Assay Detail
Binding
CHEMBL3887655
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Competitive Binding Assay: A synthetic 14-mer peptide, TN14003, was previously reported to block both SDF-1/CXCR4 mediated invasion in vitro and metastasis in vivo with a high specificity by binding competitively with its ligand SDF-1. Aa competitive binding assay using biotin-labeled TN14003 and streptavidin-conjugated rhodamine was developed to determine the binding efficiency of new chemical entities to the SDF-1 binding domain of CXCR4. Cells incubated with high affinity compounds show only blue nuclear staining, whereas compounds with low affinity result in staining CXCR4 (red; rhodamine) as well as the nuclei (blue; cytox blue).
73
Total Activities
72
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
C-X-C chemokine receptor type 4 (CHEMBL5556) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Tricyclic amino containing compounds for treatment or prevention of symptoms associated with endocrine dysfunction
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 73 | 7.97 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1802323 | — | — | 1 | 9.00 |
| CHEMBL3964805 | — | — | 1 | 9.00 |
| CHEMBL3985608 | — | — | 1 | 9.00 |
| CHEMBL1802330 | — | — | 1 | 9.00 |
| CHEMBL392423 | — | — | 1 | 9.00 |
| CHEMBL3912875 | — | — | 1 | 9.00 |
| CHEMBL3896101 | — | — | 1 | 9.00 |
| CHEMBL1802286 | — | — | 1 | 9.00 |
| CHEMBL237629 | — | — | 1 | 9.00 |
| CHEMBL3986129 | — | — | 1 | 9.00 |
| CHEMBL1802287 | — | — | 1 | 9.00 |
| CHEMBL237439 | — | — | 1 | 8.00 |
| CHEMBL1802322 | — | — | 1 | 8.00 |
| CHEMBL3958019 | — | — | 1 | 8.00 |
| CHEMBL237829 | — | — | 1 | 8.00 |
| CHEMBL1802283 | — | — | 1 | 8.00 |
| CHEMBL3909689 | — | — | 1 | 8.00 |
| CHEMBL237440 | — | — | 1 | 8.00 |
| CHEMBL1802282 | — | — | 1 | 8.00 |
| CHEMBL235310 | — | — | 1 | 8.00 |
| CHEMBL3932667 | — | — | 1 | 8.00 |
| CHEMBL1802284 | — | — | 1 | 7.00 |
| CHEMBL3986703 | — | — | 1 | 7.00 |
| CHEMBL3979002 | — | — | 1 | 7.00 |
| CHEMBL3911200 | — | — | 1 | 7.00 |
| CHEMBL3932956 | — | — | 1 | 7.00 |
| CHEMBL18442 | PLERIXAFOR | 4.0 | 1 | 7.00 |
| CHEMBL3965823 | — | — | 1 | 6.00 |
| CHEMBL3897880 | — | — | 1 | 6.00 |
| CHEMBL3974314 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1802323 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3964805 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3985608 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1802330 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL392423 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3912875 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3896101 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1802286 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL237629 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3986129 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1802287 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL235310 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1802322 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3958019 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL237829 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1802283 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3909689 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL237439 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL237440 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1802282 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3932667 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3932956 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL18442 | PLERIXAFOR | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3911200 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3986703 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1802284 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3979002 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3965823 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3897880 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3974314 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL393882 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL237830 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL3545330 | MSX-122 | IC50 | < | 10.0 | nM | - |
| CHEMBL3947084 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL3981213 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3981627 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL235068 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL398014 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL237630 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL396667 | — | IC50 | < | 100.0 | nM | - |
| CHEMBL235312 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL237631 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL391151 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL1802285 | — | IC50 | < | 100.0 | nM | - |
| CHEMBL1195113 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL393855 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL235902 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1188411 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL237164 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL237245 | — | IC50 | < | 100.0 | nM | - |