Assay Detail
Functional
CHEMBL933419
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900
76
Total Activities
76
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Trypanosoma brucei rhodesiense |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Target
Trypanosoma brucei rhodesiense (CHEMBL612348) ↗| Type | ORGANISM |
| Organism | Trypanosoma brucei rhodesiense |
Publication
New bis(2-aminoimidazoline) and bisguanidine DNA minor groove binders with potent in vivo antitrypanosomal and antiplasmodial activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 76 | 5.77 | 8.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL271809 | — | — | 1 | 8.31 |
| CHEMBL242759 | — | — | 1 | 7.66 |
| CHEMBL363001 | — | — | 1 | 7.62 |
| CHEMBL3216323 | — | — | 1 | 7.60 |
| CHEMBL3216997 | — | — | 1 | 7.44 |
| CHEMBL1203959 | — | — | 1 | 7.42 |
| CHEMBL404606 | — | — | 1 | 7.35 |
| CHEMBL75414 | — | — | 1 | 7.32 |
| CHEMBL270533 | — | — | 1 | 7.30 |
| CHEMBL429921 | — | — | 1 | 7.27 |
| CHEMBL271749 | — | — | 1 | 7.22 |
| CHEMBL242102 | — | — | 1 | 7.16 |
| CHEMBL428395 | — | — | 1 | 6.99 |
| CHEMBL271996 | — | — | 1 | 6.93 |
| CHEMBL532729 | — | — | 1 | 6.91 |
| CHEMBL77633 | — | — | 1 | 6.79 |
| CHEMBL548436 | — | — | 1 | 6.73 |
| CHEMBL243288 | — | — | 1 | 6.71 |
| CHEMBL308767 | — | — | 1 | 6.69 |
| CHEMBL557382 | — | — | 1 | 6.66 |
| CHEMBL431961 | — | — | 1 | 6.64 |
| CHEMBL407777 | — | — | 1 | 6.57 |
| CHEMBL267337 | — | — | 1 | 6.50 |
| CHEMBL244987 | — | — | 1 | 6.41 |
| CHEMBL539632 | — | — | 1 | 6.38 |
| CHEMBL405745 | — | — | 1 | 6.33 |
| CHEMBL244986 | — | — | 1 | 6.33 |
| CHEMBL556563 | — | — | 1 | 6.27 |
| CHEMBL75389 | — | — | 1 | 6.05 |
| CHEMBL407518 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL271809 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL242759 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL363001 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3216323 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3216997 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1203959 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL404606 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL75414 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL270533 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL429921 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL271749 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL242102 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL428395 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL271996 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL532729 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL77633 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL548436 | — | IC50 | = | 187.0 | nM | 6.73 |
| CHEMBL243288 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL308767 | — | IC50 | = | 206.0 | nM | 6.69 |
| CHEMBL557382 | — | IC50 | = | 217.0 | nM | 6.66 |
| CHEMBL431961 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL407777 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL267337 | — | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL244987 | — | IC50 | = | 386.0 | nM | 6.41 |
| CHEMBL539632 | — | IC50 | = | 414.0 | nM | 6.38 |
| CHEMBL405745 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL244986 | — | IC50 | = | 467.0 | nM | 6.33 |
| CHEMBL556563 | — | IC50 | = | 538.0 | nM | 6.27 |
| CHEMBL75389 | — | IC50 | = | 897.0 | nM | 6.05 |
| CHEMBL407518 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL405429 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1162154 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL430286 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL73758 | — | IC50 | = | 2050.0 | nM | 5.69 |
| CHEMBL272681 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL77670 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL1162153 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL423676 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL271534 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL270330 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL270122 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL270352 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL9441 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL270752 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL537246 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL538590 | — | IC50 | = | 14400.0 | nM | 4.84 |
| CHEMBL272259 | — | IC50 | = | 15900.0 | nM | 4.80 |
| CHEMBL270121 | — | IC50 | = | 18800.0 | nM | 4.73 |
| CHEMBL231585 | — | IC50 | = | 20100.0 | nM | 4.70 |
| CHEMBL424238 | — | IC50 | = | 32400.0 | nM | 4.49 |