Assay Detail
Binding
CHEMBL4845008
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant GST-CSF1R (residues L534 to C972) expressed in Sf9 insect cells using poly(Glu,Tyr) as substrate incubated for 20 mins by ATP Kinase Glo assay
42
Total Activities
42
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
Macrophage colony-stimulating factor 1 receptor (CHEMBL1844) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of BPR1R024, an Orally Active and Selective CSF1R Inhibitor that Exhibits Antitumor and Immunomodulatory Activity in a Murine Colon Tumor Model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 7.47 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4851545 | — | — | 1 | 8.85 |
| CHEMBL4851635 | — | — | 1 | 8.08 |
| CHEMBL4860468 | — | — | 1 | 7.98 |
| CHEMBL4877148 | — | — | 1 | 7.96 |
| CHEMBL4846384 | — | — | 1 | 7.96 |
| CHEMBL4857271 | — | — | 1 | 7.94 |
| CHEMBL4870360 | — | — | 1 | 7.90 |
| CHEMBL4870448 | — | — | 1 | 7.89 |
| CHEMBL4877440 | — | — | 1 | 7.85 |
| CHEMBL4847875 | — | — | 1 | 7.84 |
| CHEMBL4864248 | — | — | 1 | 7.81 |
| CHEMBL4849425 | — | — | 1 | 7.81 |
| CHEMBL4873828 | — | — | 1 | 7.79 |
| CHEMBL4857690 | — | — | 1 | 7.79 |
| CHEMBL4866196 | — | — | 1 | 7.73 |
| CHEMBL4864729 | — | — | 1 | 7.72 |
| CHEMBL4877247 | — | — | 1 | 7.68 |
| CHEMBL4863584 | — | — | 1 | 7.62 |
| CHEMBL4857617 | — | — | 1 | 7.52 |
| CHEMBL1277162 | — | — | 1 | 7.52 |
| CHEMBL1908396 | — | — | 1 | 7.52 |
| CHEMBL3813873 | PEXIDARTINIB | 4.0 | 1 | 7.46 |
| CHEMBL4859405 | — | — | 1 | 7.44 |
| CHEMBL4876562 | — | — | 1 | 7.39 |
| CHEMBL4877828 | — | — | 1 | 7.36 |
| CHEMBL4846051 | — | — | 1 | 7.30 |
| CHEMBL4851294 | — | — | 1 | 7.24 |
| CHEMBL4871989 | — | — | 1 | 7.20 |
| CHEMBL4878431 | — | — | 1 | 7.19 |
| CHEMBL4874053 | — | — | 1 | 7.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4851545 | — | IC50 | = | 1.41 | nM | 8.85 |
| CHEMBL4851635 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL4860468 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL4877148 | — | IC50 | = | 11.1 | nM | 7.96 |
| CHEMBL4846384 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4857271 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL4870360 | — | IC50 | = | 12.7 | nM | 7.90 |
| CHEMBL4870448 | — | IC50 | = | 12.9 | nM | 7.89 |
| CHEMBL4877440 | — | IC50 | = | 14.1 | nM | 7.85 |
| CHEMBL4847875 | — | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL4864248 | — | IC50 | = | 15.4 | nM | 7.81 |
| CHEMBL4849425 | — | IC50 | = | 15.4 | nM | 7.81 |
| CHEMBL4873828 | — | IC50 | = | 16.3 | nM | 7.79 |
| CHEMBL4857690 | — | IC50 | = | 16.3 | nM | 7.79 |
| CHEMBL4866196 | — | IC50 | = | 18.6 | nM | 7.73 |
| CHEMBL4864729 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4877247 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4863584 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4857617 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1277162 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1908396 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3813873 | PEXIDARTINIB | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4859405 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4876562 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4877828 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4846051 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4851294 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4871989 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4878431 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4874053 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4872597 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4878471 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4876396 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4854210 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4861838 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL4877038 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL4846414 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL4878293 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL4871756 | — | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL4871510 | — | IC50 | = | 753.0 | nM | 6.12 |
| CHEMBL4850463 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL4867079 | — | IC50 | > | 10.0 | nM | - |