Assay Detail
Binding
CHEMBL2434497
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 5-lipoxygenase in rat RBL1 cells
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | RBL-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL312) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Molecular modeling studies of substituted 3,4-dihydroxychalcone derivatives as 5-lipoxygenase and cyclooxygenase inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 52 | 5.13 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL341135 | — | — | 1 | 8.40 |
| CHEMBL126669 | — | — | 1 | 8.38 |
| CHEMBL128000 | BUTEIN | — | 1 | 8.34 |
| CHEMBL339587 | — | — | 1 | 7.64 |
| CHEMBL129510 | — | — | 1 | 7.37 |
| CHEMBL127409 | 3,4,2',4',6'-PENTAHYDROXYCHALCONE | — | 1 | 6.85 |
| CHEMBL2429962 | — | — | 1 | 6.00 |
| CHEMBL2429957 | — | — | 1 | 5.62 |
| CHEMBL2429960 | — | — | 1 | 5.40 |
| CHEMBL390381 | — | — | 1 | 5.33 |
| CHEMBL2429959 | — | — | 1 | 5.28 |
| CHEMBL318170 | — | — | 1 | 5.19 |
| CHEMBL1801959 | — | — | 1 | 5.11 |
| CHEMBL2430039 | — | — | 1 | 5.11 |
| CHEMBL465025 | — | — | 1 | 5.05 |
| CHEMBL126657 | — | — | 1 | 5.05 |
| CHEMBL2430042 | — | — | 1 | 5.01 |
| CHEMBL144626 | — | — | 1 | 5.00 |
| CHEMBL2429961 | — | — | 1 | 4.96 |
| CHEMBL130639 | — | — | 1 | 4.92 |
| CHEMBL2429955 | — | — | 1 | 4.85 |
| CHEMBL465457 | — | — | 1 | 4.82 |
| CHEMBL61592 | — | — | 1 | 4.80 |
| CHEMBL2429958 | — | — | 1 | 4.80 |
| CHEMBL2430038 | — | — | 1 | 4.77 |
| CHEMBL130640 | — | — | 1 | 4.77 |
| CHEMBL33943 | — | — | 1 | 4.75 |
| CHEMBL105496 | 4-METHOXY CHALCONE | — | 1 | 4.70 |
| CHEMBL106771 | — | — | 1 | 4.64 |
| CHEMBL2429869 | — | — | 1 | 4.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL341135 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL126669 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL128000 | BUTEIN | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL339587 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL129510 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL127409 | 3,4,2',4',6'-PENTAHYDROXYCHALCONE | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2429962 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2429957 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL2429960 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL390381 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL2429959 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL318170 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL2430039 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL1801959 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL126657 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL465025 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL2430042 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL144626 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL2429961 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL130639 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL2429955 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL465457 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL61592 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL2429958 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL130640 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL2430038 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL33943 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL105496 | 4-METHOXY CHALCONE | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL106771 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL2429869 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL2429956 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL2430043 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL104732 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL129795 | ISOLIQUIRITIGENIN | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL2429954 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL1999124 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL2430041 | — | IC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL2430040 | — | IC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL104575 | — | IC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL126804 | — | IC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL7976 | CHALCONE | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL1801961 | — | IC50 | = | 58000.0 | nM | 4.24 |
| CHEMBL1255773 | — | IC50 | = | 64000.0 | nM | 4.19 |
| CHEMBL375905 | — | IC50 | = | 76000.0 | nM | 4.12 |
| CHEMBL227560 | 4-CHLORO CHALCONE | IC50 | = | 85000.0 | nM | 4.07 |
| CHEMBL474682 | — | IC50 | = | 92000.0 | nM | 4.04 |
| CHEMBL338066 | 4,2',4',6'-TETRAHYDROXYCHALCONE | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL105310 | 2',4'-DIHYDROXYCHALCONE | IC50 | = | 400000.0 | nM | - |
| CHEMBL276473 | 4'-HYDROXYCHALCONE | IC50 | = | 230000.0 | nM | - |
| CHEMBL129371 | 2',4',6-TRIHYDROXYCHALCONE | IC50 | = | 140000.0 | nM | - |