TTNPB [Ligand Id: 2646] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL275311 (Ro-137410)
  • RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449]
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  • Retinoic acid receptor-α/Retinoic acid receptor alpha in Human [ChEMBL: CHEMBL2055] [GtoPdb: 590] [UniProtKB: P10276]
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  • Retinoic acid receptor-β/Retinoic acid receptor beta in Human [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826]
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  • Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631]
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  • Retinoid X receptor-α/Retinoid X receptor alpha in Human [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793]
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  • Retinoid X receptor-β/Retinoid X receptor beta in Human [ChEMBL: CHEMBL1870] [GtoPdb: 611] [UniProtKB: P28702]
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  • Retinoid X receptor-γ/Retinoid X receptor gamma in Human [ChEMBL: CHEMBL2004] [GtoPdb: 612] [UniProtKB: P48443]
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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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]