Assay Detail
Functional
CHEMBL863377
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | TT |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Extracellular calcium-sensing receptor (CHEMBL1878) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines as calcium-sensing receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 6.15 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL382741 | — | — | 1 | 7.52 |
| CHEMBL200311 | — | — | 1 | 7.30 |
| CHEMBL180672 | — | — | 1 | 7.30 |
| CHEMBL199894 | — | — | 1 | 7.22 |
| CHEMBL371936 | — | — | 1 | 7.00 |
| CHEMBL199495 | — | — | 1 | 6.85 |
| CHEMBL372820 | — | — | 1 | 6.85 |
| CHEMBL372321 | — | — | 1 | 6.85 |
| CHEMBL197863 | — | — | 1 | 6.80 |
| CHEMBL199716 | — | — | 1 | 6.72 |
| CHEMBL203479 | — | — | 1 | 6.62 |
| CHEMBL199548 | — | — | 1 | 6.60 |
| CHEMBL200312 | — | — | 1 | 6.57 |
| CHEMBL370811 | — | — | 1 | 6.57 |
| CHEMBL200361 | — | — | 1 | 6.47 |
| CHEMBL200690 | — | — | 1 | 6.44 |
| CHEMBL538155 | — | — | 1 | 6.36 |
| CHEMBL199363 | — | — | 1 | 6.22 |
| CHEMBL201137 | — | — | 1 | 6.12 |
| CHEMBL199529 | — | — | 1 | 6.10 |
| CHEMBL199785 | — | — | 1 | 6.06 |
| CHEMBL201085 | — | — | 1 | 6.01 |
| CHEMBL200041 | — | — | 1 | 6.00 |
| CHEMBL200297 | — | — | 1 | 5.94 |
| CHEMBL265362 | — | — | 1 | 5.92 |
| CHEMBL199964 | — | — | 1 | 5.90 |
| CHEMBL381685 | — | — | 1 | 5.87 |
| CHEMBL201381 | — | — | 1 | 5.86 |
| CHEMBL200422 | — | — | 1 | 5.81 |
| CHEMBL263828 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL382741 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL200311 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL180672 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL199894 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL371936 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL199495 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL372820 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL372321 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL197863 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL199716 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL203479 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL199548 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL200312 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL370811 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL200361 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL200690 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL538155 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL199363 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL201137 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL199529 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL199785 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL201085 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL200041 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL200297 | — | IC50 | = | 1160.0 | nM | 5.94 |
| CHEMBL265362 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL199964 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL381685 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL201381 | — | IC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL200422 | — | IC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL263828 | — | IC50 | = | 1570.0 | nM | 5.80 |
| CHEMBL425394 | — | IC50 | = | 2470.0 | nM | 5.61 |
| CHEMBL370671 | — | IC50 | = | 2670.0 | nM | 5.57 |
| CHEMBL383609 | — | IC50 | = | 2840.0 | nM | 5.55 |
| CHEMBL201065 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL372821 | — | IC50 | = | 3860.0 | nM | 5.41 |
| CHEMBL200423 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL199473 | — | IC50 | = | 6180.0 | nM | 5.21 |
| CHEMBL200878 | — | IC50 | = | 6840.0 | nM | 5.17 |
| CHEMBL383842 | — | IC50 | = | 8430.0 | nM | 5.07 |
| CHEMBL200248 | — | IC50 | = | 9430.0 | nM | 5.03 |
| CHEMBL434937 | — | IC50 | = | 11360.0 | nM | 4.95 |