Assay Detail
Binding
CHEMBL4337378
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Displacement of 3 nM [3H]Nalpha-methylhistamine from human H3R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
[<sup>3</sup>H]UR-DEBa176: A 2,4-Diaminopyrimidine-Type Radioligand Enabling Binding Studies at the Human, Mouse, and Rat Histamine H<sub>4</sub> Receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.30 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4454158 | — | — | 1 | 8.48 |
| CHEMBL4455324 | — | — | 1 | 7.86 |
| CHEMBL4443126 | — | — | 1 | 7.56 |
| CHEMBL4439142 | — | — | 1 | 6.84 |
| CHEMBL4543928 | — | — | 1 | 6.69 |
| CHEMBL4586599 | — | — | 1 | 6.16 |
| CHEMBL4445423 | — | — | 1 | 5.95 |
| CHEMBL4543119 | — | — | 1 | 5.62 |
| CHEMBL4538671 | — | — | 1 | 5.52 |
| CHEMBL4513421 | — | — | 1 | 5.46 |
| CHEMBL4534254 | — | — | 1 | 5.26 |
| CHEMBL4437371 | — | — | 1 | 5.25 |
| CHEMBL4576393 | — | — | 1 | 5.22 |
| CHEMBL4466349 | — | — | 1 | - |
| CHEMBL4471442 | — | — | 1 | - |
| CHEMBL4563834 | — | — | 1 | - |
| CHEMBL4513989 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4454158 | — | Ki | = | 3.311 | nM | 8.48 |
| CHEMBL4455324 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL4443126 | — | Ki | = | 27.54 | nM | 7.56 |
| CHEMBL4439142 | — | Ki | = | 144.54 | nM | 6.84 |
| CHEMBL4543928 | — | Ki | = | 204.17 | nM | 6.69 |
| CHEMBL4586599 | — | Ki | = | 691.83 | nM | 6.16 |
| CHEMBL4445423 | — | Ki | = | 1122.02 | nM | 5.95 |
| CHEMBL4543119 | — | Ki | = | 2398.83 | nM | 5.62 |
| CHEMBL4538671 | — | Ki | = | 3019.95 | nM | 5.52 |
| CHEMBL4513421 | — | Ki | = | 3467.37 | nM | 5.46 |
| CHEMBL4534254 | — | Ki | = | 5495.41 | nM | 5.26 |
| CHEMBL4437371 | — | Ki | = | 5623.41 | nM | 5.25 |
| CHEMBL4576393 | — | Ki | = | 6025.6 | nM | 5.22 |
| CHEMBL4466349 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4471442 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4563834 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4513989 | — | Ki | > | 10000.0 | nM | - |