| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA4380042 | B | Inverse agonist activity at human N-terminal His6-tagged RORgammat LBD (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as inhibition of N-terminal biotinylated co-activator SRC1 box2 peptide recruitment measured after 30 mins by TR-FRET assay | Homo sapiens | 19 | ALA4376852 | assay format | Scientific Literature | |
| 2. | ALA4380043 | B | Competitive inverse agonist activity at human N-terminal His6-tagged RORgammat LBD (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as inhibition of N-terminal biotinylated co-activator SRC1 box2 peptide recruitment measured after 30 mins in absence of RORgamma agonist cholesterol by TR-FRET assay | Homo sapiens | 4 | ALA4376852 | assay format | Scientific Literature | |
| 3. | ALA4380044 | B | Competitive inverse agonist activity at human N-terminal His6-tagged RORgammat LBD (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as inhibition of N-terminal biotinylated co-activator SRC1 box2 peptide recruitment measured after 30 mins in presence of 0.25 uM RORgamma agonist cholesterol by TR-FRET assay | Homo sapiens | 4 | ALA4376852 | assay format | Scientific Literature | |
| 4. | ALA4380045 | B | Competitive inverse agonist activity at human N-terminal His6-tagged RORgammat LBD (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as inhibition of N-terminal biotinylated co-activator SRC1 box2 peptide recruitment measured after 30 mins in presence of 1 uM RORgamma agonist cholesterol by TR-FRET assay | Homo sapiens | 4 | ALA4376852 | assay format | Scientific Literature | |
| 5. | ALA4380046 | B | Displacement of Alexa647-labeled MRL-87 from human N-terminal His6-tagged RORgammat LBD (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) measured after 30 mins by TR-FRET assay | Homo sapiens | 3 | ALA4376852 | assay format | Scientific Literature | |
| 6. | ALA4380047 | A | Inverse agonist activity at His6-tagged PPARgamma LBD (unknown origin) assessed as inhibition of rosiglitazone-induced N-terminal biotinylated co-activator SRC1 box2 peptide recruitment measured after 30 mins by TR-FRET assay | Homo sapiens | 19 | ALA4376852 | single protein format | Scientific Literature | |
| 7. | ALA4380049 | B | Inverse agonist activity at RORgammat in mouse EL4 cells assessed as inhibition of PMA/ionomycin-induced IL-17a production at 10 uM preincubated for 24 hrs followed by PMA/ionomycin stimulation and measured after 5 hrs by SYBR green dye based qRT-PCR analysis relative to control | Mus musculus | 3 | ALA4376852 | cell-based format | Scientific Literature | |
| 8. | ALA4380050 | P | Chemical stability of the compound in pH 7.4 aqueous buffer assessed as parent compound remaining at 2 uM measured after 24 hrs by LC-MS analysis | 4 | ALA4376852 | small-molecule physicochemical format | Scientific Literature | ||
| 9. | ALA4380051 | P | Kinetic solubility of the compound in pH 7.4 aqueous buffer at 500 uM measured after 90 mins by spectrophotometric method | 4 | ALA4376852 | small-molecule physicochemical format | Scientific Literature | ||
| 10. | ALA4380052 | A | Permeability of the compound at 500 uM after 20 hrs by PAMPA | 4 | ALA4376852 | assay format | Scientific Literature | ||
| 11. | ALA4380053 | A | Intrinsic clearance in human liver microsomes at 3 uM measured up to 90 mins in presence of metabolic phase 1 cofactors by LC-MS analysis | Homo sapiens | 4 | ALA4376852 | microsome format | Scientific Literature | |
| 12. | ALA4380054 | A | Stability in human liver microsomes assessed as parent compound remaining at 5 uM measured after 1 hr in presence of metabolic phase 2 cofactors UDPGA by LC-MS analysis | Homo sapiens | 4 | ALA4376852 | microsome format | Scientific Literature | |
| 13. | ALA4380055 | A | Stability of the compound in plasma (unknown origin) assessed as parent compound remaining at 5 uM measured after 1 hr by LC-MS analysis | Not specified | 4 | ALA4376852 | cell-free format | Scientific Literature | |
| 14. | ALA4380056 | A | Protein binding in plasma (unknown origin) at 5 uM measured after 6 hrs by LC-MS based equilibrium dialysis analysis | Not specified | 4 | ALA4376852 | cell-free format | Scientific Literature | |
| 15. | ALA4714674 | B | Allosteric inverse agonist activity at recombinant human N-terminal His6-tagged RORgammat ligand binding domain (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as reduction in coactivator, N-terminal biotinylated SRC-1 box2 peptide recruitment incubated for 60 mins by TR-FRET assay | Homo sapiens | 2 | ALA4706717 | assay format | Scientific Literature | |
| 16. | ALA4714676 | B | Allosteric inverse agonist activity at GW9662-ligated recombinant human N-terminal His6-tagged RORgammat ligand binding domain (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as reduction in coactivator, N-terminal biotinylated SRC-1 box2 peptide recruitment in presence of GW9662 incubated for 60 mins by TR-FRET assay | Homo sapiens | 2 | ALA4706717 | assay format | Scientific Literature | |
| 17. | ALA4714680 | B | Allosteric inverse agonist activity at 2-chloro-5-nitro-N-o-tolylbenzamide-ligated recombinant human N-terminal His6-tagged RORgammat ligand binding domain (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as reduction in coactivator, N-terminal biotinylated SRC-1 box2 peptide recruitment in presence of 2-chloro-5-nitro-N-o-tolylbenzamide incubated for 60 mins by TR-FRET assay | Homo sapiens | 2 | ALA4706717 | assay format | Scientific Literature | |
| 18. | ALA4714682 | B | Allosteric inverse agonist activity at 2-chloro-N-(2,6-dimethylphenyl)-5-nitrobenzamide-ligated recombinant human N-terminal His6-tagged RORgammat ligand binding domain (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as reduction in coactivator, N-terminal biotinylated SRC-1 box2 peptide recruitment in presence of 2-chloro-N-(2,6-dimethylphenyl)-5-nitrobenzamide incubated for 60 mins by TR-FRET assay | Homo sapiens | 2 | ALA4706717 | assay format | Scientific Literature | |
| 19. | ALA4714684 | B | Allosteric inverse agonist activity at 2-chloro-5-nitro-N-(2-(trifluoromethyl)phenyl)benzamide-ligated recombinant human N-terminal His6-tagged RORgammat ligand binding domain (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as reduction in coactivator, N-terminal biotinylated SRC-1 box2 peptide recruitment in presence of 2-chloro-5-nitro-N-(2-(trifluoromethyl)phenyl)benzamide incubated for 60 mins by TR-FRET assay | Homo sapiens | 2 | ALA4706717 | assay format | Scientific Literature | |
| 20. | ALA4714685 | B | Binding affinity to recombinant human N-terminal His6-tagged RORgammat (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as change in melting temperature at 10 uM by thermal shift assay | Homo sapiens | 6 | ALA4706717 | assay format | Scientific Literature |
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