Assay Detail
Binding
CHEMBL1109007
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Inhibition of PDE4 expressed in HEK293 cells coexpressing cyclic nucleotide gated ion channel mutant assessed as inhibition of NECA-induced cAMP production treated 15 mins before NECA challenge measured after 45 mins by FLIPR assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Water-soluble PDE4 inhibitors for the treatment of dry eye.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.64 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | 4.0 | 1 | 9.00 |
| CHEMBL42126 | PICLAMILAST | 2.0 | 1 | 7.89 |
| CHEMBL1096812 | — | — | 1 | 7.55 |
| CHEMBL1096813 | — | — | 1 | 7.52 |
| CHEMBL1098844 | — | — | 1 | 7.52 |
| CHEMBL1095210 | — | — | 1 | 7.40 |
| CHEMBL1099322 | — | — | 1 | 6.92 |
| CHEMBL1099164 | — | — | 1 | 6.82 |
| CHEMBL1099163 | — | — | 1 | 6.82 |
| CHEMBL1095865 | — | — | 1 | 6.75 |
| CHEMBL1098818 | — | — | 1 | 6.55 |
| CHEMBL1095226 | — | — | 1 | 6.18 |
| CHEMBL1098542 | — | — | 1 | 6.14 |
| CHEMBL1098541 | — | — | 1 | 6.05 |
| CHEMBL70903 | — | — | 1 | 5.96 |
| CHEMBL1095225 | — | — | 1 | 5.74 |
| CHEMBL1096814 | — | — | 1 | 5.27 |
| CHEMBL1098778 | — | — | 1 | 5.09 |
| CHEMBL1098193 | — | — | 1 | 5.00 |
| CHEMBL1098503 | — | — | 1 | - |
| CHEMBL1098502 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL42126 | PICLAMILAST | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1096812 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1096813 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1098844 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1095210 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1099322 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1099164 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1099163 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1095865 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1098818 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL1095226 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL1098542 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL1098541 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL70903 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1095225 | — | IC50 | = | 1820.0 | nM | 5.74 |
| CHEMBL1096814 | — | IC50 | = | 5350.0 | nM | 5.27 |
| CHEMBL1098778 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL1098193 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL1098503 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1098502 | — | IC50 | > | 30000.0 | nM | - |