Very high affinity ClC-2 blocker (apparent KD ~ 50 pM). Slows ClC-2 activation and inhibits slow-gating but does not inhibit open ClC-2 channels. Selective for ClC-2 over other ClC family members (ClC-0, ClC-1, ClC-3 and ClC-4), CFTR, GABAC, CaCC and KV1.
Anatoxin-a (ATX-a), a neurotoxic alkaloid, functions as an agonist for the nicotinic acetylcholine receptor (nAChR) and as an inhibitor of Acetylcholinesterase (AChE) [1] [2].
Autotaxin-IN-1 is a potent autotaxin inhibitor, which has favorable potency (IC50=2.2 nM), PK properties, and a robust PK PD relationship and it is used in treatment of osteoarthritis pain[1].