Assay Detail
Functional
CHEMBL1228488
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Extracellular calcium-sensing receptor (CHEMBL1878) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Penta-substituted benzimidazoles as potent antagonists of the calcium-sensing receptor (CaSR-antagonists).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 7.07 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1223714 | — | — | 1 | 8.80 |
| CHEMBL1223772 | — | — | 1 | 8.70 |
| CHEMBL1223771 | — | — | 1 | 8.59 |
| CHEMBL1223713 | — | — | 1 | 8.40 |
| CHEMBL1223712 | — | — | 1 | 8.40 |
| CHEMBL1222492 | — | — | 1 | 8.30 |
| CHEMBL1222427 | — | — | 1 | 8.30 |
| CHEMBL1223506 | — | — | 1 | 8.22 |
| CHEMBL1223507 | — | — | 1 | 7.96 |
| CHEMBL1223368 | — | — | 1 | 7.89 |
| CHEMBL1223505 | — | — | 1 | 7.85 |
| CHEMBL1223711 | — | — | 1 | 7.82 |
| CHEMBL1223508 | — | — | 1 | 7.80 |
| CHEMBL1223367 | — | — | 1 | 7.66 |
| CHEMBL1223509 | — | — | 1 | 7.60 |
| CHEMBL1222489 | — | — | 1 | 7.58 |
| CHEMBL1222490 | — | — | 1 | 7.37 |
| CHEMBL1223303 | — | — | 1 | 7.30 |
| CHEMBL1223369 | — | — | 1 | 7.29 |
| CHEMBL1222426 | — | — | 1 | 7.22 |
| CHEMBL1223438 | — | — | 1 | 6.72 |
| CHEMBL1222424 | — | — | 1 | 6.72 |
| CHEMBL1223439 | — | — | 1 | 6.68 |
| CHEMBL1222491 | — | — | 1 | 6.47 |
| CHEMBL1222425 | — | — | 1 | 6.44 |
| CHEMBL1223371 | — | — | 1 | 6.11 |
| CHEMBL1223440 | — | — | 1 | 6.10 |
| CHEMBL1223437 | — | — | 1 | 6.00 |
| CHEMBL1223370 | — | — | 1 | 5.74 |
| CHEMBL1223302 | — | — | 1 | 5.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1223714 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL1223772 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1223771 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL1223713 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1223712 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1222492 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1222427 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1223506 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1223507 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1223368 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1223505 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1223711 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1223508 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1223367 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1223509 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1222489 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1222490 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL1223303 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1223369 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL1222426 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1223438 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL1222424 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL1223439 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL1222491 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL1222425 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL1223371 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL1223440 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL1223437 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1223370 | — | IC50 | = | 1820.0 | nM | 5.74 |
| CHEMBL1223302 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL1223300 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL1223222 | — | IC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL1223301 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL1223221 | — | IC50 | = | 2550.0 | nM | 5.59 |
| CHEMBL1223298 | — | IC50 | = | 4690.0 | nM | 5.33 |
| CHEMBL1223299 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL1223441 | — | IC50 | > | 10000.0 | nM | - |