Assay Detail
Binding
CHEMBL4151610
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Abl1 (unknown origin) incubated for 1 hr in presence of Tyrosine-2 peptide substrate by FRET based Z'-Lyte assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2- a]pyrazin-3-ylethynyl)-4-isopropyl- N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.89 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4161036 | — | — | 1 | 9.40 |
| CHEMBL4175086 | — | — | 1 | 8.03 |
| CHEMBL4164448 | — | — | 1 | 7.92 |
| CHEMBL4164030 | — | — | 1 | 7.68 |
| CHEMBL4171640 | — | — | 1 | 7.68 |
| CHEMBL4174682 | — | — | 1 | 7.52 |
| CHEMBL4167877 | — | — | 1 | 7.01 |
| CHEMBL4176145 | — | — | 1 | 6.70 |
| CHEMBL4159558 | — | — | 1 | 6.55 |
| CHEMBL2336015 | — | — | 1 | 6.51 |
| CHEMBL4159956 | — | — | 1 | 6.46 |
| CHEMBL4168305 | — | — | 1 | 6.31 |
| CHEMBL4172767 | — | — | 1 | 6.25 |
| CHEMBL4167237 | — | — | 1 | 6.03 |
| CHEMBL4171235 | — | — | 1 | 5.11 |
| CHEMBL4160628 | — | — | 1 | 5.01 |
| CHEMBL4176591 | — | — | 1 | - |
| CHEMBL4164870 | — | — | 1 | - |
| CHEMBL4165977 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4161036 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4175086 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL4164448 | — | IC50 | = | 11.94 | nM | 7.92 |
| CHEMBL4164030 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4171640 | — | IC50 | = | 21.1 | nM | 7.68 |
| CHEMBL4174682 | — | IC50 | = | 30.2 | nM | 7.52 |
| CHEMBL4167877 | — | IC50 | = | 97.4 | nM | 7.01 |
| CHEMBL4176145 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL4159558 | — | IC50 | = | 281.0 | nM | 6.55 |
| CHEMBL2336015 | — | IC50 | = | 308.0 | nM | 6.51 |
| CHEMBL4159956 | — | IC50 | = | 346.0 | nM | 6.46 |
| CHEMBL4168305 | — | IC50 | = | 494.0 | nM | 6.31 |
| CHEMBL4172767 | — | IC50 | = | 564.0 | nM | 6.25 |
| CHEMBL4167237 | — | IC50 | = | 932.0 | nM | 6.03 |
| CHEMBL4171235 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL4160628 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL4176591 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4164870 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4165977 | — | IC50 | > | 10000.0 | nM | - |