Assay Detail
Functional
CHEMBL685650
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Ability to inhibit histamine-induced contractions of isolated guinea pig ileum
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 1 — Organism |
| Curated By | Expert |
Publication
Synthesis, structure-activity relationships, and pharmacological evaluation of pyrrolo[3,2,1-ij]quinoline derivatives: potent histamine and platelet activating factor antagonism and 5-lipoxygenase inhibitory properties. Potential therapeutic application in asthma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 45 | 6.65 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL534 | KETOTIFEN | 4.0 | 1 | 8.19 |
| CHEMBL511 | PYRILAMINE | 4.0 | 1 | 7.77 |
| CHEMBL158099 | — | — | 1 | 7.72 |
| CHEMBL639 | AZELASTINE | 4.0 | 1 | 7.70 |
| CHEMBL159099 | — | — | 1 | 7.68 |
| CHEMBL161815 | — | — | 1 | 7.64 |
| CHEMBL350328 | — | — | 1 | 7.52 |
| CHEMBL161729 | — | — | 1 | 7.50 |
| CHEMBL423606 | — | — | 1 | 7.48 |
| CHEMBL440367 | — | — | 1 | 7.43 |
| CHEMBL162638 | — | — | 1 | 7.20 |
| CHEMBL162359 | — | — | 1 | 7.19 |
| CHEMBL161822 | — | — | 1 | 7.16 |
| CHEMBL161732 | — | — | 1 | 7.12 |
| CHEMBL159095 | — | — | 1 | 7.10 |
| CHEMBL161151 | — | — | 1 | 7.07 |
| CHEMBL158098 | — | — | 1 | 7.05 |
| CHEMBL161591 | — | — | 1 | 6.96 |
| CHEMBL351670 | — | — | 1 | 6.85 |
| CHEMBL157582 | — | — | 1 | 6.75 |
| CHEMBL349081 | — | — | 1 | 6.72 |
| CHEMBL161676 | — | — | 1 | 6.60 |
| CHEMBL435656 | — | — | 1 | 6.60 |
| CHEMBL158583 | — | — | 1 | 6.58 |
| CHEMBL161654 | — | — | 1 | 6.55 |
| CHEMBL159417 | — | — | 1 | 6.54 |
| CHEMBL159054 | — | — | 1 | 6.47 |
| CHEMBL161662 | — | — | 1 | 6.46 |
| CHEMBL1000 | CETIRIZINE | 4.0 | 1 | 6.42 |
| CHEMBL161575 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL534 | KETOTIFEN | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL511 | PYRILAMINE | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL158099 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL639 | AZELASTINE | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL159099 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL161815 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL350328 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL161729 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL423606 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL440367 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL162638 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL162359 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL161822 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL161732 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL159095 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL161151 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL158098 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL161591 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL351670 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL157582 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL349081 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL435656 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL161676 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL158583 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL161654 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL159417 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL159054 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL161662 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL1000 | CETIRIZINE | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL161575 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL157994 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL162537 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL352162 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL159363 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL348539 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL159180 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL162647 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL160201 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL161161 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL158820 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL161513 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL162586 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL161089 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL159511 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL157537 | — | IC50 | = | 8300.0 | nM | 5.08 |