Assay Detail
Functional
CHEMBL3431450
Review assay metadata, readout intent, target linkage, and publication context from the same page.
GSK_TCAKS: pIC50 Leishmania donovani viability assay using fluorescence intensity. Assay plates (1536-well) were prepared by adding 30nL per well of compound. For single shot assay, the final compound concentration was 5uM. For potency determinations, eleven-point one in three dilution curves were generated with a top concentration of 50uM. Briefly, eGFP LdBOB axenic amastigotes were harvested, fixed and counted in a CASY cell counter (Roche-Applied Science). A final concentration of 1.5 * 10^5 cells per well were prepared in amastigote media containing 500 U/mL penicillin/streptomycin (Invitrogen) and 6uL was dispensed to each experimental well using a Multidrop Combi dispenser (Thermo Scientific). 6uL of assay media was dispensed to control columns used as reference for 100% compound response. Following incubation for 72 h at 37C, 5% CO2, 2 uL of resazurin was added to each well at a final concentration of 0.5 mM in phosphate buffered saline (PBS) with IGEPAL (Sigma-Aldrich), 0.05% (v/v). The plates were incubated for 4 h at room temperature and resorufin fluorescence was detected using a PerkinElmer EnVision plate reader with excitation at 528 nm and emission at 590 nm.
590
Total Activities
590
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Leishmania donovani |
| Cell Type | CASY |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
GSK Tres Cantos Anti-Kinetoplastid Screening (TCAKS) Data.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 590 | 5.34 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3431298 | — | — | 1 | 7.50 |
| CHEMBL3431297 | — | — | 1 | 7.40 |
| CHEMBL3431127 | — | — | 1 | 7.40 |
| CHEMBL3431435 | — | — | 1 | 7.20 |
| CHEMBL3431295 | — | — | 1 | 7.10 |
| CHEMBL3431194 | — | — | 1 | 7.00 |
| CHEMBL3431025 | — | — | 1 | 6.90 |
| CHEMBL2098124 | — | — | 1 | 6.90 |
| CHEMBL522630 | — | — | 1 | 6.90 |
| CHEMBL3431397 | — | — | 1 | 6.90 |
| CHEMBL3431400 | — | — | 1 | 6.80 |
| CHEMBL3431230 | — | — | 1 | 6.70 |
| CHEMBL3431433 | — | — | 1 | 6.70 |
| CHEMBL3431229 | — | — | 1 | 6.60 |
| CHEMBL523303 | — | — | 1 | 6.60 |
| CHEMBL3431258 | — | — | 1 | 6.50 |
| CHEMBL3431188 | — | — | 1 | 6.50 |
| CHEMBL491149 | — | — | 1 | 6.50 |
| CHEMBL523468 | — | — | 1 | 6.50 |
| CHEMBL3431381 | — | — | 1 | 6.50 |
| CHEMBL3431326 | — | — | 1 | 6.40 |
| CHEMBL1232777 | FORMYCIN B | — | 1 | 6.40 |
| CHEMBL3430988 | — | — | 1 | 6.40 |
| CHEMBL3431004 | — | — | 1 | 6.40 |
| CHEMBL3431011 | — | — | 1 | 6.40 |
| CHEMBL3431106 | — | — | 1 | 6.40 |
| CHEMBL3431139 | — | — | 1 | 6.40 |
| CHEMBL3431187 | — | — | 1 | 6.40 |
| CHEMBL3431363 | — | — | 1 | 6.30 |
| CHEMBL3431371 | — | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3431298 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL3431297 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL3431127 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL3431435 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL3431295 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL3431194 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3431397 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3431025 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL2098124 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL522630 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3431400 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL3431230 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL3431433 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL523303 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL3431229 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL491149 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL3431258 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL523468 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL3431381 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL3431188 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL3431187 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL3431326 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL3430988 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL3431004 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL3431011 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL3431106 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL1232777 | FORMYCIN B | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL3431139 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL3431363 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL3431371 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL3431033 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL3431003 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL3431105 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL1489081 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL3430947 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL3431082 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL3431357 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL3431193 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL3431170 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL3431345 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL3431209 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL3431129 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL1731664 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL2441267 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL3431352 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL3431376 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL530275 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL3431432 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL3431431 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL526199 | — | IC50 | = | 794.33 | nM | 6.10 |