Assay Detail
Toxicity
CHEMBL5347182
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Inhibition of human recombinant hERG expressed in CHO-K1 cells assessed as inhibition of channel current by automated patch clamp assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Toxicity |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of the thieno[2,3-d]pyrimidine-2,4-dione derivative 21a: A potent and orally bioavailable gonadotropin-releasing hormone receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 5.53 | 6.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5409192 | — | — | 1 | 6.14 |
| CHEMBL5398152 | — | — | 1 | 6.04 |
| CHEMBL5434324 | — | — | 1 | 5.91 |
| CHEMBL5425604 | — | — | 1 | 5.88 |
| CHEMBL1800157 | — | — | 1 | 5.86 |
| CHEMBL5422863 | — | — | 1 | 5.85 |
| CHEMBL5416399 | — | — | 1 | 5.83 |
| CHEMBL5395542 | — | — | 1 | 5.68 |
| CHEMBL5400302 | — | — | 1 | 5.51 |
| CHEMBL5432553 | — | — | 1 | 5.43 |
| CHEMBL5419489 | — | — | 1 | 5.41 |
| CHEMBL5420128 | — | — | 1 | 5.39 |
| CHEMBL1800159 | RELUGOLIX | 4.0 | 1 | 5.38 |
| CHEMBL5403996 | — | — | 1 | 5.37 |
| CHEMBL5419365 | — | — | 1 | 5.31 |
| CHEMBL5404509 | — | — | 1 | 5.29 |
| CHEMBL5427278 | — | — | 1 | 5.11 |
| CHEMBL5433025 | — | — | 1 | 4.93 |
| CHEMBL5413078 | — | — | 1 | 4.68 |
| CHEMBL5407004 | — | — | 1 | - |
| CHEMBL5441000 | — | — | 1 | - |
| CHEMBL5429424 | — | — | 1 | - |
| CHEMBL5414381 | — | — | 1 | - |
| CHEMBL5424526 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5409192 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL5398152 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL5434324 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL5425604 | — | IC50 | = | 1320.0 | nM | 5.88 |
| CHEMBL1800157 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL5422863 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL5416399 | — | IC50 | = | 1470.0 | nM | 5.83 |
| CHEMBL5395542 | — | IC50 | = | 2090.0 | nM | 5.68 |
| CHEMBL5400302 | — | IC50 | = | 3070.0 | nM | 5.51 |
| CHEMBL5432553 | — | IC50 | = | 3680.0 | nM | 5.43 |
| CHEMBL5419489 | — | IC50 | = | 3870.0 | nM | 5.41 |
| CHEMBL5420128 | — | IC50 | = | 4110.0 | nM | 5.39 |
| CHEMBL1800159 | RELUGOLIX | IC50 | = | 4140.0 | nM | 5.38 |
| CHEMBL5403996 | — | IC50 | = | 4270.0 | nM | 5.37 |
| CHEMBL5419365 | — | IC50 | = | 4930.0 | nM | 5.31 |
| CHEMBL5404509 | — | IC50 | = | 5140.0 | nM | 5.29 |
| CHEMBL5427278 | — | IC50 | = | 7810.0 | nM | 5.11 |
| CHEMBL5433025 | — | IC50 | = | 11630.0 | nM | 4.93 |
| CHEMBL5413078 | — | IC50 | = | 20680.0 | nM | 4.68 |
| CHEMBL5407004 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5441000 | — | IC50 | - | — | - | |
| CHEMBL5429424 | — | IC50 | - | — | - | |
| CHEMBL5414381 | — | IC50 | - | — | - | |
| CHEMBL5424526 | — | IC50 | > | 30000.0 | nM | - |