Assay Detail
Binding
CHEMBL5035814
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells assessed as reduction in OATP 1B1-mediated [3H]-pitavastatin uptake preincubated for 30 mins followed by [3H]-pitavastatin addition and measured after 2 mins by liquid scintillation analysis
5
Total Activities
5
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 |
Target
Solute carrier organic anion transporter family member 1B1 (CHEMBL1697668) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 5.98 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5091040 | — | — | 1 | 6.89 |
| CHEMBL5086475 | — | — | 1 | 6.22 |
| CHEMBL5081349 | — | — | 1 | 5.60 |
| CHEMBL5084902 | — | — | 1 | 5.22 |
| CHEMBL5084416 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5091040 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5086475 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL5081349 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5084902 | — | EC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL5084416 | — | EC50 | > | 22000.0 | nM | - |