Assay Detail
Binding
CHEMBL805320
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Binding affinity against Serotonin transporter (SERT) labelled with [125I]RTI-55 in rat.
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 35 | 6.77 | 8.76 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL341692 | — | — | 1 | 8.76 |
| CHEMBL145903 | — | — | 1 | 7.57 |
| CHEMBL147933 | — | — | 1 | 7.33 |
| CHEMBL357295 | — | — | 1 | 7.17 |
| CHEMBL358521 | — | — | 1 | 7.14 |
| CHEMBL149565 | — | — | 1 | 7.13 |
| CHEMBL26477 | — | — | 1 | 7.07 |
| CHEMBL43124 | — | — | 1 | 7.05 |
| CHEMBL146255 | — | — | 1 | 7.02 |
| CHEMBL148441 | — | — | 1 | 7.00 |
| CHEMBL149013 | — | — | 1 | 7.00 |
| CHEMBL146370 | — | — | 1 | 6.95 |
| CHEMBL417660 | — | — | 1 | 6.93 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 6.90 |
| CHEMBL286991 | — | — | 1 | 6.87 |
| CHEMBL26478 | — | — | 1 | 6.87 |
| CHEMBL149437 | — | — | 1 | 6.80 |
| CHEMBL146321 | — | — | 1 | 6.76 |
| CHEMBL422499 | — | — | 1 | 6.75 |
| CHEMBL149014 | — | — | 1 | 6.72 |
| CHEMBL146372 | — | — | 1 | 6.69 |
| CHEMBL283662 | — | — | 1 | 6.67 |
| CHEMBL356380 | — | — | 1 | 6.63 |
| CHEMBL146259 | — | — | 1 | 6.47 |
| CHEMBL347517 | — | — | 1 | 6.35 |
| CHEMBL356783 | — | — | 1 | 6.35 |
| CHEMBL278242 | — | — | 1 | 6.34 |
| CHEMBL421948 | — | — | 1 | 6.26 |
| CHEMBL26320 | — | — | 1 | 6.21 |
| CHEMBL28821 | — | — | 1 | 6.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL341692 | — | Ki | = | 1.73 | nM | 8.76 |
| CHEMBL145903 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL147933 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL357295 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL358521 | — | Ki | = | 72.2 | nM | 7.14 |
| CHEMBL149565 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL26477 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL43124 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL146255 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL148441 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL149013 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL146370 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL417660 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL281594 | VANOXERINE | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL26478 | — | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL286991 | — | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL149437 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL146321 | — | Ki | = | 174.0 | nM | 6.76 |
| CHEMBL422499 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL149014 | — | Ki | = | 191.0 | nM | 6.72 |
| CHEMBL146372 | — | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL283662 | — | Ki | = | 215.0 | nM | 6.67 |
| CHEMBL356380 | — | Ki | = | 232.0 | nM | 6.63 |
| CHEMBL146259 | — | Ki | = | 339.0 | nM | 6.47 |
| CHEMBL347517 | — | Ki | = | 448.0 | nM | 6.35 |
| CHEMBL356783 | — | Ki | = | 449.0 | nM | 6.35 |
| CHEMBL278242 | — | Ki | = | 461.0 | nM | 6.34 |
| CHEMBL421948 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL26320 | — | Ki | = | 623.0 | nM | 6.21 |
| CHEMBL28821 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL146478 | — | Ki | = | 701.0 | nM | 6.15 |
| CHEMBL145942 | — | Ki | = | 894.0 | nM | 6.05 |
| CHEMBL149622 | — | Ki | = | 939.0 | nM | 6.03 |
| CHEMBL27907 | — | Ki | = | 1310.0 | nM | 5.88 |
| CHEMBL146547 | — | Ki | = | 869000.0 | nM | - |