Assay Detail
Binding
CHEMBL4047196
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 1 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 | 6.00 | 6.45 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4096318 | — | — | 1 | 6.45 |
| CHEMBL4076705 | — | — | 1 | 6.36 |
| CHEMBL4095392 | — | — | 1 | 6.26 |
| CHEMBL3426387 | — | — | 1 | 6.23 |
| CHEMBL3426388 | — | — | 1 | 6.23 |
| CHEMBL4091036 | — | — | 1 | 6.22 |
| CHEMBL410316 | FUMITREMORGIN | — | 1 | 6.21 |
| CHEMBL4078022 | — | — | 1 | 6.21 |
| CHEMBL4098858 | — | — | 1 | 6.20 |
| CHEMBL4096070 | — | — | 1 | 6.19 |
| CHEMBL4064511 | — | — | 1 | 6.15 |
| CHEMBL4061497 | — | — | 1 | 6.14 |
| CHEMBL3885456 | — | — | 1 | 6.13 |
| CHEMBL4074879 | — | — | 1 | 6.11 |
| CHEMBL4092046 | — | — | 1 | 6.10 |
| CHEMBL4065537 | — | — | 1 | 6.08 |
| CHEMBL4083323 | — | — | 1 | 6.08 |
| CHEMBL4080817 | — | — | 1 | 6.08 |
| CHEMBL4102382 | — | — | 1 | 6.04 |
| CHEMBL4099768 | — | — | 1 | 6.01 |
| CHEMBL4072882 | — | — | 1 | 5.93 |
| CHEMBL4087699 | — | — | 1 | 5.91 |
| CHEMBL4077603 | — | — | 1 | 5.87 |
| CHEMBL4076726 | — | — | 1 | 5.82 |
| CHEMBL4066351 | — | — | 1 | 5.79 |
| CHEMBL4104064 | — | — | 1 | 5.74 |
| CHEMBL4069054 | — | — | 1 | 5.73 |
| CHEMBL4081645 | — | — | 1 | 5.60 |
| CHEMBL4102415 | — | — | 1 | 5.58 |
| CHEMBL4077458 | — | — | 1 | 5.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4096318 | — | IC50 | = | 354.0 | nM | 6.45 |
| CHEMBL4076705 | — | IC50 | = | 442.0 | nM | 6.36 |
| CHEMBL4095392 | — | IC50 | = | 549.0 | nM | 6.26 |
| CHEMBL3426387 | — | IC50 | = | 585.0 | nM | 6.23 |
| CHEMBL3426388 | — | IC50 | = | 587.0 | nM | 6.23 |
| CHEMBL4091036 | — | IC50 | = | 605.0 | nM | 6.22 |
| CHEMBL410316 | FUMITREMORGIN | IC50 | = | 612.0 | nM | 6.21 |
| CHEMBL4078022 | — | IC50 | = | 622.0 | nM | 6.21 |
| CHEMBL4098858 | — | IC50 | = | 627.0 | nM | 6.20 |
| CHEMBL4096070 | — | IC50 | = | 651.0 | nM | 6.19 |
| CHEMBL4064511 | — | IC50 | = | 711.0 | nM | 6.15 |
| CHEMBL4061497 | — | IC50 | = | 718.0 | nM | 6.14 |
| CHEMBL3885456 | — | IC50 | = | 746.0 | nM | 6.13 |
| CHEMBL4074879 | — | IC50 | = | 785.0 | nM | 6.11 |
| CHEMBL4092046 | — | IC50 | = | 798.0 | nM | 6.10 |
| CHEMBL4083323 | — | IC50 | = | 832.0 | nM | 6.08 |
| CHEMBL4080817 | — | IC50 | = | 838.0 | nM | 6.08 |
| CHEMBL4065537 | — | IC50 | = | 833.0 | nM | 6.08 |
| CHEMBL4102382 | — | IC50 | = | 913.0 | nM | 6.04 |
| CHEMBL4099768 | — | IC50 | = | 967.0 | nM | 6.01 |
| CHEMBL4072882 | — | IC50 | = | 1172.0 | nM | 5.93 |
| CHEMBL4087699 | — | IC50 | = | 1221.0 | nM | 5.91 |
| CHEMBL4077603 | — | IC50 | = | 1363.0 | nM | 5.87 |
| CHEMBL4076726 | — | IC50 | = | 1515.0 | nM | 5.82 |
| CHEMBL4066351 | — | IC50 | = | 1615.0 | nM | 5.79 |
| CHEMBL4104064 | — | IC50 | = | 1801.0 | nM | 5.74 |
| CHEMBL4069054 | — | IC50 | = | 1880.0 | nM | 5.73 |
| CHEMBL4081645 | — | IC50 | = | 2526.0 | nM | 5.60 |
| CHEMBL4102415 | — | IC50 | = | 2655.0 | nM | 5.58 |
| CHEMBL4077458 | — | IC50 | = | 2814.0 | nM | 5.55 |
| CHEMBL4092211 | — | IC50 | = | 3371.0 | nM | 5.47 |
| CHEMBL4084461 | — | IC50 | = | 3662.0 | nM | 5.44 |