Assay Detail
Binding
CHEMBL4423280
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ABCG2 (unknown origin) expressed in MDCK2 cells co-expressing BCRP (unknown origin) assessed as potentiation of SN-38-induced cytotoxicity measured after 72 hrs by MTT assay
13
Total Activities
13
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
Novel chalcone and flavone derivatives as selective and dual inhibitors of the transport proteins ABCB1 and ABCG2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 6.28 | 6.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1091644 | LINSITINIB | 3.0 | 1 | 6.98 |
| CHEMBL4283519 | — | — | 1 | 6.97 |
| CHEMBL473773 | — | — | 1 | 6.72 |
| CHEMBL4290283 | — | — | 1 | 6.35 |
| CHEMBL4540332 | — | — | 1 | 6.35 |
| CHEMBL194094 | — | — | 1 | 6.29 |
| CHEMBL4474709 | — | — | 1 | 6.10 |
| CHEMBL4282834 | — | — | 1 | 6.00 |
| CHEMBL4279728 | — | — | 1 | 5.93 |
| CHEMBL4470070 | — | — | 1 | 5.91 |
| CHEMBL4589531 | — | — | 1 | 5.90 |
| CHEMBL4289201 | — | — | 1 | 5.86 |
| CHEMBL4462468 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1091644 | LINSITINIB | EC50 | = | 104.0 | nM | 6.98 |
| CHEMBL4283519 | — | EC50 | = | 107.0 | nM | 6.97 |
| CHEMBL473773 | — | EC50 | = | 189.0 | nM | 6.72 |
| CHEMBL4290283 | — | EC50 | = | 448.0 | nM | 6.35 |
| CHEMBL4540332 | — | EC50 | = | 446.0 | nM | 6.35 |
| CHEMBL194094 | — | EC50 | = | 512.0 | nM | 6.29 |
| CHEMBL4474709 | — | EC50 | = | 793.0 | nM | 6.10 |
| CHEMBL4282834 | — | EC50 | = | 989.0 | nM | 6.00 |
| CHEMBL4279728 | — | EC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL4470070 | — | EC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL4589531 | — | EC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL4289201 | — | EC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL4462468 | — | EC50 | - | — | - |