Assay Detail
Functional
CHEMBL981856
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
40
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and evaluation of structurally constrained quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 8.34 | 9.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL484946 | — | — | 1 | 9.57 |
| CHEMBL485543 | — | — | 1 | 9.48 |
| CHEMBL458176 | — | — | 1 | 9.47 |
| CHEMBL483400 | — | — | 1 | 9.26 |
| CHEMBL517140 | GSK189254 | 2.0 | 1 | 9.26 |
| CHEMBL351231 | — | — | 1 | 9.20 |
| CHEMBL464599 | — | — | 1 | 9.08 |
| CHEMBL516697 | — | — | 1 | 9.04 |
| CHEMBL520629 | — | — | 1 | 8.92 |
| CHEMBL517937 | — | — | 1 | 8.92 |
| CHEMBL464598 | — | — | 1 | 8.89 |
| CHEMBL458359 | — | — | 1 | 8.82 |
| CHEMBL483199 | — | — | 1 | 8.82 |
| CHEMBL484189 | — | — | 1 | 8.82 |
| CHEMBL484611 | — | — | 1 | 8.80 |
| CHEMBL458954 | — | — | 1 | 8.77 |
| CHEMBL476373 | — | — | 1 | 8.77 |
| CHEMBL485388 | — | — | 1 | 8.74 |
| CHEMBL521327 | — | — | 1 | 8.74 |
| CHEMBL484610 | — | — | 1 | 8.70 |
| CHEMBL458953 | — | — | 1 | 8.52 |
| CHEMBL483366 | — | — | 1 | 8.49 |
| CHEMBL484740 | — | — | 2 | 8.47 |
| CHEMBL485389 | — | — | 1 | 8.38 |
| CHEMBL519018 | — | — | 1 | 8.15 |
| CHEMBL521022 | — | — | 1 | 8.00 |
| CHEMBL485242 | — | — | 1 | 8.00 |
| CHEMBL462605 | PITOLISANT | 4.0 | 1 | 7.92 |
| CHEMBL483194 | — | — | 1 | 7.85 |
| CHEMBL519839 | — | — | 1 | 7.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL484946 | — | IC50 | = | 0.27 | nM | 9.57 |
| CHEMBL485543 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL458176 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL483400 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL517140 | GSK189254 | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL351231 | — | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL464599 | — | IC50 | = | 0.84 | nM | 9.08 |
| CHEMBL516697 | — | IC50 | = | 0.91 | nM | 9.04 |
| CHEMBL520629 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL517937 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL464598 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL458359 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL484189 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL483199 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL484611 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL458954 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL476373 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL485388 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL521327 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL484610 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL458953 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL483366 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL484740 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL485389 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL519018 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL484740 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL521022 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL485242 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL462605 | PITOLISANT | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL519839 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL483194 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL521503 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL483367 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL483189 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL484199 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL484200 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL485234 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL520800 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL485604 | — | IC50 | = | 813.0 | nM | 6.09 |
| CHEMBL449178 | — | IC50 | > | 1000.0 | nM | - |