alitretinoin [Ligand Id: 2645] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL705 (BAL-4079, LGD-1057, Toctino, Retinoic acid 9-cis-form, Alitretinoin, ALRT-1057, NSC-659772, Panretin, AGN-192013, LG-100057, LGD1057, LG100057, ALRT1057)
  • Cellular retinoic acid-binding protein I in Chicken [ChEMBL: CHEMBL4945] [UniProtKB: P40220]
  • cellular retinoic acid binding protein 1/Cellular retinoic acid-binding protein I in Mouse [ChEMBL: CHEMBL3208] [GtoPdb: 2529] [UniProtKB: P62965]
There should be some charts here, you may need to enable JavaScript!
  • cellular retinoic acid binding protein 2/Cellular retinoic acid-binding protein II in Mouse [ChEMBL: CHEMBL4172] [GtoPdb: 2530] [UniProtKB: P22935]
There should be some charts here, you may need to enable JavaScript!
  • Liver X receptor-α/LXR-alpha in Human [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449]
There should be some charts here, you may need to enable JavaScript!
  • Nerve Growth factor IB/Nuclear receptor subfamily 4 group A member 1 in Human [ChEMBL: CHEMBL1293229] [GtoPdb: 629] [UniProtKB: P22736]
There should be some charts here, you may need to enable JavaScript!
  • Retinoic acid receptor-α/Retinoic acid receptor alpha in Human [ChEMBL: CHEMBL2055] [GtoPdb: 590] [UniProtKB: P10276]
  • Retinoic acid receptor-α/Retinoic acid receptor alpha in Mouse [ChEMBL: CHEMBL2792] [GtoPdb: 590] [UniProtKB: P11416]
There should be some charts here, you may need to enable JavaScript!
  • Retinoic acid receptor-β/Retinoic acid receptor beta in Human [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826]
  • Retinoic acid receptor-β/Retinoic acid receptor beta in Mouse [ChEMBL: CHEMBL3266] [GtoPdb: 591] [UniProtKB: P22605]
There should be some charts here, you may need to enable JavaScript!
  • Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631]
  • Retinoic acid receptor-γ/Retinoic acid receptor gamma in Mouse [ChEMBL: CHEMBL4177] [GtoPdb: 592] [UniProtKB: P18911]
There should be some charts here, you may need to enable JavaScript!
  • Retinoid X receptor-α/Retinoid X receptor alpha in Human [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793]
  • Retinoid X receptor-α/Retinoid X receptor alpha in Mouse [ChEMBL: CHEMBL3084] [GtoPdb: 610] [UniProtKB: P28700]
  • Retinoid X receptor-α/Retinoid X receptor alpha in Rat [ChEMBL: CHEMBL4431] [GtoPdb: 610] [UniProtKB: Q05343]
There should be some charts here, you may need to enable JavaScript!
  • Retinoid X receptor-β/Retinoid X receptor beta in Human [ChEMBL: CHEMBL1870] [GtoPdb: 611] [UniProtKB: P28702]
  • Retinoid X receptor-β/Retinoid X receptor beta in Mouse [ChEMBL: CHEMBL4047] [GtoPdb: 611] [UniProtKB: P28704]
There should be some charts here, you may need to enable JavaScript!
  • Retinoid X receptor-γ/Retinoid X receptor gamma in Human [ChEMBL: CHEMBL2004] [GtoPdb: 612] [UniProtKB: P48443]
  • Retinoid X receptor-γ/Retinoid X receptor gamma in Mouse [ChEMBL: CHEMBL4402] [GtoPdb: 612] [UniProtKB: P28705]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Cellular retinoic acid-binding protein I in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4945] [UniProtKB: P40220]
ChEMBL Inhibition of [3H]ATRA binding to chick skin Cytoplasmic retinoic acid binding protein B 5 pIC50 >10000 nM IC50 J. Med. Chem. (1996) 39: 3625-3635 [PMID:8809153]
cellular retinoic acid binding protein 1/Cellular retinoic acid-binding protein I in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3208] [GtoPdb: 2529] [UniProtKB: P62965]
ChEMBL Inhibition of [3H]ATRA binding to murine Cytoplasmic retinoic acid binding protein (CRABP) type 1 B 6.7 pKd >200 nM Kd J. Med. Chem. (1996) 39: 3625-3635 [PMID:8809153]
cellular retinoic acid binding protein 2/Cellular retinoic acid-binding protein II in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4172] [GtoPdb: 2530] [UniProtKB: P22935]
ChEMBL Inhibition of [3H]ATRA binding to murine Cytoplasmic retinoic acid binding protein (CRABP) type 2 B 6.7 pKd >200 nM Kd J. Med. Chem. (1996) 39: 3625-3635 [PMID:8809153]
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 5.96 pEC50 1090 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 5.76 pEC50 1730 nM EC50 Bioorg Med Chem Lett (2017) 27: 1193-1198 [PMID:28169169]
RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449]
ChEMBL Inverse agonist activity at human RoRc-LBD fusion protein with GST expressed in BL-21 (BL3) cells assessed as SRC1 coactivator peptide recruitment B 4.85 pEC50 14000 nM EC50 J. Med. Chem. (2014) 57: 5871-5892 [PMID:24502334]
Nerve Growth factor IB/Nuclear receptor subfamily 4 group A member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293229] [GtoPdb: 629] [UniProtKB: P22736]
ChEMBL Binding affinity to Nur77 Y453A mutant expressed in human BGC823 cells B 6.09 pKd 810 nM Kd Nat. Chem. Biol. (2008) 4: 548-556 [PMID:18690216]
Retinoic acid receptor-α/Retinoic acid receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2055] [GtoPdb: 590] [UniProtKB: P10276]
ChEMBL Inhibition of [3H]RA binding to retinoic acid receptor RAR alpha B 7.03 pKd 93 nM Kd Bioorg. Med. Chem. Lett. (1999) 9: 589-594 [PMID:10098670]
ChEMBL Inhibition of [3H]ATRA binding to human Retinoic acid receptor RAR alpha B 7.03 pKd 93 nM Kd Bioorg. Med. Chem. Lett. (2003) 13: 261-264 [PMID:12482435]
ChEMBL Inhibition of [3H]ATRA binding to baculovirus expressed retinoic acid receptor RAR-alpha B 7.05 pKd 90 nM Kd J. Med. Chem. (2001) 44: 2298-2303 [PMID:11428923]
ChEMBL Compound was tested for binding affinity against retinoic acid receptor using 5 nM of [3H]RA as a radioligand in baculovirus expressed receptor B 7.96 pKd 11 nM Kd Bioorg. Med. Chem. Lett. (1996) 6: 213-218
GtoPdb - - 9.5 pKd - - - J. Med. Chem. (1988) 31: 2182-92 [PMID:3184125];
Mol. Cell. Biol. (1995) 15: 3540-51 [PMID:7791761]
ChEMBL Inhibition of [3H]ATRA binding to Retinoic acid receptor RAR alpha B 7.65 pKi 22.3 nM Ki J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Binding affinity against retinoic Acid alpha receptor using [3H]- -9-cis-Retinoic Acid in competitive binding assay B 8.15 pIC50 7 nM IC50 J. Med. Chem. (1994) 37: 408-414 [PMID:8308867]
ChEMBL Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR alpha F 6.52 pEC50 304 nM EC50 J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Transcriptional activation in CV-1 cells expressing human Retinoic acid receptor RAR alpha B 6.66 pEC50 220 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 261-264 [PMID:12482435]
ChEMBL Agonist activity for retinoic acid receptor RAR alpha in transcriptional activation assay F 6.72 pEC50 191 nM EC50 Bioorg. Med. Chem. Lett. (1995) 5: 2729-2734
ChEMBL Binding affinity against retinoic Acid alpha receptors co-transfected into CV-1 cells B 6.72 pEC50 191 nM EC50 J. Med. Chem. (1994) 37: 408-414 [PMID:8308867]
ChEMBL Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoic acid receptor alpha using transactivation assay B 6.72 pEC50 191 nM EC50 Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Transcriptional activation of Retinoic acid receptor RAR alpha B 6.72 pEC50 191 nM EC50 J. Med. Chem. (1996) 39: 3556-3563 [PMID:8784454]
ChEMBL Transcriptional activation of Retinoic acid receptor RAR alpha B 6.99 pEC50 102 nM EC50 J. Med. Chem. (1995) 38: 2820-2829 [PMID:7636843]
ChEMBL Transcriptional activation for RAR alpha receptor B 6.99 pEC50 102 nM EC50 Bioorg. Med. Chem. Lett. (1994) 4: 1447-1452
ChEMBL Transcriptional activation of Retinoic acid receptor RAR alpha F 6.99 pEC50 102 nM EC50 J. Med. Chem. (1999) 42: 4961-4969 [PMID:10585206]
ChEMBL Effective concentration against RAR-alpha receptor B 7.35 pEC50 45 nM EC50 J. Med. Chem. (1993) 36: 2605-2613 [PMID:8410972]
ChEMBL Relative activity against Retinoic acid receptor RAR alpha compared to ATRA B 7.64 pEC50 23 nM EC50 J. Med. Chem. (1995) 38: 3368-3383 [PMID:7650690]
ChEMBL Transcriptional activation in CV-1 cells expressing retinoic acid receptor RAR alpha F 7.68 pEC50 21 nM EC50 J. Med. Chem. (2001) 44: 2298-2303 [PMID:11428923]
Retinoic acid receptor-α/Retinoic acid receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2792] [GtoPdb: 590] [UniProtKB: P11416]
ChEMBL Dissociation constant for binding to Retinoic acid receptor alpha B 8.15 pKd 7 nM Kd J. Med. Chem. (1996) 39: 3556-3563 [PMID:8784454]
ChEMBL Inhibition of [3H]ATRA binding to mouse Retinoic acid receptor RAR alpha B 7.51 pIC50 31 nM IC50 J. Med. Chem. (1996) 39: 3625-3635 [PMID:8809153]
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 retinoic acid receptor RAR-beta B 7 pKd 100 nM Kd J. Med. Chem. (2001) 44: 2298-2303 [PMID:11428923]
ChEMBL Inhibition of [3H]RA binding to retinoic acid receptor RAR beta B 7.01 pKd 97 nM Kd Bioorg. Med. Chem. Lett. (1999) 9: 589-594 [PMID:10098670]
ChEMBL Inhibition of [3H]-ATRA binding to human Retinoic acid receptor RAR beta B 7.01 pKd 97 nM Kd Bioorg. Med. Chem. Lett. (2003) 13: 261-264 [PMID:12482435]
ChEMBL Compound was tested for binding affinity against retinoic acid receptor using 5 nM of [3H]RA as a radioligand in baculovirus expressed receptor B 8.15 pKd 7 nM Kd Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Inhibition of [3H]ATRA binding to Retinoic acid receptor RAR beta B 7.96 pKi 10.9 nM Ki J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Binding affinity towards cRAR-beta-2 receptor by displacing 0.82 nM 3[H]all-trans-RA B 9.15 pKi 0.7 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 2313-2318
ChEMBL Binding affinity towards cRAR-beta-2 receptor by displacing 1.1 nM 3[H]-9-cis-RA B 9.3 pKi 0.5 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 2313-2318
GtoPdb - - 9.7 pKi - - - J. Mol. Biol. (2000) 302: 155-70 [PMID:10964567];
Mol. Cell. Biol. (1995) 15: 3540-51 [PMID:7791761]
ChEMBL Binding affinity against retinoic Acid beta receptor using [3H]- -9-cis-Retinoic Acid in competitive binding assay B 8.15 pIC50 7 nM IC50 J. Med. Chem. (1994) 37: 408-414 [PMID:8308867]
ChEMBL Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR beta F 7.28 pEC50 52 nM EC50 J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Agonist activity for retinoic acid receptor RAR beta in transcriptional activation assay F 7.3 pEC50 50 nM EC50 Bioorg. Med. Chem. Lett. (1995) 5: 2729-2734
ChEMBL Transcriptional activation of Retinoic acid receptor RAR beta B 7.3 pEC50 50 nM EC50 J. Med. Chem. (1996) 39: 3556-3563 [PMID:8784454]
ChEMBL Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoic acid receptor beta using transactivation assay B 7.3 pEC50 50 nM EC50 Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Binding affinity against retinoic Acid beta receptors co-transfected into CV-1 cells B 7.3 pEC50 50 nM EC50 J. Med. Chem. (1994) 37: 408-414 [PMID:8308867]
ChEMBL Transcriptional activation in CV-1 cells expressing human Retinoic acid receptor RAR beta B 7.54 pEC50 29 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 261-264 [PMID:12482435]
ChEMBL Effective concentration against Retinoic acid receptor beta B 7.66 pEC50 22 nM EC50 J. Med. Chem. (1993) 36: 2605-2613 [PMID:8410972]
ChEMBL Transcriptional activation of Retinoic acid receptor RAR beta F 8.48 pEC50 3.3 nM EC50 J. Med. Chem. (1999) 42: 4961-4969 [PMID:10585206]
ChEMBL Transcriptional activation for RAR beta receptor B 8.48 pEC50 3.3 nM EC50 Bioorg. Med. Chem. Lett. (1994) 4: 1447-1452
ChEMBL Transcriptional activation of Retinoic acid receptor RAR beta B 8.48 pEC50 3.3 nM EC50 J. Med. Chem. (1995) 38: 2820-2829 [PMID:7636843]
ChEMBL Transcriptional activation in CV-1 cells expressing retinoic acid receptor RAR beta F 8.52 pEC50 3 nM EC50 J. Med. Chem. (2001) 44: 2298-2303 [PMID:11428923]
Retinoic acid receptor-β/Retinoic acid receptor beta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3266] [GtoPdb: 591] [UniProtKB: P22605]
ChEMBL Dissociation constant for binding to Retinoic acid receptor beta B 8.15 pKd 7 nM Kd J. Med. Chem. (1996) 39: 3556-3563 [PMID:8784454]
Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631]
ChEMBL Inhibition of [3H]ATRA binding to baculovirus expressed retinoic acid receptor RAR-gamma B 6.82 pKd 150 nM Kd J. Med. Chem. (2001) 44: 2298-2303 [PMID:11428923]
ChEMBL Inhibition of [3H]RA binding to retinoic acid receptor RAR gamma B 6.83 pKd 148 nM Kd Bioorg. Med. Chem. Lett. (1999) 9: 589-594 [PMID:10098670]
ChEMBL Inhibition of [3H]ATRA binding to human Retinoic acid receptor RAR gamma B 6.83 pKd 148 nM Kd Bioorg. Med. Chem. Lett. (2003) 13: 261-264 [PMID:12482435]
ChEMBL Compound was tested for binding affinity against retinoic acid receptor using 5 nM of [3H]RA as a radioligand in baculovirus expressed receptor B 7.66 pKd 22 nM Kd Bioorg. Med. Chem. Lett. (1996) 6: 213-218
GtoPdb - - 9 pKd - - - J. Mol. Biol. (2000) 302: 155-70 [PMID:10964567];
Mol. Cell. Biol. (1995) 15: 3540-51 [PMID:7791761]
ChEMBL Dissociation constant for Retinoic acid receptor gamma B 9.1 pKd 0.8 nM Kd J. Med. Chem. (2005) 48: 6212-6219 [PMID:16190748]
ChEMBL Inhibition of [3H]ATRA binding to Retinoic acid receptor RAR gamma B 7.7 pKi 20 nM Ki J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Agonistic activity towards retinoic acid receptor-gamma F 9 pKi 1 nM Ki J. Med. Chem. (1997) 40: 4222-4234 [PMID:9435893]
ChEMBL Binding affinity against retinoic Acid gamma receptor using [3H]- -9-cis-Retinoic Acid in competitive binding assay B 7.77 pIC50 17 nM IC50 J. Med. Chem. (1994) 37: 408-414 [PMID:8308867]
ChEMBL Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR gamma F 7.13 pEC50 74 nM EC50 J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Transcriptional activation in CV-1 cells expressing human Retinoic acid receptor RAR gamma B 7.3 pEC50 50 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 261-264 [PMID:12482435]
ChEMBL Agonist activity for retinoic acid receptor RAR gamma in transcriptional activation assay F 7.35 pEC50 45 nM EC50 Bioorg. Med. Chem. Lett. (1995) 5: 2729-2734
ChEMBL Binding affinity against retinoic Acid gamma receptors co-transfected into CV-1 cells B 7.35 pEC50 45 nM EC50 J. Med. Chem. (1994) 37: 408-414 [PMID:8308867]
ChEMBL Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoic acid receptor gamma using transactivation assay B 7.35 pEC50 45 nM EC50 Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Transcriptional activation of Retinoic acid receptor RAR gamma B 7.35 pEC50 45 nM EC50 J. Med. Chem. (1996) 39: 3556-3563 [PMID:8784454]
ChEMBL Effective concentration against RAR-gamma receptor B 7.92 pEC50 12 nM EC50 J. Med. Chem. (1993) 36: 2605-2613 [PMID:8410972]
ChEMBL Transcriptional activation for RAR gamma receptor B 8.22 pEC50 6 nM EC50 Bioorg. Med. Chem. Lett. (1994) 4: 1447-1452
ChEMBL Transcriptional activation of Retinoic acid receptor RAR gamma F 8.22 pEC50 6 nM EC50 J. Med. Chem. (1999) 42: 4961-4969 [PMID:10585206]
ChEMBL Transcriptional activation of Retinoic acid receptor RAR gamma B 8.22 pEC50 6 nM EC50 J. Med. Chem. (1995) 38: 2820-2829 [PMID:7636843]
ChEMBL Transcriptional activation in CV-1 cells expressing retinoic acid receptor RAR gamma F 8.4 pEC50 4 nM EC50 J. Med. Chem. (2001) 44: 2298-2303 [PMID:11428923]
Retinoic acid receptor-γ/Retinoic acid receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4177] [GtoPdb: 592] [UniProtKB: P18911]
ChEMBL Dissociation constant for binding to Retinoic acid receptor gamma B 7.77 pKd 17 nM Kd J. Med. Chem. (1996) 39: 3556-3563 [PMID:8784454]
Retinoid X receptor-α/Retinoid X receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793]
ChEMBL Binding affinity to human RXRalpha LBD after 15 mins by isothermal titration calorimetry assay B 5.74 pKd 1810 nM Kd J. Med. Chem. (2015) 58: 7763-7774 [PMID:26331194]
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 5.81 pKd 1560 nM Kd J. Med. Chem. (2014) 57: 5370-5380 [PMID:24801499]
ChEMBL Binding affinity to RXRalpha B 6.62 pKd 240 nM Kd Nat. Chem. Biol. (2008) 4: 548-556 [PMID:18690216]
ChEMBL Dissociation constant for binding to Retinoic acid receptor RXR-alpha B 7.3 pKd 50 nM Kd Bioorg. Med. Chem. Lett. (2002) 12: 2607-2609 [PMID:12182871]
ChEMBL Binding affinity to human RXRalpha ligand binding domain by fluorescence assay B 7.85 pKd 14 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 7.85 pKd 14 nM Kd J. Med. Chem. (2014) 57: 5370-5380 [PMID:24801499]
ChEMBL Inhibition of [3H]9-cis-retinoic acid binding to baculovirus expressed retinoic acid receptor RXR-alpha B 7.89 pKd 13 nM Kd J. Med. Chem. (2001) 44: 2298-2303 [PMID:11428923]
ChEMBL Compound was tested for binding affinity against retinoid X receptor using 5 nM of [3H]-9-cis-RA as a radioligand in baculovirus expressed receptor B 8.05 pKd 9 nM Kd Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Inhibition of [3H]-9-cis RA binding to Retinoid X receptor RXR gamma B 8.1 pKd 8 nM Kd Bioorg. Med. Chem. Lett. (1999) 9: 589-594 [PMID:10098670]
ChEMBL Inhibition of [3H]9-cis-RA binding to human Retinoid X receptor RXR alpha B 8.1 pKd 8 nM Kd Bioorg. Med. Chem. Lett. (2003) 13: 261-264 [PMID:12482435]
ChEMBL Inhibition of binding to human Retinoic acid receptor RXR DEF domain B 8.52 pKd 3 nM Kd J. Med. Chem. (1996) 39: 3625-3635 [PMID:8809153]
ChEMBL Dissociation constant for Retinoid X receptor alpha B 8.82 pKd 1.5 nM Kd J. Med. Chem. (2005) 48: 6212-6219 [PMID:16190748]
ChEMBL Agonistic activity towards retinoid X receptor-alpha F 7.92 pKi 12 nM Ki J. Med. Chem. (1997) 40: 4222-4234 [PMID:9435893]
ChEMBL Inhibition of [3H]9-cis-RA binding to Retinoid X receptor RXR alpha B 8.08 pKi 8.4 nM Ki J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Inhibition of [3H]targretin binding to Retinoid X receptor RXR alpha B 8.1 pKi 8 nM Ki J. Med. Chem. (1996) 39: 3229-3234 [PMID:8765503]
ChEMBL Binding affinity against retinoic Acid X alpha receptor using [3H]- -9-cis-Retinoic Acid in competitive binding assay B 7.49 pIC50 32 nM IC50 J. Med. Chem. (1994) 37: 408-414 [PMID:8308867]
ChEMBL Inhibition of [3H]9-cis-retinoic acid binding to human retinoid X receptor alpha ligand-binding domain expressed in Escherichia coli B 7.54 pIC50 29 nM IC50 J. Med. Chem. (2004) 47: 4360-4372 [PMID:15317450]
GtoPdb - - 8.2 pIC50 - - - Proc. Natl. Acad. Sci. U.S.A. (1993) 90: 30-4 [PMID:8380496];
Mol. Cell. Biol. (1995) 15: 3540-51 [PMID:7791761];
Cell (1992) 68: 397-406 [PMID:1310260];
Nature (1996) 383: 450-3 [PMID:8837780];
Nature (1992) 355: 359-61 [PMID:1309942];
Genes Dev. (1992) 6: 329-44 [PMID:1312497]
ChEMBL Transcriptional activation in CV-1 cells expressing Retinoid X receptor RXR alpha F 6.5 pEC50 316 nM EC50 J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoid X receptor alpha using transactivation assay B 6.6 pEC50 250 nM EC50 Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Transcriptional activation in CV-1 cells expressing human Retinoid X receptor RXR-alpha B 6.71 pEC50 195 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 261-264 [PMID:12482435]
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 6.92 pEC50 120 nM EC50 J. Med. Chem. (2014) 57: 5370-5380 [PMID:24801499]
ChEMBL Binding affinity against retinoic Acid X alpha receptors co-transfected into CV-1 cells B 7 pEC50 100 nM EC50 J. Med. Chem. (1994) 37: 408-414 [PMID:8308867]
ChEMBL Agonist activity for retinoic acid receptor RXR alpha in transcriptional activation assay F 7 pEC50 100 nM EC50 Bioorg. Med. Chem. Lett. (1995) 5: 2729-2734
ChEMBL Transcriptional activation of Retinoid X receptor RXR alpha B 7 pEC50 100 nM EC50 J. Med. Chem. (1996) 39: 3556-3563 [PMID:8784454]
ChEMBL Effective concentration against RXR-alpha receptor B 7.89 pEC50 13 nM EC50 J. Med. Chem. (1993) 36: 2605-2613 [PMID:8410972]
ChEMBL Transcriptional activation of Retinoid X receptor RXR alpha B 7.89 pEC50 13 nM EC50 J. Med. Chem. (1995) 38: 2820-2829 [PMID:7636843]
ChEMBL Transcriptional activation for RXR alpha receptor B 7.89 pEC50 13 nM EC50 Bioorg. Med. Chem. Lett. (1994) 4: 1447-1452
ChEMBL Agonist activity at human RXRalpha expressed in HEK293 cells by luciferase reporter gene assay B 8 pEC50 10 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 5265-5267 [PMID:25305688]
ChEMBL Effective concentration against Retinoic acid receptor RXR-alpha B 8.22 pEC50 6 nM EC50 J. Med. Chem. (1995) 38: 3368-3383 [PMID:7650690]
ChEMBL Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR alpha F 8.82 pEC50 1.5 nM EC50 J. Med. Chem. (2001) 44: 2298-2303 [PMID:11428923]
Retinoid X receptor-α/Retinoid X receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3084] [GtoPdb: 610] [UniProtKB: P28700]
ChEMBL Dissociation constant for binding to Retinoid X receptor alpha B 7.49 pKd 32 nM Kd J. Med. Chem. (1996) 39: 3556-3563 [PMID:8784454]
ChEMBL Inhibition of [3H]-ATRA binding to mouse Retinoic acid receptor RXR alpha B 7.09 pIC50 82 nM IC50 J. Med. Chem. (1996) 39: 3625-3635 [PMID:8809153]
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 6.7 pEC50 200 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 6.92 pEC50 120 nM EC50 Bioorg. Med. Chem. (2014) 22: 178-185 [PMID:24359708]
ChEMBL Agonist activity at RXR-alpha in rat R3KE cells infected with oncogene KLF4-ER assessed as inhibition of KLF4-mediated oncogenic transformation B 6.96 pEC50 110 nM EC50 J. Med. Chem. (2014) 57: 5370-5380 [PMID:24801499]
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-retinoic acid binding to baculovirus expressed retinoic acid receptor RXR-beta B 7.46 pKd 35 nM Kd J. Med. Chem. (2001) 44: 2298-2303 [PMID:11428923]
ChEMBL Inhibition of [3H]-9-cis RA binding to Retinoid X receptor RXR beta B 7.82 pKd 15 nM Kd Bioorg. Med. Chem. Lett. (1999) 9: 589-594 [PMID:10098670]
ChEMBL Compound was tested for binding affinity against retinoid X receptor using 5 nM of [3H]9-cis-RA as a radioligand in baculovirus expressed receptor B 7.96 pKd 11 nM Kd Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Inhibition of [3H]-Targretin binding to Retinoid X receptor RXR beta B 8.05 pKi 9 nM Ki J. Med. Chem. (1996) 39: 3229-3234 [PMID:8765503]
ChEMBL Inhibition of [3H]9-cis-RA binding to Retinoid X receptor RXR beta B 8.13 pKi 7.4 nM Ki J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Agonistic activity towards retinoid X receptor-beta F