Assay Detail
Binding
CHEMBL893350
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Displacement of [125I]RTI55 from human DAT expressed in COS1 cell membrane
50
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis, inhibition and binding of simple non-nitrogen inhibitors of monoamine transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 50 | 5.45 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL242338 | IODINE 2BETA-CARBOMETHOXY-3BETA-(4 IODOPHENYL)-TROPANE | -1.0 | 1 | 8.40 |
| CHEMBL388257 | — | — | 1 | 7.10 |
| CHEMBL215988 | — | — | 1 | 6.49 |
| CHEMBL397490 | — | — | 2 | 6.49 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.20 |
| CHEMBL243141 | — | — | 1 | 6.04 |
| CHEMBL242920 | — | — | 1 | 5.90 |
| CHEMBL233088 | — | — | 1 | 5.87 |
| CHEMBL245061 | — | — | 1 | 5.72 |
| CHEMBL232299 | — | — | 1 | 5.70 |
| CHEMBL395910 | — | — | 1 | 5.68 |
| CHEMBL103936 | — | — | 1 | 5.39 |
| CHEMBL396082 | — | — | 1 | 5.39 |
| CHEMBL232675 | — | — | 1 | 5.18 |
| CHEMBL243204 | — | — | 1 | 5.07 |
| CHEMBL232498 | — | — | 1 | 4.96 |
| CHEMBL232068 | — | — | 1 | 4.92 |
| CHEMBL398009 | — | — | 1 | 4.82 |
| CHEMBL388255 | — | — | 1 | 4.76 |
| CHEMBL394585 | — | — | 1 | 4.75 |
| CHEMBL396754 | — | — | 1 | 4.69 |
| CHEMBL231858 | — | — | 1 | 4.66 |
| CHEMBL396318 | — | — | 1 | 4.66 |
| CHEMBL232671 | — | — | 1 | 4.47 |
| CHEMBL232870 | — | — | 1 | 4.07 |
| CHEMBL233532 | — | — | 1 | - |
| CHEMBL394089 | — | — | 1 | - |
| CHEMBL442234 | — | — | 1 | - |
| CHEMBL233530 | — | — | 1 | - |
| CHEMBL393701 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL242338 | IODINE 2BETA-CARBOMETHOXY-3BETA-(4 IODOPHENYL)-TROPANE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL388257 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL397490 | — | Ki | = | 322.0 | nM | 6.49 |
| CHEMBL215988 | — | Ki | = | 323.0 | nM | 6.49 |
| CHEMBL370805 | COCAINE | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL243141 | — | Ki | = | 922.0 | nM | 6.04 |
| CHEMBL242920 | — | Ki | = | 1250.0 | nM | 5.90 |
| CHEMBL233088 | — | Ki | = | 1360.0 | nM | 5.87 |
| CHEMBL245061 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL232299 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL395910 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL103936 | — | Ki | = | 4060.0 | nM | 5.39 |
| CHEMBL396082 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL232675 | — | Ki | = | 6540.0 | nM | 5.18 |
| CHEMBL243204 | — | Ki | = | 8510.0 | nM | 5.07 |
| CHEMBL232498 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL232068 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL398009 | — | Ki | = | 15000.0 | nM | 4.82 |
| CHEMBL388255 | — | Ki | = | 17400.0 | nM | 4.76 |
| CHEMBL394585 | — | Ki | = | 18000.0 | nM | 4.75 |
| CHEMBL396754 | — | Ki | = | 20600.0 | nM | 4.69 |
| CHEMBL231858 | — | Ki | = | 22000.0 | nM | 4.66 |
| CHEMBL396318 | — | Ki | = | 22000.0 | nM | 4.66 |
| CHEMBL232671 | — | Ki | = | 34000.0 | nM | 4.47 |
| CHEMBL397490 | — | Ki | = | 59400.0 | nM | 4.23 |
| CHEMBL232870 | — | Ki | = | 85000.0 | nM | 4.07 |
| CHEMBL397787 | — | Ki | - | — | - | |
| CHEMBL434959 | — | Ki | = | 392000.0 | nM | - |
| CHEMBL232879 | — | Ki | = | 239000.0 | nM | - |
| CHEMBL395649 | — | Ki | = | 231000.0 | nM | - |
| CHEMBL438321 | — | Ki | = | 590000.0 | nM | - |
| CHEMBL234128 | — | Ki | = | 1050000.0 | nM | - |
| CHEMBL234127 | — | Ki | = | 630000.0 | nM | - |
| CHEMBL397520 | — | Ki | = | 1660000.0 | nM | - |
| CHEMBL232070 | — | Ki | = | 605000.0 | nM | - |
| CHEMBL232069 | — | Ki | = | 264000.0 | nM | - |
| CHEMBL232674 | — | Ki | = | 875000.0 | nM | - |
| CHEMBL232867 | — | Ki | = | 335000.0 | nM | - |
| CHEMBL233532 | — | Ki | = | 830000.0 | nM | - |
| CHEMBL232866 | — | Ki | = | 2649000.0 | nM | - |
| CHEMBL396083 | — | Ki | = | 302000.0 | nM | - |
| CHEMBL232672 | — | Ki | = | 140000.0 | nM | - |
| CHEMBL232663 | — | Ki | = | 884000.0 | nM | - |
| CHEMBL234379 | — | Ki | = | 1140000.0 | nM | - |
| CHEMBL231684 | — | Ki | = | 313000.0 | nM | - |
| CHEMBL394373 | — | Ki | = | 222000.0 | nM | - |
| CHEMBL393701 | — | Ki | = | 569000.0 | nM | - |
| CHEMBL233530 | — | Ki | = | 975000.0 | nM | - |
| CHEMBL442234 | — | Ki | = | 1180000.0 | nM | - |
| CHEMBL394089 | — | Ki | = | 766000.0 | nM | - |