Assay Detail
Functional
CHEMBL686663
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In vitro inhibition of histamine-induced contractions in guinea pig ileum
55
Total Activities
55
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 | Expert |
Publication
Synthesis of 2-(4-substituted-1-piperazinyl)benzimidazoles as H1-antihistaminic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 55 | 7.38 | 8.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL594 | EMEDASTINE | 4.0 | 1 | 8.21 |
| CHEMBL276735 | — | — | 1 | 8.16 |
| CHEMBL275383 | — | — | 1 | 8.13 |
| CHEMBL416357 | — | — | 1 | 8.08 |
| CHEMBL17795 | — | — | 1 | 8.08 |
| CHEMBL273315 | — | — | 1 | 8.07 |
| CHEMBL418731 | — | — | 1 | 8.04 |
| CHEMBL430338 | — | — | 1 | 8.00 |
| CHEMBL18561 | — | — | 1 | 8.00 |
| CHEMBL18233 | — | — | 1 | 8.00 |
| CHEMBL279875 | — | — | 1 | 8.00 |
| CHEMBL18123 | — | — | 1 | 8.00 |
| CHEMBL278053 | — | — | 1 | 7.96 |
| CHEMBL1659 | CHLORPHENIRAMINE MALEATE | 4.0 | 1 | 7.92 |
| CHEMBL277311 | — | — | 1 | 7.92 |
| CHEMBL279872 | — | — | 1 | 7.89 |
| CHEMBL278504 | — | — | 1 | 7.82 |
| CHEMBL18255 | — | — | 1 | 7.82 |
| CHEMBL18151 | — | — | 1 | 7.80 |
| CHEMBL18234 | — | — | 1 | 7.80 |
| CHEMBL17474 | — | — | 1 | 7.80 |
| CHEMBL17246 | — | — | 1 | 7.77 |
| CHEMBL17876 | — | — | 1 | 7.77 |
| CHEMBL18060 | — | — | 1 | 7.75 |
| CHEMBL17349 | — | — | 1 | 7.75 |
| CHEMBL17893 | — | — | 1 | 7.72 |
| CHEMBL17555 | — | — | 1 | 7.72 |
| CHEMBL273320 | — | — | 1 | 7.70 |
| CHEMBL274747 | — | — | 1 | 7.60 |
| CHEMBL278457 | — | — | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL594 | EMEDASTINE | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL276735 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL275383 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL416357 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL17795 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL273315 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL418731 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL430338 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL18561 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL18233 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL279875 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL18123 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL278053 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL277311 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1659 | CHLORPHENIRAMINE MALEATE | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL279872 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL278504 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL18255 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL18151 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL18234 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL17474 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL17246 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL17876 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL18060 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL17349 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL17893 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL17555 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL273320 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL274747 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL278457 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL17742 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL18181 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL280255 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL276070 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL18122 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL278456 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL276774 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL17946 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL17763 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL17959 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL277749 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL18062 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL277956 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL17808 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL16939 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL17655 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL16938 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL17556 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL279621 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL17635 | — | IC50 | = | 1400.0 | nM | 5.85 |