Assay Detail
Functional
CHEMBL1638851
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SK-N-MC |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Histamine H4 receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 37 | 6.53 | 7.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281576 | — | — | 1 | 7.90 |
| CHEMBL19439 | IMETIT | — | 1 | 7.90 |
| CHEMBL19010 | IODOPROXYFAN | — | 1 | 7.90 |
| CHEMBL18661 | IMMEPIP | — | 1 | 7.80 |
| CHEMBL306077 | — | — | 1 | 7.70 |
| CHEMBL12160 | BURIMAMIDE | — | 1 | 7.70 |
| CHEMBL1632409 | CLOBENPROBIT | — | 1 | 7.70 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 7.70 |
| CHEMBL12608 | IMPROMIDINE | 2.0 | 1 | 7.60 |
| CHEMBL90019 | IMBUTAMINE | — | 1 | 7.50 |
| CHEMBL275443 | 4-METHYLHISTAMINE | — | 1 | 7.40 |
| CHEMBL1196470 | — | — | 1 | 7.30 |
| CHEMBL72372 | — | — | 1 | 7.20 |
| CHEMBL19173 | PROXYFAN | — | 1 | 7.20 |
| CHEMBL72769 | — | — | 1 | 7.20 |
| CHEMBL321860 | — | — | 1 | 7.10 |
| CHEMBL72431 | — | — | 1 | 7.10 |
| CHEMBL309819 | — | — | 1 | 7.00 |
| CHEMBL320331 | — | — | 1 | 6.90 |
| CHEMBL91353 | HOMOHISTAMINE | — | 1 | 6.70 |
| CHEMBL106158 | — | — | 1 | 6.70 |
| CHEMBL268229 | — | — | 1 | 6.20 |
| CHEMBL268490 | — | — | 1 | 6.10 |
| CHEMBL105803 | — | — | 1 | 6.10 |
| CHEMBL82298 | IMMETHRIDINE | — | 1 | 6.00 |
| CHEMBL308913 | — | — | 1 | 5.90 |
| CHEMBL12344 | DIMAPRIT | — | 1 | 5.80 |
| CHEMBL106612 | IMIFURAMINE | — | 1 | 5.70 |
| CHEMBL321920 | — | — | 1 | 5.30 |
| CHEMBL175782 | METHIMEPIP | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281576 | — | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL19010 | IODOPROXYFAN | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL19439 | IMETIT | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL18661 | IMMEPIP | EC50 | = | 15.85 | nM | 7.80 |
| CHEMBL306077 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL12160 | BURIMAMIDE | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL1632409 | CLOBENPROBIT | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL90 | HISTAMINE | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL12608 | IMPROMIDINE | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL90019 | IMBUTAMINE | EC50 | = | 31.62 | nM | 7.50 |
| CHEMBL275443 | 4-METHYLHISTAMINE | EC50 | = | 39.81 | nM | 7.40 |
| CHEMBL1196470 | — | EC50 | = | 50.12 | nM | 7.30 |
| CHEMBL72372 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL19173 | PROXYFAN | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL72769 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL321860 | — | EC50 | = | 79.43 | nM | 7.10 |
| CHEMBL72431 | — | EC50 | = | 79.43 | nM | 7.10 |
| CHEMBL309819 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL320331 | — | EC50 | = | 125.89 | nM | 6.90 |
| CHEMBL106158 | — | EC50 | = | 199.53 | nM | 6.70 |
| CHEMBL91353 | HOMOHISTAMINE | EC50 | = | 199.53 | nM | 6.70 |
| CHEMBL268229 | — | EC50 | = | 630.96 | nM | 6.20 |
| CHEMBL268490 | — | EC50 | = | 794.33 | nM | 6.10 |
| CHEMBL105803 | — | EC50 | = | 794.33 | nM | 6.10 |
| CHEMBL82298 | IMMETHRIDINE | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL308913 | — | EC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL12344 | DIMAPRIT | EC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL106612 | IMIFURAMINE | EC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL321920 | — | EC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL175782 | METHIMEPIP | EC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL108649 | — | EC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL106913 | — | EC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL1632410 | — | EC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL322256 | — | EC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL11919 | — | EC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL106570 | — | EC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL106931 | — | EC50 | = | 31622.78 | nM | 4.50 |