Synonyms: [(-)-N-(2S,10S,14bS)]-N-(8-cyano-1,2,3,4,10,14b-hexahydro-10-methyl dibenzo[c,f]pyrido[1,2-a]azepin-2-yl)-4-methyl-1,2,3-thiadiazole-5-carboxamide]] | ORG214007-0
Compound class:
Synthetic organic
Comment: ORG 214007-0 is a non-steroidal, selective glucocorticoid receptor (GR) modulator [1]. It retains full anti-inflammatory activity compared to traditional steroidal GR modulators.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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Bioactivity Comments |
ORG 214007-0 binds as avidly to GR as prednisolone, but is a partial agonist In a co-factor recruitment assay. Compared to prednisolone (at 100%) ORG 214007-0 achieves 32% maximum efficiency in co-factor recruitment in vitro. |
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