Assay Detail
Binding
CHEMBL5442185
Review assay metadata, readout intent, target linkage, and publication context from the same page.
PDSP Secondary Binding target: TMEM97 - 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.
74
Total Activities
74
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 | 74 | 6.30 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4164059 | PITOLISANT HYDROCHLORIDE | 4.0 | 1 | 8.15 |
| CHEMBL1256844 | — | — | 1 | 7.99 |
| CHEMBL1200809 | AZELASTINE HYDROCHLORIDE | 4.0 | 1 | 7.50 |
| CHEMBL1263 | SALMETEROL | 4.0 | 1 | 7.49 |
| CHEMBL1707 | LOPERAMIDE HYDROCHLORIDE | 4.0 | 1 | 7.44 |
| CHEMBL4750757 | — | — | 1 | 7.43 |
| CHEMBL1516474 | TEGASEROD MALEATE | 4.0 | 1 | 7.24 |
| CHEMBL2018875 | — | — | 1 | 7.20 |
| CHEMBL2105760 | BREXPIPRAZOLE | 4.0 | 1 | 7.20 |
| CHEMBL1256998 | — | — | 1 | 7.19 |
| CHEMBL2107572 | TECALCET HYDROCHLORIDE | 2.0 | 1 | 7.13 |
| CHEMBL1095777 | INDACATEROL | 4.0 | 1 | 6.97 |
| CHEMBL540612 | — | — | 1 | 6.95 |
| CHEMBL103769 | — | — | 1 | 6.82 |
| CHEMBL1722209 | TOLTERODINE TARTRATE | 4.0 | 1 | 6.78 |
| CHEMBL3039520 | LASMIDITAN | 4.0 | 1 | 6.74 |
| CHEMBL214957 | — | — | 1 | 6.73 |
| CHEMBL3215877 | — | — | 1 | 6.70 |
| CHEMBL21283 | — | — | 1 | 6.69 |
| CHEMBL74355 | VOLINANSERIN | 3.0 | 1 | 6.69 |
| CHEMBL1200492 | NEFAZODONE HYDROCHLORIDE | 4.0 | 1 | 6.65 |
| CHEMBL2030155 | — | — | 1 | 6.62 |
| CHEMBL445102 | — | — | 1 | 6.57 |
| CHEMBL5076917 | — | — | 1 | 6.51 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | 6.49 |
| CHEMBL267777 | RITANSERIN | 2.0 | 1 | 6.47 |
| CHEMBL1671 | PROPRANOLOL HYDROCHLORIDE | 4.0 | 1 | 6.45 |
| CHEMBL1633 | KETOTIFEN FUMARATE | 4.0 | 1 | 6.44 |
| CHEMBL1200776 | CINACALCET HYDROCHLORIDE | 4.0 | 1 | 6.41 |
| CHEMBL3675743 | — | — | 1 | 6.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4164059 | PITOLISANT HYDROCHLORIDE | Ki | = | 7.014 | nM | 8.15 |
| CHEMBL1256844 | — | Ki | = | 10.15 | nM | 7.99 |
| CHEMBL1200809 | AZELASTINE HYDROCHLORIDE | Ki | = | 31.96 | nM | 7.50 |
| CHEMBL1263 | SALMETEROL | Ki | = | 32.43 | nM | 7.49 |
| CHEMBL1707 | LOPERAMIDE HYDROCHLORIDE | Ki | = | 36.68 | nM | 7.44 |
| CHEMBL4750757 | — | Ki | = | 37.03 | nM | 7.43 |
| CHEMBL1516474 | TEGASEROD MALEATE | Ki | = | 57.24 | nM | 7.24 |
| CHEMBL2018875 | — | Ki | = | 63.38 | nM | 7.20 |
| CHEMBL2105760 | BREXPIPRAZOLE | Ki | = | 63.01 | nM | 7.20 |
| CHEMBL1256998 | — | Ki | = | 64.77 | nM | 7.19 |
| CHEMBL2107572 | TECALCET HYDROCHLORIDE | Ki | = | 74.59 | nM | 7.13 |
| CHEMBL1095777 | INDACATEROL | Ki | = | 106.86 | nM | 6.97 |
| CHEMBL540612 | — | Ki | = | 112.99 | nM | 6.95 |
| CHEMBL103769 | — | Ki | = | 153.25 | nM | 6.82 |
| CHEMBL1722209 | TOLTERODINE TARTRATE | Ki | = | 166.94 | nM | 6.78 |
| CHEMBL3039520 | LASMIDITAN | Ki | = | 184.06 | nM | 6.74 |
| CHEMBL214957 | — | Ki | = | 185.35 | nM | 6.73 |
| CHEMBL3215877 | — | Ki | = | 197.74 | nM | 6.70 |
| CHEMBL21283 | — | Ki | = | 205.54 | nM | 6.69 |
| CHEMBL74355 | VOLINANSERIN | Ki | = | 204.97 | nM | 6.69 |
| CHEMBL1200492 | NEFAZODONE HYDROCHLORIDE | Ki | = | 221.95 | nM | 6.65 |
| CHEMBL2030155 | — | Ki | = | 242.1 | nM | 6.62 |
| CHEMBL445102 | — | Ki | = | 269.12 | nM | 6.57 |
| CHEMBL5076917 | — | Ki | = | 308.67 | nM | 6.51 |
| CHEMBL405355 | NIGULDIPINE | Ki | = | 327.64 | nM | 6.49 |
| CHEMBL267777 | RITANSERIN | Ki | = | 339.35 | nM | 6.47 |
| CHEMBL1671 | PROPRANOLOL HYDROCHLORIDE | Ki | = | 352.9 | nM | 6.45 |
| CHEMBL1633 | KETOTIFEN FUMARATE | Ki | = | 365.88 | nM | 6.44 |
| CHEMBL1200776 | CINACALCET HYDROCHLORIDE | Ki | = | 388.24 | nM | 6.41 |
| CHEMBL3675743 | — | Ki | = | 488.65 | nM | 6.31 |
| CHEMBL2024517 | CARIPRAZINE HYDROCHLORIDE | Ki | = | 488.09 | nM | 6.31 |
| CHEMBL281350 | SB-224289 | Ki | = | 502.11 | nM | 6.30 |
| CHEMBL259656 | — | Ki | = | 508.86 | nM | 6.29 |
| CHEMBL254129 | CYCLOPAMINE | Ki | = | 598.68 | nM | 6.22 |
| CHEMBL542139 | — | Ki | = | 662.9 | nM | 6.18 |
| CHEMBL225155 | — | Ki | = | 671.81 | nM | 6.17 |
| CHEMBL5075931 | — | Ki | = | 674.99 | nM | 6.17 |
| CHEMBL531742 | — | Ki | = | 700.49 | nM | 6.16 |
| CHEMBL5089005 | — | Ki | = | 693.96 | nM | 6.16 |
| CHEMBL1474387 | — | Ki | = | 701.29 | nM | 6.15 |
| CHEMBL1256876 | — | Ki | = | 754.48 | nM | 6.12 |
| CHEMBL79834 | SPIRAMIDE | Ki | = | 899.29 | nM | 6.05 |
| CHEMBL16192 | CP-96345 | Ki | = | 906.25 | nM | 6.04 |
| CHEMBL5076314 | — | Ki | = | 936.26 | nM | 6.03 |
| CHEMBL567303 | PALOSURAN | Ki | = | 955.87 | nM | 6.02 |
| CHEMBL300555 | SPIROXATRINE | Ki | = | 1009.95 | nM | 6.00 |
| CHEMBL344159 | TOLVAPTAN | Ki | = | 1031.22 | nM | 5.99 |
| CHEMBL4743495 | — | Ki | = | 1056.17 | nM | 5.98 |
| CHEMBL113142 | ZM-241385 | Ki | = | 1067.09 | nM | 5.97 |
| CHEMBL1615374 | VILAZODONE HYDROCHLORIDE | Ki | = | 1089.05 | nM | 5.96 |