Assay Detail
Binding
CHEMBL2033344
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Competitive inhibition of Epac2 using fluorescent nucleotide analog 8-NBD-cAMP by fluorescence analysis
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Rap guanine nucleotide exchange factor 4 (CHEMBL2029198) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
5-Cyano-6-oxo-1,6-dihydro-pyrimidines as potent antagonists targeting exchange proteins directly activated by cAMP.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 4.88 | 5.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2030612 | — | — | 1 | 5.40 |
| CHEMBL2030613 | — | — | 1 | 5.23 |
| CHEMBL2030607 | — | — | 1 | 5.16 |
| CHEMBL2030452 | — | — | 1 | 5.08 |
| CHEMBL2030610 | — | — | 1 | 4.94 |
| CHEMBL2030611 | — | — | 1 | 4.90 |
| CHEMBL2030608 | — | — | 1 | 4.80 |
| CHEMBL2030609 | — | — | 1 | 4.52 |
| CHEMBL2030606 | — | — | 1 | 4.41 |
| CHEMBL316966 | CYCLIC ADENOSINE MONOPHOSPHATE | — | 1 | 4.32 |
| CHEMBL2030605 | — | — | 1 | - |
| CHEMBL2030614 | — | — | 1 | - |
| CHEMBL2030615 | — | — | 1 | - |
| CHEMBL2030616 | — | — | 1 | - |
| CHEMBL2030617 | — | — | 1 | - |
| CHEMBL2030618 | — | — | 1 | - |
| CHEMBL2030619 | — | — | 1 | - |
| CHEMBL2030620 | — | — | 1 | - |
| CHEMBL2030621 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2030612 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL2030613 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL2030607 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL2030452 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL2030610 | — | IC50 | = | 11600.0 | nM | 4.94 |
| CHEMBL2030611 | — | IC50 | = | 12700.0 | nM | 4.90 |
| CHEMBL2030608 | — | IC50 | = | 15700.0 | nM | 4.80 |
| CHEMBL2030609 | — | IC50 | = | 30500.0 | nM | 4.52 |
| CHEMBL2030606 | — | IC50 | = | 38700.0 | nM | 4.41 |
| CHEMBL316966 | CYCLIC ADENOSINE MONOPHOSPHATE | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL2030605 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL2030614 | — | IC50 | = | 127000.0 | nM | - |
| CHEMBL2030615 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL2030616 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL2030617 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL2030618 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL2030619 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL2030620 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL2030621 | — | IC50 | > | 300000.0 | nM | - |