Assay Detail
Binding
CHEMBL890218
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Inhibition of AChE in rat cortex at pH 5
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Study on dual-site inhibitors of acetylcholinesterase: Highly potent derivatives of bis- and bifunctional huperzine B.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 6.89 | 7.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL241856 | — | — | 1 | 7.93 |
| CHEMBL397232 | — | — | 1 | 7.73 |
| CHEMBL267606 | — | — | 1 | 7.70 |
| CHEMBL389375 | — | — | 1 | 7.68 |
| CHEMBL440054 | — | — | 1 | 7.64 |
| CHEMBL413240 | — | — | 1 | 7.58 |
| CHEMBL413170 | — | — | 1 | 7.47 |
| CHEMBL415423 | — | — | 1 | 7.45 |
| CHEMBL244230 | — | — | 1 | 7.42 |
| CHEMBL389779 | — | — | 1 | 7.39 |
| CHEMBL389374 | — | — | 1 | 7.38 |
| CHEMBL267591 | — | — | 1 | 7.38 |
| CHEMBL413241 | — | — | 1 | 7.30 |
| CHEMBL395282 | — | — | 1 | 7.29 |
| CHEMBL389579 | — | — | 1 | 7.28 |
| CHEMBL245081 | — | — | 1 | 7.27 |
| CHEMBL413243 | — | — | 1 | 7.25 |
| CHEMBL267836 | — | — | 1 | 7.21 |
| CHEMBL413242 | — | — | 1 | 7.18 |
| CHEMBL395280 | HUPERZINE A | 2.0 | 1 | 7.14 |
| CHEMBL245080 | — | — | 1 | 7.12 |
| CHEMBL244027 | — | — | 1 | 7.11 |
| CHEMBL242755 | — | — | 1 | 6.92 |
| CHEMBL389580 | — | — | 1 | 6.91 |
| CHEMBL263098 | — | — | 1 | 6.80 |
| CHEMBL395520 | — | — | 1 | 6.77 |
| CHEMBL438305 | — | — | 1 | 6.75 |
| CHEMBL242068 | — | — | 1 | 6.70 |
| CHEMBL395283 | — | — | 1 | 6.69 |
| CHEMBL389583 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL241856 | — | IC50 | = | 11.8 | nM | 7.93 |
| CHEMBL397232 | — | IC50 | = | 18.5 | nM | 7.73 |
| CHEMBL267606 | — | IC50 | = | 20.1 | nM | 7.70 |
| CHEMBL389375 | — | IC50 | = | 21.1 | nM | 7.68 |
| CHEMBL440054 | — | IC50 | = | 23.1 | nM | 7.64 |
| CHEMBL413240 | — | IC50 | = | 26.2 | nM | 7.58 |
| CHEMBL413170 | — | IC50 | = | 33.6 | nM | 7.47 |
| CHEMBL415423 | — | IC50 | = | 35.9 | nM | 7.45 |
| CHEMBL244230 | — | IC50 | = | 38.2 | nM | 7.42 |
| CHEMBL389779 | — | IC50 | = | 40.6 | nM | 7.39 |
| CHEMBL389374 | — | IC50 | = | 41.2 | nM | 7.38 |
| CHEMBL267591 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL413241 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL395282 | — | IC50 | = | 50.8 | nM | 7.29 |
| CHEMBL389579 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL245081 | — | IC50 | = | 53.4 | nM | 7.27 |
| CHEMBL413243 | — | IC50 | = | 56.5 | nM | 7.25 |
| CHEMBL267836 | — | IC50 | = | 62.2 | nM | 7.21 |
| CHEMBL413242 | — | IC50 | = | 65.8 | nM | 7.18 |
| CHEMBL395280 | HUPERZINE A | IC50 | = | 72.4 | nM | 7.14 |
| CHEMBL245080 | — | IC50 | = | 76.2 | nM | 7.12 |
| CHEMBL244027 | — | IC50 | = | 78.4 | nM | 7.11 |
| CHEMBL242755 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL389580 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL263098 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL395520 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL438305 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL242068 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL395283 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL389583 | — | IC50 | = | 218.0 | nM | 6.66 |
| CHEMBL413244 | — | IC50 | = | 309.0 | nM | 6.51 |
| CHEMBL263097 | — | IC50 | = | 332.0 | nM | 6.48 |
| CHEMBL389582 | — | IC50 | = | 407.0 | nM | 6.39 |
| CHEMBL413018 | — | IC50 | = | 416.0 | nM | 6.38 |
| CHEMBL395281 | — | IC50 | = | 471.0 | nM | 6.33 |
| CHEMBL395106 | — | IC50 | = | 695.0 | nM | 6.16 |
| CHEMBL397501 | — | IC50 | = | 1002.0 | nM | 6.00 |
| CHEMBL395043 | — | IC50 | = | 1005.0 | nM | 6.00 |
| CHEMBL395274 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL244870 | — | IC50 | = | 1173.0 | nM | 5.93 |
| CHEMBL244026 | — | IC50 | = | 3480.0 | nM | 5.46 |
| CHEMBL245079 | HUPERZINE B | IC50 | = | 19300.0 | nM | 4.71 |