Assay Detail
Functional
CHEMBL3870971
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 |
|---|---|---|---|
| Kd | 7 | 8.67 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL639 | AZELASTINE | 4.0 | 1 | 9.70 |
| CHEMBL1767164 | GSK-1004723 | 2.0 | 1 | 9.10 |
| CHEMBL3898341 | — | — | 1 | 8.80 |
| CHEMBL3926412 | — | — | 1 | 8.60 |
| CHEMBL3893197 | — | — | 1 | 8.30 |
| CHEMBL3917428 | — | — | 1 | 8.20 |
| CHEMBL3947980 | — | — | 1 | 8.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL639 | AZELASTINE | Kd | = | 0.1995 | nM | 9.70 |
| CHEMBL1767164 | GSK-1004723 | Kd | = | 0.7943 | nM | 9.10 |
| CHEMBL3898341 | — | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL3926412 | — | Kd | = | 2.512 | nM | 8.60 |
| CHEMBL3893197 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL3917428 | — | Kd | = | 6.31 | nM | 8.20 |
| CHEMBL3947980 | — | Kd | = | 10.0 | nM | 8.00 |