Assay Detail
Binding
CHEMBL4425808
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant GST-tagged DDR1 (440 to 876 residues) expressed in baculovirus infected Sf9 insect cells using fluorescein-poly GAT as substrate preincubated for 1 hr measured after 1 hr in presence of ATP by TR-FRET LanthaScreen assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Epithelial discoidin domain-containing receptor 1 (CHEMBL5319) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.99 | 8.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4553037 | — | — | 1 | 8.03 |
| CHEMBL4066114 | — | — | 1 | 7.61 |
| CHEMBL4435100 | — | — | 1 | 7.44 |
| CHEMBL4453539 | — | — | 1 | 6.51 |
| CHEMBL4471343 | — | — | 1 | 6.49 |
| CHEMBL4544384 | — | — | 1 | 6.48 |
| CHEMBL4095191 | — | — | 1 | 6.36 |
| CHEMBL4542873 | — | — | 1 | - |
| CHEMBL4524615 | — | — | 1 | - |
| CHEMBL4571618 | — | — | 1 | - |
| CHEMBL4565209 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4553037 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL4066114 | — | IC50 | = | 24.3 | nM | 7.61 |
| CHEMBL4435100 | — | IC50 | = | 36.4 | nM | 7.44 |
| CHEMBL4453539 | — | IC50 | = | 309.0 | nM | 6.51 |
| CHEMBL4471343 | — | IC50 | = | 326.0 | nM | 6.49 |
| CHEMBL4544384 | — | IC50 | = | 328.0 | nM | 6.48 |
| CHEMBL4095191 | — | IC50 | = | 442.0 | nM | 6.36 |
| CHEMBL4542873 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4524615 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4571618 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4565209 | — | IC50 | > | 2000.0 | nM | - |