Assay Detail
Binding
CHEMBL5165092
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PD-1/PD-L1 interaction in CHO-K1 cells transfected with PD-1-YFP/SHP-2-CFP and measured by FRET assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Programmed cell death protein 1/Programmed cell death 1 ligand 1 (CHEMBL4523993) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Pyrazolones as inhibitors of immune checkpoint blocking the PD-1/PD-L1 interaction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.10 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5194902 | — | — | 1 | 8.40 |
| CHEMBL5176505 | — | — | 1 | 8.15 |
| CHEMBL5207924 | — | — | 1 | 8.14 |
| CHEMBL5194957 | — | — | 1 | 8.05 |
| CHEMBL5171729 | — | — | 1 | 7.77 |
| CHEMBL374252 | — | — | 1 | 7.04 |
| CHEMBL5203947 | — | — | 1 | 7.01 |
| CHEMBL4089730 | — | — | 1 | 6.91 |
| CHEMBL5177267 | — | — | 1 | 6.84 |
| CHEMBL5186432 | — | — | 1 | 6.45 |
| CHEMBL5207258 | — | — | 1 | 5.96 |
| CHEMBL5177805 | — | — | 1 | 4.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5194902 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5176505 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5207924 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL5194957 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5171729 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL374252 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL5203947 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4089730 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL5177267 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL5186432 | — | IC50 | = | 359.0 | nM | 6.45 |
| CHEMBL5207258 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5177805 | — | IC50 | = | 33000.0 | nM | 4.48 |