Table 2.
Compound | Calculated affinity and cooperativity factors
|
|||
---|---|---|---|---|
alpha ± SEM | 95% C.I. | beta ± SEM | 95% C.I. | |
|
|
|||
PSNCBAM-1 | 55.01 ± 3.76 | (47.65 – 62.37) | 0.003 ± 0.001 | (0.0003 – 0.005) |
RTICBM-15 | 20.71 ± 1.43 | (17.91 – 23.51) | ~0 | ND |
RTICBM-28 | 201.1 ± 11.95 | (177.7 – 224.5) | 0.001 ± 0.001 | (0 – 0.003) |
Data were fit to allosteric operational model (see equation 2) with parameters constrained as follows: logKA=−6.6; Emax=100; TA=14; TB=0; n=1; α>0; β>0. LogKB was constrained individually to values obtained from [3H]SR141716 binding data (Table 4). Values considered significant by non-overlapping 95% confidence intervals. ND = not determined.