Nonradioactive Ligand | koff | 95% Confidence Limitsa | t value | Significanceb |
---|---|---|---|---|
h −1 | ||||
MIP-1α | 0.26c | 0.22 to 0.29 | 8.94 df=36 | P < 0.005 |
Sch-C | 0.013 | 0.008 to 0.018 | 3.73 df=34 | P < 0.005 |
Sch-D | 0.005 | 0.004 to 0.006 | 4.45 df=34 | P < 0.005 |
TAK-779 | 0.013 | 0.01 to 0.015 | 5.6 df=38 | P < 0.005 |
UK-427,857 | 0.0036 | 0.0026 to 0.0045 | 3.78 df=41 | P < 0.005 |
873140 | 0.93 df=41 | N.S. |
↵ a 95% confidence limits of the slope from a plot of ln (receptor occupancy) vs time (hours).
↵ b Value of t to determine whether a significant dependence of antagonist receptor occupancy exists on time; i.e., does washing with drug-free media cause reduction in the receptor occupancy by the antagonist? Insignificant values of t indicate no relationship between time and occupancy (i.e., operationally irreversible receptor occupancy by the antagonist over the time period of the experiment, specifically 51 h).
↵ c This value was obtained at room temperature. All other values obtained at 4°C. No reversal of receptor occupancy was observed at room temperature for other antagonists at wash periods up to 8 h.