Assay Detail
Binding
CHEMBL1780332
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PDE8B
57
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B (CHEMBL4408) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
1,5-Substituted nipecotic amides: selective PDE8 inhibitors displaying diastereomer-dependent microsomal stability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 57 | 7.55 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1780094 | — | — | 1 | 9.92 |
| CHEMBL1779987 | — | — | 1 | 9.05 |
| CHEMBL1780096 | — | — | 1 | 9.02 |
| CHEMBL1780085 | — | — | 1 | 8.71 |
| CHEMBL1780116 | — | — | 1 | 8.54 |
| CHEMBL1779988 | — | — | 1 | 8.49 |
| CHEMBL1780089 | — | — | 1 | 8.41 |
| CHEMBL1780100 | — | — | 1 | 8.41 |
| CHEMBL1780097 | — | — | 1 | 8.37 |
| CHEMBL1780111 | — | — | 1 | 8.36 |
| CHEMBL1780105 | — | — | 1 | 8.36 |
| CHEMBL1779976 | — | — | 1 | 8.30 |
| CHEMBL1779984 | — | — | 1 | 8.22 |
| CHEMBL1779985 | — | — | 1 | 8.22 |
| CHEMBL1779990 | — | — | 1 | 8.15 |
| CHEMBL1780084 | — | — | 1 | 8.14 |
| CHEMBL1780087 | — | — | 1 | 7.89 |
| CHEMBL1779986 | — | — | 1 | 7.82 |
| CHEMBL1780086 | — | — | 1 | 7.78 |
| CHEMBL1780102 | — | — | 1 | 7.71 |
| CHEMBL1780090 | — | — | 1 | 7.58 |
| CHEMBL1780104 | — | — | 1 | 7.58 |
| CHEMBL1780103 | — | — | 1 | 7.45 |
| CHEMBL1779983 | — | — | 1 | 7.40 |
| CHEMBL1777837 | — | — | 4 | 7.37 |
| CHEMBL1780118 | — | — | 1 | 7.36 |
| CHEMBL1780091 | — | — | 1 | 7.24 |
| CHEMBL1780088 | — | — | 1 | 7.19 |
| CHEMBL1780093 | — | — | 1 | 7.18 |
| CHEMBL1780101 | — | — | 1 | 7.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1780094 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL1779987 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL1780096 | — | IC50 | = | 0.955 | nM | 9.02 |
| CHEMBL1780085 | — | IC50 | = | 1.96 | nM | 8.71 |
| CHEMBL1780116 | — | IC50 | = | 2.91 | nM | 8.54 |
| CHEMBL1779988 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL1780089 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL1780100 | — | IC50 | = | 3.86 | nM | 8.41 |
| CHEMBL1780097 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL1780111 | — | IC50 | = | 4.42 | nM | 8.36 |
| CHEMBL1780105 | — | IC50 | = | 4.36 | nM | 8.36 |
| CHEMBL1779976 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1779985 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1779984 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1779990 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1780084 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL1780087 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1779986 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1780086 | — | IC50 | = | 16.5 | nM | 7.78 |
| CHEMBL1780102 | — | IC50 | = | 19.6 | nM | 7.71 |
| CHEMBL1780090 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1780104 | — | IC50 | = | 26.2 | nM | 7.58 |
| CHEMBL1780103 | — | IC50 | = | 35.2 | nM | 7.45 |
| CHEMBL1779983 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1777837 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL1780118 | — | IC50 | = | 44.1 | nM | 7.36 |
| CHEMBL1780091 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL1780088 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL1780101 | — | IC50 | = | 65.9 | nM | 7.18 |
| CHEMBL1780093 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL1779991 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1780092 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL1780112 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL1779978 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL1780115 | — | IC50 | = | 284.0 | nM | 6.55 |
| CHEMBL1779977 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL1780099 | — | IC50 | = | 516.0 | nM | 6.29 |
| CHEMBL1780117 | — | IC50 | = | 675.0 | nM | 6.17 |
| CHEMBL1780108 | — | IC50 | = | 707.0 | nM | 6.15 |
| CHEMBL1779982 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1779980 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL1779989 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL1779981 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1779979 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1780120 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1780119 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1780113 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1780109 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1780107 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1780106 | — | IC50 | > | 10000.0 | nM | - |