Assay Detail
Functional
CHEMBL1646311
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Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release treated for 5 mins before LPS challenge measured after 6 hrs by ELISA
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | PBMC |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.31 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1642545 | — | — | 1 | 7.10 |
| CHEMBL1642549 | — | — | 1 | 6.77 |
| CHEMBL1642546 | — | — | 1 | 6.66 |
| CHEMBL1642563 | — | — | 1 | 6.66 |
| CHEMBL1642547 | — | — | 1 | 6.54 |
| CHEMBL1642565 | — | — | 1 | 6.54 |
| CHEMBL521643 | — | — | 1 | 6.51 |
| CHEMBL454973 | — | — | 1 | 6.46 |
| CHEMBL1642557 | — | — | 1 | 6.40 |
| CHEMBL1642558 | — | — | 1 | 6.36 |
| CHEMBL1642561 | — | — | 1 | 6.36 |
| CHEMBL1642560 | — | — | 1 | 6.32 |
| CHEMBL1642548 | — | — | 1 | 6.28 |
| CHEMBL1642564 | — | — | 1 | 6.25 |
| CHEMBL1642550 | — | — | 1 | 6.25 |
| CHEMBL1642559 | — | — | 1 | 6.22 |
| CHEMBL1642556 | — | — | 1 | 6.16 |
| CHEMBL523189 | — | — | 1 | 6.14 |
| CHEMBL1642562 | — | — | 1 | 6.03 |
| CHEMBL249697 | BMS-345541 | — | 1 | 6.00 |
| CHEMBL1642554 | — | — | 1 | 6.00 |
| CHEMBL1642551 | — | — | 1 | 5.87 |
| CHEMBL1642552 | — | — | 1 | 5.31 |
| CHEMBL1642555 | — | — | 1 | - |
| CHEMBL1642553 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1642545 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1642549 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL1642546 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL1642563 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL1642547 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL1642565 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL521643 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL454973 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL1642557 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL1642558 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL1642561 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL1642560 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL1642548 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL1642564 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL1642550 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL1642559 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL1642556 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL523189 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL1642562 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL249697 | BMS-345541 | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1642554 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL1642551 | — | IC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL1642552 | — | IC50 | = | 4890.0 | nM | 5.31 |
| CHEMBL1642555 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1642553 | — | IC50 | - | — | - |