Assay Detail
Binding
CHEMBL4682704
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at PAC1 receptor (unknown origin) expressed in CHO cells assessed as inhibition of PACAP-induced inhibition of CREB phosphorylation preincubated for 30 mins followed by PACAP stimulation and measured after 30 mins by Western blot analysis
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Pituitary adenylate cyclase-activating polypeptide type I receptor (CHEMBL5399) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis of a novel and potent small-molecule antagonist of PAC1 receptor for the treatment of neuropathic pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 2 | - | - |
| IC50 | 2 | 9.74 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4757203 | — | — | 2 | 9.74 |
| CHEMBL4740931 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4757203 | — | IC50 | = | 0.182 | nM | 9.74 |
| CHEMBL4757203 | — | Inhibition | - | % | - | |
| CHEMBL4740931 | — | Inhibition | - | % | - | |
| CHEMBL4740931 | — | IC50 | < | 0.01 | nM | - |