Table 1.
Summary of inhibition values in binding and hedgehog functional assays for confirmed hits from chemical library screen of ShhN/heparin binding.
| Cpd No. | Sample ID | ShhN/heparin Avg. IC50 (μM) a | Inhibition of ShhN-induced AP IC50 (μM) | Inhibition of SAG-induced AP | Inhibition of ShhN-induced GLI1 and Ptch1 mRNA | Inhibition of SAG-induced GLI1 and Ptchl mRNA |
|---|---|---|---|---|---|---|
| 1 | ASN03067791 | 38 | 1.6 | Yes | ||
| 4 | BAS | 53 | 42 | No | Yes | No |
| 6 | BAS | 49 | No inhibition | |||
| 8 | BAS | 48 | No inhibition | |||
| 10 | BAS | 57 | 23 | Yes | ||
| 11 | BAS | 46 | No inhibition | |||
| 20 | BAS | 55 | No inhibition | |||
| 21 | BAS | 45 | 25 | Weak | Yes | Yes |
| 24 | BAS | 33 | 26 | No | Yes | No |
| 26 | BAS | 44 | 21 | Yes | ||
| Robotnikinin | No inhibition | 6.4 | No | Yes | No |
For IC50 determinations, serial dilutions of compounds were tested starting at a high concentration of 80 μM. Average IC50 values from cherry-picked master plates and repurchased compounds.