| Index | Ligand Name | Structure | PDB code | Compound Potency nM |
| 1 | 8pv | Design, Synthesis, and Evaluation of the First Selective and Potent G-protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure | 5uvc | 6.1 |
| 2 | afm | Human GRK2 in complex with Gbetagamma subunits and CCG258748 | 5wg3 | 8 |
| 3 | qrw | Design, Synthesis, and Evaluation of the First Selective and Potent G-protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure | 5uuu | 18 |
| 4 | qrx | Bovine GRK2 in complex with Gbetagamma subunits and a selective kinase inhibitor (CMPD103A) | 3pvw | 54 |
| 5 | afv | Human GRK2 in complex with Gbetagamma subunits and CCG257284 | 5wg4 | 100 |
| 6 | f0s | Bovine GRK2 in complex with Gbetagamma subunits and CCG224406 | 5he2 | 130 |
| 7 | 453 | Bovine GRK2 in complex with Gbetagamma subunits and CCG215022 | 5he0 | 150 |
| 8 | kzq | G protein-coupled receptor kinase 2 in complex with GSK180736A | 4pnk | 250 |
| 9 | ff1 | Bovine GRK2 in complex with Gbetagamma subunits and CCG224411 | 5he3 | 280 |
| 10 | qrw | Bovine GRK2 in complex with Gbetagamma subunits and a selective kinase inhibitor (CMPD101) | 3pvu | 290 |
| 11 | 8dj | Human GRK2 in complex with human G-beta-gamma subunits and CCG211998 (14ak) | 5ukk | 610 |
| 12 | six | Human GRK2 in complex with Gbetagamma subunits and CCG222886 (14bd) | 5ukl | 630 |
| 13 | 29x | Crystal structure of G protein-coupled receptor kinase 2 in complex with a a rationally designed paroxetine derivative | 4mk0 | 6300 |