| Assay ID | Title | Year | Journal | Article |
|---|
| AID1176716 | Antiarthritic effect in 9-day type-2 collagen-induced rat arthritis model assessed as reduction in ankle inflammation at 3 mg/kg, po qd | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1176700 | Agonist activity at GR in HFF cells assessed as suppression of IL-1-induced IL-6 production | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1380136 | Transrepression activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells assessed as inhibition of PMA-stimulated gene expression incubated for 24 hrs by beta-galactosidase reporter gene assay | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile. |
| AID1380131 | Transactivation activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells at 1 uM incubated for 24 hrs by beta-galactosidase reporter gene assay | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile. |
| AID1176721 | Antiarthritic effect in 9-day type-2 collagen-induced rat arthritis model assessed as reduction in bone resorption at 10 mg/kg, po qd | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1380145 | Transrepression of GR in human whole blood assessed as inhibition of LPS-induced TNF-alpha release preincubated for 45 mins followed by LPS addition after 18 hrs by AlphaLISA method | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile. |
| AID1176717 | Antiarthritic effect in 9-day type-2 collagen-induced rat arthritis model assessed as reduction in pannus formation at 3 mg/kg, po qd | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1176708 | Agonist activity at GR in human MG-63 cells assessed as inhibition of vitamin D-induced osteocalcin production at 2 uM relative to dexamethasone | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1176707 | Agonist activity at GR in human HeLa cells transfected with MMTV promoter at 2 uM by luciferase transactivation assay relative to dexamethasone | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1176722 | Antiarthritic effect in 9-day type-2 collagen-induced rat arthritis model assessed as reduction in ankle inflammation at 30 mg/kg, po qd | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1176719 | Antiarthritic effect in 9-day type-2 collagen-induced rat arthritis model assessed as reduction in bone resorption at 3 mg/kg, po qd | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1380139 | Aqueous solubility of the compound | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile. |
| AID1176705 | Thermodynamic solubility of the compound in buffer at pH 6.8 after 24 hrs by HPLC analysis | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1380129 | Displacement of fluormone RED from human full length glucocorticoid receptor after 4 hrs by fluorescence polarization assay | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile. |
| AID1380147 | Therapeutic index, ratio of fEC50 for transactivation of GR in cryopreserved human primary hepatocytes assessed as upregulation of TAT mRNA expression level to fIC30 for transrepression of GR in human whole blood assessed as inhibition of LPS-induced TNF- | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile. |
| AID1176723 | Antiarthritic effect in 9-day type-2 collagen-induced rat arthritis model assessed as reduction in pannus formation at 30 mg/kg, po qd | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1176720 | Antiarthritic effect in 9-day type-2 collagen-induced rat arthritis model assessed as reduction in pannus formation at 10 mg/kg, po qd | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1176718 | Antiarthritic effect in 9-day type-2 collagen-induced rat arthritis model assessed as reduction in cartilage damage at 3 mg/kg, po qd | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1176710 | Inhibition of CYP2D6 (unknown origin) | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1176711 | Inhibition of CYP2C9 (unknown origin) | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1380138 | Transrepression activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells assessed as inhibition of PMA-stimulated gene expression incubated for 24 hrs by beta-galactosidase reporter gene assay relative to dexamethasone | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile. |
| AID1176714 | Clearance in human liver microsomes after 60 mins by HPLC analysis relative to hepatic blood flow | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1176724 | Antiarthritic effect in 9-day type-2 collagen-induced rat arthritis model assessed as reduction in cartilage damage at 30 mg/kg, po qd | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1380128 | Transactivation of GR in cryopreserved human primary hepatocytes assessed as upregulation of TAT mRNA expression level after 18 hrs by RT-qPCR analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile. |
| AID1176696 | Antiarthritic effect in po dosed 9-day type-2 collagen-induced rat arthritis model administered qd | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1176715 | Agonist activity at GR in mouse RAW cells assessed as suppression of TNF-alpha-induced IL-6 production | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1176704 | Inhibition of human ERG channel expressed in recombinant HEK293 cells by whole cell patch-clamp technique | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1176697 | Toxicity in po dosed 9-day type-2 collagen-induced rat arthritis model administered qd | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1176709 | Inhibition of CYP1A2 (unknown origin) | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1380148 | Transrepression of GR in cryopreserved human fetal osteoblasts assessed as inhibition of OPG mRNA expression after 4 hrs by RT-qPCR analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile. |
| AID1176695 | Antiarthritic effect in 9-day type-2 collagen-induced rat arthritis model assessed as reduction in bone resorption at 30 mg/kg, po qd | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1380149 | Therapeutic index, ratio of fIC20 for transrepression of GR in cryopreserved human fetal osteoblasts assessed as inhibition of OPG mRNA expression to fIC30 for transrepression of GR in human whole blood assessed as inhibition of LPS-induced TNF-alpha rele | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile. |
| AID1176698 | Displacement of RU-486 from GR (unknown origin) by fluorescence polarization assay | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1176713 | Half life in rat | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1176702 | Inhibition of human recombinant CYP3A4 using 7-benzyloxy-4-(trifluoromethyl)-coumarin as substrate after 30 mins by fluorescence assay | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1176701 | Agonist activity at GR in HFF cells assessed as suppression of IL-1-induced IL-6 production at 2 uM relative to dexamethasone | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1176712 | Inhibition of CYP2C19 (unknown origin) | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| AID1346849 | Human Glucocorticoid receptor (3C. 3-Ketosteroid receptors) | 2014 | ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
| Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |