Table 2.
Activities of azaindole sulfonamides and amides (values were obtained from [74]).
| Compd. | hCRTH2 a (Ki) | cAMP b (IC50) | EOS c (IC50) |
DP a (Ki) |
TP a (Ki) |
|---|---|---|---|---|---|
| 42 | 7189 nM | > 1300 nM | > 7000 nM | ||
| 43 | 6725 nM | > 3400 nM | > 6800 nM | ||
| 44 | 139 nM | 351 nM | > 12,000 nM | > 22,000 nM | |
| 45 | 3.3 nM | 3.4 nM | 7.0 nM | > 47,000 nM | > 22,000 nM |
| 46 | 1.8 nM | 3.2 nM | 3.3 nM | > 18,000 nM | > 27,000 nM |
| 47 | 1.9 nM | 3.6 nM | 15.8 nM | > 3800 nM | > 1000 nM |
| 48 | 3.4 nM | 5.7 nM | 1.2 nM | > 38,000 nM | > 71,000 nM |
| 49 | 21.1 nM | 73.8 nM | > 12,000 nM | > 22,000 nM | |
| 50 | 4.7 nM | 3.5 nM | 2.3 nM | > 10,000 nM | > 21,000 nM |
| 51 | 3.6 nM | 7.5 nM | 3.1 nM | > 3700 nM | > 6800 nM |
| 52 d | 5.1 nM | 4.4 nM | 2.4 nM | > 4000 nM | > 7200 nM |
| 53 | 3.4 nM | 4.7 nM | 1.2 nM | > 4000 nM | > 7200 nM |
| 54 | 3.9 nM | 4.5 nM | 3.4 nM | > 4000 nM | > 7200 nM |
| 55 | 11.5 nM | 7.0 nM | > 4000 nM | > 7200 nM |
a Radioligand competition binding assay using membrane proteins from HEK293 (EBNA) cells stably expressing the receptor hCRTH2 in a 10 mM solution of HEPES/KOH (all values are mean of two or more experiments). b Functional assay: the intracellular concentration of cAMP was determined using the 125I-cAMP scintillation proximity assay. The assay was performed in Hank’s balanced salt solution 25 mM HEPES containing 5000 nM Forskolin (all values are mean of two or more experiments). c Human whole blood eosinophil shape change assay (all values are mean of two or more experiments). d Diastereomeric mixture.