Selectivity data for probe JNJ-3738 and control JNJ-6240
Coming soon
JNJ-3738
For the assay THP-1 & H1975 lysates were used. The assay was done at ~20x CDK7 cell-based IC50 (about 1 µM of probe).
Conclusion: The CDK family selectivity is good. Closest off-targets at 1 µM [% inhibition] are CAMKK2 (70) and STK16.
| Target protein | HGNC name | Species | % Inhibition at 1 µM |
|---|---|---|---|
| CDK1 | CDK1 | Homo sapiens | 11.0 |
| CDK2 | CDK2 | Homo sapiens | 6.0 |
| CDK4 | CDK4 | Homo sapiens | 0.0 |
| CDK5 | CDK5 | Homo sapiens | 2.0 |
| CDK6 | CDK6 | Homo sapiens | 0.0 |
| CDK7 | CDK7 | Homo sapiens | 95.0 |
| CDK8 | CDK8 | Homo sapiens | 7.0 |
| CDK9 | CDK9 | Homo sapiens | 45.0 |
| CDK10 | CDK10 | Homo sapiens | 3.0 |
| CDK11 |
CDK11A CDK11B |
Homo sapiens | 7.0 |
| CDK11b | CDK11b | Homo sapiens | 5.0 |
| CDK12 | CDK12 | Homo sapiens | 11.0 |
| CDK13 | CDK13 | Homo sapiens | 13.0 |
| CDK14 | CDK14 | Homo sapiens | 11.0 |
| CDK15 | CDK15 | Homo sapiens | 15.0 |
| CDK16 | CDK16 | Homo sapiens | 1.0 |
| CDK17 | CDK17 | Homo sapiens | 17.0 |
| CDK18 | CDK18 | Homo sapiens | 19.0 |
| CDK20 | CDK20 | Homo sapiens | 5.0 |
| CAMKK2 | CAMKK2 | Homo sapiens | 70.0 |
| MPSK1 | STK16 | Homo sapiens | 65.0 |
JNJ-3738
The assay was done at 1 µM probe.
Conclusion: Good CDK family selectivity.
| Target protein | HGNC name | Species | % inhibition at 1 µM | pIC50 |
|---|---|---|---|---|
| CDK2 | CDK2 | Homo sapiens | 10.0 | |
| CDK3 | CDK3 | Homo sapiens | 14.0 | |
| CDK4 | CDK4 | Homo sapiens | 10.0 | |
| CDK5 | CDK5 | Homo sapiens | 5.0 | |
| CDK7 | CDK7 | Homo sapiens | 99.0 | 8.42 |
| CDK8 | CDK8 | Homo sapiens | > 2.0 | |
| CDK9 | CDK9 | Homo sapiens | 36.0 | 6.03 |
| CDK11 |
CDK11A CDK11B |
Homo sapiens | 11.0 | |
| CDK11b | CDK11B | Homo sapiens | 0.0 | |
| CDK13 | CDK13 | Homo sapiens | 12.0 | |
| CDK14 | CDK14 | Homo sapiens | 5.0 | |
| CDK15 | CDK15 | Homo sapiens | 21.0 | |
| CDK16 | CDK16 | Homo sapiens | 5.0 | |
| CDK17 | CDK17 | Homo sapiens | 2.0 | |
| CDK18 | CDK18 | Homo sapiens | 25.0 |