Receptor Binding
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actively maintained.
Sorted by drug/model/receptor
| Drug |
Class |
Model |
Receptor |
IC50 (µM) |
Relative Potency (IKr/X) |
Ref |
Comment |
| alfuzosin |
alpha1-blocker |
HERG/CHO |
IKr |
83.3 |
--- |
92 |
|
| almokalant |
antiarrhythmic |
rabbit VM |
IKr |
0.005 |
--- |
38 |
|
| amiodarone |
antiarrhythmic |
rat VM |
ICaL |
5.8 |
|
93 |
|
| amiodarone |
antiarrhythmic |
rabbit VM |
IK1 |
50 |
|
29 |
|
| amiodarone |
antiarrhythmic |
guinea-pig AM |
IKAch |
2 |
|
24 |
|
| amiodarone |
antiarrhythmic |
guinea-pig VM |
IKNa |
1 |
|
23 |
|
| amiodarone |
antiarrhythmic |
AT-1 |
IKr |
0.7 |
--- |
129 |
|
| amiodarone |
antiarrhythmic |
AT-1 |
IKr |
1 |
--- |
130 |
|
| amiodarone |
antiarrhythmic |
HERG/L |
IKr |
1 |
--- |
130 |
|
| amiodarone |
antiarrhythmic |
rabbit VM |
IKr |
2.8 |
--- |
64 |
|
| amiodarone |
antiarrhythmic |
rabbit VM |
IKr |
10 |
--- |
21 |
|
| amiodarone |
antiarrhythmic |
HERG/XO |
IKr |
10 |
--- |
73 |
|
| amiodarone |
antiarrhythmic |
rat VM |
Ito |
4.9 |
|
22 |
|
| amiodarone |
antiarrhythmic |
rabbit VM |
Ito |
>10 |
|
21 |
|
| amitriptyline |
antidepressant |
HERG/CHO |
IKr |
>3 |
--- |
112 |
|
| amitriptyline |
antidepressant |
HERG/CHO |
IKr |
10 |
--- |
114 |
|
| amitriptyline |
antidepressant |
rat neuron |
IKr |
10 |
--- |
125 |
|
| amlodipine |
dihydropyridine |
AT-1 |
IKr |
1 |
--- |
130 |
|
| amlodipine |
dihydropyridine |
AT-1 |
IKr |
3 |
|
129 |
|
| aprinidine |
antiarrhythmic |
HERG/COS |
IKr |
0.23 |
--- |
59 |
|
| aprinidine |
antiarrhythmic |
COS |
IKs |
>10 |
|
59 |
|
| astemizole |
antihistamine |
GP cerebellum |
H1 |
0.052 |
58 |
27 |
|
| astemizole |
antihistamine |
GP LM |
H1 |
0.079 |
88 |
74 |
|
| astemizole |
antihistamine |
GP LM |
H1 |
0.3 |
333 |
63 |
|
| astemizole |
antihistamine |
guinea-pig VM |
IK1 |
>10 |
|
31 |
|
| astemizole |
antihistamine |
HERG/HEK |
IKr |
0.0009 |
--- |
138 |
|
| astemizole |
antihistamine |
guinea-pig VM |
IKr |
0.0015 |
--- |
101 |
|
| astemizole |
antihistamine |
HERG/HEK |
IKr |
0.022 |
--- |
46 |
at 37°C |
| astemizole |
antihistamine |
HERG/XO |
IKr |
0.048 |
--- |
110 |
|
| astemizole |
antihistamine |
HERG/XO |
IKr |
0.069 |
--- |
40 |
|
| astemizole |
antihistamine |
HERG/XO |
IKr |
0.33 |
--- |
111 |
|
| astemizole |
antihistamine |
|
IKs |
>10 |
|
101 |
10uM = IC0.3 |
| astemizole |
antihistamine |
XO |
IKs |
>60 |
|
110 |
|
| astemizole |
antihistamine |
XO |
IKv1.1 |
>60 |
|
110 |
|
| astemizole |
antihistamine |
XO |
IRK1 |
>60 |
|
110 |
|
| astemizole |
antihistamine |
guinea-pig VM |
Ito |
>10 |
|
31 |
|
| astemizole |
antihistamine |
|
Ito |
>10 |
|
30 |
10uM = IC23 |
| desmethylastemizole |
antihistamine |
GP LM |
H1 |
0.2 |
10 |
63 |
|
| desmethylastemizole |
antihistamine |
HERG/HEK |
IKr |
0.001 |
--- |
138 |
|
| norastemizole |
antihistamine |
HERG/HEK |
IKr |
0.028 |
--- |
138 |
|
| atropine |
anticholinergic |
|
IKr |
0.558 |
--- |
76 |
|
| azimilide |
antiarrhythmic |
GP VM |
ICaL |
>10 |
|
54 |
|
| azimilide |
antiarrhythmic |
GP VM |
IK1 |
>10 |
|
54 |
|
| azimilide |
antiarrhythmic |
GP VM |
IKr |
0.4 |
--- |
54 |
|
| azimilide |
antiarrhythmic |
HERG/XO |
IKr |
1.4 |
--- |
34 |
|
| azimilide |
antiarrhythmic |
GP VM |
IKs |
3 |
|
54 |
|
| bepridil |
antianginal |
guinea-pig VM |
ICaL |
0.5 |
|
134 |
|
| bepridil |
antianginal |
guinea-pig AM |
ICaL |
1.55 |
|
57 |
|
| bepridil |
antianginal |
sheep PF |
IK1 |
>1.8 |
|
28 |
|
| bepridil |
antianginal |
HERG/COS |
IKr |
0.55 |
--- |
42 |
|
| bepridil |
antianginal |
IKs/COS |
IKs |
10 |
|
42 |
|
| bepridil |
antianginal |
guinea-pig AM |
INa |
4.43 |
|
57 |
|
| bepridil |
antianginal |
guinea-pig VM |
INa |
30 |
|
134 |
|
| bepridil |
antianginal |
sheep PF |
Ito |
<30 |
|
28 |
|
| buprenorphine |
opiate |
HERG/HEK |
IKr |
7.5 |
--- |
71 |
|
| captopril |
ACE inhibitor |
AT-1 |
IKr |
10 |
--- |
129 |
|
| carvedilol |
beta-blocker |
HERG/XO |
IKr |
10.42 |
--- |
69 |
|
| cetirizine |
antihistamine |
GP cerebellum |
H1 |
0.47 |
0.004 |
27 |
|
| cetirizine |
antihistamine |
rabbit VM |
IK1 |
>1000 |
|
37 |
|
| cetirizine |
antihistamine |
HERG/XO |
IKr |
>30 |
--- |
111 |
|
| cetirizine |
antihistamine |
rabbit VM |
IKr |
108 |
--- |
37 |
|
| cetirizine |
antihistamine |
rabbit VM |
IKs |
>1000 |
|
37 |
1mM = IC44 |
| chlorpheniramine |
antihistamine |
GP LM |
H1 |
0.002 |
0.001 |
74 |
|
| chlorpheniramine |
antihistamine |
|
IK1 |
>10 |
|
101 |
10uM=IC0.6 |
| chlorpheniramine |
antihistamine |
|
IKr |
1.1 |
--- |
101 |
|
| chlorpheniramine |
antihistamine |
GP VM |
IKr |
1.6 |
--- |
102 |
|
| chlorpheniramine |
antihistamine |
HERG/XO |
IKr |
21 |
--- |
110 |
|
| chlorpheniramine |
antihistamine |
|
IKs |
>10 |
|
101 |
10uM = IC9.7 |
| chlorpromazine |
antipsychotic |
HERG/CHO |
IKr |
1.47 |
--- |
114 |
|
| ciprofloxacin |
antibiotic/quinolone |
HERG/CHO |
IKr |
>100 |
--- |
33 |
-40 mV |
| ciprofloxacin |
antibiotic/quinolone |
HERG/CHO |
IKr |
966 |
--- |
66 |
|
| cisapride |
prokinetic |
various |
5HT4 |
0.023-0.031 |
0.5 |
89 |
|
| cisapride |
prokinetic |
HERG/HEK |
IKr |
0.0065 |
--- |
91 |
different lab |
| cisapride |
prokinetic |
rabbit VM |
IKr |
0.009 |
--- |
36 |
|
| cisapride |
prokinetic |
guinea-pig VM |
IKr |
0.015 |
--- |
48 |
|
| cisapride |
prokinetic |
HERG/CHO |
IKr |
0.016 |
--- |
123 |
at 20-22°C |
| cisapride |
prokinetic |
HERG/CHO |
IKr |
0.024 |
--- |
123 |
at 37°C |
| cisapride |
prokinetic |
HERG/HEK |
IKr |
0.044 |
--- |
95 |
|
| cisapride |
prokinetic |
HERG |
IKr |
0.044 |
--- |
76 |
at 32-37°C |
| cisapride |
prokinetic |
|
IKs |
3.39 |
|
76 |
at 32-37°C |
| cisapride |
prokinetic |
guinea-pig VM |
IKs |
>10 |
|
48 |
|
| cisapride |
prokinetic |
|
IKv1.5 |
21.2 |
|
76 |
at 32-37°C |
| cisapride |
prokinetic |
|
Ito |
9.33 |
|
76 |
at 32-37°C |
| clarithromycin |
antibiotic/macrolide |
HERG/CHO |
IKr |
20 |
--- |
2 |
+MiRP1 |
| clarithromycin |
antibiotic/macrolide |
HERG/CHO |
IKr |
59 |
--- |
2 |
WT |
| clobutinol |
antitussive |
|
IKr |
2.9 |
--- |
26 |
|
| clofilium |
antiarrhythmic |
AT-1 |
IKr |
1.25 |
--- |
32 |
|
| clotrimazole |
antifungal |
GP VM |
ICaL |
<25 |
|
113 |
5=IC16, 25 = IC59 |
| clozapine |
antipsychotic |
human AM |
IK1 |
>100 |
|
46 |
|
| clozapine |
antipsychotic |
HERG/HEK |
IKr |
0.191 |
--- |
46 |
at 37°C |
| clozapine |
antipsychotic |
human AM |
INa |
29.0 |
|
46 |
|
| clozapine |
antipsychotic |
human AM |
Isus |
>100 |
|
46 |
|
| clozapine |
antipsychotic |
human AM |
Ito |
50-100 |
|
46 |
|
| cocaine |
local anesthetic |
HERG/HEK |
IKr |
7.2 |
--- |
135 |
|
| codeine |
opiate |
HERG/HEK |
IKr |
> 300 |
--- |
71 |
|
| cromakalim |
chromanol deriv |
GP VM |
IKr |
>20 |
--- |
58 |
|
| cromakalim |
chromanol deriv |
IKs/COS |
IKs |
>10 |
|
85 |
|
| cromakalim |
chromanol deriv |
GP VM |
IKs |
>20 |
|
58 |
|
| cyproheptadine |
antihistamine |
GP cerebellum |
H1 |
0.003 |
|
27 |
|
| diltiazem |
calcium antagonist |
HERG/COS |
IKr |
>10 |
--- |
42 |
|
| diltiazem |
calcium antagonist |
HERG/HEK |
IKr |
17.3 |
--- |
136 |
|
| diltiazem |
calcium antagonist |
IKs/COS |
IKs |
>10 |
|
42 |
|
| diphenhydramine |
antihistamine |
GP LM |
H1 |
0.042 |
0.038 |
74 |
|
| diphenhydramine |
antihistamine |
GP VM |
IKr |
0.03 |
--- |
72 |
|
| diphenhydramine |
antihistamine |
GP VM |
IKr |
1.1 |
--- |
102 |
|
| diphenhydramine |
antihistamine |
HERG/XO |
IKr |
27 |
--- |
110 |
|
| disopyramide |
antiarrhythmic |
rabbit VM |
IKr |
1.8 |
--- |
120 |
|
| disopyramide |
antiarrhythmic |
AT-1 |
IKr |
58 |
--- |
98 |
|
| disopyramide |
antiarrhythmic |
AT-1 |
IKr |
60-100 |
--- |
130 |
|
| disopyramide |
antiarrhythmic |
HERG/L |
IKr |
92 |
|
129 |
|
| disopyramide |
antiarrhythmic |
|
INa |
28 |
|
132 |
|
| disopyramide |
antiarrhythmic |
rabbit VM |
Ito |
14 |
|
120 |
|
| dofetilide |
antiarrhythmic |
GP VM |
IK1 |
>1 |
|
61 |
|
| dofetilide |
antiarrhythmic |
rabbit VM |
IKr |
0.0039 |
--- |
39 |
|
| dofetilide |
antiarrhythmic |
HERG/HEK |
IKr |
0.0095 |
--- |
94 |
|
| dofetilide |
antiarrhythmic |
HERG/L |
IKr |
0.0095 |
--- |
94 |
|
| dofetilide |
antiarrhythmic |
AT-1 |
IKr |
0.011 |
--- |
129 |
|
| dofetilide |
antiarrhythmic |
AT-1 |
IKr |
0.012 |
--- |
131 |
|
| dofetilide |
antiarrhythmic |
HERG/HEK |
IKr |
0.012 |
--- |
105 |
|
| dofetilide |
antiarrhythmic |
HERG-HEK |
IKr |
0.015 |
--- |
95 |
|
| dofetilide |
antiarrhythmic |
HERG/L |
IKr |
0.015 |
--- |
129 |
|
| dofetilide |
antiarrhythmic |
HERG |
IKr |
0.015 |
--- |
76 |
at 22°C |
| dofetilide |
antiarrhythmic |
GP VM |
IKr |
0.032 |
--- |
61 |
|
| dofetilide |
antiarrhythmic |
HL-1 |
IKr |
0.047 |
--- |
43 |
|
| dofetilide |
antiarrhythmic |
mouse heart |
IKr |
0.054 |
--- |
81 |
|
| dofetilide |
antiarrhythmic |
HERG/XO |
IKr |
0.125 |
--- |
80 |
|
| dofetilide |
antiarrhythmic |
GP VM |
IKs |
>100 |
|
61 |
|
| dofetilide |
antiarrhythmic |
HEK-293 |
IKv1.5 |
>10 |
|
94 |
|
| doxazosin |
alpha1-blocker |
HERG/CHO |
IKr |
2.5 |
--- |
92 |
|
| E-4031 |
antiarrhythmic |
HERG/HEK |
IKr |
0.0077 |
--- |
137 |
|
| E-4031 |
antiarrhythmic |
ferret heart |
IKr |
0.0103 |
--- |
83 |
|
| E-4031 |
antiarrhythmic |
HERG/XO |
IKr |
0.38 |
--- |
2 |
+MiRP1 |
| E-4031 |
antiarrhythmic |
GP VM |
IKr |
0.397 |
--- |
103 |
|
| E-4031 |
antiarrhythmic |
GP VM |
IKr |
<5 |
--- |
99 |
|
| E-4031 |
antiarrhythmic |
HERG/XO |
IKr |
0.588 |
--- |
116 |
|
| E-4031 |
antiarrhythmic |
HERG/XO |
IKr |
1.25 |
--- |
2 |
WT |
| E-4031 |
antiarrhythmic |
HERG/XO |
IKr |
1.4 |
--- |
34 |
different lab |
| ebastine |
antihistamine |
GP LM |
H1 |
0.27 |
1.9 |
74 |
|
| ebastine |
antihistamine |
rat VM |
IK1 |
>3 |
|
75 |
|
| ebastine |
antihistamine |
guinea-pig VM |
IKr |
0.14 |
--- |
75 |
|
| ebastine |
antihistamine |
guinea-pig VM |
IKs |
2 |
|
75 |
|
| ebastine |
antihistamine |
|
IKv1.5 |
>1 |
|
20 |
1uM = IC6.5 |
| ebastine |
antihistamine |
rat VM |
Ito |
>3 |
|
75 |
|
| EDDP |
opiate |
HERG/HEK |
IKr |
>50 |
--- |
71 |
methadone metabolite |
| encainide |
antiarrhythmic |
feline VM |
IKr |
6 |
--- |
55 |
|
| epinastine |
antihistamine |
HERG/XO |
IKr |
>100 |
--- |
40 |
|
| erythromycin |
antibiotic/macrolide |
AT-1 |
IKr |
54.6 |
--- |
127 |
|
| erythromycin |
antibiotic/macrolide |
GP VM |
IKr |
>100 |
--- |
47 |
|
| erythromycin |
antibiotic/macrolide |
|
IKr |
387 |
--- |
76 |
at 32-37°C |
| erythromycin |
antibiotic/macrolide |
|
Ito |
606 |
|
76 |
at 32-37°C |
| erythromycin |
antibiotic/macrolide |
S. pneumoniae |
MIC |
1.36 |
<0.014 |
68 |
|
| fentanyl |
opiate |
HERG/HEK |
IKr |
1.8 |
--- |
71 |
|
| fexofenadine |
antihistamine |
GP LM |
H1 |
0.26 |
0.024 |
74 |
|
| fexofenadine |
antihistamine |
feline VM |
IKr |
>5 |
--- |
126 |
|
| fexofenadine |
antihistamine |
|
IKr |
>10 |
|
96 |
|
| fexofenadine |
antihistamine |
HERG |
IKr |
13.1 |
--- |
76 |
at 32-37°C |
| fexofenadine |
antihistamine |
HERG/HEK |
IKr |
21.57 |
--- |
46 |
at 37°C |
| fexofenadine |
antihistamine |
HERG/XO |
IKr |
>500 |
--- |
100 |
|
| fexofenadine |
antihistamine |
|
IKs |
20.4 |
|
76 |
at 32-37°C |
| fexofenadine |
antihistamine |
|
IKv1.5 |
>50 |
|
128 |
|
| fexofenadine |
antihistamine |
feline VM |
IKv1.5 |
214 |
|
96 |
|
| fexofenadine |
antihistamine |
|
IKv1.5 |
389 |
|
76 |
at 32-37°C |
| fexofenadine |
antihistamine |
XO |
IKv1.5 |
>500 |
|
100 |
|
| fexofenadine |
antihistamine |
|
Ito |
112 |
|
76 |
at 32-37°C |
| flecainide |
antiarrhythmic |
feline VM |
IKr |
2.2 |
--- |
55 |
|
| gatifloxacin |
antibiotic/quinolone |
AT-1 |
IKr |
26.5 |
--- |
4 |
|
| gatifloxacin |
antibiotic/quinolone |
HERG/CHO |
IKr |
130 |
--- |
66 |
|
| glibenclamide |
sulfonylurea |
neuroblastoma |
IKr |
74.8 |
--- |
99 |
|
| glibenclamide |
sulfonylurea |
GP VM |
IKr |
<100 |
--- |
99 |
|
| grepafloxacin |
antibiotic/quinolone |
AT-1 |
IKr |
27.2 |
--- |
4 |
|
| grepafloxacin |
antibiotic/quinolone |
HERG/CHO |
IKr |
27.5 |
--- |
33 |
-40 mV |
| grepafloxacin |
antibiotic/quinolone |
HERG/CHO |
IKr |
50 |
--- |
66 |
|
| haloperidol |
antipsychotic |
human AM |
IK1 |
>100 |
|
46 |
|
| haloperidol |
antipsychotic |
HERG/HEK |
IKr |
0.0281 |
--- |
46 |
at 37°C |
| haloperidol |
antipsychotic |
HERG/XO |
IKr |
1 |
--- |
108 |
|
| haloperidol |
antipsychotic |
human AM |
INa |
14.4 |
|
46 |
|
| haloperidol |
antipsychotic |
human AM |
Isus |
10-100 |
|
46 |
|
| haloperidol |
antipsychotic |
human AM |
Ito |
10-100 |
|
46 |
|
| hesperetin |
flavonoid |
HERG/XO |
IKr |
288.8 |
--- |
139 |
|
| ibutilide |
antiarrhythmic |
HERG/L |
IKr |
0.015 |
--- |
129 |
|
| ibutilide |
antiarrhythmic |
AT-1 |
IKr |
0.02 |
--- |
131 |
|
| imipramine |
antidepressant |
HERG/CHO |
IKr |
3.4 |
--- |
112 |
|
| indapamide |
diuretic |
GP VM |
IKs |
196 |
|
117 |
|
| ketanserin |
serotonin antagonist |
guinea-pig VM |
IKr |
>32 |
--- |
79 |
|
| ketanserin |
serotonin antagonist |
rabbit VM |
Ito |
2.25 |
|
78 |
|
| ketoconazole |
antifungal |
feline VM |
IKr |
2.5 |
--- |
41 |
|
| ketoconazole |
antifungal |
HERG/XO |
IKr |
49 |
--- |
51 |
|
| ketoconazole |
antifungal |
XO |
IKv1.5 |
107 |
|
51 |
|
| ketoconazole |
antifungal |
feline VM |
Ito |
10 |
|
41 |
|
| LAAM |
opiate |
HERG/HEK |
IKr |
2.2 |
--- |
71 |
|
| levofloxacin |
antibiotic/quinolone |
HERG/CHO |
IKr |
915 |
--- |
66 |
|
| lopinavir |
antiviral |
HERG/HEK |
IKr |
8.6 |
--- |
5 |
|
| loratidine |
antihistamine |
GP cerebellum |
H1 |
1 |
0.3 |
27 |
|
| loratidine |
antihistamine |
HERG/HEK |
IK1 |
>1 |
|
45 |
|
| loratidine |
antihistamine |
rat VM |
IK1 |
>10 |
|
50 |
|
| loratidine |
antihistamine |
HERG/HEK |
IKr |
0.173 |
--- |
45 |
|
| loratidine |
antihistamine |
|
IKr |
>1 |
--- |
50 |
1uM = IC5 |
| loratidine |
antihistamine |
HERG/XO |
IKr |
100 |
--- |
111 |
|
| loratidine |
antihistamine |
|
IKs |
<10 |
|
50 |
10uM = IC58 |
| loratidine |
antihistamine |
guinea-pig VM |
IKs |
<25 |
|
50 |
|
| loratidine |
antihistamine |
HEK 293 |
IKv1.5 |
0.8 |
|
77 |
|
| loratidine |
antihistamine |
|
IKv1.5 |
1.2 |
|
19 |
|
| loratidine |
antihistamine |
HERG/HEK |
Isus |
>1 |
|
45 |
|
| loratidine |
antihistamine |
HERG/HEK |
Ito |
>1 |
|
45 |
|
| loratidine |
antihistamine |
rat VM |
Ito |
2.6 |
|
50 |
|
| loratidine |
antihistamine |
|
Ito |
>10 |
|
50 |
10uM = IC12 |
| DC-loratidine |
antihistamine |
HERG/HEK |
IKr |
1.82 |
--- |
46 |
at 37°C |
| LY97241 |
antiarrhythmic |
HERG/XO |
IKr |
0.15 |
--- |
109 |
|
| meperidine |
opiate |
HERG/HEK |
IKr |
75 |
--- |
71 |
|
| methadone |
opiate |
HERG/HEK |
IKr |
9.8 |
--- |
71 |
|
| methadone |
opiate |
HERG/HEK |
IKr |
10 |
--- |
70 |
|
| mexiletine |
antiarrhythmic |
rat VM |
ICaL |
5.8 |
--- |
93 |
|
| mibefradil |
calcium antagonist |
guinea pig |
ICaL |
0.2 |
|
52 |
-50 mV |
| mibefradil |
calcium antagonist |
guinea pig |
ICaL |
12 |
|
52 |
-80 mV |
| mibefradil |
calcium antagonist |
|
ICaL |
18.6 |
|
88 |
|
| mibefradil |
calcium antagonist |
|
ICaT |
2.7 |
|
88 |
|
| mibefradil |
calcium antagonist |
AT-1 |
IKr |
0.4-0.8 |
--- |
130 |
|
| mibefradil |
calcium antagonist |
AT-1 |
IKr |
0.75 |
--- |
98 |
|
| mibefradil |
calcium antagonist |
HERG/COS |
IKr |
1.43 |
--- |
42 |
|
| mibefradil |
calcium antagonist |
IKs/COS |
IKs |
11.8 |
|
42 |
|
| mizolastine |
antihistamine |
HERG/HEK |
IKr |
0.441 |
--- |
46 |
at 37°C |
| MK-499 |
antiarrhythmic |
HERG/XO |
IKr |
0.123 |
--- |
106 |
|
| MK-499 |
antiarrhythmic |
guinea-pig VM |
IKr |
0.4 |
--- |
54 |
|
| morin |
flavonoid |
HERG/XO |
IKr |
111.4 |
--- |
139 |
|
| morphine |
opiate |
HERG/HEK |
IKr |
> 1000 |
--- |
71 |
|
| moxifloxacin |
antibiotic/quinolone |
AT-1 |
IKr |
0.75 |
--- |
4 |
|
| moxifloxacin |
antibiotic/quinolone |
HERG/CHO |
IKr |
1 |
--- |
97 |
-40 mV |
| moxifloxacin |
antibiotic/quinolone |
HERG/CHO |
IKr |
41.2 |
--- |
33 |
-40 mV |
| moxifloxacin |
antibiotic/quinolone |
HERG/CHO |
IKr |
129 |
--- |
66 |
|
| naringenin |
flavonoid |
HERK/HEK |
IKr |
36.5 |
--- |
139 |
13.8% @ 1 uM |
| naringenin |
flavonoid |
HERG/XO |
IKr |
102.3 |
--- |
139 |
|
| nelfinavir |
antiviral |
HERG/HEK |
IKr |
11.5 |
--- |
5 |
|
| nifedipine |
dihydropyridine |
HERG/HEK |
IKr |
>50 |
--- |
136 |
|
| nitrendipine |
dihydropyridine |
HERG/COS |
IKr |
>10 |
--- |
42 |
|
| nitrendipine |
dihydropyridine |
IKs/COS |
IKs |
>10 |
|
42 |
|
| nitrendipine |
dihydropyridine |
rat VM |
INa |
3 |
|
133 |
|
| ofloxacin |
antibiotic/quinolone |
HERG/CHO |
IKr |
1420 |
--- |
66 |
|
| olanzipine |
antipsychotic |
human AM |
IK1 |
>>100 |
|
46 |
|
| olanzipine |
antipsychotic |
HERG/HEK |
IKr |
0.181 |
--- |
46 |
at 37°C |
| olanzipine |
antipsychotic |
human AM |
INa |
>100 |
|
46 |
|
| olanzipine |
antipsychotic |
human AM |
Isus |
>100 |
|
46 |
|
| olanzipine |
antipsychotic |
human AM |
Ito |
>100 |
|
46 |
|
| OPC-18790 |
inotrope |
AT-1 |
IKr |
0.96 |
--- |
129 |
|
| perhexiline |
antianginal |
HERG/CHO |
IKr |
7.8 |
--- |
124 |
|
| pimozide |
antipsychotic |
rat brain |
5HT2 |
0.031 |
1.7 |
44 |
|
| pimozide |
antipsychotic |
human AM |
IK1 |
>100 |
|
46 |
|
| pimozide |
antipsychotic |
HERG |
IKr |
0.018 |
--- |
65 |
|
| pimozide |
antipsychotic |
HERG/HEK |
IKr |
0.0497 |
--- |
46 |
at 37°C |
| pimozide |
antipsychotic |
HERG |
IKs |
>10 |
|
65 |
|
| pimozide |
antipsychotic |
HERG |
IKv1.5 |
>10 |
|
65 |
|
| pimozide |
antipsychotic |
human AM |
INa |
21.9 |
|
46 |
|
| pimozide |
antipsychotic |
human AM |
Isus |
>>100 |
|
46 |
|
| pimozide |
antipsychotic |
human AM |
Ito |
>>100 |
|
46 |
|
| prazosin |
alpha1-blocker |
HERG/CHO |
IKr |
3.4 |
--- |
92 |
|
| procainamide |
antiarrhythmic |
AT-1 |
IKr |
380 |
--- |
130 |
|
| N-acetylprocainamide |
antiarrhythmic |
AT-1 |
IKr |
92 |
--- |
98 |
|
| propranolol |
beta blocker |
AT-1 |
IKr |
15 |
--- |
127 |
|
| pyrilamine |
antihistamine |
GP cerebellum |
H1 |
0.006 |
0.005 |
27 |
|
| pyrilamine |
antihistamine |
|
IK1 |
>10 |
|
101 |
10uM = IC1.3 |
| pyrilamine |
antihistamine |
guinea-pig VM |
IKr |
1.1 |
--- |
102 |
|
| pyrilamine |
antihistamine |
|
IKr |
1.1 |
--- |
101 |
|
| pyrilamine |
antihistamine |
|
IKs |
>10 |
|
101 |
10uM = IC16 |
| quinidine |
antiarrhythmic |
feline VM |
IKr |
0.18 |
--- |
126 |
|
| quinidine |
antiarrhythmic |
HERG/L |
IKr |
0.3 |
--- |
130 |
|
| quinidine |
antiarrhythmic |
AT-1 |
IKr |
1 |
--- |
130 |
|
| quinidine |
antiarrhythmic |
HERG/XO |
IKr |
8 |
--- |
80 |
|
| ranolazine |
antianginal |
canine VM |
ICaL(late) |
50 |
4.2 |
6 |
|
| ranolazine |
antianginal |
canine VM |
ICaL(peak) |
296 |
49 |
6 |
|
| ranolazine |
antianginal |
canine VM |
IK1 |
>100 |
|
140 |
|
| ranolazine |
antianginal |
canine VM |
IKr |
11.5 |
--- |
140 |
|
| ranolazine |
antianginal |
canine VM |
IKr |
12 |
--- |
6 |
|
| ranolazine |
antianginal |
canine VM |
IKs |
13.4 |
|
140 |
|
| ranolazine |
antianginal |
canine VM |
IKs |
>> 30 |
>> 5 |
6 |
17% at 30 uM |
| ranolazine |
antianginal |
canine VM |
INa |
21 |
|
140 |
|
| ranolazine |
antianginal |
canine VM |
INa(late) |
6 |
0.5 |
6 |
|
| ranolazine |
antianginal |
canine VM |
INaCa |
91 |
15 |
6 |
|
| ranolazine |
antianginal |
canine VM |
Ito |
>100 |
>9 |
140 |
17% at 100 uM |
| risperidone |
antipsychotic |
|
5HT2 |
0.00016 |
0.0004 |
104 |
|
| risperidone |
antipsychotic |
|
D2 |
0.0033 |
0.008 |
104 |
|
| risperidone |
antipsychotic |
human AM |
IK1 |
>100 |
|
46 |
|
| risperidone |
antipsychotic |
HERG/HEK |
IKr |
0.163 |
--- |
46 |
at 37°C |
| risperidone |
antipsychotic |
|
IKr |
0.394 |
--- |
76 |
at 32-37°C |
| risperidone |
antipsychotic |
|
IKs |
9.7 |
|
76 |
at 32-37°C |
| risperidone |
antipsychotic |
|
IKv1.5 |
9.5 |
|
76 |
at 32-37°C |
| risperidone |
antipsychotic |
human AM |
INa |
50-100 |
|
46 |
|
| risperidone |
antipsychotic |
human AM |
Isus |
>100 |
|
46 |
|
| risperidone |
antipsychotic |
|
Ito |
25.5 |
|
76 |
at 32-37°C |
| risperidone |
antipsychotic |
human AM |
Ito |
>100 |
|
46 |
|
| ritonavir |
antiviral |
HERK/HEK |
IKr |
8.2 |
--- |
5 |
|
| RP-58866 |
antiarrhythmic |
guinea-pig VM |
IKr |
0.02 |
--- |
62 |
|
| RP-58866 |
antiarrhythmic |
HERG/XO |
IKr |
0.2 |
--- |
62 |
|
| saquinavir |
antiviral |
HERG/HEK |
IKr |
15.3 |
--- |
5 |
|
| sertindole |
antipsychotic |
|
5HT2 |
0.00085 |
0.17 |
104 |
|
| sertindole |
antipsychotic |
|
D2 |
0.0074 |
1.5 |
104 |
|
| sertindole |
antipsychotic |
human AM |
IK1 |
>10 |
|
46 |
|
| sertindole |
antipsychotic |
HERG |
IKr |
0.005 |
--- |
76 |
at 32-37°C |
| sertindole |
antipsychotic |
HERG/HEK |
IKr |
0.0126 |
--- |
46 |
at 37°C |
| sertindole |
antipsychotic |
HERG/L |
IKr |
0.014 |
--- |
94 |
|
| sertindole |
antipsychotic |
|
IKs |
0.88 |
|
76 |
at 32-37°C |
| sertindole |
antipsychotic |
HEK |
IKv1.5 |
2.12 |
|
94 |
|
| sertindole |
antipsychotic |
|
IKv1.5 |
4 |
|
76 |
at 32-37°C |
| sertindole |
antipsychotic |
human AM |
INa |
>10 |
|
46 |
|
| sertindole |
antipsychotic |
human AM |
Isus |
>10 |
|
46 |
|
| sertindole |
antipsychotic |
|
Ito |
8.8 |
|
76 |
at 32-37°C |
| sertindole |
antipsychotic |
human AM |
Ito |
>10 |
|
46 |
|
| sildenafil |
PDE inhibitor |
HERG/HEK |
IKr |
100 |
--- |
56 |
|
| sildenafil |
PDE inhibitor |
PDE5 |
PDE5 |
0.001 |
0.00001 |
118 |
|
| d-sotalol |
antiarrhythmic |
GP VM |
IKr |
100 |
--- |
103 |
|
| d-sotalol |
antiarrhythmic |
human AM |
IKv1.5 |
>500 |
--- |
53 |
|
| d-sotalol |
antiarrhythmic |
human AM |
Ito |
>500 |
|
53 |
|
| sparfloxacin |
antibiotic/quinolone |
AT-1 |
IKr |
0.23 |
--- |
4 |
|
| sparfloxacin |
antibiotic/quinolone |
HERG/CHO |
IKr |
13.5 |
--- |
33 |
-40 mV |
| sparfloxacin |
antibiotic/quinolone |
HERG/CHO |
IKr |
18 |
--- |
66 |
|
| spironolactone |
aldosterone antagonist |
HERG/CHO |
IKr |
23 |
--- |
35 |
|
| tamoxifen |
antiestrogen |
rabbit VM |
IKr |
1 |
--- |
84 |
|
| tamsulosin |
alpha1-blocker |
HERG/CHO |
IKr |
104.8 |
--- |
92 |
|
| terazosin |
alpha1-blocker |
HERG/CHO |
IKr |
21.4 |
--- |
92 |
|
| terfenadine |
antihistamine |
GP cerebellum |
H1 |
0.45 |
9 |
27 |
|
| terfenadine |
antihistamine |
GP LM |
H1 |
0.56 |
3.7 |
74 |
|
| terfenadine |
antihistamine |
guinea-pig VM |
ICa |
<3 |
|
90 |
|
| terfenadine |
antihistamine |
rat VM |
ICaL |
0.14 |
|
82 |
|
| terfenadine |
antihistamine |
HERG/HEK |
IK1 |
>1 |
|
45 |
|
| terfenadine |
antihistamine |
|
IK1 |
>10 |
|
31 |
|
| terfenadine |
antihistamine |
guinea-pig VM |
IK1 |
>10 |
|
31 |
|
| terfenadine |
antihistamine |
guinea-pig VM |
IKr |
0.05 |
--- |
101 |
|
| terfenadine |
antihistamine |
HERG/HEK |
IKr |
0.056 |
--- |
95 |
|
| terfenadine |
antihistamine |
HERG |
IKr |
0.056 |
--- |
76 |
at 32-37°C |
| terfenadine |
antihistamine |
rabbit VM |
IKr |
0.096 |
--- |
37 |
|
| terfenadine |
antihistamine |
AT-1 |
IKr |
0.097 |
--- |
127 |
|
| terfenadine |
antihistamine |
feline VM |
IKr |
0.15 |
--- |
126 |
|
| terfenadine |
antihistamine |
HERG/HEK |
IKr |
0.204 |
--- |
45 |
|
| terfenadine |
antihistamine |
HERG/XO |
IKr |
0.246 |
--- |
110 |
|
| terfenadine |
antihistamine |
HERG/XO |
IKr |
0.431 |
--- |
40 |
|
| terfenadine |
antihistamine |
HERG/XO |
IKr |
0.48 |
--- |
111 |
|
| terfenadine |
antihistamine |
|
IKs |
4.4 |
|
76 |
at 32-37°C |
| terfenadine |
antihistamine |
|
IKs |
<10 |
|
101 |
10uM = IC58 |
| terfenadine |
antihistamine |
XO |
IKs |
29 |
|
110 |
|
| terfenadine |
antihistamine |
XO |
IKv1.1 |
34 |
|
110 |
|
| terfenadine |
antihistamine |
|
IKv1.5 |
0.367 |
|
76 |
at 32-37°C |
| terfenadine |
antihistamine |
feline VM |
IKv1.5 |
0.37 |
|
96 |
|
| terfenadine |
antihistamine |
XO |
IKv1.5 |
1 |
|
128 |
|
| terfenadine |
antihistamine |
|
IKv1.5 |
1.1 |
|
18 |
|
| terfenadine |
antihistamine |
XO |
IKv1.5 |
2.6 |
|
100 |
|
| terfenadine |
antihistamine |
guinea-pig VM |
INa |
<3 |
|
90 |
|
| terfenadine |
antihistamine |
XO |
IRK1 |
23 |
|
110 |
|
| terfenadine |
antihistamine |
HERG/HEK |
Isus |
>1 |
|
45 |
|
| terfenadine |
antihistamine |
guinea-pig VM |
Ito |
>1 |
|
31 |
|
| terfenadine |
antihistamine |
HERG/HEK |
Ito |
>1 |
|
45 |
|
| terfenadine |
antihistamine |
|
Ito |
>1 |
|
30 |
1uM = IC11 |
| terfenadine |
antihistamine |
|
Ito |
2.7 |
|
76 |
at 32-37°C |
| terikalant |
antiarrhythmic |
guinea-pig VM |
IKr |
0.031 |
--- |
62 |
|
| terikalant |
antiarrhythmic |
HERG/XO |
IKr |
0.25 |
--- |
62 |
|
| terodiline |
antispasmodic |
AT-1 |
IKr |
0.0037 |
--- |
127 |
|
| terodiline |
antispasmodic |
guinea-pig VM |
IKr |
0.7 |
--- |
60 |
|
| thioridazine |
antipsychotic |
human AM |
IK1 |
>100 |
|
46 |
|
| thioridazine |
antipsychotic |
HERG/HEK |
IKr |
0.0357 |
--- |
46 |
at 37°C |
| thioridazine |
antipsychotic |
HERG/CHO |
IKr |
1.07 |
--- |
114 |
|
| thioridazine |
antipsychotic |
HERG/tsA-201 |
IKr |
1.25 |
--- |
49 |
|
| thioridazine |
antipsychotic |
guinea-pig VM |
IKr |
1.25 |
--- |
49 |
|
| thioridazine |
antipsychotic |
guinea-pig VM |
IKs |
14 |
|
49 |
|
| thioridazine |
antipsychotic |
human AM |
INa |
7.0 |
|
46 |
|
| thioridazine |
antipsychotic |
human AM |
Isus |
>100 |
|
46 |
|
| thioridazine |
antipsychotic |
human AM |
Ito |
27 |
|
46 |
|
| trimethaphan |
antihypertensive |
AT-1 |
IKr |
10 |
--- |
127 |
|
| valproic acid |
antiepileptic |
AT-1 |
IKr |
20 |
--- |
127 |
|
| verapamil |
calcium antagonist |
guinea pig |
ICaL |
0.7 |
|
52 |
|
| verapamil |
calcium antagonist |
HERG/HEK |
IKr |
0.143 |
--- |
136 |
|
| verapamil |
calcium antagonist |
HERG/L |
IKr |
0.34 |
--- |
129 |
|
| verapamil |
calcium antagonist |
AT-1 |
IKr |
0.3-1 |
--- |
130 |
|
| verapamil |
calcium antagonist |
HERG/COS |
IKr |
0.83 |
--- |
42 |
|
| verapamil |
calcium antagonist |
AT-1 |
IKr |
1.3 |
--- |
98 |
|
| verapamil |
calcium antagonist |
HERG/XO |
IKr |
3.8 |
--- |
122 |
|
| verapamil |
calcium antagonist |
IKs/COS |
IKs |
>10 |
|
42 |
|
| vesnarinone |
PDE inhibitor |
rabbit VM |
IKr |
5.7 |
--- |
115 |
|
| vesnarinone |
PDE inhibitor |
human heart |
PDE3 |
6.2 |
1.1 |
87 |
|
| WAY-123,398 |
antiarrhythmic |
feline VM |
IKr |
0.019 |
--- |
107 |
|
| ziprasidone |
antipsychotic |
human AM |
IK1 |
>10 |
|
46 |
|
| ziprasidone |
antipsychotic |
HERG/HEK |
IKr |
0.152 |
--- |
46 |
at 37°C |
| ziprasidone |
antipsychotic |
human AM |
INa |
>10 |
|
46 |
|
| ziprasidone |
antipsychotic |
human AM |
Isus |
>10 |
|
46 |
|
| ziprasidone |
antipsychotic |
human AM |
Ito |
>10 |
|
46 |
|
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