Assay Detail
Binding
CHEMBL5112502
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Inhibition of Cryptococcus neoformans farnesyltransferase assessed as inhibition of farnesylation of dansyl-GCVVM peptide using fluorescent peptide dansyl-GCVVM and 1uM farnesyl diphosphate as substrate by fluorescence assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cryptococcus neoformans |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Structure-Guided Discovery of Potent Antifungals that Prevent Ras Signaling by Inhibiting Protein Farnesyltransferase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.30 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5189765 | — | — | 1 | 7.40 |
| CHEMBL125162 | — | — | 1 | 7.00 |
| CHEMBL5196678 | — | — | 1 | 6.92 |
| CHEMBL5204302 | — | — | 1 | 6.82 |
| CHEMBL5174289 | — | — | 1 | 6.80 |
| CHEMBL5195805 | — | — | 1 | 6.75 |
| CHEMBL5182445 | — | — | 1 | 6.72 |
| CHEMBL5180405 | — | — | 1 | 6.68 |
| CHEMBL5171383 | — | — | 1 | 6.58 |
| CHEMBL5202247 | — | — | 1 | 6.55 |
| CHEMBL5176914 | — | — | 1 | 6.50 |
| CHEMBL5209874 | — | — | 1 | 6.47 |
| CHEMBL5179982 | — | — | 1 | 6.26 |
| CHEMBL5171138 | — | — | 1 | 6.15 |
| CHEMBL5206115 | — | — | 1 | 6.13 |
| CHEMBL5195372 | — | — | 1 | 6.04 |
| CHEMBL5182735 | — | — | 1 | 5.96 |
| CHEMBL5197720 | — | — | 1 | 5.96 |
| CHEMBL5199791 | — | — | 1 | 5.80 |
| CHEMBL5198833 | — | — | 1 | 5.72 |
| CHEMBL125648 | — | — | 1 | 5.66 |
| CHEMBL5199356 | — | — | 1 | 5.58 |
| CHEMBL5205812 | — | — | 1 | 5.57 |
| CHEMBL279433 | L-778123 FREE BASE | 1.0 | 1 | 5.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5189765 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL125162 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5196678 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5204302 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5174289 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5195805 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL5182445 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5180405 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5171383 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5202247 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL5176914 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL5209874 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5179982 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5171138 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL5206115 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL5195372 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL5182735 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5197720 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5199791 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL5198833 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL125648 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL5199356 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL5205812 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL279433 | L-778123 FREE BASE | IC50 | = | 5800.0 | nM | 5.24 |