Assay Detail
Binding
CHEMBL4605675
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Inhibition of SYK (unknown origin) using XL665-labeled peptide as substrate in presence of ATP measured after 30 mins by TR-FRET assay
36
Total Activities
36
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
Discovery of Lanraplenib (GS-9876): A Once-Daily Spleen Tyrosine Kinase Inhibitor for Autoimmune Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 8.10 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4649800 | — | — | 1 | 9.10 |
| CHEMBL4638089 | — | — | 1 | 9.05 |
| CHEMBL4637943 | — | — | 1 | 9.05 |
| CHEMBL4643354 | — | — | 1 | 8.96 |
| CHEMBL4647927 | — | — | 1 | 8.92 |
| CHEMBL4643695 | — | — | 1 | 8.77 |
| CHEMBL4634466 | — | — | 1 | 8.55 |
| CHEMBL4637326 | — | — | 1 | 8.49 |
| CHEMBL4642016 | — | — | 1 | 8.31 |
| CHEMBL4634723 | — | — | 1 | 8.30 |
| CHEMBL4633338 | — | — | 1 | 8.30 |
| CHEMBL4640287 | — | — | 1 | 8.28 |
| CHEMBL3986824 | LANRAPLENIB | 2.0 | 1 | 8.21 |
| CHEMBL4644977 | — | — | 1 | 8.17 |
| CHEMBL4640138 | — | — | 1 | 8.16 |
| CHEMBL4633180 | — | — | 1 | 8.11 |
| CHEMBL4636843 | — | — | 1 | 8.08 |
| CHEMBL4643774 | — | — | 1 | 8.05 |
| CHEMBL4634721 | — | — | 1 | 8.04 |
| CHEMBL4637020 | — | — | 1 | 8.02 |
| CHEMBL4633153 | — | — | 1 | 7.95 |
| CHEMBL4641358 | — | — | 1 | 7.95 |
| CHEMBL4645149 | — | — | 1 | 7.94 |
| CHEMBL4649107 | — | — | 1 | 7.87 |
| CHEMBL4642075 | — | — | 1 | 7.86 |
| CHEMBL4648053 | — | — | 1 | 7.80 |
| CHEMBL3265032 | ENTOSPLETINIB | 3.0 | 1 | 7.78 |
| CHEMBL4635157 | — | — | 1 | 7.76 |
| CHEMBL3265033 | — | — | 1 | 7.71 |
| CHEMBL4645344 | — | — | 1 | 7.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4649800 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4638089 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4637943 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4643354 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4647927 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4643695 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4634466 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4637326 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4642016 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL4633338 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4634723 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4640287 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL3986824 | LANRAPLENIB | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL4644977 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL4640138 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL4633180 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4636843 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL4643774 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4634721 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL4637020 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL4633153 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL4641358 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL4645149 | — | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL4649107 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL4642075 | — | IC50 | = | 13.7 | nM | 7.86 |
| CHEMBL4648053 | — | IC50 | = | 15.7 | nM | 7.80 |
| CHEMBL3265032 | ENTOSPLETINIB | IC50 | = | 16.5 | nM | 7.78 |
| CHEMBL4635157 | — | IC50 | = | 17.3 | nM | 7.76 |
| CHEMBL3265033 | — | IC50 | = | 19.5 | nM | 7.71 |
| CHEMBL4645344 | — | IC50 | = | 21.5 | nM | 7.67 |
| CHEMBL4649400 | — | IC50 | = | 28.6 | nM | 7.54 |
| CHEMBL4647318 | — | IC50 | = | 31.9 | nM | 7.50 |
| CHEMBL4640486 | — | IC50 | = | 44.1 | nM | 7.36 |
| CHEMBL4641986 | — | IC50 | = | 44.3 | nM | 7.35 |
| CHEMBL4644206 | — | IC50 | = | 54.6 | nM | 7.26 |
| CHEMBL4632513 | — | IC50 | = | 61.6 | nM | 7.21 |