Assay Detail
Functional
CHEMBL911046
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
71
Total Activities
71
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 | Expert |
Publication
Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzamide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 70 | 7.11 | 9.00 |
| Efficacy | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL216922 | — | — | 1 | 9.00 |
| CHEMBL219129 | — | — | 1 | 9.00 |
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 8.66 |
| CHEMBL219179 | — | — | 1 | 8.62 |
| CHEMBL216921 | — | — | 1 | 8.42 |
| CHEMBL53 | APOMORPHINE | 4.0 | 1 | 8.37 |
| CHEMBL443838 | — | — | 1 | 8.10 |
| CHEMBL216450 | — | — | 1 | 8.10 |
| CHEMBL45244 | PD-168,077 | — | 1 | 8.08 |
| CHEMBL216794 | — | — | 1 | 8.05 |
| CHEMBL220083 | — | — | 1 | 8.01 |
| CHEMBL127226 | — | — | 1 | 7.92 |
| CHEMBL440687 | ABT-724 | — | 1 | 7.91 |
| CHEMBL375596 | — | — | 1 | 7.85 |
| CHEMBL373963 | — | — | 1 | 7.75 |
| CHEMBL219185 | — | — | 1 | 7.50 |
| CHEMBL385418 | — | — | 1 | 7.44 |
| CHEMBL219566 | — | — | 1 | 7.42 |
| CHEMBL444881 | — | — | 1 | 7.40 |
| CHEMBL385781 | — | — | 1 | 7.35 |
| CHEMBL219186 | — | — | 1 | 7.30 |
| CHEMBL219210 | — | — | 1 | 7.28 |
| CHEMBL375120 | — | — | 1 | 7.27 |
| CHEMBL219394 | — | — | 1 | 7.22 |
| CHEMBL219261 | — | — | 1 | 7.22 |
| CHEMBL414706 | — | — | 1 | 7.21 |
| CHEMBL219263 | — | — | 1 | 7.20 |
| CHEMBL219211 | — | — | 1 | 7.18 |
| CHEMBL436527 | — | — | 1 | 7.17 |
| CHEMBL219966 | — | — | 1 | 7.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL216922 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL219129 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL59 | DOPAMINE | EC50 | = | 2.2 | nM | 8.66 |
| CHEMBL219179 | — | EC50 | = | 2.4 | nM | 8.62 |
| CHEMBL216921 | — | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL53 | APOMORPHINE | EC50 | = | 4.3 | nM | 8.37 |
| CHEMBL443838 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL216450 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL45244 | PD-168,077 | EC50 | = | 8.3 | nM | 8.08 |
| CHEMBL216794 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL220083 | — | EC50 | = | 9.8 | nM | 8.01 |
| CHEMBL127226 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL440687 | ABT-724 | EC50 | = | 12.4 | nM | 7.91 |
| CHEMBL375596 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL373963 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL219185 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL385418 | — | EC50 | = | 36.0 | nM | 7.44 |
| CHEMBL219566 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL444881 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL385781 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL219186 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL219210 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL375120 | — | EC50 | = | 54.0 | nM | 7.27 |
| CHEMBL219394 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL219261 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL414706 | — | EC50 | = | 62.0 | nM | 7.21 |
| CHEMBL219263 | — | EC50 | = | 63.0 | nM | 7.20 |
| CHEMBL219211 | — | EC50 | = | 66.0 | nM | 7.18 |
| CHEMBL436527 | — | EC50 | = | 68.0 | nM | 7.17 |
| CHEMBL219966 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL264286 | — | EC50 | = | 76.0 | nM | 7.12 |
| CHEMBL436491 | — | EC50 | = | 85.0 | nM | 7.07 |
| CHEMBL216215 | — | EC50 | = | 85.0 | nM | 7.07 |
| CHEMBL219182 | — | EC50 | = | 89.0 | nM | 7.05 |
| CHEMBL218798 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL219389 | — | EC50 | = | 95.0 | nM | 7.02 |
| CHEMBL219570 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL373964 | — | EC50 | = | 103.0 | nM | 6.99 |
| CHEMBL219567 | — | EC50 | = | 111.0 | nM | 6.96 |
| CHEMBL220015 | — | EC50 | = | 115.0 | nM | 6.94 |
| CHEMBL385417 | — | EC50 | = | 126.0 | nM | 6.90 |
| CHEMBL220139 | — | EC50 | = | 134.0 | nM | 6.87 |
| CHEMBL218852 | — | EC50 | = | 135.0 | nM | 6.87 |
| CHEMBL218797 | — | EC50 | = | 145.0 | nM | 6.84 |
| CHEMBL219417 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL220192 | — | EC50 | = | 159.0 | nM | 6.80 |
| CHEMBL425288 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL216393 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL219340 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL219564 | — | EC50 | = | 180.0 | nM | 6.75 |