ChEMBL ligand: CHEMBL275311 (Ro-137410)
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!
Plasmodium falciparum [ChEMBL: CHEMBL364] 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] 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] 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] 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] 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] 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] 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
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	5.05	pEC50	9000	nM	EC50	J Med Chem (2014) 57: 5871-5892 [PMID:24502334]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay	F	4.8	pIC50	15848.93	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
Retinoic acid receptor-α/Retinoic acid receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2055] [GtoPdb: 590] [UniProtKB: P10276]
ChEMBL	Binding affinity for Retinoic acid receptor alpha	B	7.44	pKd	36	nM	Kd	Bioorg Med Chem Lett (1997) 7: 2373-2378
ChEMBL	Binding affinity to retinoic acid receptor alpha using [3H]CD 367 as radioligand	B	7.68	pKi	21	nM	Ki	J Med Chem (1995) 38: 4993-5006 [PMID:8544175]
GtoPdb	-	-	7.44	pIC50	-	-	-	Mol Cell Biol (1994) 14: 287-98 [PMID:8264595]; J Mol Biol (2000) 302: 155-70 [PMID:10964567]; Mol Cell Biol (1995) 15: 3540-51 [PMID:7791761]; Curr Pharm Des (2000) 6: 25-58 [PMID:10637371]
ChEMBL	Binding affinity against retinoic Acid alpha receptor using [3H]- -9-cis-Retinoic Acid in competitive binding assay	B	7.44	pIC50	36	nM	IC50	J Med Chem (1994) 37: 408-414 [PMID:8308867]
ChEMBL	Effective concentration against RAR-alpha receptor	B	7.07	pEC50	85	nM	EC50	J Med Chem (1993) 36: 2605-2613 [PMID:8410972]
ChEMBL	Transactivation potency for Retinoic acid receptor alpha	B	7.52	pEC50	30	nM	EC50	Bioorg Med Chem Lett (1997) 7: 2373-2378
ChEMBL	Binding affinity against retinoic Acid alpha receptors co-transfected into CV-1 cells	B	7.52	pEC50	30	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	7.52	pEC50	30	nM	EC50	Bioorg Med Chem Lett (1995) 5: 2729-2734
ChEMBL	Transcriptional activation of retinoic acid receptor RAR alpha	B	7.68	pEC50	21	nM	EC50	Bioorg Med Chem Lett (1995) 5: 523-527
ChEMBL	Transcriptional activation of Retinoic acid receptor RAR alpha	B	7.68	pEC50	21	nM	EC50	J Med Chem (1995) 38: 2820-2829 [PMID:7636843]
ChEMBL	Transcriptional activation for RAR alpha receptor	B	7.68	pEC50	21	nM	EC50	Bioorg Med Chem Lett (1994) 4: 1447-1452
ChEMBL	Agonist activity at human RARalpha expressed in HEK293 cells by luciferase reporter gene assay	B	9.74	pEC50	0.18	nM	EC50	Bioorg Med Chem Lett (2014) 24: 5265-5267 [PMID:25305688]
Retinoic acid receptor-β/Retinoic acid receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826]
ChEMBL	Binding affinity for Retinoic acid receptor beta	B	8.3	pKd	5	nM	Kd	Bioorg Med Chem Lett (1997) 7: 2373-2378
ChEMBL	Binding affinity to retinoic acid receptor beta using [3H]CD 367 as radioligand	B	8.3	pKi	5	nM	Ki	J Med Chem (1995) 38: 4993-5006 [PMID:8544175]
ChEMBL	Binding affinity towards cRAR-beta-2 receptor by displacing 0.82 nM 3[H]all-trans-RA	B	9.3	pKi	0.5	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	-	-	8	pIC50	-	-	-	Mol Cell Biol (1994) 14: 287-98 [PMID:8264595]; J Mol Biol (2000) 302: 155-70 [PMID:10964567]; Mol Cell Biol (1995) 15: 3540-51 [PMID:7791761]; Curr Pharm Des (2000) 6: 25-58 [PMID:10637371]
ChEMBL	Binding affinity against retinoic Acid beta receptor using [3H]- -9-cis-Retinoic Acid in competitive binding assay	B	8.3	pIC50	5	nM	IC50	J Med Chem (1994) 37: 408-414 [PMID:8308867]
ChEMBL	Effective concentration against Retinoic acid receptor beta	B	8.22	pEC50	6	nM	EC50	J Med Chem (1993) 36: 2605-2613 [PMID:8410972]
ChEMBL	Transcriptional activation of retinoic acid receptor RAR beta	B	8.4	pEC50	4	nM	EC50	Bioorg Med Chem Lett (1995) 5: 523-527
ChEMBL	Transcriptional activation of Retinoic acid receptor RAR beta	B	8.4	pEC50	4	nM	EC50	J Med Chem (1995) 38: 2820-2829 [PMID:7636843]
ChEMBL	Transcriptional activation for RAR beta receptor	B	8.4	pEC50	4	nM	EC50	Bioorg Med Chem Lett (1994) 4: 1447-1452
ChEMBL	Transactivation potency for Retinoic acid receptor beta	B	8.52	pEC50	3	nM	EC50	Bioorg Med Chem Lett (1997) 7: 2373-2378
ChEMBL	Binding affinity against retinoic Acid beta receptors co-transfected into CV-1 cells	B	8.52	pEC50	3	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	8.52	pEC50	3	nM	EC50	Bioorg Med Chem Lett (1995) 5: 2729-2734
Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631]
ChEMBL	Binding affinity for Retinoic acid receptor gamma	B	7.59	pKd	26	nM	Kd	Bioorg Med Chem Lett (1997) 7: 2373-2378
ChEMBL	Dissociation constant for Retinoic acid receptor gamma	B	7.59	pKd	26	nM	Kd	J Med Chem (2005) 48: 6212-6219 [PMID:16190748]
ChEMBL	Binding affinity to retinoic acid receptor (RAR) gamma using [3H]CD 367 as radioligand	B	8.3	pKi	5	nM	Ki	J Med Chem (1995) 38: 4993-5006 [PMID:8544175]
ChEMBL	Binding affinity against retinoic Acid gamma receptor using [3H]- -9-cis-Retinoic Acid in competitive binding assay	B	7.59	pIC50	26	nM	IC50	J Med Chem (1994) 37: 408-414 [PMID:8308867]
GtoPdb	-	-	7.82	pIC50	-	-	-	Mol Cell Biol (1994) 14: 287-98 [PMID:8264595]; J Mol Biol (2000) 302: 155-70 [PMID:10964567]
ChEMBL	Effective concentration against RAR-gamma receptor	B	7.62	pEC50	24	nM	EC50	J Med Chem (1993) 36: 2605-2613 [PMID:8410972]
ChEMBL	Transcriptional activation of retinoic acid receptor RAR gamma	B	8.62	pEC50	2.4	nM	EC50	Bioorg Med Chem Lett (1995) 5: 523-527
ChEMBL	Transcriptional activation of Retinoic acid receptor RAR gamma	B	8.62	pEC50	2.4	nM	EC50	J Med Chem (1995) 38: 2820-2829 [PMID:7636843]
ChEMBL	Transcriptional activation for RAR gamma receptor	B	8.62	pEC50	2.4	nM	EC50	Bioorg Med Chem Lett (1994) 4: 1447-1452
ChEMBL	Transactivation potency for Retinoic acid receptor gamma	B	8.7	pEC50	2	nM	EC50	Bioorg Med Chem Lett (1997) 7: 2373-2378
ChEMBL	Binding affinity against retinoic Acid gamma receptors co-transfected into CV-1 cells	B	8.7	pEC50	2	nM	EC50	J Med Chem (1994) 37: 408-414 [PMID:8308867]
ChEMBL	Agonist activity for retinoic acid receptor RAR gamma in transcriptional activation assay	F	8.7	pEC50	2	nM	EC50	Bioorg Med Chem Lett (1995) 5: 2729-2734
Retinoid X receptor-α/Retinoid X receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793]
ChEMBL	Binding affinity against retinoic Acid X alpha receptor using [3H]- -9-cis-Retinoic Acid in competitive binding assay	B	6	pIC50	>1000	nM	IC50	J Med Chem (1994) 37: 408-414 [PMID:8308867]
ChEMBL	Transcriptional activation of retinoid X receptor RXR alpha; not active	B	5	pEC50	10000	nM	EC50	Bioorg Med Chem Lett (1995) 5: 523-527
ChEMBL	Binding affinity against retinoic Acid X alpha receptors co-transfected into CV-1 cells	B	5	pEC50	>10000	nM	EC50	J Med Chem (1994) 37: 408-414 [PMID:8308867]
Retinoid X receptor-β/Retinoid X receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1870] [GtoPdb: 611] [UniProtKB: P28702]
ChEMBL	Binding affinity against retinoic Acid X beta receptor using [3H]- -9-cis-Retinoic Acid in competitive binding assay	B	6	pIC50	>1000	nM	IC50	J Med Chem (1994) 37: 408-414 [PMID:8308867]
ChEMBL	Binding affinity against retinoic Acid X beta receptors co-transfected into CV-1 cells	B	5	pEC50	>10000	nM	EC50	J Med Chem (1994) 37: 408-414 [PMID:8308867]
Retinoid X receptor-γ/Retinoid X receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2004] [GtoPdb: 612] [UniProtKB: P48443]
ChEMBL	Binding affinity against retinoic Acid X gamma receptor using [3H]- -9-cis-Retinoic Acid in competitive binding assay	B	6	pIC50	>1000	nM	IC50	J Med Chem (1994) 37: 408-414 [PMID:8308867]
ChEMBL	Binding affinity against retinoic Acid X gamma receptors co-transfected into CV-1 cells	B	5	pEC50	>10000	nM	EC50	J Med Chem (1994) 37: 408-414 [PMID:8308867]

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]