Assay Detail
Binding
CHEMBL880254
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Inhibition of recombinant Trypanosoma brucei soluble vacuolar pyrophosphatase expressed in Escherichia coli
81
Total Activities
81
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Trypanosoma brucei |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Vacuolar-type proton translocating pyrophosphatase 1 (CHEMBL4386) ↗| Type | SINGLE PROTEIN |
| Organism | Trypanosoma brucei |
Publication
Bisphosphonate inhibition of the exopolyphosphatase activity of the Trypanosoma brucei soluble vacuolar pyrophosphatase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 81 | 4.69 | 5.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL414849 | — | — | 1 | 5.68 |
| CHEMBL54925 | — | — | 1 | 5.62 |
| CHEMBL370662 | — | — | 1 | 5.42 |
| CHEMBL191613 | 2,4-DICHLOROPHENYLAMINOMETHYLENEBISPHOSPHONIC ACID | — | 1 | 5.37 |
| CHEMBL55371 | — | — | 1 | 5.37 |
| CHEMBL102478 | — | — | 1 | 5.26 |
| CHEMBL196254 | — | — | 1 | 5.21 |
| CHEMBL450938 | (3-NITROPHENYLAMINO)METHYLENEDIPHOSPHONIC ACID | — | 1 | 5.19 |
| CHEMBL195034 | — | — | 1 | 5.12 |
| CHEMBL199206 | — | — | 1 | 5.10 |
| CHEMBL371456 | — | — | 1 | 5.05 |
| CHEMBL55889 | — | — | 1 | 5.01 |
| CHEMBL364728 | — | — | 1 | 5.01 |
| CHEMBL198409 | — | — | 1 | 5.01 |
| CHEMBL198826 | — | — | 1 | 5.00 |
| CHEMBL443750 | — | — | 1 | 4.99 |
| CHEMBL299988 | — | — | 1 | 4.99 |
| CHEMBL192881 | — | — | 1 | 4.95 |
| CHEMBL198126 | — | — | 1 | 4.95 |
| CHEMBL197836 | — | — | 1 | 4.91 |
| CHEMBL299491 | — | — | 1 | 4.90 |
| CHEMBL333503 | — | — | 1 | 4.88 |
| CHEMBL198380 | — | — | 1 | 4.83 |
| CHEMBL300755 | — | — | 1 | 4.79 |
| CHEMBL125188 | — | — | 1 | 4.78 |
| CHEMBL196631 | — | — | 1 | 4.76 |
| CHEMBL196554 | — | — | 1 | 4.73 |
| CHEMBL370330 | — | — | 1 | 4.72 |
| CHEMBL52761 | — | — | 1 | 4.67 |
| CHEMBL194800 | — | — | 1 | 4.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL414849 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL54925 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL370662 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL191613 | 2,4-DICHLOROPHENYLAMINOMETHYLENEBISPHOSPHONIC ACID | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL55371 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL102478 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL196254 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL450938 | (3-NITROPHENYLAMINO)METHYLENEDIPHOSPHONIC ACID | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL195034 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL199206 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL371456 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL55889 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL364728 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL198409 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL198826 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL443750 | — | IC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL299988 | — | IC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL192881 | — | IC50 | = | 11300.0 | nM | 4.95 |
| CHEMBL198126 | — | IC50 | = | 11300.0 | nM | 4.95 |
| CHEMBL197836 | — | IC50 | = | 12300.0 | nM | 4.91 |
| CHEMBL299491 | — | IC50 | = | 12700.0 | nM | 4.90 |
| CHEMBL333503 | — | IC50 | = | 13300.0 | nM | 4.88 |
| CHEMBL198380 | — | IC50 | = | 14700.0 | nM | 4.83 |
| CHEMBL300755 | — | IC50 | = | 16300.0 | nM | 4.79 |
| CHEMBL125188 | — | IC50 | = | 16700.0 | nM | 4.78 |
| CHEMBL196631 | — | IC50 | = | 17300.0 | nM | 4.76 |
| CHEMBL196554 | — | IC50 | = | 18700.0 | nM | 4.73 |
| CHEMBL370330 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL52761 | — | IC50 | = | 21500.0 | nM | 4.67 |
| CHEMBL194800 | — | IC50 | = | 24300.0 | nM | 4.61 |
| CHEMBL127588 | — | IC50 | = | 25300.0 | nM | 4.60 |
| CHEMBL199012 | — | IC50 | = | 25300.0 | nM | 4.60 |
| CHEMBL194801 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL198013 | — | IC50 | = | 28300.0 | nM | 4.55 |
| CHEMBL198439 | — | IC50 | = | 28700.0 | nM | 4.54 |
| CHEMBL381465 | — | IC50 | = | 29700.0 | nM | 4.53 |
| CHEMBL196676 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL196726 | — | IC50 | = | 35300.0 | nM | 4.45 |
| CHEMBL431139 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL434978 | — | IC50 | = | 39700.0 | nM | 4.40 |
| CHEMBL382754 | — | IC50 | = | 42700.0 | nM | 4.37 |
| CHEMBL55608 | (BUTYLAMINO)METHYLENEDIPHOSPHONIC ACID | IC50 | = | 43300.0 | nM | 4.36 |
| CHEMBL53950 | INCADRONIC ACID | IC50 | = | 44300.0 | nM | 4.35 |
| CHEMBL199254 | — | IC50 | = | 44700.0 | nM | 4.35 |
| CHEMBL192793 | — | IC50 | = | 46700.0 | nM | 4.33 |
| CHEMBL299717 | (PROPYLAMINO)METHYLENEDIPHOSPHONIC ACID | IC50 | = | 47700.0 | nM | 4.32 |
| CHEMBL110971 | — | IC50 | = | 47700.0 | nM | 4.32 |
| CHEMBL371673 | — | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL197935 | — | IC50 | = | 49700.0 | nM | 4.30 |
| CHEMBL371264 | — | IC50 | = | 52300.0 | nM | 4.28 |