| Index | Ligand Name | Structure | PDB code | Compound Potency nM |
| 1 | 684 | Human dihydrofolate reductase binary complex with PT684 | 3s7a | 1.1 |
| 2 | oag | Structural and Kinetic Data for Antifolate Interactions Against Pneumocystis jirovecii, Pneumocystis carinii and Human Dihydrofolate Reductase and Thier Active Site Mutants | 3oaf | 1.6 |
| 3 | oag | hDHFR-OAG binary complex | 4g95 | 24.4 |
| 4 | mxa | Understanding the Role of Leu22 Variants in Methotrexate Resistance: Comparison of Wild-type and Leu22Arg Variant Mouse and Human Dihydrofolate Reductase Ternary Crystal Complexes with Methotrexate and NADPH | 1u71 | 33 |
| 5 | lii | HUMAN DIHYDROFOLATE REDUCTASE COMPLEXED WITH NADPH AND (Z)-6-(2-[2,5-DIMETHOXYPHENYL]ETHEN-1-YL)-2,4-DIAMINO-5-METHYLPYRIDO[2,3-D]PYRIMIDINE (SRI-9662), A LIPOPHILIC ANTIFOLATE | 1kmv | 112 |
| 6 | top | human dihydrofolate reductase Q35K/N64F double mutant binary complex with trimethoprim | 3s3v | 593 |
| 7 | top | hDHFR double mutant Q35S/N64F Trimethoprim Binary Complex | 3n0h | 617 |