Assay Detail
Binding
CHEMBL4047181
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ABCG2 in human H460/MX20 cells assessed as potentiation of mitoxantrone induced antiproliferative activity by measuring mitoxantrone IC50 at 10 uM preincubated for 2 hrs followed by mitoxantrone addition measured after 72 hrs by MTT assay (Rvb = 6.161 +/- 0.172 microM)
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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
Design, synthesis and biological evaluation of benzamide and phenyltetrazole derivatives with amide and urea linkers as BCRP inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 6.25 | 6.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4096318 | — | — | 1 | 6.88 |
| CHEMBL4091036 | — | — | 1 | 6.55 |
| CHEMBL4095392 | — | — | 1 | 6.52 |
| CHEMBL3426387 | — | — | 1 | 6.51 |
| CHEMBL4078022 | — | — | 1 | 6.49 |
| CHEMBL410316 | FUMITREMORGIN | — | 1 | 6.49 |
| CHEMBL4098858 | — | — | 1 | 6.49 |
| CHEMBL4061497 | — | — | 1 | 6.48 |
| CHEMBL4096070 | — | — | 1 | 6.46 |
| CHEMBL4076705 | — | — | 1 | 6.45 |
| CHEMBL4080817 | — | — | 1 | 6.42 |
| CHEMBL3426388 | — | — | 1 | 6.42 |
| CHEMBL4083323 | — | — | 1 | 6.39 |
| CHEMBL4064511 | — | — | 1 | 6.34 |
| CHEMBL4092046 | — | — | 1 | 6.33 |
| CHEMBL3885456 | — | — | 1 | 6.31 |
| CHEMBL4074879 | — | — | 1 | 6.29 |
| CHEMBL4076726 | — | — | 1 | 6.26 |
| CHEMBL4065537 | — | — | 1 | 6.23 |
| CHEMBL4102382 | — | — | 1 | 6.16 |
| CHEMBL4099768 | — | — | 1 | 6.12 |
| CHEMBL4104064 | — | — | 1 | 6.06 |
| CHEMBL4072882 | — | — | 1 | 6.05 |
| CHEMBL4087699 | — | — | 1 | 6.02 |
| CHEMBL4102415 | — | — | 1 | 6.02 |
| CHEMBL4092211 | — | — | 1 | 6.01 |
| CHEMBL4069054 | — | — | 1 | 5.96 |
| CHEMBL4084461 | — | — | 1 | 5.95 |
| CHEMBL4077603 | — | — | 1 | 5.92 |
| CHEMBL4066351 | — | — | 1 | 5.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4096318 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL4091036 | — | IC50 | = | 283.0 | nM | 6.55 |
| CHEMBL4095392 | — | IC50 | = | 299.0 | nM | 6.52 |
| CHEMBL3426387 | — | IC50 | = | 307.0 | nM | 6.51 |
| CHEMBL4078022 | — | IC50 | = | 325.0 | nM | 6.49 |
| CHEMBL410316 | FUMITREMORGIN | IC50 | = | 321.0 | nM | 6.49 |
| CHEMBL4098858 | — | IC50 | = | 325.0 | nM | 6.49 |
| CHEMBL4061497 | — | IC50 | = | 331.0 | nM | 6.48 |
| CHEMBL4096070 | — | IC50 | = | 348.0 | nM | 6.46 |
| CHEMBL4076705 | — | IC50 | = | 355.0 | nM | 6.45 |
| CHEMBL4080817 | — | IC50 | = | 379.0 | nM | 6.42 |
| CHEMBL3426388 | — | IC50 | = | 378.0 | nM | 6.42 |
| CHEMBL4083323 | — | IC50 | = | 403.0 | nM | 6.39 |
| CHEMBL4064511 | — | IC50 | = | 452.0 | nM | 6.34 |
| CHEMBL4092046 | — | IC50 | = | 472.0 | nM | 6.33 |
| CHEMBL3885456 | — | IC50 | = | 492.0 | nM | 6.31 |
| CHEMBL4074879 | — | IC50 | = | 512.0 | nM | 6.29 |
| CHEMBL4076726 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4065537 | — | IC50 | = | 594.0 | nM | 6.23 |
| CHEMBL4102382 | — | IC50 | = | 685.0 | nM | 6.16 |
| CHEMBL4099768 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL4104064 | — | IC50 | = | 866.0 | nM | 6.06 |
| CHEMBL4072882 | — | IC50 | = | 882.0 | nM | 6.05 |
| CHEMBL4087699 | — | IC50 | = | 952.0 | nM | 6.02 |
| CHEMBL4102415 | — | IC50 | = | 952.0 | nM | 6.02 |
| CHEMBL4092211 | — | IC50 | = | 985.0 | nM | 6.01 |
| CHEMBL4069054 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4084461 | — | IC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL4077603 | — | IC50 | = | 1202.0 | nM | 5.92 |
| CHEMBL4066351 | — | IC50 | = | 1267.0 | nM | 5.90 |
| CHEMBL4081645 | — | IC50 | = | 1656.0 | nM | 5.78 |
| CHEMBL4077458 | — | IC50 | = | 1713.0 | nM | 5.77 |