LG100268 [Ligand Id: 2808] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL288436 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2129] [GtoPdb: 593] [UniProtKB: P37230] | ||||||||
| ChEMBL | Binding affinity for Peroxisome proliferator activated receptor alpha was determined | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2003) 46: 4087-4103 [PMID:12954061] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
| ChEMBL | In vitro agonist efficacy against PPAR gamma along with 100 nM BRL-49653 | F | 6.79 | pEC50 | 161 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 4071-4075 [PMID:14592510] |
| ChEMBL | In vitro agonistic activity against PPAR gamma along with 100 nM BRL-49653 | F | 7.73 | pEC50 | 18.6 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 4071-4075 [PMID:14592510] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4797] [GtoPdb: 595] [UniProtKB: O88275] | ||||||||
| ChEMBL | Binding affinity for Peroxisome proliferator activated receptor gamma was determined | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2003) 46: 4087-4103 [PMID:12954061] |
| Retinoic acid receptor-α/Retinoic acid receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2055] [GtoPdb: 590] [UniProtKB: P10276] | ||||||||
| ChEMBL | Binding affinity against retinoic acid receptor alpha by [3H]ATRA displacement. | B | 5.56 | pKi | 2745 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1593-1598 [PMID:15006411] |
| ChEMBL | Binding affinity against RAR alpha receptor using [3H]ATRA as radioligand in CV-1 cells | B | 5.81 | pKi | 1550 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 4071-4075 [PMID:14592510] |
| Retinoic acid receptor alpha in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2269] [UniProtKB: A6HIV9] | ||||||||
| ChEMBL | Binding affinity for Retinoic acid receptor alpha was determined by competing with 3[H]-ATRA | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2003) 46: 4087-4103 [PMID:12954061] |
| Retinoic acid receptor-β/Retinoic acid receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826] | ||||||||
| ChEMBL | Binding affinity against RAR beta receptor using [3H]ATRA as radioligand in CV-1 cells | B | 5 | pKi | 9901 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 4071-4075 [PMID:14592510] |
| ChEMBL | Binding affinity for Retinoic acid receptor beta was determined by competing with 3[H]-ATRA | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2003) 46: 4087-4103 [PMID:12954061] |
| Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631] | ||||||||
| ChEMBL | Binding affinity against Retinoic acid receptor gamma was determined in vitro by using [3H]ATRA as radioligand | B | 5 | pKi | 10000 | nM | Ki | J Med Chem (2003) 46: 2683-2696 [PMID:12801232] |
| ChEMBL | Binding affinity against RAR gamma receptor using [3H]ATRA as radioligand in CV-1 cells | B | 5 | pKi | 9901 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 4071-4075 [PMID:14592510] |
| Retinoic acid receptor gamma in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2630] [UniProtKB: D3ZWV0] | ||||||||
| ChEMBL | Binding affinity for Retinoic acid receptor gamma was determined by competing with 3[H]-ATRA | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2003) 46: 4087-4103 [PMID:12954061] |
| Retinoid X receptor-α/Retinoid X receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793] | ||||||||
| ChEMBL | Ability to bind directly to Retinoic acid receptor RXR-alpha was evaluated in a competitive binding assay. | B | 8.52 | pKd | 3 | nM | Kd | J Med Chem (1995) 38: 3146-3155 [PMID:7636877] |
| ChEMBL | Binding affinity against Retinoic acid receptor RXR-alpha was determined in vitro by using [3H]9-cis-RA as radioligand | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (2003) 46: 2683-2696 [PMID:12801232] |
| ChEMBL | Binding affinity against RXR alpha receptor using [3H]9-cis-RA as radioligand in CV-1 cells | B | 7.89 | pKi | 12.9 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 4071-4075 [PMID:14592510] |
| ChEMBL | Binding affinity against Retinoic acid receptor RXR-alpha by [3H]9-cis-RA displacement. | B | 8.52 | pKi | 3 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1593-1598 [PMID:15006411] |
| ChEMBL | Antagonist activity for Retinoic X receptor alpha in CV1 cells | F | 8.1 | pIC50 | 8 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1593-1598 [PMID:15006411] |
| GtoPdb | - | - | 8.5 | pIC50 | - | - | - |
Curr Pharm Des (2000) 6: 25-58 [PMID:10637371]; Nature (1996) 383: 450-3 [PMID:8837780]; J Med Chem (1994) 37: 408-14 [PMID:8308867] |
| ChEMBL | Activation of human RXRalpha activity expressed in COS1 cells after 12 hrs by RXRE-luciferase reporter gene assay | B | 7.4 | pEC50 | 40 | nM | EC50 | J Med Chem (2013) 56: 2581-2605 [PMID:23472886] |
| ChEMBL | In vitro agonistic activity against RXR alpha in CV-1 cells | F | 7.77 | pEC50 | 17 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 4071-4075 [PMID:14592510] |
| ChEMBL | Inhibition of Retinoic acid receptor RXR-alpha agonist activity in vitro | F | 7.96 | pEC50 | 11 | nM | EC50 | J Med Chem (2003) 46: 2683-2696 [PMID:12801232] |
| ChEMBL | Ability to activate gene expression at Retinoic acid receptor RXR-alpha was evaluated in a cotransfection assay. | B | 8.4 | pEC50 | 4 | nM | EC50 | J Med Chem (1995) 38: 3146-3155 [PMID:7636877] |
| Retinoid X receptor-α/Retinoid X receptor alpha in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4431] [GtoPdb: 610] [UniProtKB: Q05343] | ||||||||
| ChEMBL | Binding affinity for Retinoic acid receptor RXR-alpha was determined by competing with 3[H]-9-cis-RA | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (2003) 46: 4087-4103 [PMID:12954061] |
| ChEMBL | In vitro transcriptional activation in CV-1 cells expressing RXR-alpha | B | 7.96 | pEC50 | 11 | nM | EC50 | J Med Chem (2003) 46: 4087-4103 [PMID:12954061] |
| Retinoid X receptor-β/Retinoid X receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1870] [GtoPdb: 611] [UniProtKB: P28702] | ||||||||
| ChEMBL | Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cells | B | 7.12 | pKi | 75 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 4071-4075 [PMID:14592510] |
| ChEMBL | Displacement of [3H]9-cis-RA from Retinoic X receptor beta | B | 8.12 | pKi | 7.5 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1593-1598 [PMID:15006411] |
| Retinoid X receptor-β/Retinoid X receptor beta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4047] [GtoPdb: 611] [UniProtKB: P28704] | ||||||||
| ChEMBL | Binding affinity to Retinoic acid receptor RXR-beta was determined in a competitive binding assay. | B | 8.52 | pKd | 3 | nM | Kd | J Med Chem (1995) 38: 3146-3155 [PMID:7636877] |
| ChEMBL | Binding affinity against retinoic acid receptor beta by [3H]ATRA displacement. | B | 5.45 | pKi | 3515 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1593-1598 [PMID:15006411] |
| ChEMBL | Ability to activate gene expression at Retinoic acid receptor RXR-beta was evaluated in a cotransfection assay. | B | 8.52 | pEC50 | 3 | nM | EC50 | J Med Chem (1995) 38: 3146-3155 [PMID:7636877] |
| Retinoid X receptor-β/Retinoid X receptor beta in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2805] [GtoPdb: 611] [UniProtKB: P49743] | ||||||||
| ChEMBL | Binding affinity for Retinoic acid receptor RXR-beta was determined by competing with 3[H]-9-cis-RA | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2003) 46: 4087-4103 [PMID:12954061] |
| Retinoid X receptor-γ/Retinoid X receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2004] [GtoPdb: 612] [UniProtKB: P48443] | ||||||||
| ChEMBL | Binding affinity against RXR gamma receptor using [3H]9-cis-RA as radioligand in CV-1 cells | B | 7.92 | pKi | 12 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 4071-4075 [PMID:14592510] |
| ChEMBL | Displacement of [3H]9-cis-RA from retinoic X receptor gamma | B | 7.92 | pKi | 12 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1593-1598 [PMID:15006411] |
| Retinoid X receptor-γ/Retinoid X receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4402] [GtoPdb: 612] [UniProtKB: P28705] | ||||||||
| ChEMBL | Binding affinity to Retinoic acid receptor RXR-gamma was evaluated in a competitive binding assay. | B | 8.52 | pKd | 3 | nM | Kd | J Med Chem (1995) 38: 3146-3155 [PMID:7636877] |
| ChEMBL | Binding affinity against retinoic acid receptor gamma by [3H]ATRA displacement. | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1593-1598 [PMID:15006411] |
| ChEMBL | Ability to activate gene expression at Retinoic acid receptor RXR-gamma was evaluated in a cotransfection assay. | B | 8.4 | pEC50 | 4 | nM | EC50 | J Med Chem (1995) 38: 3146-3155 [PMID:7636877] |
| Retinoid X receptor-γ/Retinoid X receptor gamma in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4277] [GtoPdb: 612] [UniProtKB: Q5BJR8] | ||||||||
| ChEMBL | Binding affinity for Retinoic acid receptor RXR-gamma was determined by competing with 3[H]-9-cis-RA | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (2003) 46: 4087-4103 [PMID:12954061] |
| Retinoid X receptor-α/Peroxisome proliferator-activated receptor-γ/RXR alpha/PPAR gamma in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111394] [GtoPdb: 610, 595] [UniProtKB: P19793, P37231] | ||||||||
| GtoPdb | - | - | 8.5 | pIC50 | - | - | - |
Curr Pharm Des (2000) 6: 25-58 [PMID:10637371]; Nature (1996) 383: 450-3 [PMID:8837780]; J Med Chem (1994) 37: 408-14 [PMID:8308867] |
| ChEMBL | Transcriptional activity against RXR:PPAR-gamma synergy was determined in vitro | F | 7.42 | pEC50 | 38 | nM | EC50 | J Med Chem (2003) 46: 2683-2696 [PMID:12801232] |
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]
