Assay Detail
Binding
CHEMBL5161377
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Ca2+/ CAM stimulated human AC8 activity expressed in AC3 and AC6-knockout HEK293 cells assessed as A23187 stimulated cAMP accumulation incubated for 30 mins followed by A2318 stimulation in presence of IBMX for 1 hr by HTRF assay
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimization of a Pyrimidinone Series for Selective Inhibition of Ca<sup>2+</sup>/Calmodulin-Stimulated Adenylyl Cyclase 1 Activity for the Treatment of Chronic Pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 5.61 | 6.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5190252 | — | — | 1 | 6.42 |
| CHEMBL5170189 | — | — | 1 | 6.24 |
| CHEMBL5195432 | — | — | 1 | 6.16 |
| CHEMBL5182403 | — | — | 1 | 6.15 |
| CHEMBL5178772 | — | — | 1 | 6.11 |
| CHEMBL5187427 | — | — | 1 | 6.00 |
| CHEMBL5205425 | — | — | 1 | 6.00 |
| CHEMBL2098167 | — | — | 1 | 5.92 |
| CHEMBL5197311 | — | — | 1 | 5.89 |
| CHEMBL5197376 | — | — | 1 | 5.89 |
| CHEMBL5186455 | — | — | 1 | 5.80 |
| CHEMBL5178349 | — | — | 1 | 5.77 |
| CHEMBL5186344 | — | — | 1 | 5.72 |
| CHEMBL5187824 | — | — | 1 | 5.72 |
| CHEMBL5199983 | — | — | 1 | 5.68 |
| CHEMBL5203054 | — | — | 1 | 5.60 |
| CHEMBL5174303 | — | — | 1 | 5.58 |
| CHEMBL5188949 | — | — | 1 | 5.57 |
| CHEMBL5180340 | — | — | 1 | 5.55 |
| CHEMBL5172009 | — | — | 1 | 5.47 |
| CHEMBL5193541 | — | — | 1 | 5.47 |
| CHEMBL5202029 | — | — | 1 | 5.46 |
| CHEMBL5176376 | — | — | 1 | 5.36 |
| CHEMBL5169392 | — | — | 1 | 5.18 |
| CHEMBL5176001 | — | — | 1 | 5.02 |
| CHEMBL5182341 | — | — | 1 | 4.97 |
| CHEMBL5203795 | — | — | 1 | 4.80 |
| CHEMBL5193391 | — | — | 1 | 4.80 |
| CHEMBL5190265 | — | — | 1 | 4.45 |
| CHEMBL5171368 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5190252 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL5170189 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL5195432 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL5182403 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL5178772 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL5187427 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5205425 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2098167 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL5197311 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL5197376 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL5186455 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL5178349 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL5186344 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL5187824 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL5199983 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL5203054 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5174303 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL5188949 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL5180340 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL5193541 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL5172009 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL5202029 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL5176376 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL5169392 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL5176001 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL5182341 | — | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL5193391 | — | IC50 | = | 15700.0 | nM | 4.80 |
| CHEMBL5203795 | — | IC50 | = | 15700.0 | nM | 4.80 |
| CHEMBL5190265 | — | IC50 | = | 35900.0 | nM | 4.45 |
| CHEMBL5171368 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL5178255 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL5192342 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5178615 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL5186697 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL5201467 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL5186517 | — | IC50 | > | 60000.0 | nM | - |