Assay Detail
Functional
CHEMBL698813
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonistic activity by inhibition histamine H2 receptor from rats.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and pharmacological evaluation of highly potent dual histamine H2 and gastrin receptor antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 17 | 6.37 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL285556 | — | — | 1 | 7.80 |
| CHEMBL284374 | — | — | 1 | 7.30 |
| CHEMBL33398 | — | — | 1 | 6.80 |
| CHEMBL30 | CIMETIDINE | 4.0 | 1 | 6.60 |
| CHEMBL33698 | — | — | 1 | 6.60 |
| CHEMBL285719 | — | — | 1 | 6.50 |
| CHEMBL406844 | — | — | 1 | 6.50 |
| CHEMBL290122 | — | — | 1 | 6.40 |
| CHEMBL287295 | — | — | 1 | 6.30 |
| CHEMBL33412 | — | — | 1 | 6.20 |
| CHEMBL285995 | — | — | 1 | 6.10 |
| CHEMBL284976 | — | — | 1 | 6.10 |
| CHEMBL432671 | — | — | 1 | 6.00 |
| CHEMBL33743 | — | — | 1 | 6.00 |
| CHEMBL284975 | — | — | 1 | 5.90 |
| CHEMBL286835 | — | — | 1 | 5.70 |
| CHEMBL282175 | — | — | 1 | 5.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL285556 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL284374 | — | Kd | = | 50.12 | nM | 7.30 |
| CHEMBL33398 | — | Kd | = | 158.49 | nM | 6.80 |
| CHEMBL30 | CIMETIDINE | Kd | = | 251.19 | nM | 6.60 |
| CHEMBL33698 | — | Kd | = | 251.19 | nM | 6.60 |
| CHEMBL285719 | — | Kd | = | 316.23 | nM | 6.50 |
| CHEMBL406844 | — | Kd | = | 316.23 | nM | 6.50 |
| CHEMBL290122 | — | Kd | = | 398.11 | nM | 6.40 |
| CHEMBL287295 | — | Kd | = | 501.19 | nM | 6.30 |
| CHEMBL33412 | — | Kd | = | 630.96 | nM | 6.20 |
| CHEMBL285995 | — | Kd | = | 794.33 | nM | 6.10 |
| CHEMBL284976 | — | Kd | = | 794.33 | nM | 6.10 |
| CHEMBL432671 | — | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL33743 | — | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL284975 | — | Kd | = | 1258.93 | nM | 5.90 |
| CHEMBL286835 | — | Kd | = | 1995.26 | nM | 5.70 |
| CHEMBL282175 | — | Kd | = | 3162.28 | nM | 5.50 |