 334-338 [PMID:25815156] |
| ChEMBL | Agonist activity at RXRalpha by luciferase reporter gene assay | F | 7.7 | pEC50 | 19.8 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 5139-5142 [PMID:20656484] |
| ChEMBL | Agonist activity at human RXRalpha LBD by cell based luciferase reporter gene assay | F | 8.57 | pEC50 | 2.7 | nM | EC50 | J Med Chem (2011) 54: 788-808 [PMID:21218783] |
| Retinoid X receptor-α/Retinoid X receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3084] [GtoPdb: 610] [UniProtKB: P28700] | ||||||||
| ChEMBL | 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 | B | 7.4 | pEC50 | 40 | nM | EC50 | Eur J Med Chem (2009) 44: 2434-2446 [PMID:19216008] |
| Retinoid X receptor-α/Retinoid X receptor alpha in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4431] [GtoPdb: 610] [UniProtKB: Q05343] | ||||||||
| ChEMBL | Agonist activity at RXRalpha in rat RK3E cells assessed as transcriptional activation by luciferase reporter gene assay | B | 7.4 | pEC50 | 40 | nM | EC50 | Bioorg Med Chem (2014) 22: 178-185 [PMID:24359708] |
| Retinoid X receptor-β/Retinoid X receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1870] [GtoPdb: 611] [UniProtKB: P28702] | ||||||||
| ChEMBL | Inhibition of [3H]9-cis-RA binding to RXR beta receptor | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2747-2752 |
| ChEMBL | Binding affinity towards recombinantly expressed Retinoic acid receptor RXR-beta in baculoviral system, by using 5 nM [3H]targretin in a competitive binding assay | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (1999) 42: 742-750 [PMID:10052980] |
| ChEMBL | Selective activity towards retinoid X receptor-beta | B | 8.23 | pKi | 5.9 | nM | Ki | J Med Chem (1997) 40: 4222-4234 [PMID:9435893] |
| GtoPdb | - | - | 7.7 | pIC50 | - | - | - |
Curr Pharm Des (2000) 6: 25-58 [PMID:10637371]; J Med Chem (1999) 42: 742-50 [PMID:10052980]; J Med Chem (1994) 37: 2930-41 [PMID:8071941] |
| ChEMBL | Effective concentrations against Retinoic acid receptor RXR-beta | B | 6.95 | pEC50 | 112 | nM | EC50 | J Med Chem (1995) 38: 3368-3383 [PMID:7650690] |
| ChEMBL | Transcriptional activity was evaluated in CV-1 cells transfected with expression vector for Retinoic acid receptor RXR-beta | F | 7.6 | pEC50 | 25 | nM | EC50 | J Med Chem (1999) 42: 742-750 [PMID:10052980] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR beta | F | 7.62 | pEC50 | 24 | nM | EC50 | Bioorg Med Chem Lett (1997) 7: 2747-2752 |
| ChEMBL | Agonist activity at RXRbeta (unknown origin) | B | 7.62 | pEC50 | 24 | nM | EC50 | J Med Chem (2018) 61: 2166-2210 [PMID:28850227] |
| ChEMBL | Agonist activity at human RXRbeta expressed in African green monkey CV1 cells | B | 7.62 | pEC50 | 24 | nM | EC50 | Medchemcomm (2018) 9: 1289-1292 [PMID:30151082] |
| ChEMBL | Agonist activity RXRbeta (unknown origin) | B | 7.62 | pEC50 | 24 | nM | EC50 | J Med Chem (2019) 62: 2112-2126 [PMID:30702885] |
| Retinoid X receptor-β/Retinoid X receptor beta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4047] [GtoPdb: 611] [UniProtKB: P28704] | ||||||||
| ChEMBL | Binding affinity to Retinoic acid receptor RXR-beta was determined in a competitive binding assay. | B | 7.68 | pKd | 21 | nM | Kd | J Med Chem (1995) 38: 3146-3155 [PMID:7636877] |
| ChEMBL | Inhibition of [3H]9-cis-RA binding to baculovirus expressed retinoid receptor RXR beta | B | 7.68 | pKd | 21 | nM | Kd | J Med Chem (1994) 37: 2930-2941 [PMID:8071941] |
| ChEMBL | Inhibition of [3H]-9-cis-RA binding to Retinoid X receptor RXR beta | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2393-2398 |
| ChEMBL | Ability to activate gene expression at Retinoic acid receptor RXR-beta was evaluated in a cotransfection assay. | B | 7.6 | pEC50 | 25 | nM | EC50 | J Med Chem (1995) 38: 3146-3155 [PMID:7636877] |
| ChEMBL | Effective potency in transcriptional activation assay in CV-1 cells expressing Retinoid X receptor RXR beta | F | 7.6 | pEC50 | 25 | nM | EC50 | Bioorg Med Chem Lett (1997) 7: 2393-2398 |
| ChEMBL | Effective concentration against retinoid receptor isoform (RXR beta) expressed in CV-1 cells | B | 7.62 | pEC50 | 24 | nM | EC50 | J Med Chem (1994) 37: 2930-2941 [PMID:8071941] |
| Retinoid X receptor-γ/Retinoid X receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2004] [GtoPdb: 612] [UniProtKB: P48443] | ||||||||
| ChEMBL | Binding affinity towards Retinoic acid receptor RXR-gamma | B | 7.12 | pKi | 75 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2313-2318 |
| ChEMBL | Inhibition of [3H]9-cis-RA binding to RXR gamma receptor | B | 7.54 | pKi | 29 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2747-2752 |
| ChEMBL | Binding affinity towards recombinantly expressed Retinoic acid receptor RXR-gamma in baculoviral system, by using 5 nM [3H]targretin in a competitive binding assay | B | 7.54 | pKi | 29 | nM | Ki | J Med Chem (1999) 42: 742-750 [PMID:10052980] |
| ChEMBL | Selective activity towards retinoid X receptor-gamma | B | 8.08 | pKi | 8.3 | nM | Ki | J Med Chem (1997) 40: 4222-4234 [PMID:9435893] |
| GtoPdb | - | - | 7.54 | pIC50 | - | - | - |
Curr Pharm Des (2000) 6: 25-58 [PMID:10637371]; J Med Chem (1999) 42: 742-50 [PMID:10052980]; J Med Chem (1994) 37: 2930-41 [PMID:8071941] |
| ChEMBL | Effective concentrations against Retinoic acid receptor RXR-gamma | B | 6.91 | pEC50 | 122 | nM | EC50 | J Med Chem (1995) 38: 3368-3383 [PMID:7650690] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR gamma | F | 7.6 | pEC50 | 25 | nM | EC50 | Bioorg Med Chem Lett (1997) 7: 2747-2752 |
| ChEMBL | Agonist activity at RXRgamma (unknown origin) | B | 7.6 | pEC50 | 25 | nM | EC50 | J Med Chem (2018) 61: 2166-2210 [PMID:28850227] |
| ChEMBL | Agonist activity at human RXRgamma expressed in African green monkey CV1 cells | B | 7.6 | pEC50 | 25 | nM | EC50 | Medchemcomm (2018) 9: 1289-1292 [PMID:30151082] |
| ChEMBL | Agonist activity RXRgamma (unknown origin) | B | 7.6 | pEC50 | 25 | nM | EC50 | J Med Chem (2019) 62: 2112-2126 [PMID:30702885] |
| ChEMBL | Transcriptional activity was evaluated in CV-1 cells transfected with expression vector for Retinoic acid receptor RXR-gamma | F | 7.7 | pEC50 | 20 | nM | EC50 | J Med Chem (1999) 42: 742-750 [PMID:10052980] |
| Retinoid X receptor-γ/Retinoid X receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4402] [GtoPdb: 612] [UniProtKB: P28705] | ||||||||
| ChEMBL | Binding affinity to Retinoic acid receptor RXR-gamma was evaluated in a competitive binding assay. | B | 7.54 | pKd | 29 | nM | Kd | J Med Chem (1995) 38: 3146-3155 [PMID:7636877] |
| ChEMBL | Inhibition of [3H]9-cis-RA binding to baculovirus expressed retinoid receptor RXR gamma | B | 7.54 | pKd | 29 | nM | Kd | J Med Chem (1994) 37: 2930-2941 [PMID:8071941] |
| ChEMBL | Inhibition of [3H]9-cis-RA binding to Retinoid X receptor RXR gamma | B | 7.54 | pKi | 29 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2393-2398 |
| ChEMBL | Effective concentration against retinoid receptor isoform (RXR gamma) expressed in CV-1 cells | B | 7.6 | pEC50 | 25 | nM | EC50 | J Med Chem (1994) 37: 2930-2941 [PMID:8071941] |
| ChEMBL | Ability to activate gene expression at Retinoic acid receptor RXR-gamma was evaluated in a cotransfection assay. | B | 7.7 | pEC50 | 20 | nM | EC50 | J Med Chem (1995) 38: 3146-3155 [PMID:7636877] |
| ChEMBL | Effective potency in transcriptional activation assay in CV-1 cells expressing Retinoid X receptor RXR gamma | B | 7.7 | pEC50 | 20 | nM | EC50 | Bioorg Med Chem Lett (1997) 7: 2393-2398 |
| Peroxisome proliferator-activated receptor-γ in Human [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
| GtoPdb | Measured using a TR-FRET competitive displacement assay. | - | 5.52 | pIC50 | ~3000 | nM | IC50 | PPAR Res (2015) 2015: 254560 [PMID:26451138] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
