Parameters | Human Hepatocyte: Add Method | Human Hepatocyte: Dilution Method | Human Hepatocyte: Add Method (Mean) | Human Hepatocyte: Dilution Method (Mean) | HLMa (Mean ± S.D.) | ||
---|---|---|---|---|---|---|---|
Assay 1 | Assay 2 | Assay 1 | Assay 2 | ||||
Diltiazem | |||||||
KI | 6.6 | 6.0 | 10.5 | 7.4 | 6.3 | 8.9 | 1.53 ± 0.565 |
kinact | 0.0162 | 0.0219 | 0.0234 | 0.0222 | 0.019 | 0.0228 | 0.024 ± 0.011 |
kinact/KI | 0.0024 | 0.0037 | 0.0022 | 0.003 | 0.0031 | 0.0026 | 0.016 ± 0.001 |
Erythromycin | |||||||
KI | 61.3 | 58.7 | 67.1 | 68.6 | 60.0 | 67.9 | 5.33 ± 2.57 |
kinact | 0.0856 | 0.0760 | 0.0868 | 0.0712 | 0.081 | 0.079 | 0.061 ± 0.002 |
kinact/KI | 0.0014 | 0.0013 | 0.0013 | 0.0010 | 0.0013 | 0.0012 | 0.013 ± 0.005 |
Verapamil | |||||||
KI | 2.4 | 1.4 | 2.2 | 2.1 | 1.9 | 2.1 | 3.19 ± 0.251 |
kinact | 0.02 | 0.0203 | 0.0249 | 0.0295 | 0.02 | 0.0272 | 0.076 ± 0.004 |
kinact/KI | 0.0083 | 0.0149 | 0.0113 | 0.0141 | 0.0116 | 0.0127 | 0.024 ± 0.003 |
TAO | |||||||
KI | 2.7 | 3.3 | 3.7 | 3.2 | 3.0 | 3.4 | 0.440 ± 0.140 |
kinact | 0.237 | 0.238 | 0.356 | 0.382 | 0.238 | 0.369 | 0.078 ± 0.053 |
kinact/KI | 0.088 | 0.072 | 0.098 | 0.119 | 0.0798 | 0.1081 | 0.205 ± 0.180 |
↵a Mean values are from at least three assays collected from historical data.