ABT-724
| Target | DRD4 |
| Mode of action | Agonist |
| Control | A-769 |
| Orthogonal probe | UCSF924 |
| Recommended cellular usage concentration | 1 - 10000 nM |
| In vivo use | yes |
| Synonyms | A-369724 |
| Donated by | Abbvie |
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, KD) | Surpasses criterion: hDRD4.2: Ki=57.5 nM; hDRD4.4: Ki=63.6 nM; hDRD4.7: Ki= 46.8 nM (radioligand assay) |
| Selectivity within target family: > 30-fold | Surpasses criterion: No activity up to 10 µM for (hDRD2) Closest hit in CEREP panel at 10 µM: HTR1A with Ki=2780 nM (73% inhibition) (not confirmed in MSD) |
| Selectivity outside target family | No activity in CEREP panel of other targets at 10 µM |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion: hDRD4: EC50= 12.4 nM (61% compared to Dopamine; cellular FLIPR assay); EC50= 2.2 nM (HEK293 with DRD4.4 and G protein chimera) |
| Control compound (100 times less potent than the probe) | Surpasses criterion: A-769: inactive up to 10 µM against hDRD4.4 (cellular FLIPR assay) |