Compound Detail
CHEMBL293802
ARPROMIDINE 🧪 Phase II
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🧪 Phase II
Basic Information
| ChEMBL ID | CHEMBL293802 |
| Name | ARPROMIDINE |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | KZZIVOLMJPSDEP-UHFFFAOYSA-N |
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
8
Publications
2
Known Names
Molecular Properties
380.5
MW (Da)
3.21
ALogP
3
HBA
4
HBD
89.5
PSA (Ų)
0.26
QED
0
Ro5 Violations
9
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Racemic |
Activity Summary
Kd 2 meas. best 7.65
EC50 1 meas. best 8.01
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Histamine H2 receptor CHEMBL2882 | EC50 | 8.01 | 8.01 | 9.8 | 1 |
| Histamine H1 receptor CHEMBL3943 | Kd | 7.65 | 7.65 | 22.4 | 2 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Histamine H2 receptor | EC50 | = | 9.772 | nM | 8.01 | Agonist activity at histamine H2 receptor in guinea pig spontaneously beating ri... | 18950149 |
| Histamine H1 receptor | Kd | = | 22.39 | nM | 7.65 | Antagonist activity at histamine H1 receptor against histamine in isolated ileum... | 2569042 |
| Histamine H1 receptor | Kd | = | 22.39 | nM | 7.65 | Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inh... | 18950149 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 2569042 | 10.1021/jm00128a045 | Histamine H2 receptor | 5 |
| 2569042 | 10.1021/jm00128a045 | Cavia porcellus | 4 |
| 18950149 | 10.1021/jm800841w | Histamine H2 receptor | 3 |
| - | 10.1016/0960-894X(95)00369-5 | Neuropeptide Y receptor type 1 | 2 |
| - | 10.1016/0960-894X(95)00369-5 | Histamine H2 receptor | 2 |
| 2569042 | 10.1021/jm00128a045 | Histamine H1 receptor | 1 |
| - | 10.1016/0960-894X(95)00369-5 | Histamine H1 receptor | 1 |
| 18950149 | 10.1021/jm800841w | Histamine H1 receptor | 1 |
Data from ChEMBL 36 via Core Engine