Assay Detail
Functional
CHEMBL4047731
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 intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
22
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H1 receptor antagonists for use in allergic rhinitis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 22 | 9.10 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4060529 | — | — | 1 | 9.70 |
| CHEMBL4059750 | — | — | 1 | 9.70 |
| CHEMBL639 | AZELASTINE | 4.0 | 1 | 9.70 |
| CHEMBL4084325 | — | — | 1 | 9.58 |
| CHEMBL4098917 | — | — | 1 | 9.46 |
| CHEMBL4102287 | — | — | 1 | 9.40 |
| CHEMBL4098192 | — | — | 1 | 9.40 |
| CHEMBL4088036 | — | — | 1 | 9.27 |
| CHEMBL4069073 | — | — | 1 | 9.20 |
| CHEMBL4080880 | — | — | 1 | 9.13 |
| CHEMBL4082646 | — | — | 1 | 9.08 |
| CHEMBL4088039 | — | — | 1 | 9.00 |
| CHEMBL4065123 | — | — | 1 | 9.00 |
| CHEMBL4063163 | — | — | 1 | 9.00 |
| CHEMBL4080166 | — | — | 1 | 8.90 |
| CHEMBL4095759 | — | — | 1 | 8.85 |
| CHEMBL4060765 | — | — | 1 | 8.70 |
| CHEMBL4068414 | — | — | 2 | 8.70 |
| CHEMBL4090136 | — | — | 1 | 8.70 |
| CHEMBL4079248 | — | — | 1 | 8.68 |
| CHEMBL4085417 | — | — | 1 | 8.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4060529 | — | Kd | = | 0.1995 | nM | 9.70 |
| CHEMBL4059750 | — | Kd | = | 0.1995 | nM | 9.70 |
| CHEMBL639 | AZELASTINE | Kd | = | 0.1995 | nM | 9.70 |
| CHEMBL4084325 | — | Kd | = | 0.263 | nM | 9.58 |
| CHEMBL4098917 | — | Kd | = | 0.3467 | nM | 9.46 |
| CHEMBL4102287 | — | Kd | = | 0.3981 | nM | 9.40 |
| CHEMBL4098192 | — | Kd | = | 0.3981 | nM | 9.40 |
| CHEMBL4088036 | — | Kd | = | 0.537 | nM | 9.27 |
| CHEMBL4069073 | — | Kd | = | 0.631 | nM | 9.20 |
| CHEMBL4080880 | — | Kd | = | 0.7413 | nM | 9.13 |
| CHEMBL4082646 | — | Kd | = | 0.8318 | nM | 9.08 |
| CHEMBL4088039 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL4063163 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL4065123 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL4080166 | — | Kd | = | 1.259 | nM | 8.90 |
| CHEMBL4095759 | — | Kd | = | 1.413 | nM | 8.85 |
| CHEMBL4060765 | — | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL4068414 | — | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL4090136 | — | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL4079248 | — | Kd | = | 2.089 | nM | 8.68 |
| CHEMBL4068414 | — | Kd | = | 2.512 | nM | 8.60 |
| CHEMBL4085417 | — | Kd | = | 3.715 | nM | 8.43 |