Target | IC50 or EC50 | ||
---|---|---|---|
Compound A | Compound B | Compound C | |
μM | μM | μM | |
G-protein receptors | |||
Adenosine A2a | >30.0 | >30.0 | >30.0 |
Adrenergic α 1B | >30.0 | >30.0 | >30.0 |
Adrenergic α 1D | ∼4.5 | >30.0 | >30.0 |
Adrenergic α 2A | >30.0 | >30.0 | >30.0 |
Adrenergic α 2C | >30.0 | >30.0 | >30.0 |
Adrenergic β1 | >30.0 | >30.0 | >30.0 |
Adrenergic β2 | >30.0 | >30.0 | >30.0 |
Cannabinoid CB1 | >30.0 | >30.0 | >30.0 |
Dopamine D1 | >30.0 | >30.0 | >30.0 |
Dopamine D2 | >30.0 | >30.0 | >30.0 |
Histamine H1 | >30.0 | >30.0 | >30.0 |
Histamine H2 | >30.0 | >30.0 | >30.0 |
Muscarinic M2 | >30.0 | >30.0 | >30.0 |
Opioid kappa | >30.0 | >30.0 | >30.0 |
Opioid mu | >30.0 | >30.0 | >30.0 |
Serotonin 5HT1B | >30.0 | >30.0 | >30.0 |
Serotonin 5HT2A agonist | >10.0 | >10.0 | N.D. |
Serotonin 5HT2B agonist | >5.0 | >10.0 | N.D. |
Serotonin 5HT4 | >30.0 | >30.0 | >30.0 |
Transporters | |||
Dopamine | >30.0 | >30.0 | >30.0 |
Norepinephrine | >30.0 | >30.0 | >30.0 |
Serotonin | >30.0 | >30.0 | >30.0 |
Nuclear hormone receptors | |||
Androgen | >150.0 | 16.1 | >150.0 |
Estrogen α | >150.0 | ∼63.9 | ∼114.1 |
Glucocorticoid | >150.0 | >150.0 | >150.0 |
Progesterone | >150.0 | 59.9 | >150.0 |
Ion channel receptors | |||
Calcium channel L-type (Cav1.2) antagonist | >25.0 | >25.0 | >25.0 |
Calcium channel T-type (Cav3.2) activator | >25.0 | >25.0 | >25.0 |
Cardiac sodium channel (hNAV1.5) antagonist | 11.5 | >30.0 | >30.0 |
GABA-A (α1β2γ2) antagonist | >30.0 | >30.0 | >30.0 |
GABA-A (α1β2γ2) potentiator | 1.7 | >30.0 | >30.0 |
GABA-A (α5β2γ2) antagonist | >30.0 | >30.0 | >30.0 |
Nicotinic acetylcholine α1 antagonist | >30.0 | >30.0 | >30.0 |
Nicotinic acetylcholine α4β2 agonist | >30.0 | >30.0 | >30.0 |
Nicotinic acetylcholine α7 antagonist | >30.0 | >30.0 | >30.0 |
NMDA glutamate NR1/2A agonist | >25.0 | N.D. | >30.0 |
NMDA glutamate NR1/2A antagonist | >30.0 | >30.0 | >30.0 |
NMDA glutamate NR1/2B agonist | >25.0 | >25 | >30.0 |
Enzymes | |||
Acetylcholinesterase | >60.0 | >60 | >30.0 |
Monoamine oxidase A | 14.3 | >30.0 | >30.0 |
Monoamine oxidase B | >30.0 | >30.0 | >30.0 |
Phosphodiesterase 3 | >30.0 | >30.0 | >50.0 |
Phosphodiesterase 4 | 12.6 | >30.0 | >50.0 |
N.D., not determined.