Assay Detail
Functional
CHEMBL3396802
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human kappa opioid receptor expressed in COS7 cells after 60 mins IP1 assay
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimisation of in silico derived 2-aminobenzimidazole hits as unprecedented selective kappa opioid receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 43 | 6.71 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1190199 | ASIMADOLINE | 3.0 | 1 | 9.30 |
| CHEMBL3394003 | — | — | 1 | 9.00 |
| CHEMBL3394005 | — | — | 1 | 8.70 |
| CHEMBL1449023 | — | — | 1 | 8.15 |
| CHEMBL3393991 | — | — | 1 | 8.15 |
| CHEMBL3394000 | — | — | 1 | 8.10 |
| CHEMBL3394006 | — | — | 1 | 8.00 |
| CHEMBL3393998 | — | — | 1 | 7.66 |
| CHEMBL3394004 | — | — | 1 | 7.51 |
| CHEMBL3393881 | — | — | 1 | 7.48 |
| CHEMBL3394007 | — | — | 1 | 7.43 |
| CHEMBL1488893 | — | — | 1 | 7.41 |
| CHEMBL3393993 | — | — | 1 | 7.16 |
| CHEMBL3393885 | — | — | 1 | 7.14 |
| CHEMBL3393893 | — | — | 1 | 6.93 |
| CHEMBL3393999 | — | — | 1 | 6.91 |
| CHEMBL3393994 | — | — | 1 | 6.82 |
| CHEMBL3393883 | — | — | 1 | 6.45 |
| CHEMBL3394008 | — | — | 1 | 6.40 |
| CHEMBL3393882 | — | — | 1 | 6.37 |
| CHEMBL3393891 | — | — | 1 | 6.32 |
| CHEMBL3393069 | — | — | 1 | 6.27 |
| CHEMBL3393996 | — | — | 1 | 6.13 |
| CHEMBL3394002 | — | — | 1 | 6.12 |
| CHEMBL3393879 | — | — | 1 | 6.06 |
| CHEMBL3393890 | — | — | 1 | 6.01 |
| CHEMBL3393995 | — | — | 1 | 5.98 |
| CHEMBL3393884 | — | — | 1 | 5.91 |
| CHEMBL3393880 | — | — | 1 | 5.85 |
| CHEMBL3394001 | — | — | 1 | 5.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1190199 | ASIMADOLINE | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3394003 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3394005 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1449023 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3393991 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3394000 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3394006 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3393998 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3394004 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3393881 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3394007 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL1488893 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3393993 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3393885 | — | EC50 | = | 72.0 | nM | 7.14 |
| CHEMBL3393893 | — | EC50 | = | 118.0 | nM | 6.93 |
| CHEMBL3393999 | — | EC50 | = | 122.0 | nM | 6.91 |
| CHEMBL3393994 | — | EC50 | = | 152.0 | nM | 6.82 |
| CHEMBL3393883 | — | EC50 | = | 355.0 | nM | 6.45 |
| CHEMBL3394008 | — | EC50 | = | 395.0 | nM | 6.40 |
| CHEMBL3393882 | — | EC50 | = | 423.0 | nM | 6.37 |
| CHEMBL3393891 | — | EC50 | = | 478.0 | nM | 6.32 |
| CHEMBL3393069 | — | EC50 | = | 537.0 | nM | 6.27 |
| CHEMBL3393996 | — | EC50 | = | 734.0 | nM | 6.13 |
| CHEMBL3394002 | — | EC50 | = | 765.0 | nM | 6.12 |
| CHEMBL3393879 | — | EC50 | = | 878.0 | nM | 6.06 |
| CHEMBL3393890 | — | EC50 | = | 970.0 | nM | 6.01 |
| CHEMBL3393995 | — | EC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL3393884 | — | EC50 | = | 1225.0 | nM | 5.91 |
| CHEMBL3393880 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3394001 | — | EC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL3393989 | — | EC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL3393886 | — | EC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL3393990 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1427072 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3393992 | — | EC50 | = | 2050.0 | nM | 5.69 |
| CHEMBL3393988 | — | EC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3393987 | — | EC50 | = | 2950.0 | nM | 5.53 |
| CHEMBL3393887 | — | EC50 | = | 4250.0 | nM | 5.37 |
| CHEMBL3393070 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3393888 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3393889 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3393997 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3393892 | — | EC50 | > | 10000.0 | nM | - |