Assay Detail
Binding
CHEMBL5146067
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Tag2-PD1/Tag1-PD-L1 (unknown origin) protein-protein interaction preincubated for 15 mins followed by addition of anti-Tag1-Eu3+ and anti-Tag2-XL665 and measured after 2 hrs by HTRF analysis
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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
Discovery of 4-phenylindolines containing a (5-cyanopyridin-3-yl)methoxy moiety as potent inhibitors of the PD-1/PD-L1 interaction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.75 | 7.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5175245 | — | — | 1 | 7.27 |
| CHEMBL5184588 | — | — | 1 | 7.22 |
| CHEMBL5201125 | — | — | 1 | 7.13 |
| CHEMBL5181918 | — | — | 1 | 7.06 |
| CHEMBL5189268 | — | — | 1 | 6.98 |
| CHEMBL5191926 | — | — | 1 | 6.94 |
| CHEMBL5199860 | — | — | 1 | 6.91 |
| CHEMBL5181313 | — | — | 1 | 6.89 |
| CHEMBL5199681 | — | — | 1 | 6.88 |
| CHEMBL5205437 | — | — | 1 | 6.81 |
| CHEMBL4749782 | — | — | 1 | 6.79 |
| CHEMBL5198702 | — | — | 1 | 6.72 |
| CHEMBL5209536 | — | — | 1 | 6.64 |
| CHEMBL5189706 | — | — | 1 | 6.60 |
| CHEMBL5190181 | — | — | 1 | 6.51 |
| CHEMBL5200124 | — | — | 1 | 6.42 |
| CHEMBL5181413 | — | — | 1 | 6.20 |
| CHEMBL5172837 | — | — | 1 | 6.20 |
| CHEMBL5185877 | — | — | 1 | 6.06 |
| CHEMBL5198826 | — | — | 1 | - |
| CHEMBL5197289 | — | — | 1 | - |
| CHEMBL5172854 | — | — | 1 | - |
| CHEMBL5191650 | — | — | 1 | - |
| CHEMBL5206183 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5175245 | — | IC50 | = | 53.2 | nM | 7.27 |
| CHEMBL5184588 | — | IC50 | = | 60.1 | nM | 7.22 |
| CHEMBL5201125 | — | IC50 | = | 74.6 | nM | 7.13 |
| CHEMBL5181918 | — | IC50 | = | 87.3 | nM | 7.06 |
| CHEMBL5189268 | — | IC50 | = | 104.5 | nM | 6.98 |
| CHEMBL5191926 | — | IC50 | = | 115.7 | nM | 6.94 |
| CHEMBL5199860 | — | IC50 | = | 124.1 | nM | 6.91 |
| CHEMBL5181313 | — | IC50 | = | 127.8 | nM | 6.89 |
| CHEMBL5199681 | — | IC50 | = | 132.1 | nM | 6.88 |
| CHEMBL5205437 | — | IC50 | = | 154.2 | nM | 6.81 |
| CHEMBL4749782 | — | IC50 | = | 160.6 | nM | 6.79 |
| CHEMBL5198702 | — | IC50 | = | 192.1 | nM | 6.72 |
| CHEMBL5209536 | — | IC50 | = | 229.2 | nM | 6.64 |
| CHEMBL5189706 | — | IC50 | = | 251.5 | nM | 6.60 |
| CHEMBL5190181 | — | IC50 | = | 307.7 | nM | 6.51 |
| CHEMBL5200124 | — | IC50 | = | 378.4 | nM | 6.42 |
| CHEMBL5181413 | — | IC50 | = | 625.7 | nM | 6.20 |
| CHEMBL5172837 | — | IC50 | = | 635.2 | nM | 6.20 |
| CHEMBL5185877 | — | IC50 | = | 875.7 | nM | 6.06 |
| CHEMBL5198826 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5197289 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5172854 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5191650 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5206183 | — | IC50 | > | 5000.0 | nM | - |