Assay Detail
Binding
CHEMBL1769751
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of equine BChE incubated with compounf for 5 mins before addition of substrate S-butyrylthiocholine iodide by Ellman's method
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Equus caballus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis and structure-activity relationship (SAR) studies of 2,4-disubstituted pyrimidine derivatives: dual activity as cholinesterase and Aβ-aggregation inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 5.24 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL32823 | — | — | 1 | 8.00 |
| CHEMBL1677 | TACRINE HYDROCHLORIDE | 4.0 | 1 | 7.72 |
| CHEMBL1766151 | — | — | 1 | 5.66 |
| CHEMBL1084213 | — | — | 1 | 5.58 |
| CHEMBL1082977 | — | — | 1 | 5.47 |
| CHEMBL1766019 | — | — | 1 | 5.47 |
| CHEMBL1678 | DONEPEZIL HYDROCHLORIDE | 4.0 | 1 | 5.44 |
| CHEMBL1086014 | — | — | 1 | 5.21 |
| CHEMBL1766020 | — | — | 1 | 5.19 |
| CHEMBL1766144 | — | — | 1 | 5.14 |
| CHEMBL1766018 | — | — | 1 | 5.12 |
| CHEMBL1766146 | — | — | 1 | 5.09 |
| CHEMBL1084210 | — | — | 1 | 5.05 |
| CHEMBL1766142 | — | — | 1 | 4.97 |
| CHEMBL1555 | GALANTAMINE HYDROBROMIDE | 4.0 | 1 | 4.90 |
| CHEMBL1082978 | — | — | 1 | 4.86 |
| CHEMBL1766143 | — | — | 1 | 4.84 |
| CHEMBL1082981 | — | — | 1 | 4.75 |
| CHEMBL1085780 | — | — | 1 | 4.58 |
| CHEMBL1084211 | — | — | 1 | 4.55 |
| CHEMBL1084212 | — | — | 1 | 4.46 |
| CHEMBL1766139 | — | — | 1 | 4.22 |
| CHEMBL1085781 | — | — | 1 | 4.17 |
| CHEMBL1082979 | — | — | 1 | - |
| CHEMBL1766141 | — | — | 1 | - |
| CHEMBL1766140 | — | — | 1 | - |
| CHEMBL1766149 | — | — | 1 | - |
| CHEMBL1082980 | — | — | 1 | - |
| CHEMBL1085505 | — | — | 1 | - |
| CHEMBL1766150 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL32823 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1677 | TACRINE HYDROCHLORIDE | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1766151 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL1084213 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL1082977 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL1766019 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL1678 | DONEPEZIL HYDROCHLORIDE | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL1086014 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL1766020 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL1766144 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL1766018 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL1766146 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL1084210 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL1766142 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL1555 | GALANTAMINE HYDROBROMIDE | IC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL1082978 | — | IC50 | = | 13800.0 | nM | 4.86 |
| CHEMBL1766143 | — | IC50 | = | 14300.0 | nM | 4.84 |
| CHEMBL1082981 | — | IC50 | = | 17700.0 | nM | 4.75 |
| CHEMBL1085780 | — | IC50 | = | 26400.0 | nM | 4.58 |
| CHEMBL1084211 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL1084212 | — | IC50 | = | 34700.0 | nM | 4.46 |
| CHEMBL1766139 | — | IC50 | = | 59900.0 | nM | 4.22 |
| CHEMBL1085781 | — | IC50 | = | 68300.0 | nM | 4.17 |
| CHEMBL1766148 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1766147 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1084808 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1766145 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1766016 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1766017 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1766150 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1085505 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1082980 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1766149 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1766140 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1766141 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1082979 | — | IC50 | > | 100000.0 | nM | - |