Assay Detail
Functional
CHEMBL986350
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
35
Total Activities
35
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, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 8.54 | 9.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL479241 | — | — | 1 | 9.18 |
| CHEMBL515004 | — | — | 1 | 9.16 |
| CHEMBL478395 | — | — | 1 | 9.14 |
| CHEMBL479036 | — | — | 1 | 9.09 |
| CHEMBL477364 | — | — | 1 | 9.02 |
| CHEMBL479242 | — | — | 1 | 9.01 |
| CHEMBL477991 | — | — | 1 | 8.96 |
| CHEMBL478615 | — | — | 1 | 8.92 |
| CHEMBL477990 | — | — | 1 | 8.89 |
| CHEMBL477363 | — | — | 1 | 8.89 |
| CHEMBL515150 | — | — | 1 | 8.82 |
| CHEMBL476723 | — | — | 1 | 8.80 |
| CHEMBL476579 | — | — | 1 | 8.80 |
| CHEMBL479252 | — | — | 1 | 8.80 |
| CHEMBL478616 | — | — | 1 | 8.77 |
| CHEMBL476323 | MK-0249 | 2.0 | 1 | 8.77 |
| CHEMBL476106 | — | — | 1 | 8.74 |
| CHEMBL476322 | — | — | 1 | 8.66 |
| CHEMBL477360 | — | — | 1 | 8.66 |
| CHEMBL477356 | — | — | 1 | 8.66 |
| CHEMBL477201 | — | — | 1 | 8.64 |
| CHEMBL487063 | — | — | 1 | 8.51 |
| CHEMBL518431 | — | — | 1 | 8.46 |
| CHEMBL476373 | — | — | 1 | 8.46 |
| CHEMBL477152 | — | — | 1 | 8.43 |
| CHEMBL478406 | — | — | 1 | 8.41 |
| CHEMBL477361 | — | — | 1 | 8.37 |
| CHEMBL515477 | — | — | 1 | 8.24 |
| CHEMBL478621 | — | — | 1 | 8.00 |
| CHEMBL478628 | — | — | 1 | 7.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL479241 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL515004 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL478395 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL479036 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL477364 | — | IC50 | = | 0.96 | nM | 9.02 |
| CHEMBL479242 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL477991 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL478615 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL477363 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL477990 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL515150 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL476723 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL476579 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL479252 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL476323 | MK-0249 | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL478616 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL476106 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL476322 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL477356 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL477360 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL477201 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL487063 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL518431 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL476373 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL477152 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL478406 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL477361 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL515477 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL478621 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL478628 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL443958 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL477556 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL446516 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL516725 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL516126 | — | IC50 | = | 41.0 | nM | 7.39 |