Inhibition of radioligand binding by BIX 02565 (compound 1) at 68 protein targets tested at a standard concentration of 10 μM (MDS Pharma Services, Saint Laurent, QC, Canada)
At five targets (adrenergic α1A, α1B, α2A, β2, and imidazoline I2) with inhibition values between 86 and 106%, IC50 values (micromoles) were calculated.
| Target | % [I], (IC50) | Target | % [I] | Target | % [I], (IC50) | Target | % [I] |
|---|---|---|---|---|---|---|---|
| Adenosine A1 | −2 | Dopamine D3 | 7 | Histamine H3 | 11 | Potassium Ch. (KATP) | 2 |
| Adenosine A2A | 5 | Dopamine D4.2 | 15 | Imidazoline I2 | 86 (0.097) | Potassium Ch. (hERG) | 10 |
| Adenosine A3 | −14 | Endothelin ETA | 0 | Interleukin IL-1 | −5 | Prostanoid EP4 | 0 |
| Adrenergic α1A | 90 (0.914) | Endothelin ETB | 10 | Leukotriene (CysLT1) | 5 | Purinergic P2X | 5 |
| Adrenergic α1B | 106 (0.052) | EGF | 16 | Melatonin MT1 | 3 | Purinergic P2Y | 16 |
| Adrenergic α1D | 93 | Estrogen Erα | 2 | Muscarinic M1 | 11 | Rolipram | −2 |
| Adrenergic α2A | 86 (1.42) | GPCR (GPR103) | 26 | Muscarinic M2 | 14 | Serotonin (5-HT1A) | 36 |
| Adrenergic β1 | 6 | GABAA (flunitrazepam) | 9 | Muscarinic M3 | 2 | Serotonin (5-HT3) | 5 |
| Adrenergic β2 | 88 (1.82) | GABAA (muscimol) | 4 | Neuropeptide Y Y1 | 10 | Sigma σ1 | 9 |
| Androgen AR | 5 | GABAB1A | −14 | Neuropeptide Y Y2 | −7 | Sigma σ2 | 4 |
| Bradykinin B1 | 8 | Glucocorticoid | 5 | Nicotinic ACh | 20 | Sodium Ch., Site 2 | 21 |
| Bradykinin B2 | 17 | Glutamate (kainate) | −10 | Nicotinic ACh α1 (BNGTX) | 24 | Tachykinin NK1 | 4 |
| Ca2+ Ch. (L-Type; BTP) | 15 | Glutamate (NMDA, Ag) | 24 | Opiate ð | 6 | Thyroid Hormone | 4 |
| Ca2+ Ch. (L-Type; DHP) | 13 | Glutamate (NMDA, Glycine) | 12 | Opiate κ | 12 | Transporter, Dopamine | 1 |
| Ca2+ Ch. (N-Type) | 2 | Glutamate (NMDA, PCP) | −2 | Opiate μ | 13 | Transporter, GABA | −8 |
| Dopamine D1 | 21 | Histamine H1 | −5 | Phorbol ester | −5 | Transporter, NE | 3 |
| Dopamine D2s | 6 | Histamine H2 | 15 | Platelet-activating factor | −8 | Transporter, 5-HT | −4 |
EGF, epidermal growth factor; GPCR, G protein-coupled receptor; NMDA, N-methyl-d-aspartate; ACh, acetylcholine; DHP, dihydropyridine; BTP, benzothiazepine; BNGTX, bungarotoxin; NE, norepinephrine; PCP, phencyclidine; hERG, human Ether-à-go-go-related gene.