Table 3.
Summary of the results before and after ALiBERO optimization of a homology model of the A2A adenosine receptor in complex with the ligand ZM24138. The RMSD of the ligand (with and without the very flexible phenoxy-ring) was performed after receptor superimposition to the PDB ID 3EML. The coverage of contacts was defined as the number of equivalent ligand-receptor atomic contacts between the reference and the target, divided by the contacts in the reference (4 Å cutoff used).44
| Raw Homology Model | |||||
|---|---|---|---|---|---|
| Training Set | AUC | NSQ_AUC | Ligand RMSD (Å) | Contacts Coverage | ICM Docking Score |
| Tr1:1 | 0.63 | 0.29 | 7.5 / 7.4 | 21% | −17.9 (kcal/mol) |
| Tr1:15 | 0.66 | 0.26 | ~ | ~ | ~ |
| ALiBERO | |||||
| Training Set | AUC | NSQ_AUC | Ligand RMSD (Å) | Contacts Coverage | ICM Docking Score |
| Tr1:1 | 0.96 | 0.92 | 6.2 / 4.3 | 47% | −28.7 (kcal/mol) |
| Tr1:15 | 0.92 | 0.78 | 4.6 / 2.8 | 51% | −28.8 (kcal/mol) |