Assay Detail
Functional
CHEMBL860123
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Inhibition of LPS-induced TNFalpha production in human whole blood
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 9.09 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL371037 | — | — | 1 | 10.15 |
| CHEMBL199015 | — | — | 1 | 10.05 |
| CHEMBL196969 | — | — | 1 | 9.92 |
| CHEMBL197392 | — | — | 1 | 9.92 |
| CHEMBL371089 | — | — | 1 | 9.85 |
| CHEMBL372575 | — | — | 1 | 9.80 |
| CHEMBL198732 | — | — | 1 | 9.70 |
| CHEMBL198722 | — | — | 1 | 9.68 |
| CHEMBL198853 | — | — | 1 | 9.68 |
| CHEMBL381681 | — | — | 1 | 9.59 |
| CHEMBL198674 | — | — | 1 | 9.21 |
| CHEMBL198527 | — | — | 1 | 9.03 |
| CHEMBL197494 | — | — | 1 | 8.92 |
| CHEMBL197386 | — | — | 1 | 8.80 |
| CHEMBL370220 | — | — | 1 | 8.11 |
| CHEMBL198432 | — | — | 1 | 8.08 |
| CHEMBL198464 | — | — | 1 | 7.96 |
| CHEMBL198564 | — | — | 1 | 7.92 |
| CHEMBL32442 | CDP840 | — | 1 | 7.85 |
| CHEMBL382545 | — | — | 1 | 7.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL371037 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL199015 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL196969 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL197392 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL371089 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL372575 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL198732 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL198722 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL198853 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL381681 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL198674 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL198527 | — | IC50 | = | 0.93 | nM | 9.03 |
| CHEMBL197494 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL197386 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL370220 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL198432 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL198464 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL198564 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL32442 | CDP840 | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL382545 | — | IC50 | = | 31.0 | nM | 7.51 |