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ChEMBL ligand: CHEMBL275311 (Ro-137410) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]