Assay Detail
Functional
CHEMBL3431446
Review assay metadata, readout intent, target linkage, and publication context from the same page.
GSK_TCAKS: pIC50 Trypanosoma cruzi viability assay using beta-GAL activity. This assay was run at single shot at 5uM compound concentration per well. The biological reagents consisted of NIH-3T3 host cells and trypomastigotes parasitic cells; both cell types were set to a 3.3 * 10^5 cells/mL dilution in assay DMEM by means of a CASY cell counter device using a 60um capillary. 6 uL of the mixture were dispensed per well (about 1 * 10^3 host-cells and 1 * 10^3 parasites) with a Multidrop Combi dispenser. Previously, a solution of 1.67 * 10^5 trypomastigotes per mL in assay DMEM had been prepared and 6uL per well dispensed in the allotted control columns that defined 100% inhibition. The 0% inhibition of parasitic growth control was obtained by leaving the assay mixture untreated in its corresponding plate columns. In all wells, the percentage of DMSO never exceeded 0.5%. Plates incubated for four days at 37C, 5% CO2. The substrate used for the assay fluorescence intensity (FLINT) readout was resorufin-beta-D-galactopiranoside (Sigma-Aldrich) at 5uM per well. It was diluted in PBS supplemented with the soft detergent Igepal (Fluka). Upon addition to the plates, the substrate solution was incubated for 4h at room temperature and the signal read with the EnVision microtiter plate reader (Perkin-Elmer) using the corresponding set of filters (excitation/emission at 531/595nm).
584
Total Activities
584
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | NIH3T3 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
GSK Tres Cantos Anti-Kinetoplastid Screening (TCAKS) Data.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 584 | 5.92 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL528583 | — | — | 1 | 8.20 |
| CHEMBL3431117 | — | — | 1 | 7.80 |
| CHEMBL3431025 | — | — | 1 | 7.70 |
| CHEMBL3431261 | — | — | 1 | 7.70 |
| CHEMBL3431266 | — | — | 1 | 7.70 |
| CHEMBL3431326 | — | — | 1 | 7.60 |
| CHEMBL3431435 | — | — | 1 | 7.60 |
| CHEMBL3431128 | — | — | 1 | 7.50 |
| CHEMBL3431155 | — | — | 1 | 7.50 |
| CHEMBL3431368 | — | — | 1 | 7.40 |
| CHEMBL1325144 | — | — | 1 | 7.40 |
| CHEMBL3431434 | — | — | 1 | 7.40 |
| CHEMBL3431140 | — | — | 1 | 7.30 |
| CHEMBL3431433 | — | — | 1 | 7.30 |
| CHEMBL3431318 | — | — | 1 | 7.25 |
| CHEMBL3431129 | — | — | 1 | 7.20 |
| CHEMBL3430960 | — | — | 1 | 7.15 |
| CHEMBL3431003 | — | — | 1 | 7.15 |
| CHEMBL3431257 | — | — | 1 | 7.15 |
| CHEMBL3431130 | — | — | 1 | 7.10 |
| CHEMBL3431192 | — | — | 1 | 7.10 |
| CHEMBL3431206 | — | — | 1 | 7.10 |
| CHEMBL3431291 | — | — | 1 | 7.10 |
| CHEMBL3431381 | — | — | 1 | 7.10 |
| CHEMBL3431029 | — | — | 1 | 7.00 |
| CHEMBL1458931 | — | — | 1 | 7.00 |
| CHEMBL3431238 | — | — | 1 | 7.00 |
| CHEMBL3431354 | — | — | 1 | 7.00 |
| CHEMBL3431376 | — | — | 1 | 7.00 |
| CHEMBL3431400 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL528583 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL3431117 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL3431261 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL3431266 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL3431025 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL3431435 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL3431326 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL3431155 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL3431128 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL1325144 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL3431368 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL3431434 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL3431140 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL3431433 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL3431318 | — | IC50 | = | 56.23 | nM | 7.25 |
| CHEMBL3431129 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL3431257 | — | IC50 | = | 70.79 | nM | 7.15 |
| CHEMBL3430960 | — | IC50 | = | 70.79 | nM | 7.15 |
| CHEMBL3431003 | — | IC50 | = | 70.79 | nM | 7.15 |
| CHEMBL3431192 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL3431206 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL3431381 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL3431291 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL3431130 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL3431354 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3431376 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3431400 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3431238 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3431029 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1458931 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3431028 | — | IC50 | = | 112.2 | nM | 6.95 |
| CHEMBL487186 | TEBUCONAZOLE | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3431337 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3431338 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3431004 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL2441267 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3431405 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3431289 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3430915 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3431193 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3431263 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3431133 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3431151 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3431220 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3430980 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3431375 | — | IC50 | = | 141.25 | nM | 6.85 |
| CHEMBL3431408 | — | IC50 | = | 141.25 | nM | 6.85 |
| CHEMBL1232777 | FORMYCIN B | IC50 | = | 141.25 | nM | 6.85 |
| CHEMBL3431107 | — | IC50 | = | 141.25 | nM | 6.85 |
| CHEMBL3431331 | — | IC50 | = | 141.25 | nM | 6.85 |