Name | IC50 Values against TRP Channels | Additional Targets | |||||
---|---|---|---|---|---|---|---|
TRPV1 | TRPV2 | TRPV3 | TRPV4 | TRPA1 | TRPM8 | ||
nM | |||||||
A-425619 | 10 | — | >20,000b | >20,000a | >10,000b | 8000b | 0 (of 83 tested)b |
ABT-102 | 1 | — | >20,000c | >20,000c | >20,000c | >20,000c | 0 (of 75 tested)c |
AMG0347 | 0.7 | >10,000d | >10,000d | >10,000d | >10,000d | >10,000d | — |
AMG1629 | 0.6 | >4000e | >4000e | >4000e | >4000e | >4000e | — |
AMG3731 | 6 | >4000e | >4000e | >4000e | >4000e | >4000e | — |
AMG 517 | 1 | >20,000f | >20,000f | >20,000f | >20,000f | >20,000f | 3 (of 90 tested)f |
AMG8163 | 0.6 | >4000g | >4000e | >4000e | >4000e | >4000e | — |
AMG9810 | 79–86 | — | >4000g | >4000g | >4000g | >4000g | 4 (of 90 tested)g |
BCTC | 0.4–0.5 | — | >20,000a | 1500a | >20,000a | 143–800h,i | — |
AMG7905 | 39 | >4000j | >4000j | >4000j | >4000j | >4000j | — |
AMG8562 | 2 | >20,000j | >20,000j | >20,000j | >20,000j | >20,000j | 0 (of 50 tested)j |
CPZ | 420–887g,k,l | >10,000l,m | >10,000l–o | >10,000l,n,p | >100,000l | 18,000h,i,l | 3q |
Ruthenium red | 50–512b,r | 200–2028f,j,m,s | <10,000o | 24–1000f,j,p | 367f,j | — | 3t |
—, no information available.
↵a M. H. Norman, personal communication.
↵b El Kouhen et al. (2005).
↵c Surowy et al. (2008).
↵d Steiner et al. (2007).
↵e Gavva et al. (2007b).
↵f Gavva et al. (2007a). Of 90 targets tested in this study, AMG 517 interacted with three: monoamine oxidase B, AEA transporter, and Na+ channel (site 2).
↵g Gavva et al. (2005b). Of 90 targets tested in this study, AMG9810 interacted with four: Ca2+ channel (L-type: DHP site), Na+ channel (site 2), dopamine transporter, and angiotensin-II.
↵h Behrendt et al. (2004).
↵i Weil et al. (2005).
↵j Lehto et al. (2008).
↵k Bevan et al. (1992).
↵l C.R. Faltynek, P.R. Kym, and R.M. Reilly, personal communication.
↵m Caterina et al. (1999).
↵n M. J. Caterina, personal communication.
↵o Smith et al. (2002).
↵p Watanabe et al. (2002).
↵q CPZ has been reported to interact with hyperpolarization-activated cation channel (Gill et al., 2004), nicotinic-acetylcholine receptor (Liu and Simon, 1997), and voltage-gated calcium channel (Docherty et al., 1997).
↵r Wood et al. (1988).
↵s Ahluwalia et al. (2002).
↵t Ruthenium red has been reported to interact with TRPV5 (Nilius et al., 2001), TRPV6 (Nilius et al., 2001), voltage-gated calcium channel (Cibulsky and Sather, 1999), and ryanodine receptor (Lukyanenko et al., 2000).