Table 2.
CEREP screening of 1 μM BT13.
| Assay (assay type)a | Cat. No. | Percentage of inhibition/potentiation from control | Reference compound | IC50 Ref (M) | Ki Ref (M) |
|---|---|---|---|---|---|
| G PROTEIN-COUPLED RECEPTORS | |||||
| Adenosine receptors | |||||
| A1 (h) (antagonist radioligand) | 0002 | 5 | DPCPX | 8.8E-10 | 5.6E-10 |
| A2B (h) (antagonist radioligand) | 0005 | −14 | NECA | 5.8E-07 | 5.3E-07 |
| Adrenergic receptors | |||||
| Alpha 1 (non-selective; antagonist radioligand) | 0008 | 2 | Prazosin | 4.3E-10 | 1.1E-10 |
| Alpha 2 (non-selective; antagonist radioligand) | 0011 | −6 | Yohimbine | 8.6E-08 | 3.7E-08 |
| Beta 3 (non-selective; antagonist radioligand) | 3963 | −5 | Alprenolol | 1.7E-07 | 1.3E-07 |
| Cannabinoid receptors | |||||
| CB1 (h) (agonist radioligand) | 0036 | 9 | CP 55940 | 1.4E-09 | 1.3E-09 |
| Cholecystokinin receptors | |||||
| CK1 (CCKA) (h) (agonist radioligand) | 0039 | 3 | CCK-8s | 8.3E-11 | 6.2E-11 |
| CCK2 (CCKB) (h) (agonist radioligand) | 0041 | 1 | CCK-8s | 1.1E-10 | 4.3E-11 |
| Dopamine receptors | |||||
| D1 (h) (antagonist radioligand) | 0044 | −17 | SCH 23390 | 2.9E-10 | 1.1E-10 |
| D2L (h) (antagonist radioligand) | 1405 | −3 | Butaclamol | 1.9E-09 | 4.9E-10 |
| GABA receptors | |||||
| GABAB(1b) (h) (antagonist radioligand) | 0885 | −2 | CGP 54626 | 1.2E-09 | 5.9E-10 |
| Histamine receptors | |||||
| H1 (h) (antagonist radioligand) | 0870 | 5 | Pyrilamine | 1.9E-09 | 1.2E-09 |
| H2 (h) (antagonist radioligand) | 1208 | 9 | Cimetidine | 4.6E-07 | 4.5E-07 |
| Neurokinin receptors | |||||
| NK1 (h) (agonist radioligand) | 0100 | −19 | [Sar9,Met(O2)11]-SP | 3.6E-10 | 1.6E-10 |
| NK2 (h) (agonist radioligand) | 0102 | 5 | [Nleu10]-NKA | 2.2E-09 | 1.2E-09 |
| NK3 (h) (antagonist radioligand) | 0104 | 0 | SB 222200 | 1.2E-08 | 6.5E-09 |
| Neurotensin receptors | |||||
| NT (non-selective; agonist radioligand) | 0465 | −6 | Neurotensin | 2.9E-09 | 2.7E-09 |
| Opioid receptors | |||||
| Delta (DOP) (h) (agonist radioligand) | 0114 | 3 | DPDPE | 4.1E-09 | 2.4E-09 |
| Delta (DOP) (agonist effect) | 2568 | −5.2 | DPDPE | 1.9E-09 | |
| Kappa (KOP) (agonist radioligand) | 1971 | 0 | U 50488 | 1.2E-09 | 8.2E-10 |
| Mu (MOP) (h) (agonist radioligand) | 0118 | 1 | DAMGO | 4.1E-10 | 1.7E-10 |
| Vasoactive intestinal peptide receptor | |||||
| PAC1 (PACAP) (h) (agonist radioligand) | 1518 | 14 | PACAP1-38 | 2.2E-10 | 1.9E-10 |
| Serotonin receptors | |||||
| 5-HT1A (h) (agonist radioligand) | 0131 | −8 | 8-OH-DPAT | 1.1E-09 | 6.7E-10 |
| 5-HT1D (agonist radioligand) | 1974 | 1 | Serotonin | 4.4E-09 | 1.5E-09 |
| 5-HT2A (h) (agonist radioligand) | 0471 | −11 | (±)DOI | 2.3E-10 | 1.7E-10 |
| 5-HT2C (h) (antagonist radioligand) | 0137 | 11 | RS 102221 | 3.0E-09 | 9.9E-10 |
| 5-HT2C (h) (agonist radioligand) | 1003 | 6 | (±)DOI | 4.6E-10 | 4.2E-10 |
| Ion channels and transporters | |||||
| Ca2+ channel (L, diltiazem site) (benzothiazepines) (antagonist radioligand) | 0162 | 16 | Diltiazem | 3.3E-08 | 2.6E-08 |
| KATP channel (antagonist radioligand) | 0165 | 8 | Glibenclamide | 1.1E-10 | 3.7E-11 |
| Norepinephrine transporter (h) (antagonist radioligand) | 0355 | −5 | Protriptyline | 6.4E-09 | 4.8E-09 |
| Dopamine transporter (h) (antagonist radioligand) | 0052 | 6 | BTCP | 1.2E-08 | 6.5E-09 |
| 5-HT transporter (h) (antagonist radioligand) | 0439 | 0 | Imipramine | 3.2E-09 | 1.5E-09 |
| Neurotransmitters synthesis and metabolism | |||||
| MAO-A (antagonist radioligand) | 0443 | 5 | Clorgyline | 1.3E-09 | 7.8E-10 |
| COMT (catechol-O-methyl transferase) | 0457 | −2 | Ro 41-0960 | 2.8E-08 | 1.6 |
| Phosphatases | |||||
| Protein Serine/Threonine Phosphatase, PP2A | 3953 | 4 | Calyculin A | 4.9E-10 | 1.4 |
| Protein Tyrosine Phosphatase, PTPRC (CD45) | 3956 | −3 | (NH4)6Mo7O24 | 9.9E-08 | 1.7 |
a
All tests were performed in duplicate and average of two repeats is presented in the table.