Assay Detail
Functional
CHEMBL1815951
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human CCR5 receptor assessed as inhibition of HIV1 gp120-induced cell-cell fusion between viral envolop protein expressing human HEK293 cells to human CD4/CCR5 receptor expressing HOS cells after 24 hrs by luciferase reporter gene assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HOS |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 4-[4-({(3R)-1-butyl-3-[(R)-cyclohexyl(hydroxy)methyl]-2,5-dioxo-1,4,9-triazaspiro[5.5]undec-9-yl}methyl)phenoxy]benzoic acid hydrochloride: a highly potent orally available CCR5 selective antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 5.03 | 5.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1813435 | — | — | 1 | 5.85 |
| CHEMBL1813270 | — | — | 1 | 5.55 |
| CHEMBL1813433 | — | — | 1 | 5.46 |
| CHEMBL1813450 | — | — | 1 | 5.41 |
| CHEMBL1813440 | — | — | 1 | 5.28 |
| CHEMBL1668019 | APLAVIROC HYDROCHLORIDE | 3.0 | 1 | 5.25 |
| CHEMBL1813269 | — | — | 1 | 5.15 |
| CHEMBL1813432 | — | — | 1 | 5.13 |
| CHEMBL536754 | — | — | 1 | 5.11 |
| CHEMBL1813439 | — | — | 1 | 4.89 |
| CHEMBL1813449 | — | — | 1 | 4.68 |
| CHEMBL1813451 | — | — | 1 | 4.46 |
| CHEMBL1813438 | — | — | 1 | 4.18 |
| CHEMBL1813454 | — | — | 1 | 4.01 |
| CHEMBL3216516 | — | — | 1 | - |
| CHEMBL1813453 | — | — | 1 | - |
| CHEMBL1813452 | — | — | 1 | - |
| CHEMBL1813448 | — | — | 1 | - |
| CHEMBL1813447 | — | — | 1 | - |
| CHEMBL1813446 | — | — | 1 | - |
| CHEMBL1668022 | — | — | 1 | - |
| CHEMBL1813444 | — | — | 1 | - |
| CHEMBL1813443 | — | — | 1 | - |
| CHEMBL1813442 | — | — | 1 | - |
| CHEMBL1813441 | — | — | 1 | - |
| CHEMBL1813445 | — | — | 1 | - |
| CHEMBL1813437 | — | — | 1 | - |
| CHEMBL1813436 | — | — | 1 | - |
| CHEMBL1813271 | — | — | 1 | - |
| CHEMBL1813434 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1813435 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1813270 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL1813433 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL1813450 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL1813440 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL1668019 | APLAVIROC HYDROCHLORIDE | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL1813269 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL1813432 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL536754 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL1813439 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL1813449 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL1813451 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL1813438 | — | IC50 | = | 66000.0 | nM | 4.18 |
| CHEMBL1813454 | — | IC50 | = | 98000.0 | nM | 4.01 |
| CHEMBL1668021 | — | IC50 | = | 380000.0 | nM | - |
| CHEMBL1668020 | — | IC50 | = | 182000.0 | nM | - |
| CHEMBL1813458 | — | IC50 | - | — | - | |
| CHEMBL1813457 | — | IC50 | = | 1148000.0 | nM | - |
| CHEMBL3215636 | — | IC50 | - | — | - | |
| CHEMBL3216516 | — | IC50 | - | — | - | |
| CHEMBL1813453 | — | IC50 | = | 10000000.0 | nM | - |
| CHEMBL1813452 | — | IC50 | = | 316000.0 | nM | - |
| CHEMBL1813448 | — | IC50 | = | 112000.0 | nM | - |
| CHEMBL1813447 | — | IC50 | = | 178000.0 | nM | - |
| CHEMBL1813446 | — | IC50 | = | 295000.0 | nM | - |
| CHEMBL1668022 | — | IC50 | = | 447000.0 | nM | - |
| CHEMBL1813444 | — | IC50 | = | 10000000.0 | nM | - |
| CHEMBL1813443 | — | IC50 | = | 129000.0 | nM | - |
| CHEMBL1813442 | — | IC50 | = | 537000.0 | nM | - |
| CHEMBL1813441 | — | IC50 | = | 302000.0 | nM | - |
| CHEMBL1813445 | — | IC50 | = | 1862000.0 | nM | - |
| CHEMBL1813437 | — | IC50 | = | 10000000.0 | nM | - |
| CHEMBL1813436 | — | IC50 | = | 229000.0 | nM | - |
| CHEMBL1813271 | — | IC50 | - | — | - | |
| CHEMBL1813434 | — | IC50 | - | — | - |