Assay Detail
Functional
CHEMBL863602
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Inhibition of LPS-stimulated TNFalpha production in THP1 cells
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| Confidence | 1 — Organism |
| Curated By | Expert |
Publication
The development of novel C-2, C-8, and N-9 trisubstituted purines as inhibitors of TNF-alpha production.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 6.55 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL380373 | — | — | 1 | 8.40 |
| CHEMBL210164 | — | — | 1 | 8.40 |
| CHEMBL211469 | — | — | 1 | 7.85 |
| CHEMBL380207 | — | — | 1 | 7.46 |
| CHEMBL211748 | — | — | 1 | 7.32 |
| CHEMBL119385 | NEFLAMAPIMOD | 2.0 | 1 | 7.25 |
| CHEMBL384525 | — | — | 1 | 7.16 |
| CHEMBL10 | SB-203580 | — | 1 | 7.14 |
| CHEMBL380029 | — | — | 1 | 7.07 |
| CHEMBL377470 | — | — | 1 | 7.00 |
| CHEMBL377453 | — | — | 1 | 6.77 |
| CHEMBL213788 | — | — | 1 | 6.68 |
| CHEMBL425606 | — | — | 1 | 6.62 |
| CHEMBL209597 | — | — | 1 | 6.56 |
| CHEMBL213600 | — | — | 1 | 6.52 |
| CHEMBL213837 | — | — | 1 | 6.33 |
| CHEMBL425616 | — | — | 1 | 6.27 |
| CHEMBL209867 | — | — | 1 | 6.20 |
| CHEMBL377469 | — | — | 1 | 6.19 |
| CHEMBL386575 | — | — | 1 | 6.10 |
| CHEMBL209866 | — | — | 1 | 6.04 |
| CHEMBL212826 | — | — | 1 | 5.81 |
| CHEMBL209596 | — | — | 1 | 5.69 |
| CHEMBL214244 | — | — | 1 | 5.68 |
| CHEMBL427222 | — | — | 1 | 5.50 |
| CHEMBL213957 | — | — | 1 | 5.18 |
| CHEMBL213303 | — | — | 1 | 5.18 |
| CHEMBL214245 | — | — | 1 | 5.00 |
| CHEMBL214014 | — | — | 1 | - |
| CHEMBL213232 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL380373 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL210164 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL211469 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL380207 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL211748 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL119385 | NEFLAMAPIMOD | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL384525 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL10 | SB-203580 | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL380029 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL377470 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL377453 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL213788 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL425606 | — | IC50 | = | 237.0 | nM | 6.62 |
| CHEMBL209597 | — | IC50 | = | 273.0 | nM | 6.56 |
| CHEMBL213600 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL213837 | — | IC50 | = | 473.0 | nM | 6.33 |
| CHEMBL425616 | — | IC50 | = | 542.0 | nM | 6.27 |
| CHEMBL209867 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL377469 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL386575 | — | IC50 | = | 798.0 | nM | 6.10 |
| CHEMBL209866 | — | IC50 | = | 906.0 | nM | 6.04 |
| CHEMBL212826 | — | IC50 | = | 1541.0 | nM | 5.81 |
| CHEMBL209596 | — | IC50 | = | 2050.0 | nM | 5.69 |
| CHEMBL214244 | — | IC50 | = | 2110.0 | nM | 5.68 |
| CHEMBL427222 | — | IC50 | = | 3171.0 | nM | 5.50 |
| CHEMBL213957 | — | IC50 | = | 6579.0 | nM | 5.18 |
| CHEMBL213303 | — | IC50 | = | 6556.0 | nM | 5.18 |
| CHEMBL214245 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL214014 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL213232 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL379805 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL211421 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL386097 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL387277 | — | IC50 | > | 1000.0 | nM | - |