Potency data for probe C3TD879 and control C3TD879-N
In vitro potency
| Target name | Target information | Species | Assay description | C3TD879 | C3TD879-N | Publication of assay conditions |
|---|---|---|---|---|---|---|
| CIT | kinase domain | Homo sapiens | Eurofins Radiometric Activity Assay GST-CITKKD | IC50 = 12 nM (n=5) | IC50 > 30 µM (n=1) | |
| CIT | recombinant E. coli dephosphorylated; kinase domain | Homo sapiens | DSF (CITKKD-c006 dephosphorylated) | deltaTm = 2.1 °C | deltaTm = -0.2 °C | |
| CIT | recombinant Sf9 hyperphosphorylated; kinase domain | Homo sapiens | DSF (CITKKD-c014 hyperphosphorylated) | deltaTm = 2.1 °C | deltaTm = -0.3 °C | |
| AAK1 | Homo sapiens | Eurofins KinomeScan follow up (AAK1) | IC50 = 212 nM | |||
| BMP2K | Homo sapiens | Eurofins KinomeScan follow up (BIKE) | IC50 = 902 nM | |||
| MKNK2 | Homo sapiens | Eurofins KinomeScan follow up (MNK2) | IC50 = 2180 nM | |||
| HIPK4 | Homo sapiens | Eurofins KinomeScan follow up (HIPK4) | IC50 = 2275 nM | |||
| TNK2 | Homo sapiens | Eurofins KinomeScan follow up (ACK) | IC50 > 3 µM | |||
| STK17B | Homo sapiens | Eurofins KinomeScan follow up (DRAK2) | IC50 > 3 µM |
In cell potency
| Target name | Target information | Species | Assay description | C3TD879 | C3TD879-N | Publication of assay conditions |
|---|---|---|---|---|---|---|
| CIT | full length | Homo sapiens | Promega NanoBRET (CIT) | IC50 = 51 nM | ||
| CIT | Implied Kd values calculated using Tracer K10 Kd = 230 nM; Tracer K10 used at 1 µM for CITK NanoBRET; kinase domain | Homo sapiens | NanoLuc NanoBRET (CITKD) | Kd = 0.3 nM ± 0.200 nM (n=2) | Kd = no binding | |
| CIT | Implied Kd values calculated using Tracer K10 Kd = 230 nM; Tracer K10 used at 1 µM for CITK NanoBRET; full length | Homo sapiens | NanoLuc NanoBRET (CIT) | Kd = 9.5 nM ± 0.500 nM (n=2) | Kd = no binding | |
| AAK1 | Homo sapiens | Promega NanoBRET (AAK1) | IC50 = 6.2 µM | |||
| BMP2K | Homo sapiens | Promega NanoBRET (BMP2K) | IC50 > 10 µM | |||
| MKNK2 | Homo sapiens | Promega NanoBRET (MKNK2) | IC50 = 5.5 µM | |||
| HIPK4 | Homo sapiens | Promega NanoBRET (HIPK4) | IC50 > 10 µM | |||
| STK17B | Homo sapiens | Promega NanoBRET (STK17B) | IC50 > 10 µM | |||
| AURKA | Homo sapiens | Promega NanoBRET (AURKA) | IC50 > 10 µM | |||
| AURKB | Homo sapiens | Promega NanoBRET (AURKB) | IC50 > 10 µM | |||
| GAK | Homo sapiens | Promega NanoBRET (GAK) | IC50 > 10 µM | |||
| PRKACA | Homo sapiens | Promega NanoBRET (PRKACA) | IC50 > 10 µM |