Chemical probes are cell-active, selective, highly validated research tools that can be used to decipher the biology of their target. They are useful assets for example, in phenotypic assays, or as a starting point for medicinal chemistry campaigns. Chemical probes developed by the EUbOPEN consortium are peer reviewed by an external committee and available upon request. The probes are released with a structurally similar inactive negative control compound (where feasible) and fulfill the following criteria:
| Potency | ≤ 100 nM in a biochemical or biophysical assay |
| Selectivity |
≥ 30-fold over related proteins |
| Evidence of target engagement in cells | ≤ 1 µM for the druggable target or 10 µM for shallow PPI targets |
| Cytotoxicity | ≥ 10 µM, unless target mediated |
For more information, or to request a probe, click on the probe link below.
| Probe name | Target | Negative control | Web link | Probe package |
|---|---|---|---|---|
| GSK778 | BRD2, BRD3, BRD4, BRDT | N/A | GSK778: A pan-BD1 Chemical Probe for the BET family | EUbOPEN_ProbeSheet_GSK778_v1_0.pdf891.92 KB |
| GSK620 | BRD2, BRD3, BRD4, BRDT | N/A | GSK620: A pan-BD2 Chemical Probe for the BET family | EUbOPEN_ProbeSheet_GSK620_v1_0.pdf901.08 KB |
| NR162 | CASK | NR187 | NR162: A Chemical Probe for CASK | EUbOPEN_ProbeSheet_CASK_v1_0.pdf867.59 KB |
| BAY-6672 | PTGFR | BAY-403 | BAY-6672: A Chemical Probe for PTGFR | EUbOPEN_ProbeSheet_BAY_6672_v1_0.pdf882.23 KB |
| BAY-3153 | CCR1 | BAY-173 | BAY-3153 A Chemical Probe for CCR1 | EUbOPEN_ProbeSheet_BAY_3153_v1_0.pdf879.16 KB |
| BAY-390 | TRPA1 (transient receptor potential cation channel subfamily A member 1; ANKTM1) | BAY-9897 | BAY-390: A Chemical Probe for BAY-390 | EUbOPEN_ProbeSheet_BAY_390_v2.pdf168.74 KB |