Table 3.
Receptor selectivity profiling for KR36676
| Target | Species | Concentration of KR36676 | % inhibition | Target | Species | Concentration of KR36676 | % inhibition |
|---|---|---|---|---|---|---|---|
| ATPase, Na+/K+, heart | Pig | 10 μM | 0 | Adrenoceptor α1A | Rat | 1 μM | 21 |
| Cholinesterase, acetyl, ACES | Human | 10 μM | 16 | Adrenoceptor α1B | Rat | 1 μM | 24 |
| COX-1 | Human | 10 μM | 20 | Adrenoceptor α2A | Human | 1 μM | 32 |
| COX-2 | Human | 10 μM | 0 | Adrenoceptor α2B | Human | 1 μM | 30 |
| Monoamine oxidase MAO-A | Human | 10 μM | 24 | Adrenoceptor β1 | Human | 1 μM | 5 |
| Monoamine oxidase MAO-B | Human | 10 μM | 1 | Androgen (testosterone) | Human | 1 μM | 2 |
| Peptidase, ACE | Rabbit | 10 μM | 0 | Angiotensin AT1 | Human | 1 μM | 7 |
| Peptidase, CTSG (cathepsin G) | Human | 10 μM | 0 | Calcium channel L-type, phenylalkylamine | Rat | 1 μM | 47 |
| PDE3 | Human | 10 μM | 8 | Cannabinoid CB1 | Human | 1 μM | 16 |
| PDE4 | Human | 10 μM | 21 | Cholecystokinin CCK1 | Human | 1 μM | 18 |
| Protein serine/threonine kinase, PKC, non-selective | Rat | 10 μM | 31 | Dopamine D1 | Human | 1 μM | 9 |
| Protein tyrosine kinase, insulin receptor | Human | 10 μM | 6 | Dopamine D2L | Human | 1 μM | 19 |
| Protein tyrosine kinase, LCK | Human | 10 μM | 0 | Dopamine D2S | Human | 1 μM | 25 |
| Adenosine A1 | Human | 10 μM | 0 | Histamine H1 | Human | 1 μM | 13 |
| Adenosine A2A | Human | 10 μM | 0 | Histamine H2 | Human | 1 μM | 54 |
| Adrenoceptor α1D | Human | 10 μM | 32 | Melanocortin MC4 | Human | 1 μM | 9 |
| Adrenoceptor β2 | Human | 10 μM | 11 | Muscarinic M1 | Human | 1 μM | 2 |
| Bradykinin B2 | Human | 10 μM | 0 | Neuropeptide YY1 | Human | 1 μM | 12 |
| Calcium channel L-type, benzothiazepine | Rat | 10 μM | 39 | Opioid δ1 | Human | 1 μM | 28 |
| Calcium channel L-type, dihydropyridine | Rat | 10 μM | 32 | Opioid κ | Human | 1 μM | 100 |
| Calcium channel N-type | Rat | 10 μM | 9 | Opioid μ | Human | 1 μM | 98 |
| Cannabinoid CB2 | Human | 10 μM | 25 | Progesterone PR-B | Human | 1 μM | 29 |
| Chemokine CCR1 | Human | 10 μM | 0 | 5-HT1A receptor | Human | 1 μM | 49 |
| Chemokine CCR2 | Human | 10 μM | 17 | 5-HT1B receptor | Human | 1 μM | 17 |
| Cholecystokinin CCK2 | Human | 10 μM | 5 | 5-HT2A receptor | Human | 1 μM | 53 |
| Endothelin ETA | Human | 10 μM | 28 | 5-HT2B receptor | Human | 1 μM | 36 |
| Oestrogen ERα | Human | 10 μM | 24 | 5-HT2C receptor | Human | 1 μM | 45 |
| GABAA, chloride channel, TBOB | Rat | 10 μM | 6 | Sodium channel, site 2 | Rat | 1 μM | 82 |
| GABAA, flunitrazepam, central | Rat | 10 μM | 9 | Tachykinin NK1 | Human | 1 μM | 9 |
| GABAA, Ro-15–1788, hippocampus | Rat | 10 μM | 2 | Transporter, dopamine (DAT) | Human | 1 μM | 68 |
| GABAB1A | Human | 10 μM | 32 | Transporter, GABA | Rat | 1 μM | 0 |
| Glucocorticoid | Human | 10 μM | 29 | Transporter, noradrenaline (NET) | Human | 1 μM | 62 |
| Glutamate, AMPA | Rat | 10 μM | 11 | Transporter, 5-HT (SERT) | Human | 1 μM | 39 |
| Glutamate, kainate | Rat | 10 μM | 1 | ||||
| Glutamate, metabotropic, mGlu5 | Human | 10 μM | 3 | ||||
| Glutamate, NMDA, agonism | Rat | 10 μM | 13 | ||||
| Glutamate, NMDA, glycine | Rat | 10 μM | 14 | ||||
| Glutamate, NMDA, phencyclidine | Rat | 10 μM | 5 | ||||
| Glutamate, NMDA, polyamine | Rat | 10 μM | 3 | ||||
| Glycine, strychnine-sensitive | Rat | 10 μM | 38 | ||||
| LT, cysteinyl CysLT1 | Human | 10 μM | 13 | ||||
| Melanocortin MC1 | Human | 10 μM | 41 | ||||
| Muscarinic M2 | Human | 10 μM | 34 | ||||
| Muscarinic M3 | Human | 10 μM | 45 | ||||
| Muscarinic M4 | Human | 10 μM | 36 | ||||
| Nicotinic ACh | Human | 10 μM | 7 | ||||
| Nicotinic ACh α1, bungarotoxin | Human | 10 μM | 17 | ||||
| Platelet activating factor (PAF) | Human | 10 μM | 16 | ||||
| Potassium channel (KATP) | Human | 10 μM | 0 | ||||
| PPARγ | Human | 10 μM | 7 | ||||
| 5-HT3 receptor | Human | 10 μM | 29 | ||||
| Transporter, adenosine | Guinea pig | 10 μM | 11 | ||||
| Vasopressin V1A | Human | 10 μM | 16 |
The final concentration of KR36676 used in the assay was kept at 1 or 10 μM and the results were expressed as % inhibition relative to the control reaction without an antagonist. Results with more than 60% of inhibition are bold typeface.