ChEMBL ligand: CHEMBL705 (9-cis retinoic acid, 9-cis-retinoic acid, AGN 192013, AGN-192013, AGN192013, Alitretinoin, Alitretinoina, Alitretinoine, ALRT-1057, ALRT1057, BAL-4079, LG-100057, LG100057, LGD-1057, LGD1057, NSC-659772, Panretin, Retinoic acid 9-cis-form, Toctino)
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]
cellular retinoic acid binding protein 2/Cellular retinoic acid-binding protein II in Mouse [ChEMBL: CHEMBL4172] [GtoPdb: 2530] [UniProtKB: P22935]
Liver X receptor-α/LXR-alpha in Human [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133]
Liver X receptor-β/LXR-beta in Human [ChEMBL: CHEMBL4093] [GtoPdb: 601] [UniProtKB: P55055]
RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449]
Nerve Growth factor IB/Nuclear receptor subfamily 4 group A member 1 in Human [ChEMBL: CHEMBL1293229] [GtoPdb: 629] [UniProtKB: P22736]
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]
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]
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]
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]
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]
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]

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	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	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	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	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 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	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	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]
ChEMBL	Agonist activity at human RAR-alpha expressed in CHO-K1 cells by PathHunter assay	B	9	pEC50	1	nM	EC50	J Med Chem (2022) 65: 9974-10000 [PMID:35797110]
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	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	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 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]
ChEMBL	Agonist activity at human RAR-beta expressed in CHO-K1 cells by PathHunter assay	B	9.1	pEC50	0.8	nM	EC50	J Med Chem (2022) 65: 9974-10000 [PMID:35797110]
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 LBD (T225 to T462 residues) by fluorescence quenching assay	B	7.8	pKd	16	nM	Kd	J Med Chem (2022) 65: 14409-14423 [PMID:36318154]
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	Displacement of CU-6PMN from human RXRalpha LBD incubated for 2 hrs by fluorescence based assay	B	6.23	pKi	583	nM	Ki	J Med Chem (2019) 62: 8809-8818 [PMID:31483660]
ChEMBL	Displacement of 6-(Ethyl-{5-isobutoxy-4-isopropyl-2-[(10-oxo-2,3,5,6-tetrahydro-1H,4H,10H-11-oxa-3a-aza-benzo[de]anthracene-9-carbonyl)-amino]-phenyl}-amino)-nicotinic acid from human RXRalpha-LBD by by fluorescence binding assay	B	6.32	pKi	478	nM	Ki	J Med Chem (2021) 64: 861-870 [PMID:33378197]
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 USA (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 human GAL4-fused RXRalpha LBD (T225 to T462 residues) expressed in HEK293 cells incubated for 24 hrs by Dual-Glo luciferase assay	B	6.77	pEC50	170	nM	EC50	J Med Chem (2022) 65: 14409-14423 [PMID:36318154]
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	Transcriptional activation of Retinoid X receptor RXR alpha	B	7	pEC50	100	nM	EC50	J Med Chem (1996) 39: 3556-3563 [PMID:8784454]
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	Agonist activity at RXRalpha-LBD (unknown origin) assessed as transactivation by measuring increase in fluorescein-labelled coactivator PGC-1alpha peptide recruitment by Lanthascreen TR-FRET	B	7.59	pEC50	26	nM	EC50	J Nat Prod (2022) 85: 2804-2816 [PMID:36475432]
ChEMBL	Transcriptional activation for RXR alpha receptor	B	7.89	pEC50	13	nM	EC50	Bioorg Med Chem Lett (1994) 4: 1447-1452
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	Effective concentration against RXR-alpha receptor	B	7.89	pEC50	13	nM	EC50	J Med Chem (1993) 36: 2605-2613 [PMID:8410972]
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	Agonist activity at human RXR-alpha expressed in U2OS cells by PathHunter assay	B	8.22	pEC50	6	nM	EC50	J Med Chem (2022) 65: 9974-10000 [PMID:35797110]
ChEMBL	Agonist activity at human RXR-alpha	B	8.4	pEC50	4	nM	EC50	J Med Chem (2016) 59: 9201-9214 [PMID:27652492]
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	8.42	pKi	3.8	nM	Ki	J Med Chem (1997) 40: 4222-4234 [PMID:9435893]
ChEMBL	Binding affinity against retinoic Acid X beta receptor using [3H]- -9-cis-Retinoic Acid in competitive binding assay	B	7.92	pIC50	12	nM	IC50	J Med Chem (1994) 37: 408-414 [PMID:8308867]
ChEMBL	Transcriptional activation of Retinoid X receptor RXR beta	B	6.7	pEC50	200	nM	EC50	J Med Chem (1996) 39: 3556-3563 [PMID:8784454]
ChEMBL	Binding affinity against retinoic Acid X beta receptors co-transfected into CV-1 cells	B	6.7	pEC50	200	nM	EC50	J Med Chem (1994) 37: 408-414 [PMID:8308867]
ChEMBL	Agonist activity for retinoic acid receptor RXR beta in transcriptional activation assay	F	6.7	pEC50	200	nM	EC50	Bioorg Med Chem Lett (1995) 5: 2729-2734
ChEMBL	Transcriptional activation in CV-1 cells expressing Retinoid X receptor RXR beta	F	6.7	pEC50	200	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 beta using transactivation assay	B	6.7	pEC50	200	nM	EC50	Bioorg Med Chem Lett (1996) 6: 213-218
ChEMBL	Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR beta	F	7.54	pEC50	29	nM	EC50	J Med Chem (2001) 44: 2298-2303 [PMID:11428923]
ChEMBL	Agonist activity at human RXR-beta expressed in U2OS cells by PathHunter assay	B	8.22	pEC50	6	nM	EC50	J Med Chem (2022) 65: 9974-10000 [PMID:35797110]
ChEMBL	Effective concentrations against Retinoic acid receptor RXR-beta	B	8.59	pEC50	2.6	nM	EC50	J Med Chem (1995) 38: 3368-3383 [PMID:7650690]
Retinoid X receptor-β/Retinoid X receptor beta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4047] [GtoPdb: 611] [UniProtKB: P28704]
ChEMBL	Inhibition of [3H]9-cis-RA binding to mouse Retinoid X receptor RXR beta	B	7.82	pKd	15	nM	Kd	Bioorg Med Chem Lett (2003) 13: 261-264 [PMID:12482435]
ChEMBL	Dissociation constant for binding to Retinoid X receptor beta	B	7.92	pKd	12	nM	Kd	J Med Chem (1996) 39: 3556-3563 [PMID:8784454]
ChEMBL	Transcriptional activation in CV-1 cells expressing mouse Retinoid X receptor RXR beta	B	6.89	pEC50	128	nM	EC50	Bioorg Med Chem Lett (2003) 13: 261-264 [PMID:12482435]
Retinoid X receptor-γ/Retinoid X receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2004] [GtoPdb: 612] [UniProtKB: P48443]
ChEMBL	Inhibition of [3H]9-cis-retinoic acid binding to baculovirus expressed retinoic acid receptor RXR-gamma	B	7.52	pKd	30	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	7.8	pKd	16	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	7.85	pKd	14	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 gamma	B	7.85	pKd	14	nM	Kd	Bioorg Med Chem Lett (2003) 13: 261-264 [PMID:12482435]
ChEMBL	Binding affinity towards Retinoic acid receptor RXR-gamma by displacing 3.4 nM 3[H]-9-cis-RA	B	7.57	pKi	27	nM	Ki	Bioorg Med Chem Lett (1997) 7: 2313-2318
ChEMBL	Inhibition of [3H]targretin binding to Retinoid X receptor RXR gamma	B	7.85	pKi	14	nM	Ki	J Med Chem (1996) 39: 3229-3234 [PMID:8765503]
ChEMBL	Inhibition of [3H]9-cis-RA binding to Retinoid X receptor RXR gamma	B	7.89	pKi	13	nM	Ki	J Med Chem (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL	Agonistic activity towards retinoid X receptor-gamma	F	7.96	pKi	11	nM	Ki	J Med Chem (1997) 40: 4222-4234 [PMID:9435893]
GtoPdb	-	-	8	pIC50	-	-	-	Proc Natl Acad Sci USA (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	Binding affinity against retinoic Acid X gamma receptor using [3H]- -9-cis-Retinoic Acid in competitive binding assay	B	8.4	pIC50	4	nM	IC50	J Med Chem (1994) 37: 408-414 [PMID:8308867]
ChEMBL	Transcriptional activation in CV-1 cells expressing Retinoid X receptor RXR gamma	F	6.66	pEC50	219	nM	EC50	J Med Chem (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL	Binding affinity against retinoic Acid X gamma receptors co-transfected into CV-1 cells	B	6.85	pEC50	140	nM	EC50	J Med Chem (1994) 37: 408-414 [PMID:8308867]
ChEMBL	Agonist activity for retinoic acid receptor RXR gamma in transcriptional activation assay	F	6.85	pEC50	140	nM	EC50	Bioorg Med Chem Lett (1995) 5: 2729-2734
ChEMBL	Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoid X receptor gamma using transactivation assay	B	6.85	pEC50	140	nM	EC50	Bioorg Med Chem Lett (1996) 6: 213-218
ChEMBL	Transcriptional activation of Retinoid X receptor RXR gamma	B	6.85	pEC50	140	nM	EC50	J Med Chem (1996) 39: 3556-3563 [PMID:8784454]
ChEMBL	Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR gamma	F	8.35	pEC50	4.5	nM	EC50	J Med Chem (2001) 44: 2298-2303 [PMID:11428923]
ChEMBL	Effective concentrations against Retinoic acid receptor RXR-gamma	B	8.37	pEC50	4.3	nM	EC50	J Med Chem (1995) 38: 3368-3383 [PMID:7650690]
Retinoid X receptor-γ/Retinoid X receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4402] [GtoPdb: 612] [UniProtKB: P28705]
ChEMBL	Dissociation constant for binding to Retinoid X receptor gamma	B	8.4	pKd	4	nM	Kd	J Med Chem (1996) 39: 3556-3563 [PMID:8784454]
ChEMBL	Transcriptional activation in CV-1 cells expressing mouse Retinoid X receptor RXR gamma	B	6.91	pEC50	124	nM	EC50	Bioorg Med Chem Lett (2003) 13: 261-264 [PMID:12482435]

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]