Table 1.

Percent inhibition^*1 of specific radioligand binding or enzyme activity by IMQ and TMX-202

Target Compounds	Species	Incubation temperature (°C)	Incubation time (min)	Imiquimod*2	TMX-202*2
CYP450, 1A2*3	human	37	30	66*4	−4
CYP450, 2C19*3	human	37	45	10	1
CYP450, 2C9*3	human	37	45	3	−4
CYP450, 2D6*3	human	37	45	29	0
CYP450, 3A4*3	human	37	30	1	−1
Adenosine A1	human	25	90	50	10
Adenosine A2A	human	25	90	89	−8
Adenosine A3	human	25	60	16	6
Adrenergic a1A	rat	25	60	65	−11
Adrenergic a1B	rat	25	60	40	0
Adrenergic a1D	human	25	60	76	6
Adrenergic a2A	human	25	60	58	3
Adrenergic β1	human	25	120	19	18
Adrenergic β2	human	25	60	18	3
Androgen (Testosterone) AR	rat	4	240	7	55
Bradykinin B1	human	25	60	4	3
Bradykinin B2	human	25	60	−1	−2
Calcium Channel L-Type, Benzothiazepine	rat	4	180	4	1
Calcium Channel L-Type, Dihydropyridine	rat	25	90	−14	10
Calcium Channel N-Type	rat	4	30	2	−12
Cannabinoid CB1	human	37	90	−4	−14
Dopamine D1	human	37	120	66	15
Dopamine D24	human	37	120	14	25
Dopamine D3	human	37	120	18	15
Dopamine D4.2	human	25	120	2	14
Endothelin ETA	human	37	120	8	13
Endothelin ETB	human	25	120	0	−7
Epidermal Growth Factor (EG F)	human	25	60	−1	6
Estrogen ERa	human	25	120	0	7
GABAA, Flunitrazepam, Cent ral	rat	25	120	37	−23
GABAA, Muscimol, Central	rat	4	10	19	−3
GABAB1A	human	25	180	−26	−20
Glucocorticoid	human	25	120	−2	−1
Glutamate, Kainate	rat	4	60	−8	1
Glutamate, NMDA, Agonism	rat	4	20	2	10
Glutamate, NMDA, Glycine	rat	4	30	−6	20
Glutamate, NMDA, Phencyclidine	rat	25	45	4	2
Histamine H1	human	25	180	8	−6
Histamine H2	human	25	120	63	40
Histamine H3	human	25	120	4	−14
Imidazoline I2, Central	rat	25	30	57	−3
Interleukin IL-1	mouse	37	120	5	5
Leukotriene, Cysteinyl CysLT 1	human	25	30	10	10
Melatonin MT1	human	25	180	32	3
Muscarinic M1	human	25	120	16	0
Muscarinic M2	human	25	120	3	0
Muscarinic M3	human	25	120	6	−6
Neuropeptide Y Y1	human	37	60	13	11
Neuropeptide Y Y2	human	37	120	6	4
Nicotinic Acetylcholine	human	25	60	3	9
Nicotinic Acetylcholine a1, Bungarotoxin	human	25	120	7	−3
Opiate 51 (OP1, DOP)	human	25	60	5	5
Opiate K (OP2, KOP)	human	25	60	8	−9
Opiate n (OP3, MOP)	human	25	60	14	42
Phorbol Ester	mouse	25	60	21	−8
Platelet Activating Factor (PA F)	human	25	180	2	33
Potassium Channel [KATP]	human	25	120	−5	8
Potassium Channel hERG	human	25	60	45	−4
Prostanoid EP4	human	25	120	6	7
Purinergic P2x	rabbit	25	30	−7	9
Purinergic P2,	rat	25	60	10	8
Rolipram	rat	4	60	41	21
Serotonin (5-Hydroxytryptam ine) 5-HT1A	human	25	60	19	−7
Serotonin (5-Hydroxytryptam ine) 5-HT2B	human	37	60	45	1
Serotonin (5-Hydroxytryptam ine) 5-HT3	human	37	60	8	3
Sigma al	human	37	240	15	−5
Sodium Channel, Site 2 289593	rat	37	60	72	15
Tachykinin NK1	human	4	90	−8	23
Thyroid Hormone	rat	4	18 hrs	−5	11
Transporter, Dopamine (DAT)	human	4	180	25	64
Transporter, GABA	rat	25	20	2	1
Transporter, Norepinephrine (NET)	human	4	180	30	57
Transporter, Serotonin (5-Hyd roxytryptamine) (SERT)	human	25	60	0	18

^*1Assays were performed in duplicates. The values are average of the duplicate data.

^*210 μM

^*3Activities of cytochrome (CYP 450) isozyme were determined by spectrofluorimetric quantitation of 3-cyano-7-hydroxycoumarin. Other target compounds were studied using the radioligand assays.

^*4Bold letter indicates ≥ 50% inhibition.