Assay Detail
Binding
CHEMBL5737550
Review assay metadata, readout intent, target linkage, and publication context from the same page.
LanthaScreen Eu Kinase Binding Assay: FMS: IC50 values of compounds against FMS kinase were determined by LanthaScreen™ Eu Kinase Binding Assay at Invitrogen (Life Technologies Grand Island, N.Y.) where total reaction volume was 10 μL in low-volume 384-well plates (#4511, Corning). Serially diluted compounds (3-fold) were incubated with kinase (1.25 nM) for 10 min, following which a mixture of ATP (10 μM) (#A1852, Sigma, St-Louis, Mo.) and fluorescent-PolyGT substrate (200 nM) (#PV3610, Invitrogen, Life Technologies Grand Island, N.Y.) was added and incubated in dark at room temperature for 1 h. After 1 h, 10 μL stop solution containing Terbium labeled antibody (4 nM) (#PV3529, Invitrogen, Life Technologies Grand Island, N.Y.) and EDTA (#E5134, Sigma, St-Louis, Mo.) (20 mM) in TR-FRET dilution buffer (#PV3574, Invitrogen, Life Technologies Grand Island, N.Y.) was added. Readings were taken in a Synergy Neo Plate reader (BioTek, Winooski) at single excitation of 340 nm and Dual emission at 495 nm and 520 nm respectively.
285
Total Activities
95
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Macrophage colony-stimulating factor 1 receptor (CHEMBL1844) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Heterocyclic compounds as kinase inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 95 | 7.28 | 8.82 |
| kon | 95 | - | - |
| k_off | 95 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5951978 | — | — | 3 | 8.82 |
| CHEMBL5956531 | — | — | 3 | 8.70 |
| CHEMBL5996434 | — | — | 3 | 8.60 |
| CHEMBL5945809 | — | — | 3 | 8.60 |
| CHEMBL5944626 | — | — | 3 | 8.60 |
| CHEMBL5861777 | — | — | 3 | 8.60 |
| CHEMBL6059314 | — | — | 3 | 8.52 |
| CHEMBL6043217 | — | — | 3 | 8.52 |
| CHEMBL5782876 | — | — | 3 | 8.40 |
| CHEMBL5875698 | — | — | 3 | 8.30 |
| CHEMBL6058548 | — | — | 3 | 8.30 |
| CHEMBL5770062 | — | — | 3 | 8.30 |
| CHEMBL5887566 | — | — | 3 | 8.22 |
| CHEMBL5740706 | — | — | 3 | 8.19 |
| CHEMBL5877068 | — | — | 3 | 8.15 |
| CHEMBL6034655 | — | — | 3 | 8.12 |
| CHEMBL6013201 | — | — | 3 | 8.10 |
| CHEMBL5858807 | — | — | 3 | 8.10 |
| CHEMBL6023260 | — | — | 3 | 8.02 |
| CHEMBL5961536 | — | — | 3 | 7.85 |
| CHEMBL5997157 | — | — | 3 | 7.85 |
| CHEMBL5907786 | — | — | 3 | 7.85 |
| CHEMBL5942169 | — | — | 3 | 7.77 |
| CHEMBL5843565 | — | — | 3 | 7.77 |
| CHEMBL5746967 | — | — | 3 | 7.77 |
| CHEMBL5992232 | — | — | 3 | 7.75 |
| CHEMBL5876164 | — | — | 3 | 7.72 |
| CHEMBL5914936 | — | — | 3 | 7.68 |
| CHEMBL5934647 | — | — | 3 | 7.66 |
| CHEMBL5976864 | — | — | 3 | 7.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5951978 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5956531 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5996434 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5944626 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5861777 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5945809 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL6059314 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL6043217 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5782876 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL6058548 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5770062 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5875698 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5887566 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5740706 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL5877068 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL6034655 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL5858807 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL6013201 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL6023260 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL5907786 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5961536 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5997157 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5843565 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5746967 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5942169 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5992232 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5876164 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5914936 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5934647 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5976864 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5917565 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5774057 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL6049510 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5803114 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5758578 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5877196 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5822252 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5887109 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL5760232 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5899619 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL6052625 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL6045551 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL5955040 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5965360 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5869636 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5792947 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5779951 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL5968635 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL5996998 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL6012324 | — | IC50 | = | 67.0 | nM | 7.17 |