However, inhibiting MYC-MAX interaction in vivo has been limited by fast metabolism, poor potency, resistance mechanisms, and poor tumor penetrability of these small molecule inhibitors [26,27,28,29,30].
However, when the nucleants are of a poor potency then a calculation of the fraction solid necessary to develop the constitutional undercooling required for nucleation needs to be performed.
Similarly, a series of bis(n -tacrine dimer series, bivalen -tacrineors andimeripheral seriesChE inhibivalentossess poor potency toward BmAChE.
The biological data revealed that most compounds exhibited moderate-to-excellent activity against HT-29, MKN-45, A549 cancer cell lines and relative poor potency toward MDA-MB-231 cell as well as hardly any cytotoxicity in normal PBL cell.
Whatever the mechanism, this finding represents a previously unrecognized side-effect of crystalloid resuscitation in sepsis that is likely to contribute both to relatively poor potency and short duration of crystalloids as plasma volume expanders in sepsis.
The inability of acutely administered Boc5 to elicit insulin responses under hyperinsulinemia may result from its poor potency as the compound is approximately 2700 times less potent than exenatide (Fig. 4B).
Consequently, these drugs exhibit poor potency and limited treatment success.
Interestingly, the Cy7 conjugate 67 inhibited COX-2 with poor potency, while inhibitory activity but lack of selectivity was observed with the NIR641 conjugate (68), a chloride salt.
Furthermore, apart from a series of SCAs described by Schmidt et al. (20), which, because of their small size, also have poor potency, the only FFA2-selective ligands currently described derive from the phenylacetamide 4-CMTB (21, 33).
However, given their metabolic instability and poor potency (minimum cidal concentrations of 17 μ m), it is highly unlikely that either would deliver efficacy in a mouse model of HAT.
