Assay Detail
Functional
CHEMBL1248645
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
29
Total Activities
28
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and synthesis of novel tricyclic benzoxazines as potent 5-HT(1A/B/D) receptor antagonists leading to the discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide (GSK588045).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 9.68 | 10.20 |
| Kd | 1 | 9.69 | 9.69 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL490417 | — | — | 1 | 10.20 |
| CHEMBL1241546 | — | — | 1 | 10.10 |
| CHEMBL1241738 | — | — | 1 | 10.10 |
| CHEMBL522257 | — | — | 1 | 10.10 |
| CHEMBL1242081 | — | — | 1 | 9.90 |
| CHEMBL1242904 | — | — | 1 | 9.90 |
| CHEMBL1242345 | — | — | 1 | 9.90 |
| CHEMBL1242533 | — | — | 1 | 9.90 |
| CHEMBL1242167 | — | — | 1 | 9.80 |
| CHEMBL1241912 | — | — | 1 | 9.80 |
| CHEMBL1241824 | — | — | 1 | 9.80 |
| CHEMBL1242436 | — | — | 1 | 9.80 |
| CHEMBL1241641 | — | — | 1 | 9.80 |
| CHEMBL469345 | — | — | 1 | 9.80 |
| CHEMBL1241642 | — | — | 1 | 9.70 |
| CHEMBL1241998 | — | — | 1 | 9.70 |
| CHEMBL1241547 | — | — | 1 | 9.70 |
| CHEMBL1241548 | — | — | 1 | 9.70 |
| CHEMBL1241913 | — | — | 2 | 9.69 |
| CHEMBL1242257 | — | — | 1 | 9.60 |
| CHEMBL513715 | — | — | 1 | 9.60 |
| CHEMBL1241736 | — | — | 1 | 9.50 |
| CHEMBL1242623 | — | — | 1 | 9.40 |
| CHEMBL1242717 | — | — | 1 | 9.40 |
| CHEMBL1241639 | — | — | 1 | 9.30 |
| CHEMBL1241640 | — | — | 1 | 9.20 |
| CHEMBL1241825 | — | — | 1 | 9.00 |
| CHEMBL1241737 | — | — | 1 | 8.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL490417 | — | Ki | = | 0.0631 | nM | 10.20 |
| CHEMBL1241546 | — | Ki | = | 0.07943 | nM | 10.10 |
| CHEMBL1241738 | — | Ki | = | 0.07943 | nM | 10.10 |
| CHEMBL522257 | — | Ki | = | 0.07943 | nM | 10.10 |
| CHEMBL1242533 | — | Ki | = | 0.1259 | nM | 9.90 |
| CHEMBL1242081 | — | Ki | = | 0.1259 | nM | 9.90 |
| CHEMBL1242345 | — | Ki | = | 0.1259 | nM | 9.90 |
| CHEMBL1242904 | — | Ki | = | 0.1259 | nM | 9.90 |
| CHEMBL1241641 | — | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL1242436 | — | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL1241824 | — | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL1242167 | — | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL1241912 | — | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL469345 | — | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL1241548 | — | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL1241998 | — | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL1241547 | — | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL1241642 | — | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL1241913 | — | Kd | = | 0.2042 | nM | 9.69 |
| CHEMBL513715 | — | Ki | = | 0.2512 | nM | 9.60 |
| CHEMBL1242257 | — | Ki | = | 0.2512 | nM | 9.60 |
| CHEMBL1241736 | — | Ki | = | 0.3162 | nM | 9.50 |
| CHEMBL1241913 | — | Ki | = | 0.3162 | nM | 9.50 |
| CHEMBL1242623 | — | Ki | = | 0.3981 | nM | 9.40 |
| CHEMBL1242717 | — | Ki | = | 0.3981 | nM | 9.40 |
| CHEMBL1241639 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL1241640 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL1241825 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1241737 | — | Ki | = | 1.585 | nM | 8.80 |