Assay Detail
Binding
CHEMBL2423205
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of pheophorbide-A preincubated for 30 mins before pheophorbide-A addition measured after 120 mins by flow cytometry
32
Total Activities
32
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
Synthesis and biological evaluation of flavones and benzoflavones as inhibitors of BCRP/ABCG2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 5.60 | 6.45 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL488910 | — | — | 1 | 6.45 |
| CHEMBL2420084 | — | — | 1 | 6.34 |
| CHEMBL2420094 | — | — | 1 | 6.34 |
| CHEMBL2420091 | — | — | 1 | 6.33 |
| CHEMBL77966 | RETUSIN | — | 1 | 6.24 |
| CHEMBL2420083 | — | — | 1 | 5.95 |
| CHEMBL144625 | — | — | 1 | 5.89 |
| CHEMBL2420082 | — | — | 1 | 5.89 |
| CHEMBL2420103 | — | — | 1 | 5.87 |
| CHEMBL283196 | ALPHA-NAPHTHOFLAVONE | — | 1 | 5.85 |
| CHEMBL2420087 | — | — | 1 | 5.82 |
| CHEMBL2420085 | — | — | 1 | 5.80 |
| CHEMBL2420093 | — | — | 1 | 5.77 |
| CHEMBL77198 | — | — | 1 | 5.75 |
| CHEMBL19032 | PENTAMETHYLQUERCETIN | — | 1 | 5.73 |
| CHEMBL575808 | FISETIN TETRAMETHYL ETHER | — | 1 | 5.67 |
| CHEMBL2420089 | — | — | 1 | 5.64 |
| CHEMBL2420090 | — | — | 1 | 5.51 |
| CHEMBL2075017 | MORIN PENTAMETHYL ETHER | — | 1 | 5.41 |
| CHEMBL2420092 | — | — | 1 | 5.40 |
| CHEMBL2420097 | — | — | 1 | 5.32 |
| CHEMBL2420086 | — | — | 1 | 5.30 |
| CHEMBL2420100 | — | — | 1 | 5.28 |
| CHEMBL75169 | — | — | 1 | 5.23 |
| CHEMBL26260 | BETA-NAPHTHOFLAVONE | — | 1 | 5.22 |
| CHEMBL2420096 | — | — | 1 | 5.21 |
| CHEMBL2420102 | — | — | 1 | 5.19 |
| CHEMBL2420099 | — | — | 1 | 5.10 |
| CHEMBL2331821 | — | — | 1 | 5.05 |
| CHEMBL2420098 | — | — | 1 | 4.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL488910 | — | IC50 | = | 354.0 | nM | 6.45 |
| CHEMBL2420084 | — | IC50 | = | 457.0 | nM | 6.34 |
| CHEMBL2420094 | — | IC50 | = | 458.0 | nM | 6.34 |
| CHEMBL2420091 | — | IC50 | = | 468.0 | nM | 6.33 |
| CHEMBL77966 | RETUSIN | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL2420083 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL144625 | — | IC50 | = | 1280.0 | nM | 5.89 |
| CHEMBL2420082 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL2420103 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL283196 | ALPHA-NAPHTHOFLAVONE | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2420087 | — | IC50 | = | 1520.0 | nM | 5.82 |
| CHEMBL2420085 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL2420093 | — | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL77198 | — | IC50 | = | 1770.0 | nM | 5.75 |
| CHEMBL19032 | PENTAMETHYLQUERCETIN | IC50 | = | 1880.0 | nM | 5.73 |
| CHEMBL575808 | FISETIN TETRAMETHYL ETHER | IC50 | = | 2140.0 | nM | 5.67 |
| CHEMBL2420089 | — | IC50 | = | 2310.0 | nM | 5.64 |
| CHEMBL2420090 | — | IC50 | = | 3070.0 | nM | 5.51 |
| CHEMBL2075017 | MORIN PENTAMETHYL ETHER | IC50 | = | 3890.0 | nM | 5.41 |
| CHEMBL2420092 | — | IC50 | = | 4010.0 | nM | 5.40 |
| CHEMBL2420097 | — | IC50 | = | 4840.0 | nM | 5.32 |
| CHEMBL2420086 | — | IC50 | = | 4970.0 | nM | 5.30 |
| CHEMBL2420100 | — | IC50 | = | 5250.0 | nM | 5.28 |
| CHEMBL75169 | — | IC50 | = | 5940.0 | nM | 5.23 |
| CHEMBL26260 | BETA-NAPHTHOFLAVONE | IC50 | = | 6050.0 | nM | 5.22 |
| CHEMBL2420096 | — | IC50 | = | 6120.0 | nM | 5.21 |
| CHEMBL2420102 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL2420099 | — | IC50 | = | 8020.0 | nM | 5.10 |
| CHEMBL2331821 | — | IC50 | = | 8950.0 | nM | 5.05 |
| CHEMBL2420098 | — | IC50 | = | 12500.0 | nM | 4.90 |
| CHEMBL2420095 | — | IC50 | = | 13600.0 | nM | 4.87 |
| CHEMBL2420088 | — | IC50 | = | 17900.0 | nM | 4.75 |