Assay Detail
Binding
CHEMBL1696307
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Pdr5p-mediated rhodamine 6G transport in Saccharomyces cerevisiae MKPDR5h plasma membrane by spectrofluorometric assay
23
Total Activities
23
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
Pleiotropic ABC efflux transporter of multiple drugs (CHEMBL1697658) ↗| Type | SINGLE PROTEIN |
| Organism | Saccharomyces cerevisiae S288c |
Publication
New high-throughput screening assay to reveal similarities and differences in inhibitory sensitivities of multidrug ATP-binding cassette transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 5.41 | 6.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1688548 | — | — | 1 | 6.16 |
| CHEMBL1688549 | — | — | 1 | 5.89 |
| CHEMBL479 | THIORIDAZINE | 4.0 | 1 | 5.89 |
| CHEMBL567 | PERPHENAZINE | 4.0 | 1 | 5.85 |
| CHEMBL422 | TRIFLUOPERAZINE | 4.0 | 1 | 5.85 |
| CHEMBL726 | FLUPHENAZINE | 4.0 | 1 | 5.77 |
| CHEMBL728 | PROCHLORPERAZINE | 4.0 | 1 | 5.77 |
| CHEMBL1378 | THIETHYLPERAZINE | 4.0 | 1 | 5.64 |
| CHEMBL1688550 | — | — | 1 | 5.51 |
| CHEMBL824 | NOR2-CHLORPROMAZINE | — | 1 | 5.50 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 1 | 5.35 |
| CHEMBL570 | TRIFLUPROMAZINE | 4.0 | 1 | 5.31 |
| CHEMBL908 | CHLORPROTHIXENE | 4.0 | 1 | 5.29 |
| CHEMBL1688551 | — | — | 1 | 5.19 |
| CHEMBL288110 | — | — | 1 | 5.13 |
| CHEMBL1323355 | DEXTROMEPROMAZINE | — | 1 | 5.05 |
| CHEMBL1764 | LEVOMEPROMAZINE | 4.0 | 1 | 5.02 |
| CHEMBL1620412 | DIETHAZINE | 2.0 | 1 | 4.99 |
| CHEMBL564 | PROMAZINE | 4.0 | 1 | 4.95 |
| CHEMBL643 | PROMETHAZINE | 4.0 | 1 | 4.75 |
| CHEMBL11 | IMIPRAMINE | 4.0 | 1 | 4.66 |
| CHEMBL828 | PHENOTHIAZINE | 2.0 | 1 | - |
| CHEMBL418995 | AMINEPTINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1688548 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL1688549 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL479 | THIORIDAZINE | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL567 | PERPHENAZINE | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL422 | TRIFLUOPERAZINE | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL726 | FLUPHENAZINE | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL728 | PROCHLORPERAZINE | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1378 | THIETHYLPERAZINE | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL1688550 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL824 | NOR2-CHLORPROMAZINE | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL71 | CHLORPROMAZINE | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL570 | TRIFLUPROMAZINE | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL908 | CHLORPROTHIXENE | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL1688551 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL288110 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL1323355 | DEXTROMEPROMAZINE | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL1764 | LEVOMEPROMAZINE | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL1620412 | DIETHAZINE | IC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL564 | PROMAZINE | IC50 | = | 11300.0 | nM | 4.95 |
| CHEMBL643 | PROMETHAZINE | IC50 | = | 17700.0 | nM | 4.75 |
| CHEMBL11 | IMIPRAMINE | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL828 | PHENOTHIAZINE | IC50 | > | 400000.0 | nM | - |
| CHEMBL418995 | AMINEPTINE | IC50 | > | 400000.0 | nM | - |