Assay Detail
Functional
CHEMBL785240
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Reuptake inhibition of [3H]-5-HT (5-HT) in rat.
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Oxygenated analogues of 1-[2-(Diphenylmethoxy)ethyl]- and 1-[2-[Bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as potential extended-action cocaine-abuse therapeutic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 6.30 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL417660 | — | — | 1 | 7.16 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 7.14 |
| CHEMBL26477 | — | — | 1 | 7.00 |
| CHEMBL149565 | — | — | 1 | 6.95 |
| CHEMBL26478 | — | — | 1 | 6.75 |
| CHEMBL146255 | — | — | 1 | 6.66 |
| CHEMBL147933 | — | — | 1 | 6.65 |
| CHEMBL358521 | — | — | 1 | 6.59 |
| CHEMBL149013 | — | — | 1 | 6.58 |
| CHEMBL146321 | — | — | 1 | 6.53 |
| CHEMBL26320 | — | — | 1 | 6.53 |
| CHEMBL149014 | — | — | 1 | 6.47 |
| CHEMBL357295 | — | — | 1 | 6.41 |
| CHEMBL43124 | — | — | 1 | 6.41 |
| CHEMBL145903 | — | — | 1 | 6.40 |
| CHEMBL283662 | — | — | 1 | 6.34 |
| CHEMBL146370 | — | — | 1 | 6.33 |
| CHEMBL356380 | — | — | 1 | 6.31 |
| CHEMBL149437 | — | — | 1 | 6.30 |
| CHEMBL286991 | — | — | 1 | 6.24 |
| CHEMBL145942 | — | — | 1 | 6.06 |
| CHEMBL422499 | — | — | 1 | 6.06 |
| CHEMBL356783 | — | — | 1 | 6.05 |
| CHEMBL421948 | — | — | 1 | 6.01 |
| CHEMBL146547 | — | — | 1 | 5.96 |
| CHEMBL149622 | — | — | 1 | 5.96 |
| CHEMBL146259 | — | — | 1 | 5.93 |
| CHEMBL148441 | — | — | 1 | 5.93 |
| CHEMBL347517 | — | — | 1 | 5.84 |
| CHEMBL28821 | — | — | 1 | 5.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL417660 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL281594 | VANOXERINE | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL26477 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL149565 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL26478 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL146255 | — | IC50 | = | 219.0 | nM | 6.66 |
| CHEMBL147933 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL358521 | — | IC50 | = | 258.0 | nM | 6.59 |
| CHEMBL149013 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL146321 | — | IC50 | = | 297.0 | nM | 6.53 |
| CHEMBL26320 | — | IC50 | = | 298.0 | nM | 6.53 |
| CHEMBL149014 | — | IC50 | = | 342.0 | nM | 6.47 |
| CHEMBL357295 | — | IC50 | = | 391.0 | nM | 6.41 |
| CHEMBL43124 | — | IC50 | = | 392.0 | nM | 6.41 |
| CHEMBL145903 | — | IC50 | = | 397.0 | nM | 6.40 |
| CHEMBL283662 | — | IC50 | = | 452.0 | nM | 6.34 |
| CHEMBL146370 | — | IC50 | = | 473.0 | nM | 6.33 |
| CHEMBL356380 | — | IC50 | = | 494.0 | nM | 6.31 |
| CHEMBL149437 | — | IC50 | = | 499.0 | nM | 6.30 |
| CHEMBL286991 | — | IC50 | = | 576.0 | nM | 6.24 |
| CHEMBL145942 | — | IC50 | = | 872.0 | nM | 6.06 |
| CHEMBL422499 | — | IC50 | = | 866.0 | nM | 6.06 |
| CHEMBL356783 | — | IC50 | = | 881.0 | nM | 6.05 |
| CHEMBL421948 | — | IC50 | = | 982.0 | nM | 6.01 |
| CHEMBL146547 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL149622 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL146259 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL148441 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL347517 | — | IC50 | = | 1430.0 | nM | 5.84 |
| CHEMBL28821 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL146372 | — | IC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL278242 | — | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL146478 | — | IC50 | = | 1920.0 | nM | 5.72 |
| CHEMBL27907 | — | IC50 | = | 2990.0 | nM | 5.52 |