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BIBO3304

2D structure
Target NPY1R 
Mode of action Antagonist
Control BIBO3457
Recommended cellular usage concentration 100 nM
In vivo use Yes
Donated by Boehringer Ingelheim


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) no data
Selectivity within target family: > 30-fold Human NPY2R: IC50 > 10 µM (SMS-KAN cells), IC50 > 1 µM (BHK cells), Rat hippocampus NPY2R: IC50 > 10 µM; Human NPY4R: IC50 = 12.3 ± 5 µM (CHO cells); Rat NPY4R: IC50 > 10 µM (CHO cells); Human NPY5R: IC50 > 10 µM (HEK293 cells); Rat NPY5R: IC50 > 21 ± 4.5 µM (CHO cells)
Selectivity outside target family Eurofins SafteyScreen (146 targets) at 10 µM [% ctrl]: Closest off-targets are AVPR1A (29), OPRK1 (30), DRD2 (D2S) (40)
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Surpasses criterion: Human NPY1R:IC50 = 0.69 ± 0.16 nM (radioligand binding assay, NPY1R expressed in BHK cells); IC50 = 0.38 ± 0.06 nM (SK-N-MC cells, neuroblastoma cell line ), Rat NPY1R: IC50 = 0.72 ± 0.42 nM (HEK293 cells)
Control compound (100 times less potent than the probe) BIBO3457 (enantiomer): Human NPY1R: IC50 > 10 µM (human BHK cells), IC50 = 1300 ± 70 nM (SK-N-MC cells), Rat NPY1R: IC50 > 1 µM (HEK293 cells); Human NPY2R: IC50 > 10 µM (SMS-KAN cells), IC50 > 1 µM (BHK cells); Human NPY4R: IC50 = 24 ± 6.5 µM (CHO cells); Rat NPY4R: IC50 > 10 µM (CHO cells); Human NPY5R: IC50 = 28 ± 4µM (HEK293 cells); Rat NPY5R: IC50 = 23 ± 2 µM (CHO cells)
BIBO3422 (close analog): Eurofins SafteyScreen (44 targets) at 10 µM [% ctrl]: Closest off-targets are OPRM1 (4), SLC6A3 (17), HTR1B (19), CCKAR (43), KCNH2 (46), OPRK1 (46)