LG100268 [Ligand Id: 2808] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL288436 |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 |
|---|---|---|---|---|---|---|---|---|
| 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: Q499N1] | ||||||||
| 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 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]
