bexarotene [Ligand Id: 2807] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1023 (Bexarotene, Bexaroteno, 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] |
| ChEMBL | Inhibition of Nurr1-RXRalpha in HEK293T cells by BRET assay | B | 8.3 | pEC50 | 5.01 | nM | EC50 | J Med Chem (2021) 64: 9592-9638 [PMID:34251209] |
| 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 | 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 | Agonist activity at RXRalpha (unknown origin) | B | 7.48 | pEC50 | 33 | nM | EC50 | J Med Chem (2021) 64: 9592-9638 [PMID:34251209] |
| 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 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 at RXRaplha (unknown origin) | B | 7.48 | pEC50 | 33 | nM | EC50 | J Med Chem (2018) 61: 2166-2210 [PMID:28850227] |
| 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 | Inhibition of RXRalpha in HEK293T cells by BRET assay | B | 7.5 | pEC50 | 31.62 | nM | EC50 | J Med Chem (2021) 64: 9592-9638 [PMID:34251209] |
| 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 | 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 | 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 | 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 (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 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 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 | 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] |
| ChEMBL | Agonist activity at RXRbeta (unknown origin) | B | 7.62 | pEC50 | 24 | nM | EC50 | J Med Chem (2021) 64: 9592-9638 [PMID:34251209] |
| ChEMBL | Agonist activity at RXRbeta (unknown origin) | B | 7.62 | pEC50 | 24 | nM | EC50 | J Med Chem (2018) 61: 2166-2210 [PMID:28850227] |
| 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 |
| 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 RXRgamma (unknown origin) | B | 7.6 | pEC50 | 25 | nM | EC50 | J Med Chem (2021) 64: 9592-9638 [PMID:34251209] |
| 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 |
| Retinoid X receptor-α/Peroxisome proliferator-activated receptor-γ/RXR alpha/PPAR gamma in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111394] [GtoPdb: 610, 595] [UniProtKB: P19793, P37231] | ||||||||
| GtoPdb | Measured using a TR-FRET competitive displacement assay. | - | 5.52 | pIC50 | ~3000 | nM | IC50 | PPAR Res (2015) 2015: 254560 [PMID:26451138] |
| ChEMBL | Displacement of CU-6PMN from human PPARgamma-LBD (206 to 477 residues)/human RXRalpha-LBD (224 to 462 residues) heterodimer incubated for 30 mins by fluorospectrometer | B | 6.41 | pIC50 | 389 | nM | IC50 | ACS Med Chem Lett (2023) 14: 291-296 [PMID:36923911] |
| 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 data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
