Assay Detail
ADMET
CHEMBL4407670
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Inhibition of GST-tagged recombinant human DDR2 expressed in baculovirus using fluorescein-poly GAT as substrate after 1 hr by FRET-based LanthaScreen Eu kinase binding assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Discoidin domain-containing receptor 2 (CHEMBL5122) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
2-Amino-2,3-dihydro-1<i>H</i>-indene-5-carboxamide-Based Discoidin Domain Receptor 1 (DDR1) Inhibitors: Design, Synthesis, and in Vivo Antipancreatic Cancer Efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.62 | 7.67 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4558430 | — | — | 1 | 7.67 |
| CHEMBL4472004 | — | — | 1 | 6.99 |
| CHEMBL4441609 | — | — | 1 | 6.68 |
| CHEMBL4553037 | — | — | 1 | 6.47 |
| CHEMBL4541139 | — | — | 1 | 6.33 |
| CHEMBL4472914 | — | — | 1 | 6.20 |
| CHEMBL4437631 | — | — | 1 | 6.03 |
| CHEMBL4482862 | — | — | 1 | - |
| CHEMBL4568103 | — | — | 1 | - |
| CHEMBL4443543 | — | — | 1 | - |
| CHEMBL4570381 | — | — | 1 | - |
| CHEMBL4470262 | — | — | 1 | - |
| CHEMBL4585974 | — | — | 1 | - |
| CHEMBL4560079 | — | — | 1 | - |
| CHEMBL4574620 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4558430 | — | IC50 | = | 21.5 | nM | 7.67 |
| CHEMBL4472004 | — | IC50 | = | 102.2 | nM | 6.99 |
| CHEMBL4441609 | — | IC50 | = | 207.3 | nM | 6.68 |
| CHEMBL4553037 | — | IC50 | = | 340.9 | nM | 6.47 |
| CHEMBL4541139 | — | IC50 | = | 467.0 | nM | 6.33 |
| CHEMBL4472914 | — | IC50 | = | 634.0 | nM | 6.20 |
| CHEMBL4437631 | — | IC50 | = | 933.0 | nM | 6.03 |
| CHEMBL4482862 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4568103 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4443543 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4570381 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4470262 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4585974 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4560079 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4574620 | — | IC50 | > | 1000.0 | nM | - |