Table 1.
Pharmacological profile of SM-345431 (part 1)
| Enzymes | IC50 (μm) |
|---|---|
| Semaphorin |
0.1-0.2 |
| Matrix Metalloproteinase-1 (MMP-1) |
>10 |
| Matrix Metalloproteinase-7 (MMP-7) |
10 |
| Matrix Metalloproteinase-2 (MMP-2) |
>10 |
| Matrix Metalloproteinase-3 (MMP-3) |
>10 |
| Matrix Metalloproteinase-9 (MMP-9) |
>10 |
| Phospholipase PLA2-1 |
>10 |
| Phospholipase PLC |
>10 |
| Caspase 1 |
>10 |
| Caspase 3 |
>10 |
| Caspase 6 |
>10 |
| Caspase 7 |
>10 |
| Caspase 8 |
>10 |
| Protein Tyrosine Phosphatase, CD45 |
>10 |
| Protein Tyrosine Phosphatase, PTP1B |
>10 |
| Protein Tyrosine Phosphatase, PTP1C |
>10 |
| Protein Tyrosine Phosphatase, T-Cell |
>10 |
| Sphingomyelinase, Neutral (N-SMase) |
>10 |
| Chemokine CCR1 |
>10 |
| Chemokine CCR2B |
>10 |
| Chemokine CCR4 |
>10 |
| Chemokine CCR5 |
>10 |
| Chemokine CXCR2 (IL-8B) |
>10 |
| Glucocorticoid |
>10 |
| Interleukin IL-1 |
>10 |
| Interleukin IL-2 |
>10 |
| Interleukin IL-6 |
>10 |
| Tumor Necrosis Factor (TNF), Non-selective |
>10 |
| Adhesion, fibronectin-mediated |
>10 |
| Adhesion, ICAM-1-Mediated |
>10 |
| Adhesion, VCAM-1-Mediated |
>10 |
| Cell proliferation, B-Cell+LPS |
>10 |
| Cell proliferation, T-Cell+Con A |
>10 |
| Mediator release, IL-1beta |
>10 |
| Mediator release, IFN-gamma |
>10 |
| Mediator release, IL-10 |
>10 |
| Mediator release, IL-2 |
>10 |
| Mediator release, IL-4 |
>10 |
| Mediator release, IL-5 |
>10 |
| Mediator release, IL-6 |
>10 |
| Mediator release, TNF-alfa, PBML |
>10 |
| Transcription response, NF-AT |
>10 |
| Transcription response, NF-kB | >10 |
Summary of the IC50 values for binding assays of various receptors and ion channels, and IC50 values for the inhibition of various enzymes. The IC50 value for semaphorin3A inhibition was extremely low compared to that of the other factors.