Potency data for probe PF-04554878 and control PF-00911705
In vitro potency
| Target name | Target information | Species | Assay description | Compound conc. | PF-04554878 | PF-00911705 | Publication of assay conditions |
|---|---|---|---|---|---|---|---|
| PTK2 | human recombinant; kinase domain | Homo sapiens | Binding assay (PTK2) | IC50 = 0.2 nM | IC50 = 721 nM | ||
| PTK2B | human recombinant; kinase domain | Homo sapiens | Binding assay (PTK2B) | IC50 = 0.2 nM | IC50 = 721 nM | ||
| ADORA3 | Homo sapiens | Cerep profiling assay (ADORA3) | 10 µM | Ki = 27 nM | |||
| ADORA2A | Homo sapiens | Cerep profiling assay (ADORA2A) | 10 µM | Ki = 370 nM | |||
| FLT1 | Homo sapiens | Cerep profiling assay (FLT1) | 10 µM | IC50 = 2500 nM | |||
| LYN | Homo sapiens | Cerep profiling assay (LYN) | 10 µM | IC50 = 1100 nM |
In cell potency
| Target name | Target information | Species | Assay description | PF-04554878 | PF-00911705 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| PTK2 | A431 cells | Homo sapiens | Inhibition of human PTK2 phosphorylation in A431 cells | IC50 = 3 nM | ||
| GRK2, PTK2B | Homo sapiens | NanoBRET (GRK2) | EC50 = 520 nM ± 84.000 nM (n=3) | EC50 = 37 µM ± 7.100 µM (n=3) | ||
| PTK2 | Homo sapiens | NanoBRET assay (PTK2, SGC Frankfurt) | EC50 = 28 nM ± 4.400 nM (n=3) | EC50 = 3.2 µM ± 0.300 µM (n=3) |