Assay Detail
Binding
CHEMBL1251540
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Inhibition of rabbit sarcoplasmic reticulum calcium ATPase by ATP regeneration assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sarcoplasmic/endoplasmic reticulum calcium ATPase 1 (CHEMBL4693) ↗| Type | SINGLE PROTEIN |
| Organism | Oryctolagus cuniculus |
Publication
Elucidation of the topography of the thapsigargin binding site in the sarco-endoplasmic calcium ATPase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 8.13 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL96926 | THAPSIGARGIN | — | 1 | 9.70 |
| CHEMBL1253591 | — | — | 1 | 9.10 |
| CHEMBL1253563 | — | — | 1 | 8.80 |
| CHEMBL1253557 | — | — | 1 | 8.60 |
| CHEMBL1253594 | — | — | 1 | 8.52 |
| CHEMBL1253592 | — | — | 1 | 8.05 |
| CHEMBL1253562 | DEBUTANOYLTHAPSIGARGIN | — | 1 | 8.00 |
| CHEMBL1253589 | — | — | 1 | 7.96 |
| CHEMBL1253559 | — | — | 1 | 7.81 |
| CHEMBL1253558 | — | — | 1 | 7.80 |
| CHEMBL1253593 | — | — | 1 | 7.75 |
| CHEMBL1253588 | — | — | 1 | 7.72 |
| CHEMBL1253556 | — | — | 1 | 7.70 |
| CHEMBL1253555 | — | — | 1 | 7.70 |
| CHEMBL1253561 | — | — | 1 | 7.57 |
| CHEMBL1253595 | — | — | 1 | 7.36 |
| CHEMBL1253596 | — | — | 1 | - |
| CHEMBL1253590 | — | — | 1 | - |
| CHEMBL1253587 | — | — | 1 | - |
| CHEMBL1253560 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL96926 | THAPSIGARGIN | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL1253591 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL1253563 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL1253557 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL1253594 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1253592 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1253562 | DEBUTANOYLTHAPSIGARGIN | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1253589 | — | IC50 | = | 11.1 | nM | 7.96 |
| CHEMBL1253559 | — | IC50 | = | 15.6 | nM | 7.81 |
| CHEMBL1253558 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1253593 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1253588 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1253556 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1253555 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1253561 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1253595 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL1253596 | — | IC50 | > | 70.0 | nM | - |
| CHEMBL1253590 | — | IC50 | > | 70.0 | nM | - |
| CHEMBL1253587 | — | IC50 | > | 70.0 | nM | - |
| CHEMBL1253560 | — | IC50 | > | 70.0 | nM | - |