Assay Detail
Binding
CHEMBL4713573
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ABCG2 (unknown origin) expressed in MDCK-II cells assessed as potentiation of SN-38-induced cytotoxicity measured after 72 hrs by MTT assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDCK-II |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Broad substrate specificity ATP-binding cassette transporter ABCG2 (CHEMBL5393) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Rational drug design of 6-substituted 4-anilino-2-phenylpyrimidines for exploration of novel ABCG2 binding site.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 7.27 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4799327 | — | — | 1 | 7.82 |
| CHEMBL4750965 | — | — | 1 | 7.81 |
| CHEMBL4782268 | — | — | 1 | 7.75 |
| CHEMBL4747679 | — | — | 1 | 7.66 |
| CHEMBL4800631 | — | — | 1 | 7.59 |
| CHEMBL4783240 | — | — | 1 | 7.53 |
| CHEMBL4764020 | — | — | 1 | 7.39 |
| CHEMBL4762956 | — | — | 1 | 7.36 |
| CHEMBL4741738 | — | — | 1 | 7.35 |
| CHEMBL4792783 | — | — | 1 | 7.17 |
| CHEMBL4794767 | — | — | 1 | 7.14 |
| CHEMBL4798521 | — | — | 1 | 6.83 |
| CHEMBL4744165 | — | — | 1 | 6.77 |
| CHEMBL4754067 | — | — | 1 | 6.74 |
| CHEMBL4752426 | — | — | 1 | 6.73 |
| CHEMBL4761715 | — | — | 1 | 6.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4799327 | — | EC50 | = | 15.3 | nM | 7.82 |
| CHEMBL4750965 | — | EC50 | = | 15.5 | nM | 7.81 |
| CHEMBL4782268 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4747679 | — | EC50 | = | 21.7 | nM | 7.66 |
| CHEMBL4800631 | — | EC50 | = | 25.5 | nM | 7.59 |
| CHEMBL4783240 | — | EC50 | = | 29.8 | nM | 7.53 |
| CHEMBL4764020 | — | EC50 | = | 40.5 | nM | 7.39 |
| CHEMBL4762956 | — | EC50 | = | 43.5 | nM | 7.36 |
| CHEMBL4741738 | — | EC50 | = | 44.3 | nM | 7.35 |
| CHEMBL4792783 | — | EC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4794767 | — | EC50 | = | 72.5 | nM | 7.14 |
| CHEMBL4798521 | — | EC50 | = | 147.0 | nM | 6.83 |
| CHEMBL4744165 | — | EC50 | = | 171.0 | nM | 6.77 |
| CHEMBL4754067 | — | EC50 | = | 181.0 | nM | 6.74 |
| CHEMBL4752426 | — | EC50 | = | 187.0 | nM | 6.73 |
| CHEMBL4761715 | — | EC50 | = | 231.0 | nM | 6.64 |