Assay Detail
Binding
CHEMBL1042745
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PDE6
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha (CHEMBL3878) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Optimization of the aminopyridopyrazinones class of PDE5 inhibitors: discovery of 3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 47 | 7.31 | 8.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL565305 | — | — | 1 | 8.33 |
| CHEMBL584270 | — | — | 1 | 8.07 |
| CHEMBL566797 | — | — | 1 | 8.03 |
| CHEMBL567470 | — | — | 1 | 8.01 |
| CHEMBL569481 | — | — | 1 | 7.97 |
| CHEMBL551052 | — | — | 1 | 7.95 |
| CHEMBL567447 | — | — | 1 | 7.86 |
| CHEMBL585918 | — | — | 1 | 7.83 |
| CHEMBL566820 | — | — | 1 | 7.82 |
| CHEMBL568839 | — | — | 1 | 7.82 |
| CHEMBL566367 | — | — | 1 | 7.82 |
| CHEMBL567471 | — | — | 1 | 7.82 |
| CHEMBL565306 | — | — | 1 | 7.79 |
| CHEMBL569492 | — | — | 1 | 7.75 |
| CHEMBL566375 | — | — | 1 | 7.75 |
| CHEMBL569045 | — | — | 1 | 7.63 |
| CHEMBL583854 | — | — | 1 | 7.63 |
| CHEMBL569264 | — | — | 1 | 7.61 |
| CHEMBL585327 | — | — | 1 | 7.58 |
| CHEMBL567016 | — | — | 1 | 7.50 |
| CHEMBL569491 | — | — | 1 | 7.46 |
| CHEMBL566598 | — | — | 1 | 7.40 |
| CHEMBL565308 | — | — | 1 | 7.34 |
| CHEMBL585015 | — | — | 1 | 7.30 |
| CHEMBL584056 | — | — | 1 | 7.29 |
| CHEMBL567445 | — | — | 1 | 7.25 |
| CHEMBL584317 | — | — | 1 | 7.24 |
| CHEMBL551250 | — | — | 1 | 7.21 |
| CHEMBL585352 | — | — | 1 | 7.20 |
| CHEMBL567446 | — | — | 1 | 7.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL565305 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL584270 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL566797 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL567470 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL569481 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL551052 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL567447 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL585918 | — | IC50 | = | 14.7 | nM | 7.83 |
| CHEMBL566820 | — | IC50 | = | 15.3 | nM | 7.82 |
| CHEMBL568839 | — | IC50 | = | 15.2 | nM | 7.82 |
| CHEMBL566367 | — | IC50 | = | 15.3 | nM | 7.82 |
| CHEMBL567471 | — | IC50 | = | 15.1 | nM | 7.82 |
| CHEMBL565306 | — | IC50 | = | 16.1 | nM | 7.79 |
| CHEMBL569492 | — | IC50 | = | 17.7 | nM | 7.75 |
| CHEMBL566375 | — | IC50 | = | 17.9 | nM | 7.75 |
| CHEMBL569045 | — | IC50 | = | 23.6 | nM | 7.63 |
| CHEMBL583854 | — | IC50 | = | 23.2 | nM | 7.63 |
| CHEMBL569264 | — | IC50 | = | 24.6 | nM | 7.61 |
| CHEMBL585327 | — | IC50 | = | 26.3 | nM | 7.58 |
| CHEMBL567016 | — | IC50 | = | 31.4 | nM | 7.50 |
| CHEMBL569491 | — | IC50 | = | 34.5 | nM | 7.46 |
| CHEMBL566598 | — | IC50 | = | 39.5 | nM | 7.40 |
| CHEMBL565308 | — | IC50 | = | 45.5 | nM | 7.34 |
| CHEMBL585015 | — | IC50 | = | 49.7 | nM | 7.30 |
| CHEMBL584056 | — | IC50 | = | 51.8 | nM | 7.29 |
| CHEMBL567445 | — | IC50 | = | 55.9 | nM | 7.25 |
| CHEMBL584317 | — | IC50 | = | 57.4 | nM | 7.24 |
| CHEMBL551250 | — | IC50 | = | 61.8 | nM | 7.21 |
| CHEMBL585352 | — | IC50 | = | 63.2 | nM | 7.20 |
| CHEMBL567446 | — | IC50 | = | 68.2 | nM | 7.17 |
| CHEMBL584285 | — | IC50 | = | 80.2 | nM | 7.10 |
| CHEMBL571693 | — | IC50 | = | 86.6 | nM | 7.06 |
| CHEMBL571469 | — | IC50 | = | 86.6 | nM | 7.06 |
| CHEMBL571913 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL579669 | — | IC50 | = | 98.9 | nM | 7.00 |
| CHEMBL571912 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL569265 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL567255 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL583835 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL567229 | — | IC50 | = | 261.0 | nM | 6.58 |
| CHEMBL567252 | — | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL565331 | — | IC50 | = | 398.0 | nM | 6.40 |
| CHEMBL566819 | — | IC50 | = | 398.0 | nM | 6.40 |
| CHEMBL565518 | — | IC50 | = | 576.0 | nM | 6.24 |
| CHEMBL567469 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL567251 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL566596 | — | IC50 | > | 2000.0 | nM | - |