Potency data for probe BAY 1816032 and control BAY-283
In vitro potency
| Target name | Target information | Species | Assay description | BAY 1816032 | BAY-283 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| BUB1 | Homo sapiens | BUB1 biochemical assay (low ATP): w/o preincubation | IC50 = 6.5 nM | IC50 = 1.7 µM | PMID: 30429199 | |
| BUB1 | Homo sapiens | BUB1 biochemical assay (high ATP): w/o preincubation/ 2 mM ATP | IC50 = 1.9 µM | IC50 > 20 µM | PMID: 30429199 | |
| BUB1 | Homo sapiens | BUB1 surface plasmon resonance (SPR) assay | Kd = 2.1 nM | PMID: 30429199 | ||
| BUB1 | Homo sapiens | ePCA binding competition (equilibrium binding assay) | IC50 = 1 nM ± 0.500 nM | PMID: 30429199 | ||
| BUB1 | catalytic domain (amino acids 704–1085) | Homo sapiens | TR-FRET: 10 μM ATP | EC50 = 6.1 nM ± 2.500 nM | PMID: 30429199 |
In cell potency
| Target name | Target information | Species | Assay description | BAY 1816032 | BAY-283 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| BUB1 | nocodazole arrested HeLa cells | Homo sapiens | Abrogation of histone H2A-Thr120 phosphorylation: Measured after 1 hour compound incubation | IC50 = 29 nM ± 23.000 nM | PMID: 30429199 |