Table 1.

Cell-based GR ligand-binding competition assay with 1.5 nM [³H]-dexamethasone upon competition treatment with 1 µM of the different ligands indicated (14).

Ligand	% inhibition of GR ligand binding	IC50 (nM)	Ki (nM)
Dex	100
Dex-mesylate	99	7.3	3.7
GSK866	100	4.6	2.3
1158	−2
1159	−12
1217	92	22	11
1218	96	34	17

% inhibition of GR radioligand binding, IC50 (nM) and Ki (nM) are indicated.

Gray shade indicates values not applicable.