TABLE 2.
Validation of purchased candidate compounds.
| Compound number | Chemotype | MW (g/mol) | CXCL8 production. Relative to LPS b (original library) | CXCL8 production. Relative to LPS c (purchased) | % Cellular Viability (Purchased) |
|---|---|---|---|---|---|
| 1–1a | 1H-pyrazolo [3,4 d] pyrimidin-4-amine | 321 | 50.6% | 47.1% | 98.7 |
| 1–2a | 1H-pyrazolo [3,4 d] pyrimidin-4-amine | 295 | 62.7% | 70.1% | 100.1 |
| 3–1a | Bis-aryl urea | 261 | 50.6% | 60.7% | 105.6 |
| 5–1a | 2-Nitro furan arylamide | 276 | 21.9% | 18.8% | 98.7 |
| 5–2a | 2-Nitro furan arylamide | 300 | 54.3% | 29.8% | 101.8 |
| 5–3a | 2-Nitro furan arylamide | 312 | 66.7% | 37.7% | 100.1 |
| 13–1 | 2-Imino-1,2-dihydro-5H-dipyrido [1,2-a:2′,3′-d]pyrimidin-5-one | 454 | 25.8% | 95% | 106.1 |
| 13–2 | 2-Imino-1,2-dihydro-5H-dipyrido [1,2-a:2′,3′-d]pyrimidin-5-one | 454 | 32.3% | 124.8% | 104 |
| 13–3 | 2-Imino-1,2-dihydro-5H-dipyrido [1,2-a:2′,3′-d]pyrimidin-5-one | 454 | 54.8% | 129% | 101.4 |
| 17–1 | Thiophene pyrazine peperidine analog | 417 | 30.1% | 82.2% | 91.3 |
a
Candidate compounds validated in rescreening.
b
The mean CXCL8 induced by LPS was 185.3 pg/ml and was normalized as 100%.
c
The mean CXCL8 induced by LPS was 201.1 pg/ml and was normalized as 100%.