Assay Detail
Binding
CHEMBL5260629
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human OATP2B1 expressed in Flp-In-CHO cells assessed as inhibition of OATP2B1 mediated DBF uptake using DBF as fluorescent substrate incubated for 2 mins by BCA assay
48
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Flp-In-CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Solute carrier organic anion transporter family member 2B1 (CHEMBL1743124) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Investigating the interactions of flavonoids with human OATP2B1: inhibition assay, IC<sub>50</sub> determination, and structure-activity relationship analysis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 48 | 4.80 | 6.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL55415 | SCUTELLAREIN | — | 2 | 6.46 |
| CHEMBL5277249 | — | — | 2 | 6.04 |
| CHEMBL151 | LUTEOLIN | 2.0 | 2 | 5.41 |
| CHEMBL44 | GENISTEIN | 2.0 | 2 | 5.28 |
| CHEMBL31574 | FISETIN | 2.0 | 2 | 5.17 |
| CHEMBL183513 | OROXYLIN A | — | 2 | 5.15 |
| CHEMBL50 | QUERCETIN | 3.0 | 2 | 5.14 |
| CHEMBL487017 | APIGETRIN | — | 2 | 4.98 |
| CHEMBL250450 | ISOQUERCETIN | 2.0 | 2 | 4.83 |
| CHEMBL28 | APIGENIN | — | 2 | 4.74 |
| CHEMBL9352 | NARINGENIN | — | 2 | 4.68 |
| CHEMBL164 | MYRICETIN | — | 2 | 4.57 |
| CHEMBL8996 | ERIODICTYOL | — | 2 | 4.54 |
| CHEMBL117 | CHRYSIN | — | 2 | 4.54 |
| CHEMBL150 | KAEMPFEROL | 1.0 | 2 | 4.39 |
| CHEMBL522983 | — | — | 2 | 4.34 |
| CHEMBL36327 | EPICATECHIN GALLATE | — | 2 | 4.33 |
| CHEMBL509624 | — | — | 2 | 4.21 |
| CHEMBL82242 | QUERCITRIN | — | 2 | 4.20 |
| CHEMBL297453 | EPIGALOCATECHIN GALLATE | 3.0 | 2 | 4.10 |
| CHEMBL253570 | GOSSYPETIN | — | 2 | 4.09 |
| CHEMBL469654 | PRUNIN | — | 2 | 4.00 |
| CHEMBL251254 | HYPEROSIDE | — | 2 | - |
| CHEMBL226335 | RUTIN | 3.0 | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL55415 | SCUTELLAREIN | IC50 | = | 346.74 | nM | 6.46 |
| CHEMBL55415 | SCUTELLAREIN | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL5277249 | — | IC50 | = | 912.01 | nM | 6.04 |
| CHEMBL5277249 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL151 | LUTEOLIN | IC50 | = | 3890.45 | nM | 5.41 |
| CHEMBL151 | LUTEOLIN | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL44 | GENISTEIN | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL44 | GENISTEIN | IC50 | = | 5248.07 | nM | 5.28 |
| CHEMBL31574 | FISETIN | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL31574 | FISETIN | IC50 | = | 6760.83 | nM | 5.17 |
| CHEMBL183513 | OROXYLIN A | IC50 | = | 7079.46 | nM | 5.15 |
| CHEMBL183513 | OROXYLIN A | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL50 | QUERCETIN | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL50 | QUERCETIN | IC50 | = | 7244.36 | nM | 5.14 |
| CHEMBL487017 | APIGETRIN | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL487017 | APIGETRIN | IC50 | = | 10471.29 | nM | 4.98 |
| CHEMBL250450 | ISOQUERCETIN | IC50 | = | 14800.0 | nM | 4.83 |
| CHEMBL250450 | ISOQUERCETIN | IC50 | = | 14791.08 | nM | 4.83 |
| CHEMBL28 | APIGENIN | IC50 | = | 18100.0 | nM | 4.74 |
| CHEMBL28 | APIGENIN | IC50 | = | 18197.01 | nM | 4.74 |
| CHEMBL9352 | NARINGENIN | IC50 | = | 20892.96 | nM | 4.68 |
| CHEMBL9352 | NARINGENIN | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL164 | MYRICETIN | IC50 | = | 26915.35 | nM | 4.57 |
| CHEMBL164 | MYRICETIN | IC50 | = | 26800.0 | nM | 4.57 |
| CHEMBL117 | CHRYSIN | IC50 | = | 28840.32 | nM | 4.54 |
| CHEMBL117 | CHRYSIN | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL8996 | ERIODICTYOL | IC50 | = | 28700.0 | nM | 4.54 |
| CHEMBL8996 | ERIODICTYOL | IC50 | = | 28840.32 | nM | 4.54 |
| CHEMBL150 | KAEMPFEROL | IC50 | = | 40900.0 | nM | 4.39 |
| CHEMBL150 | KAEMPFEROL | IC50 | = | 40738.03 | nM | 4.39 |
| CHEMBL522983 | — | IC50 | = | 45708.82 | nM | 4.34 |
| CHEMBL36327 | EPICATECHIN GALLATE | IC50 | = | 46773.51 | nM | 4.33 |
| CHEMBL522983 | — | IC50 | = | 46200.0 | nM | 4.33 |
| CHEMBL36327 | EPICATECHIN GALLATE | IC50 | = | 47200.0 | nM | 4.33 |
| CHEMBL509624 | — | IC50 | = | 61659.5 | nM | 4.21 |
| CHEMBL509624 | — | IC50 | = | 61500.0 | nM | 4.21 |
| CHEMBL82242 | QUERCITRIN | IC50 | = | 63100.0 | nM | 4.20 |
| CHEMBL82242 | QUERCITRIN | IC50 | = | 63095.73 | nM | 4.20 |
| CHEMBL297453 | EPIGALOCATECHIN GALLATE | IC50 | = | 79432.82 | nM | 4.10 |
| CHEMBL297453 | EPIGALOCATECHIN GALLATE | IC50 | = | 79600.0 | nM | 4.10 |
| CHEMBL253570 | GOSSYPETIN | IC50 | = | 82000.0 | nM | 4.09 |
| CHEMBL253570 | GOSSYPETIN | IC50 | = | 81283.05 | nM | 4.09 |
| CHEMBL469654 | PRUNIN | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL251254 | HYPEROSIDE | IC50 | = | 125800.0 | nM | - |
| CHEMBL251254 | HYPEROSIDE | IC50 | = | 125892.54 | nM | - |
| CHEMBL226335 | RUTIN | IC50 | = | 138038.43 | nM | - |
| CHEMBL469654 | PRUNIN | IC50 | = | 101000.0 | nM | - |
| CHEMBL226335 | RUTIN | IC50 | = | 136900.0 | nM | - |