Assay Detail
Binding
CHEMBL4478426
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ABCG2 expressed in MDCK2 cells assessed as reduction in pheophorbide A efflux pre-incubated for 30 mins before Hoechst 33342 addition and measured for 120 mins by flow cytometry
42
Total Activities
42
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
Synthesis and Investigation of Tetrahydro-β-carboline Derivatives as Inhibitors of the Breast Cancer Resistance Protein (ABCG2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 6.14 | 6.69 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4568473 | — | — | 1 | 6.69 |
| CHEMBL4534001 | — | — | 1 | 6.62 |
| CHEMBL4483061 | — | — | 1 | 6.44 |
| CHEMBL428402 | — | — | 1 | 6.13 |
| CHEMBL4517488 | — | — | 1 | 6.11 |
| CHEMBL4549202 | — | — | 1 | 6.09 |
| CHEMBL4521174 | — | — | 1 | 5.75 |
| CHEMBL269538 | HARMINE | 1.0 | 1 | 5.29 |
| CHEMBL4483626 | — | — | 1 | - |
| CHEMBL4522353 | — | — | 1 | - |
| CHEMBL488910 | — | — | 1 | - |
| CHEMBL241083 | — | — | 1 | - |
| CHEMBL4563533 | — | — | 1 | - |
| CHEMBL4529064 | — | — | 1 | - |
| CHEMBL4575807 | — | — | 1 | - |
| CHEMBL4575180 | — | — | 1 | - |
| CHEMBL4519253 | — | — | 1 | - |
| CHEMBL4555019 | — | — | 1 | - |
| CHEMBL4586159 | — | — | 1 | - |
| CHEMBL4582183 | — | — | 1 | - |
| CHEMBL4549093 | — | — | 1 | - |
| CHEMBL4530389 | — | — | 1 | - |
| CHEMBL4536788 | — | — | 1 | - |
| CHEMBL4571543 | — | — | 1 | - |
| CHEMBL4575544 | — | — | 1 | - |
| CHEMBL4538097 | — | — | 1 | - |
| CHEMBL4592538 | — | — | 1 | - |
| CHEMBL4559337 | — | — | 1 | - |
| CHEMBL241098 | — | — | 1 | - |
| CHEMBL4533470 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4568473 | — | IC50 | = | 206.0 | nM | 6.69 |
| CHEMBL4534001 | — | IC50 | = | 237.0 | nM | 6.62 |
| CHEMBL4483061 | — | IC50 | = | 365.0 | nM | 6.44 |
| CHEMBL428402 | — | IC50 | = | 741.0 | nM | 6.13 |
| CHEMBL4517488 | — | IC50 | = | 784.0 | nM | 6.11 |
| CHEMBL4549202 | — | IC50 | = | 811.0 | nM | 6.09 |
| CHEMBL4521174 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL269538 | HARMINE | IC50 | = | 5080.0 | nM | 5.29 |
| CHEMBL4575180 | — | IC50 | - | — | - | |
| CHEMBL4568684 | — | IC50 | - | — | - | |
| CHEMBL4519253 | — | IC50 | - | — | - | |
| CHEMBL4555019 | — | IC50 | - | — | - | |
| CHEMBL4586159 | — | IC50 | - | — | - | |
| CHEMBL4522353 | — | IC50 | - | — | - | |
| CHEMBL4576040 | — | IC50 | - | — | - | |
| CHEMBL4559383 | — | IC50 | - | — | - | |
| CHEMBL4549558 | — | IC50 | - | — | - | |
| CHEMBL4578134 | — | IC50 | - | — | - | |
| CHEMBL4550890 | — | IC50 | - | — | - | |
| CHEMBL4516431 | — | IC50 | - | — | - | |
| CHEMBL4542075 | — | IC50 | - | — | - | |
| CHEMBL4581843 | — | IC50 | - | — | - | |
| CHEMBL4593846 | — | IC50 | - | — | - | |
| CHEMBL4534271 | — | IC50 | - | — | - | |
| CHEMBL4545795 | — | IC50 | - | — | - | |
| CHEMBL4530389 | — | IC50 | - | — | - | |
| CHEMBL4533470 | — | IC50 | - | — | - | |
| CHEMBL241098 | — | IC50 | - | — | - | |
| CHEMBL4559337 | — | IC50 | - | — | - | |
| CHEMBL4592538 | — | IC50 | - | — | - | |
| CHEMBL4538097 | — | IC50 | - | — | - | |
| CHEMBL4575544 | — | IC50 | - | — | - | |
| CHEMBL4571543 | — | IC50 | - | — | - | |
| CHEMBL4536788 | — | IC50 | - | — | - | |
| CHEMBL4575807 | — | IC50 | - | — | - | |
| CHEMBL4549093 | — | IC50 | - | — | - | |
| CHEMBL4582183 | — | IC50 | - | — | - | |
| CHEMBL4483626 | — | IC50 | - | — | - | |
| CHEMBL488910 | — | IC50 | - | — | - | |
| CHEMBL241083 | — | IC50 | - | — | - | |
| CHEMBL4563533 | — | IC50 | - | — | - | |
| CHEMBL4529064 | — | IC50 | - | — | - |