Assay Detail
Binding
CHEMBL3888705
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Fluorescence Polarization Assay: PDE activity was measured using the IMAP fluorescence polarization assay (Molecular Devices) in which binding of hydrolyzed cyclic nucleotide substrate to immobilized metal coordination complexes increases fluorescence polarization (FP). Tetramethylrhodamine (TAMRA)-cGMP and fluorescein-cAMP were used as substrates, each at final concentration of 50 nmol/L. The PDE assay was done according to the manufacturer's specifications using either whole cell lysates or recombinant enzymes. FP was measured at excitation, emission wavelengths of either 530,590 nm for TAMRA-cGMP or 485,530 nm for fluorescein-cAMP using a Synergy4 (Biotek) microplate reader.
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Derivatives of celeboxib, use thereof and preparation thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 5.35 | 5.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3979746 | — | — | 1 | 5.92 |
| CHEMBL3912685 | — | — | 1 | 5.75 |
| CHEMBL3909725 | — | — | 1 | 5.72 |
| CHEMBL3918044 | — | — | 1 | 5.70 |
| CHEMBL3912663 | — | — | 1 | 5.70 |
| CHEMBL3323320 | — | — | 1 | 5.68 |
| CHEMBL3963234 | — | — | 1 | 5.57 |
| CHEMBL3976289 | — | — | 1 | 5.54 |
| CHEMBL3954425 | — | — | 1 | 5.51 |
| CHEMBL3960150 | — | — | 1 | 5.51 |
| CHEMBL3927064 | — | — | 1 | 5.50 |
| CHEMBL3937157 | — | — | 1 | 5.50 |
| CHEMBL3921118 | — | — | 1 | 5.48 |
| CHEMBL3906921 | — | — | 1 | 5.48 |
| CHEMBL3899621 | — | — | 1 | 5.43 |
| CHEMBL1370630 | — | — | 1 | 5.42 |
| CHEMBL3893185 | — | — | 1 | 5.26 |
| CHEMBL3914590 | — | — | 1 | 5.24 |
| CHEMBL3918115 | — | — | 1 | 5.21 |
| CHEMBL3922249 | — | — | 1 | 5.16 |
| CHEMBL3926786 | — | — | 1 | 5.16 |
| CHEMBL3963184 | — | — | 1 | 5.14 |
| CHEMBL3908967 | — | — | 1 | 5.11 |
| CHEMBL3965079 | — | — | 1 | 5.08 |
| CHEMBL3910060 | — | — | 1 | 5.06 |
| CHEMBL3931444 | — | — | 1 | 5.00 |
| CHEMBL3909240 | — | — | 1 | 4.63 |
| CHEMBL118 | CELECOXIB | 4.0 | 1 | 4.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3979746 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3912685 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3909725 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3918044 | — | IC50 | = | 2020.0 | nM | 5.70 |
| CHEMBL3912663 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3323320 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3963234 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3976289 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL3954425 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL3960150 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL3927064 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL3937157 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL3921118 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3906921 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3899621 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL1370630 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL3893185 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL3914590 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL3918115 | — | IC50 | = | 6220.0 | nM | 5.21 |
| CHEMBL3922249 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL3926786 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL3963184 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL3908967 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL3965079 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL3910060 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL3931444 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL3909240 | — | IC50 | = | 23500.0 | nM | 4.63 |
| CHEMBL118 | CELECOXIB | IC50 | = | 36000.0 | nM | 4.44 |