Assay Detail
ADMET
CHEMBL3870964
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at adrenergic alpha1A receptor (unknown origin) expressed in Rat1 cells assessed as inhibition of phenylephrine-induced Ca2+ flux preincubated for 30 mins followed by phenylephrine addition by Fluo-4-AM-dye based FLIPR assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | Rat1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
The discovery of quinoline based single-ligand human H1 and H3 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.22 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3947980 | — | — | 1 | 8.10 |
| CHEMBL3921827 | — | — | 1 | 7.50 |
| CHEMBL1767164 | GSK-1004723 | 2.0 | 1 | 7.40 |
| CHEMBL639 | AZELASTINE | 4.0 | 1 | 7.30 |
| CHEMBL3917428 | — | — | 1 | 7.30 |
| CHEMBL3952802 | — | — | 1 | 7.20 |
| CHEMBL3893197 | — | — | 1 | 7.10 |
| CHEMBL3926412 | — | — | 1 | 6.60 |
| CHEMBL3898341 | — | — | 1 | 6.50 |
| CHEMBL3917794 | — | — | 1 | - |
| CHEMBL3967709 | — | — | 1 | - |
| CHEMBL3896541 | — | — | 1 | - |
| CHEMBL3953018 | — | — | 1 | - |
| CHEMBL3925332 | — | — | 1 | - |
| CHEMBL3925977 | — | — | 1 | - |
| CHEMBL3935303 | — | — | 1 | - |
| CHEMBL3907368 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3947980 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL3921827 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL1767164 | GSK-1004723 | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL639 | AZELASTINE | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL3917428 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL3952802 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL3893197 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL3926412 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL3898341 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL3917794 | — | Ki | > | 1995.26 | nM | - |
| CHEMBL3967709 | — | Ki | > | 1995.26 | nM | - |
| CHEMBL3896541 | — | Ki | > | 1995.26 | nM | - |
| CHEMBL3953018 | — | Ki | > | 1995.26 | nM | - |
| CHEMBL3925332 | — | Ki | > | 1995.26 | nM | - |
| CHEMBL3925977 | — | Ki | > | 1995.26 | nM | - |
| CHEMBL3935303 | — | Ki | > | 1995.26 | nM | - |
| CHEMBL3907368 | — | Ki | > | 1995.26 | nM | - |