Table 1.
Number of ligand-binding sites detected across 24 in-house fragment screening campaigns
| Target | No. sites observed | Target | No. sites observed |
| MetAP2 | 2 | FGFR1 | 1 |
| MELK | 2 | hRAS | 2 |
| PGDS (r)* | 4 | KEAP1 (m)* | 2 |
| Lp-PLA2 | 2 | PKM2 | 6 |
| CDK2 | 3 | ERK2 | 2 |
| Urokinase | 1 | eIF4E | 2 |
| PARP1 (m)* | 1 | XIAP | 1 |
| HCV NS3 | 4 | DNA ligase (s.a)* | 3 |
| iNOS (m)* | 1 | ATAD2 | 2 |
| SolAC | 1† | BACE1 | 1 |
| JAK2 | 1 | HSPA2 | 5 |
| HSP90A | 2 | SETD2 | 2 |
In total, 53 sites were discovered, with an average of 2.2 ± 1.2 sites per target.
*
Mouse (m), rat (r), and Staphylococcus aureus (s.a) proteins were used for these targets.
†
Although we did identify an allosteric bicarbonate site for SolAC (20), we considered this too close to the main active site to be counted as a separate site for this analysis.