Assay Detail
Functional
CHEMBL858539
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity on halphaCGRP-induced cAMP accumulation at human neuroblastoma SK-N-MC cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SK-N-MC |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Calcitonin-gene-related peptide receptor, CALCRL/RAMP1 (CHEMBL2107838) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Identification of the key residue of calcitonin gene related peptide (CGRP) 27-37 to obtain antagonists with picomolar affinity at the CGRP receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 4 | 7.83 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2371890 | — | — | 1 | 8.20 |
| CHEMBL386763 | — | — | 1 | 8.00 |
| CHEMBL385986 | — | — | 1 | 7.60 |
| CHEMBL2371891 | — | — | 1 | 7.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2371890 | — | Kd | = | 6.31 | nM | 8.20 |
| CHEMBL386763 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL385986 | — | Kd | = | 25.12 | nM | 7.60 |
| CHEMBL2371891 | — | Kd | = | 31.62 | nM | 7.50 |