Assay Detail
Binding
CHEMBL1769750
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human AChE incubated with compounf for 5 mins before addition of substrate acetylthiocholine iodide by Ellman's method
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 5.02 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL32823 | — | — | 1 | 8.40 |
| CHEMBL1678 | DONEPEZIL HYDROCHLORIDE | 4.0 | 1 | 7.50 |
| CHEMBL1677 | TACRINE HYDROCHLORIDE | 4.0 | 1 | 7.03 |
| CHEMBL1555 | GALANTAMINE HYDROBROMIDE | 4.0 | 1 | 5.42 |
| CHEMBL1084210 | — | — | 1 | 5.26 |
| CHEMBL1085780 | — | — | 1 | 5.06 |
| CHEMBL1082981 | — | — | 1 | 5.06 |
| CHEMBL1082978 | — | — | 1 | 5.01 |
| CHEMBL1766146 | — | — | 1 | 4.91 |
| CHEMBL1766147 | — | — | 1 | 4.90 |
| CHEMBL1084212 | — | — | 1 | 4.89 |
| CHEMBL1085781 | — | — | 1 | 4.85 |
| CHEMBL1766020 | — | — | 1 | 4.85 |
| CHEMBL1084211 | — | — | 1 | 4.83 |
| CHEMBL1766139 | — | — | 1 | 4.82 |
| CHEMBL1766149 | — | — | 1 | 4.81 |
| CHEMBL1766016 | — | — | 1 | 4.78 |
| CHEMBL1084213 | — | — | 1 | 4.76 |
| CHEMBL1082977 | — | — | 1 | 4.74 |
| CHEMBL1766017 | — | — | 1 | 4.73 |
| CHEMBL1085505 | — | — | 1 | 4.71 |
| CHEMBL1766142 | — | — | 1 | 4.70 |
| CHEMBL1766150 | — | — | 1 | 4.70 |
| CHEMBL1082980 | — | — | 1 | 4.69 |
| CHEMBL1766144 | — | — | 1 | 4.67 |
| CHEMBL1766018 | — | — | 1 | 4.64 |
| CHEMBL1086014 | — | — | 1 | 4.63 |
| CHEMBL1766148 | — | — | 1 | 4.62 |
| CHEMBL1084808 | — | — | 1 | 4.60 |
| CHEMBL1766019 | — | — | 1 | 4.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL32823 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1678 | DONEPEZIL HYDROCHLORIDE | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1677 | TACRINE HYDROCHLORIDE | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL1555 | GALANTAMINE HYDROBROMIDE | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL1084210 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL1085780 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL1082981 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL1082978 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL1766146 | — | IC50 | = | 12400.0 | nM | 4.91 |
| CHEMBL1766147 | — | IC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL1084212 | — | IC50 | = | 12800.0 | nM | 4.89 |
| CHEMBL1085781 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL1766020 | — | IC50 | = | 14200.0 | nM | 4.85 |
| CHEMBL1084211 | — | IC50 | = | 14700.0 | nM | 4.83 |
| CHEMBL1766139 | — | IC50 | = | 15300.0 | nM | 4.82 |
| CHEMBL1766149 | — | IC50 | = | 15500.0 | nM | 4.81 |
| CHEMBL1766016 | — | IC50 | = | 16600.0 | nM | 4.78 |
| CHEMBL1084213 | — | IC50 | = | 17500.0 | nM | 4.76 |
| CHEMBL1082977 | — | IC50 | = | 18400.0 | nM | 4.74 |
| CHEMBL1766017 | — | IC50 | = | 18800.0 | nM | 4.73 |
| CHEMBL1085505 | — | IC50 | = | 19700.0 | nM | 4.71 |
| CHEMBL1766142 | — | IC50 | = | 20200.0 | nM | 4.70 |
| CHEMBL1766150 | — | IC50 | = | 19900.0 | nM | 4.70 |
| CHEMBL1082980 | — | IC50 | = | 20400.0 | nM | 4.69 |
| CHEMBL1766144 | — | IC50 | = | 21600.0 | nM | 4.67 |
| CHEMBL1766018 | — | IC50 | = | 22900.0 | nM | 4.64 |
| CHEMBL1086014 | — | IC50 | = | 23200.0 | nM | 4.63 |
| CHEMBL1766148 | — | IC50 | = | 24200.0 | nM | 4.62 |
| CHEMBL1084808 | — | IC50 | = | 24900.0 | nM | 4.60 |
| CHEMBL1766019 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL1766151 | — | IC50 | = | 25800.0 | nM | 4.59 |
| CHEMBL1766143 | — | IC50 | = | 25500.0 | nM | 4.59 |
| CHEMBL1766140 | — | IC50 | = | 26400.0 | nM | 4.58 |
| CHEMBL1082979 | — | IC50 | = | 26400.0 | nM | 4.58 |
| CHEMBL1766141 | — | IC50 | = | 26700.0 | nM | 4.57 |
| CHEMBL1766145 | — | IC50 | = | 28800.0 | nM | 4.54 |