Assay Detail
Functional
CHEMBL649930
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonism of recombinant human bombesin receptor (bb1) labeled with [125I]- [Tyr] bombesin stably expressed in CHO cells
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 8.86 | 10.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL403317 | — | — | 1 | 10.17 |
| CHEMBL329650 | — | — | 1 | 9.82 |
| CHEMBL405908 | — | — | 1 | 9.77 |
| CHEMBL327388 | — | — | 1 | 9.52 |
| CHEMBL327840 | — | — | 1 | 9.49 |
| CHEMBL86370 | — | — | 1 | 9.41 |
| CHEMBL85400 | — | — | 1 | 9.36 |
| CHEMBL312926 | — | — | 1 | 9.34 |
| CHEMBL433143 | — | — | 1 | 9.28 |
| CHEMBL85291 | — | — | 1 | 9.23 |
| CHEMBL87846 | — | — | 1 | 9.21 |
| CHEMBL313346 | — | — | 1 | 9.01 |
| CHEMBL313030 | — | — | 1 | 8.82 |
| CHEMBL437027 | BOMBESIN | 1.0 | 1 | 8.70 |
| CHEMBL327678 | — | — | 1 | 8.68 |
| CHEMBL314375 | — | — | 1 | 8.68 |
| CHEMBL316085 | — | — | 1 | 8.55 |
| CHEMBL90614 | — | — | 1 | 8.54 |
| CHEMBL89734 | — | — | 1 | 8.47 |
| CHEMBL86828 | — | — | 1 | 8.20 |
| CHEMBL413196 | — | — | 1 | 8.04 |
| CHEMBL88010 | — | — | 1 | 8.03 |
| CHEMBL87079 | — | — | 1 | 7.57 |
| CHEMBL89813 | — | — | 1 | 6.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL403317 | — | Ki | = | 0.068 | nM | 10.17 |
| CHEMBL329650 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL405908 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL327388 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL327840 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL86370 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL85400 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL312926 | — | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL433143 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL85291 | — | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL87846 | — | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL313346 | — | Ki | = | 0.97 | nM | 9.01 |
| CHEMBL313030 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL437027 | BOMBESIN | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL327678 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL314375 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL316085 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL90614 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL89734 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL86828 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL413196 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL88010 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL87079 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL89813 | — | Ki | = | 184.0 | nM | 6.74 |