Assay Detail
Binding
CHEMBL3419557
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Inhibition of Vps75-stimulated recombinant Saccharomyces cerevisiae histone acetyltransferase Rtt109 using [3H]-acetyl-CoA assessed as acetate incorporation after 30 mins by liquid scintillation counting
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Saccharomyces cerevisiae |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Histone acetyltransferase RTT109 (CHEMBL3414417) ↗| Type | SINGLE PROTEIN |
| Organism | Saccharomyces cerevisiae (strain ATCC 204508 / S288c) (Baker's yeast) |
Publication
PAINS in the assay: chemical mechanisms of assay interference and promiscuous enzymatic inhibition observed during a sulfhydryl-scavenging HTS.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 5.81 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1331211 | — | — | 1 | 6.89 |
| CHEMBL2031566 | — | — | 1 | 6.82 |
| CHEMBL3416552 | — | — | 1 | 6.58 |
| CHEMBL3416536 | — | — | 1 | 6.28 |
| CHEMBL1385343 | — | — | 1 | 6.19 |
| CHEMBL2030281 | — | — | 1 | 6.17 |
| CHEMBL3416321 | — | — | 1 | 6.11 |
| CHEMBL3416335 | — | — | 1 | 6.09 |
| CHEMBL3416526 | — | — | 1 | 5.92 |
| CHEMBL3416537 | — | — | 1 | 5.80 |
| CHEMBL3235887 | — | — | 1 | 5.77 |
| CHEMBL1600114 | — | — | 1 | 5.77 |
| CHEMBL3416316 | — | — | 1 | 5.47 |
| CHEMBL502489 | GARCINOL | — | 1 | 5.46 |
| CHEMBL3416525 | — | — | 1 | 5.41 |
| CHEMBL3416317 | — | — | 1 | 5.41 |
| CHEMBL3235890 | — | — | 1 | 5.37 |
| CHEMBL3416315 | — | — | 1 | 5.34 |
| CHEMBL1602759 | — | — | 1 | 5.21 |
| CHEMBL3416528 | — | — | 1 | 5.07 |
| CHEMBL3416307 | — | — | 1 | 4.82 |
| CHEMBL106 | FLUCONAZOLE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1331211 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2031566 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3416552 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3416536 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL1385343 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL2030281 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL3416321 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL3416335 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL3416526 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3416537 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3235887 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1600114 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3416316 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL502489 | GARCINOL | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL3416525 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL3416317 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL3235890 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL3416315 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL1602759 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL3416528 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL3416307 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL106 | FLUCONAZOLE | IC50 | - | — | - |