Assay Detail
Binding
CHEMBL859562
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Displacement of [3H-propionyl-K24] from halphaCGRP expressed in human neuroblastoma SK-N-MC cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 14 | 9.21 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL264010 | — | — | 1 | 10.70 |
| CHEMBL2371890 | — | — | 1 | 10.70 |
| CHEMBL427759 | — | — | 1 | 9.15 |
| CHEMBL2371892 | — | — | 1 | 8.74 |
| CHEMBL385986 | — | — | 1 | 8.08 |
| CHEMBL406459 | — | — | 1 | 7.87 |
| CHEMBL374233 | — | — | 1 | - |
| CHEMBL386763 | — | — | 1 | - |
| CHEMBL2371891 | — | — | 1 | - |
| CHEMBL2371889 | — | — | 1 | - |
| CHEMBL269736 | — | — | 1 | - |
| CHEMBL402700 | — | — | 1 | - |
| CHEMBL269734 | — | — | 1 | - |
| CHEMBL218907 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL264010 | — | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL2371890 | — | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL427759 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL2371892 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL385986 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL406459 | — | Ki | = | 13.6 | nM | 7.87 |
| CHEMBL374233 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL386763 | — | Ki | = | 0.002 | nM | - |
| CHEMBL2371891 | — | Ki | = | 0.006 | nM | - |
| CHEMBL2371889 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL269736 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL402700 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL269734 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL218907 | — | Ki | > | 10000.0 | nM | - |