Assay Detail
Binding
CHEMBL4728927
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of AlexaFluor-labeled tracer 236 binding to recombinant human His-tagged CSF1R (538 to 910 residues) preincubated for 20 mins followed by Eu-labeled anti-His antibody addition and measured after 90 mins by FRET based LanthaScreen assay
33
Total Activities
33
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 |
Target
Macrophage colony-stimulating factor 1 receptor (CHEMBL1844) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of IACS-9439, a Potent, Exquisitely Selective, and Orally Bioavailable Inhibitor of CSF1R.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 7.84 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4758092 | — | — | 1 | 9.10 |
| CHEMBL4751287 | — | — | 1 | 9.00 |
| CHEMBL4763875 | — | — | 1 | 9.00 |
| CHEMBL4798876 | — | — | 1 | 8.96 |
| CHEMBL4795462 | — | — | 1 | 8.96 |
| CHEMBL4798601 | — | — | 1 | 8.92 |
| CHEMBL4740157 | — | — | 1 | 8.92 |
| CHEMBL4759047 | — | — | 1 | 8.85 |
| CHEMBL4748740 | — | — | 1 | 8.77 |
| CHEMBL4741283 | — | — | 1 | 8.70 |
| CHEMBL4779878 | — | — | 1 | 8.70 |
| CHEMBL4756510 | — | — | 1 | 8.62 |
| CHEMBL4779197 | — | — | 1 | 8.59 |
| CHEMBL4754431 | — | — | 1 | 8.40 |
| CHEMBL4746711 | — | — | 1 | 8.40 |
| CHEMBL4788945 | — | — | 1 | 8.40 |
| CHEMBL4763289 | — | — | 1 | 8.24 |
| CHEMBL4762843 | — | — | 1 | 8.15 |
| CHEMBL4787609 | — | — | 1 | 8.05 |
| CHEMBL4790139 | — | — | 1 | 7.96 |
| CHEMBL4798920 | — | — | 1 | 7.77 |
| CHEMBL4788832 | — | — | 1 | 7.68 |
| CHEMBL4764974 | — | — | 1 | 7.52 |
| CHEMBL4743008 | — | — | 1 | 7.32 |
| CHEMBL4777344 | — | — | 1 | 7.28 |
| CHEMBL4751359 | — | — | 1 | 7.12 |
| CHEMBL4781950 | — | — | 1 | 6.52 |
| CHEMBL4797083 | — | — | 1 | 6.35 |
| CHEMBL4783368 | — | — | 1 | 6.20 |
| CHEMBL4742978 | — | — | 1 | 6.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4758092 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4751287 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4763875 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4798876 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4795462 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4798601 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4740157 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4759047 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4748740 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4741283 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4779878 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4756510 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4779197 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4788945 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4746711 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4754431 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4763289 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL4762843 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4787609 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4790139 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4798920 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4788832 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4764974 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4743008 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4777344 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4751359 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4781950 | — | IC50 | = | 303.0 | nM | 6.52 |
| CHEMBL4797083 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4783368 | — | IC50 | = | 626.0 | nM | 6.20 |
| CHEMBL4742978 | — | IC50 | = | 655.0 | nM | 6.18 |
| CHEMBL4745859 | — | IC50 | = | 781.0 | nM | 6.11 |
| CHEMBL4742128 | — | IC50 | = | 4413.0 | nM | 5.36 |
| CHEMBL4791937 | — | IC50 | = | 27712.0 | nM | 4.56 |