Assay Detail
Functional
CHEMBL695158
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Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis and pharmacological activity of fluorescent histamine H1 receptor antagonists related to mepyramine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 21 | 7.91 | 9.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL511 | PYRILAMINE | 4.0 | 1 | 9.42 |
| CHEMBL277848 | — | — | 1 | 8.71 |
| CHEMBL21721 | — | — | 1 | 8.47 |
| CHEMBL21525 | — | — | 1 | 8.35 |
| CHEMBL281365 | — | — | 1 | 8.33 |
| CHEMBL277850 | — | — | 1 | 8.30 |
| CHEMBL624 | 2-[(2-METHYLAMINOETHYL)(P-METHOXYBENZYL)AMINO]PYRIDINE | — | 1 | 8.18 |
| CHEMBL21735 | — | — | 1 | 8.01 |
| CHEMBL21278 | — | — | 1 | 7.89 |
| CHEMBL416378 | — | — | 1 | 7.88 |
| CHEMBL1169587 | — | — | 1 | 7.83 |
| CHEMBL22749 | — | — | 1 | 7.75 |
| CHEMBL21833 | — | — | 1 | 7.67 |
| CHEMBL21520 | — | — | 1 | 7.65 |
| CHEMBL21898 | — | — | 1 | 7.58 |
| CHEMBL24940 | — | — | 1 | 7.58 |
| CHEMBL21514 | — | — | 1 | 7.50 |
| CHEMBL20713 | — | — | 1 | 7.48 |
| CHEMBL21727 | — | — | 1 | 7.44 |
| CHEMBL22152 | — | — | 1 | 7.16 |
| CHEMBL283527 | — | — | 1 | 6.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL511 | PYRILAMINE | Kd | = | 0.3802 | nM | 9.42 |
| CHEMBL277848 | — | Kd | = | 1.95 | nM | 8.71 |
| CHEMBL21721 | — | Kd | = | 3.388 | nM | 8.47 |
| CHEMBL21525 | — | Kd | = | 4.467 | nM | 8.35 |
| CHEMBL281365 | — | Kd | = | 4.677 | nM | 8.33 |
| CHEMBL277850 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL624 | 2-[(2-METHYLAMINOETHYL)(P-METHOXYBENZYL)AMINO]PYRIDINE | Kd | = | 6.607 | nM | 8.18 |
| CHEMBL21735 | — | Kd | = | 9.772 | nM | 8.01 |
| CHEMBL21278 | — | Kd | = | 12.88 | nM | 7.89 |
| CHEMBL416378 | — | Kd | = | 13.18 | nM | 7.88 |
| CHEMBL1169587 | — | Kd | = | 14.79 | nM | 7.83 |
| CHEMBL22749 | — | Kd | = | 17.78 | nM | 7.75 |
| CHEMBL21833 | — | Kd | = | 21.38 | nM | 7.67 |
| CHEMBL21520 | — | Kd | = | 22.39 | nM | 7.65 |
| CHEMBL21898 | — | Kd | = | 26.3 | nM | 7.58 |
| CHEMBL24940 | — | Kd | = | 26.3 | nM | 7.58 |
| CHEMBL21514 | — | Kd | = | 31.62 | nM | 7.50 |
| CHEMBL20713 | — | Kd | = | 33.11 | nM | 7.48 |
| CHEMBL21727 | — | Kd | = | 36.31 | nM | 7.44 |
| CHEMBL22152 | — | Kd | = | 69.18 | nM | 7.16 |
| CHEMBL283527 | — | Kd | = | 144.54 | nM | 6.84 |