Assay Detail
Functional
CHEMBL4237076
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at CCR5 (unknown origin) expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of RANTES-induced calcium flux preincubated for 10 mins followed by RANTES addition by fluo-4AM-based fluorescence assay
35
Total Activities
35
Compounds Tested
1
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
Structure-Based Design of 1-Heteroaryl-1,3-propanediamine Derivatives as a Novel Series of CC-Chemokine Receptor 5 Antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 8.05 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4242114 | — | — | 1 | 8.64 |
| CHEMBL4248009 | — | — | 1 | 8.64 |
| CHEMBL4248472 | — | — | 1 | 8.59 |
| CHEMBL4242489 | — | — | 1 | 8.59 |
| CHEMBL4242913 | — | — | 1 | 8.59 |
| CHEMBL4240475 | — | — | 1 | 8.55 |
| CHEMBL4248282 | — | — | 1 | 8.55 |
| CHEMBL4244672 | — | — | 1 | 8.54 |
| CHEMBL4241721 | — | — | 1 | 8.54 |
| CHEMBL4239790 | — | — | 1 | 8.54 |
| CHEMBL4249798 | — | — | 1 | 8.52 |
| CHEMBL4237964 | — | — | 1 | 8.52 |
| CHEMBL4238063 | — | — | 1 | 8.51 |
| CHEMBL4250366 | — | — | 1 | 8.40 |
| CHEMBL4240242 | — | — | 1 | 8.33 |
| CHEMBL4238007 | — | — | 1 | 8.28 |
| CHEMBL4241284 | — | — | 1 | 8.27 |
| CHEMBL4249941 | — | — | 1 | 8.17 |
| CHEMBL4237581 | — | — | 1 | 8.17 |
| CHEMBL256907 | MARAVIROC | 4.0 | 1 | 8.10 |
| CHEMBL4241066 | — | — | 1 | 8.09 |
| CHEMBL4244935 | — | — | 1 | 8.04 |
| CHEMBL4238266 | — | — | 1 | 8.01 |
| CHEMBL4243842 | — | — | 1 | 7.92 |
| CHEMBL4240763 | — | — | 1 | 7.80 |
| CHEMBL4242034 | — | — | 1 | 7.79 |
| CHEMBL4248119 | — | — | 1 | 7.69 |
| CHEMBL4250560 | — | — | 1 | 7.61 |
| CHEMBL4240742 | — | — | 1 | 7.57 |
| CHEMBL4249259 | — | — | 1 | 7.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4242114 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4248009 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4248472 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4242489 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4242913 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4240475 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4248282 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4244672 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4241721 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4239790 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4249798 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4237964 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4238063 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4250366 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4240242 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL4238007 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL4241284 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4249941 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL4237581 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL256907 | MARAVIROC | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4241066 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL4244935 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL4238266 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL4243842 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4240763 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL4242034 | — | IC50 | = | 16.2 | nM | 7.79 |
| CHEMBL4248119 | — | IC50 | = | 20.6 | nM | 7.69 |
| CHEMBL4250560 | — | IC50 | = | 24.5 | nM | 7.61 |
| CHEMBL4240742 | — | IC50 | = | 27.1 | nM | 7.57 |
| CHEMBL4249259 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4242946 | — | IC50 | = | 51.7 | nM | 7.29 |
| CHEMBL4248733 | — | IC50 | = | 82.6 | nM | 7.08 |
| CHEMBL4249241 | — | IC50 | = | 87.9 | nM | 7.06 |
| CHEMBL4244470 | — | IC50 | = | 251.6 | nM | 6.60 |
| CHEMBL4246290 | — | IC50 | = | 296.4 | nM | 6.53 |