Selectivity data from the Guide to Receptors and Channels (GRAC), 5th Edition.
| Selectivity at human targets (unless otherwise stated) |
|
Key to terms and symbols
|
Click column headers to sort
|
|
α1
|
Antagonist |
Antagonist |
5.5
|
pIC50
|
- |
|
|
α3
|
Antagonist |
Antagonist |
4.5
|
pIC50
|
- |
|
|
β
(when co-expressed with the α1 subunit)
|
Antagonist |
Antagonist |
5.9
|
pIC50
|
- |
|
|
β
(when co-expressed with the α3 subunit)
|
Antagonist |
Antagonist |
4.9
|
pIC50
|
- |
|
|
Cav1.1
|
Channel blocker |
- |
-
|
-
|
- |
|
|
Cav1.2
|
Channel blocker |
- |
-
|
-
|
- |
|
|
TRPM3
|
Activator |
- |
-
|
-
|
- |
|
|
Selectivity data from IUPHAR-DB
| Selectivity at human ion channels |
|
Key to terms and symbols
|
Click column headers to sort
|
|
Kv1.5
|
Pore Blocker |
None |
4.1
|
pKd
|
- |
5
|
|
Cav1.2
|
Gating inhibitor |
Antagonist |
7.0 – 8.0
|
pIC50
|
- |
2
|
|
Cav1.4
|
Gating inhibitor |
None |
6.0
|
pIC50
|
- |
4
|
|
| Selectivity at rat ion channels |
|
Key to terms and symbols
|
Click column headers to sort
|
|
Cav1.2
|
Gating inhibitor |
Antagonist |
7.66
|
pIC50
|
- |
3
|
|
Cav1.1
|
Gating inhibitor |
Antagonist |
6.3
|
pIC50
|
1x10-7 - 1x10-4 |
1
|
|
Please note: The activity data given on this ligand page represents selected literature values and may not include all reported data. For more details please contact: curators@iuphar-db.org
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