Assay Detail
Binding
CHEMBL5442182
Review assay metadata, readout intent, target linkage, and publication context from the same page.
PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Category | PDSP assay |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
EUbOPEN Chemogenomics Library - PDSP Secondary Binding
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 39 | 6.62 | 8.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1256863 | — | — | 1 | 8.94 |
| CHEMBL1256844 | — | — | 1 | 8.86 |
| CHEMBL2164327 | — | — | 1 | 8.64 |
| CHEMBL589390 | LATREPIRDINE | 3.0 | 1 | 7.83 |
| CHEMBL540612 | — | — | 1 | 7.53 |
| CHEMBL2105760 | BREXPIPRAZOLE | 4.0 | 1 | 7.52 |
| CHEMBL2138684 | FROVATRIPTAN SUCCINATE | 4.0 | 1 | 7.44 |
| CHEMBL267777 | RITANSERIN | 2.0 | 1 | 7.33 |
| CHEMBL1200517 | DIHYDROERGOTAMINE MESYLATE | 4.0 | 1 | 7.22 |
| CHEMBL300555 | SPIROXATRINE | 2.0 | 1 | 7.18 |
| CHEMBL1200492 | NEFAZODONE HYDROCHLORIDE | 4.0 | 1 | 7.15 |
| CHEMBL2024517 | CARIPRAZINE HYDROCHLORIDE | 4.0 | 1 | 7.12 |
| CHEMBL543113 | — | — | 1 | 6.90 |
| CHEMBL1263 | SALMETEROL | 4.0 | 1 | 6.59 |
| CHEMBL1489369 | — | — | 1 | 6.56 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | 6.50 |
| CHEMBL1257131 | RAUWOLSCINE HYDROCHLORIDE | — | 1 | 6.48 |
| CHEMBL79834 | SPIRAMIDE | 2.0 | 1 | 6.47 |
| CHEMBL1200809 | AZELASTINE HYDROCHLORIDE | 4.0 | 1 | 6.41 |
| CHEMBL1633 | KETOTIFEN FUMARATE | 4.0 | 1 | 6.39 |
| CHEMBL5076314 | — | — | 1 | 6.38 |
| CHEMBL24778 | SILODOSIN | 4.0 | 1 | 6.32 |
| CHEMBL4743049 | — | — | 1 | 6.25 |
| CHEMBL1200776 | CINACALCET HYDROCHLORIDE | 4.0 | 1 | 6.24 |
| CHEMBL83894 | FANANSERIN | 2.0 | 1 | 6.13 |
| CHEMBL1615374 | VILAZODONE HYDROCHLORIDE | 4.0 | 1 | 6.10 |
| CHEMBL3342358 | — | — | 1 | 6.09 |
| CHEMBL1705 | CLONIDINE HYDROCHLORIDE | 4.0 | 1 | 6.06 |
| CHEMBL2106195 | DEXMEDETOMIDINE HYDROCHLORIDE | 4.0 | 1 | 6.04 |
| CHEMBL5089005 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1256863 | — | Ki | = | 1.157 | nM | 8.94 |
| CHEMBL1256844 | — | Ki | = | 1.378 | nM | 8.86 |
| CHEMBL2164327 | — | Ki | = | 2.302 | nM | 8.64 |
| CHEMBL589390 | LATREPIRDINE | Ki | = | 14.67 | nM | 7.83 |
| CHEMBL540612 | — | Ki | = | 29.83 | nM | 7.53 |
| CHEMBL2105760 | BREXPIPRAZOLE | Ki | = | 30.43 | nM | 7.52 |
| CHEMBL2138684 | FROVATRIPTAN SUCCINATE | Ki | = | 36.05 | nM | 7.44 |
| CHEMBL267777 | RITANSERIN | Ki | = | 47.3 | nM | 7.33 |
| CHEMBL1200517 | DIHYDROERGOTAMINE MESYLATE | Ki | = | 60.17 | nM | 7.22 |
| CHEMBL300555 | SPIROXATRINE | Ki | = | 66.12 | nM | 7.18 |
| CHEMBL1200492 | NEFAZODONE HYDROCHLORIDE | Ki | = | 70.25 | nM | 7.15 |
| CHEMBL2024517 | CARIPRAZINE HYDROCHLORIDE | Ki | = | 76.08 | nM | 7.12 |
| CHEMBL543113 | — | Ki | = | 126.22 | nM | 6.90 |
| CHEMBL1263 | SALMETEROL | Ki | = | 256.92 | nM | 6.59 |
| CHEMBL1489369 | — | Ki | = | 273.53 | nM | 6.56 |
| CHEMBL405355 | NIGULDIPINE | Ki | = | 312.96 | nM | 6.50 |
| CHEMBL1257131 | RAUWOLSCINE HYDROCHLORIDE | Ki | = | 333.46 | nM | 6.48 |
| CHEMBL79834 | SPIRAMIDE | Ki | = | 335.35 | nM | 6.47 |
| CHEMBL1200809 | AZELASTINE HYDROCHLORIDE | Ki | = | 385.48 | nM | 6.41 |
| CHEMBL1633 | KETOTIFEN FUMARATE | Ki | = | 407.28 | nM | 6.39 |
| CHEMBL5076314 | — | Ki | = | 413.9 | nM | 6.38 |
| CHEMBL24778 | SILODOSIN | Ki | = | 480.34 | nM | 6.32 |
| CHEMBL4743049 | — | Ki | = | 556.1 | nM | 6.25 |
| CHEMBL1200776 | CINACALCET HYDROCHLORIDE | Ki | = | 571.15 | nM | 6.24 |
| CHEMBL83894 | FANANSERIN | Ki | = | 744.3 | nM | 6.13 |
| CHEMBL1615374 | VILAZODONE HYDROCHLORIDE | Ki | = | 793.78 | nM | 6.10 |
| CHEMBL3342358 | — | Ki | = | 803.06 | nM | 6.09 |
| CHEMBL1705 | CLONIDINE HYDROCHLORIDE | Ki | = | 878.51 | nM | 6.06 |
| CHEMBL2106195 | DEXMEDETOMIDINE HYDROCHLORIDE | Ki | = | 922.68 | nM | 6.04 |
| CHEMBL5089005 | — | Ki | = | 1097.99 | nM | 5.96 |
| CHEMBL1215 | PHENYLEPHRINE | Ki | = | 1110.07 | nM | 5.96 |
| CHEMBL2062257 | — | Ki | = | 1108.41 | nM | 5.96 |
| CHEMBL4164059 | PITOLISANT HYDROCHLORIDE | Ki | = | 1100.4 | nM | 5.96 |
| CHEMBL5075931 | — | Ki | = | 1429.55 | nM | 5.84 |
| CHEMBL103769 | — | Ki | = | 1541.52 | nM | 5.81 |
| CHEMBL1766103 | — | Ki | = | 2179.72 | nM | 5.66 |
| CHEMBL1215661 | PRUVANSERIN | Ki | = | 2387.81 | nM | 5.62 |
| CHEMBL4743495 | — | Ki | = | 3300.27 | nM | 5.48 |
| CHEMBL3039520 | LASMIDITAN | Ki | = | 5406.92 | nM | 5.27 |