Assay Detail
Binding
CHEMBL1909094
Review assay metadata, readout intent, target linkage, and publication context from the same page.
DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | MDCK |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
DrugMatrix in vitro pharmacology data
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 871 | 5.77 | 8.49 |
| Ki | 871 | 5.77 | 8.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL445 | NORTRIPTYLINE | 4.0 | 2 | 8.50 |
| CHEMBL1113 | AMOXAPINE | 4.0 | 2 | 7.89 |
| CHEMBL564 | PROMAZINE | 4.0 | 2 | 7.89 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 2 | 7.72 |
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 2 | 7.66 |
| CHEMBL1628227 | DOXEPIN | 4.0 | 2 | 7.54 |
| CHEMBL21731 | MAPROTILINE | 4.0 | 2 | 7.52 |
| CHEMBL415 | CLOMIPRAMINE | 4.0 | 2 | 7.16 |
| CHEMBL490 | PAROXETINE | 4.0 | 2 | 7.07 |
| CHEMBL6437 | MIANSERIN | 4.0 | 2 | 6.79 |
| CHEMBL81 | RALOXIFENE | 4.0 | 2 | 6.55 |
| CHEMBL19215 | METERGOLINE | 2.0 | 2 | 6.44 |
| CHEMBL926 | DOBUTAMINE | 4.0 | 2 | 6.42 |
| CHEMBL728 | PROCHLORPERAZINE | 4.0 | 2 | 6.40 |
| CHEMBL1909072 | PIPAMAZINE | 4.0 | 2 | 6.35 |
| CHEMBL305660 | EBASTINE | 4.0 | 2 | 6.34 |
| CHEMBL828 | PHENOTHIAZINE | 2.0 | 2 | 6.34 |
| CHEMBL95 | TACRINE | 4.0 | 2 | 6.29 |
| CHEMBL723 | CARVEDILOL | 4.0 | 2 | 6.27 |
| CHEMBL516 | CYPROHEPTADINE | 4.0 | 2 | 6.25 |
| CHEMBL1333512 | N,N'-DIPHENYL-P-PHENYLENEDIAMINE | — | 2 | 6.11 |
| CHEMBL1670 | MITOTANE | 4.0 | 2 | 6.09 |
| CHEMBL954 | ENCLOMIPHENE | 3.0 | 2 | 6.07 |
| CHEMBL221753 | BENZETHONIUM CHLORIDE | 2.0 | 2 | 6.05 |
| CHEMBL508338 | THIMEROSAL | 3.0 | 2 | 6.04 |
| CHEMBL691 | ETHINYL ESTRADIOL | 4.0 | 2 | 6.02 |
| CHEMBL809 | SERTRALINE | 4.0 | 2 | 6.01 |
| CHEMBL1601669 | ALFACALCIDOL | 3.0 | 2 | 6.00 |
| CHEMBL115769 | — | — | 2 | 5.97 |
| CHEMBL1172 | DESLORATADINE | 4.0 | 2 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL445 | NORTRIPTYLINE | Ki | = | 3.184 | nM | 8.50 |
| CHEMBL445 | NORTRIPTYLINE | IC50 | = | 3.21 | nM | 8.49 |
| CHEMBL1113 | AMOXAPINE | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1113 | AMOXAPINE | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL564 | PROMAZINE | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL564 | PROMAZINE | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL71 | CHLORPROMAZINE | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL629 | AMITRIPTYLINE | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL629 | AMITRIPTYLINE | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1628227 | DOXEPIN | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1628227 | DOXEPIN | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL21731 | MAPROTILINE | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL21731 | MAPROTILINE | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL415 | CLOMIPRAMINE | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL415 | CLOMIPRAMINE | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL490 | PAROXETINE | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL490 | PAROXETINE | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL6437 | MIANSERIN | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL6437 | MIANSERIN | Ki | = | 161.0 | nM | 6.79 |
| CHEMBL81 | RALOXIFENE | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL81 | RALOXIFENE | IC50 | = | 282.0 | nM | 6.55 |
| CHEMBL19215 | METERGOLINE | IC50 | = | 366.0 | nM | 6.44 |
| CHEMBL19215 | METERGOLINE | Ki | = | 363.0 | nM | 6.44 |
| CHEMBL926 | DOBUTAMINE | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL926 | DOBUTAMINE | IC50 | = | 383.0 | nM | 6.42 |
| CHEMBL728 | PROCHLORPERAZINE | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL728 | PROCHLORPERAZINE | Ki | = | 396.0 | nM | 6.40 |
| CHEMBL1909072 | PIPAMAZINE | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL1909072 | PIPAMAZINE | Ki | = | 446.0 | nM | 6.35 |
| CHEMBL305660 | EBASTINE | IC50 | = | 460.3 | nM | 6.34 |
| CHEMBL828 | PHENOTHIAZINE | IC50 | = | 461.0 | nM | 6.34 |
| CHEMBL828 | PHENOTHIAZINE | Ki | = | 457.0 | nM | 6.34 |
| CHEMBL305660 | EBASTINE | Ki | = | 456.4 | nM | 6.34 |
| CHEMBL95 | TACRINE | Ki | = | 513.0 | nM | 6.29 |
| CHEMBL95 | TACRINE | IC50 | = | 517.0 | nM | 6.29 |
| CHEMBL723 | CARVEDILOL | IC50 | = | 538.0 | nM | 6.27 |
| CHEMBL723 | CARVEDILOL | Ki | = | 533.0 | nM | 6.27 |
| CHEMBL516 | CYPROHEPTADINE | IC50 | = | 564.0 | nM | 6.25 |
| CHEMBL516 | CYPROHEPTADINE | Ki | = | 559.0 | nM | 6.25 |
| CHEMBL1333512 | N,N'-DIPHENYL-P-PHENYLENEDIAMINE | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL1333512 | N,N'-DIPHENYL-P-PHENYLENEDIAMINE | IC50 | = | 786.0 | nM | 6.11 |
| CHEMBL1670 | MITOTANE | IC50 | = | 819.0 | nM | 6.09 |
| CHEMBL1670 | MITOTANE | Ki | = | 812.0 | nM | 6.09 |
| CHEMBL954 | ENCLOMIPHENE | Ki | = | 855.0 | nM | 6.07 |
| CHEMBL954 | ENCLOMIPHENE | IC50 | = | 862.0 | nM | 6.06 |
| CHEMBL221753 | BENZETHONIUM CHLORIDE | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL221753 | BENZETHONIUM CHLORIDE | IC50 | = | 907.0 | nM | 6.04 |
| CHEMBL508338 | THIMEROSAL | Ki | = | 923.0 | nM | 6.04 |
| CHEMBL508338 | THIMEROSAL | IC50 | = | 931.0 | nM | 6.03 |