Assay Detail
Functional
CHEMBL2175349
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Antihyperproliferative activity against human HaCaT cells after 48 hrs by phase contrast microscopy
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HaCaT |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Synthesis and structure-activity relationships of lapacho analogues. 1. Suppression of human keratinocyte hyperproliferation by 2-substituted naphtho[2,3-b]furan-4,9-diones, activation by enzymatic one- and two-electron reduction, and intracellular generation of superoxide.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 5.83 | 6.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2171357 | — | — | 1 | 6.77 |
| CHEMBL2171380 | — | — | 1 | 6.62 |
| CHEMBL2171366 | — | — | 1 | 6.43 |
| CHEMBL2171362 | — | — | 1 | 6.36 |
| CHEMBL64130 | NAPABUCASIN | 3.0 | 1 | 6.30 |
| CHEMBL2171365 | — | — | 1 | 6.26 |
| CHEMBL2171369 | — | — | 1 | 6.21 |
| CHEMBL2171361 | — | — | 1 | 6.20 |
| CHEMBL2171364 | — | — | 1 | 6.17 |
| CHEMBL46469 | ANTHRALIN | 2.0 | 1 | 6.16 |
| CHEMBL2171363 | — | — | 1 | 6.14 |
| CHEMBL2171358 | — | — | 1 | 6.10 |
| CHEMBL15192 | LAPACHONE | 2.0 | 1 | 6.05 |
| CHEMBL2171355 | — | — | 1 | 6.05 |
| CHEMBL2171368 | — | — | 1 | 6.04 |
| CHEMBL2171359 | — | — | 1 | 6.04 |
| CHEMBL2171371 | — | — | 1 | 6.00 |
| CHEMBL2171351 | — | — | 1 | 5.96 |
| CHEMBL2171370 | — | — | 1 | 5.88 |
| CHEMBL2171360 | — | — | 1 | 5.70 |
| CHEMBL2171354 | — | — | 1 | 5.63 |
| CHEMBL2171350 | — | — | 1 | 5.60 |
| CHEMBL476506 | — | — | 1 | 5.56 |
| CHEMBL2171372 | — | — | 1 | 5.54 |
| CHEMBL2171373 | — | — | 1 | 5.53 |
| CHEMBL62539 | — | — | 1 | 5.42 |
| CHEMBL62074 | — | — | 1 | 5.12 |
| CHEMBL2171353 | — | — | 1 | 5.11 |
| CHEMBL2171377 | — | — | 1 | 5.08 |
| CHEMBL62292 | — | — | 1 | 4.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2171357 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2171380 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2171366 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL2171362 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL64130 | NAPABUCASIN | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2171365 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL2171369 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL2171361 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL2171364 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL46469 | ANTHRALIN | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL2171363 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL2171358 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL15192 | LAPACHONE | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL2171355 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL2171359 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL2171368 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL2171371 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL2171351 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL2171370 | — | IC50 | = | 1320.0 | nM | 5.88 |
| CHEMBL2171360 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2171354 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL2171350 | — | IC50 | = | 2510.0 | nM | 5.60 |
| CHEMBL476506 | — | IC50 | = | 2760.0 | nM | 5.56 |
| CHEMBL2171372 | — | IC50 | = | 2860.0 | nM | 5.54 |
| CHEMBL2171373 | — | IC50 | = | 2930.0 | nM | 5.53 |
| CHEMBL62539 | — | IC50 | = | 3850.0 | nM | 5.42 |
| CHEMBL62074 | — | IC50 | = | 7540.0 | nM | 5.12 |
| CHEMBL2171353 | — | IC50 | = | 7730.0 | nM | 5.11 |
| CHEMBL2171377 | — | IC50 | = | 8230.0 | nM | 5.08 |
| CHEMBL62292 | — | IC50 | = | 12180.0 | nM | 4.91 |
| CHEMBL2171376 | — | IC50 | = | 14340.0 | nM | 4.84 |
| CHEMBL590 | MENADIONE | IC50 | = | 15800.0 | nM | 4.80 |
| CHEMBL2171375 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2171367 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2171374 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2171378 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2171379 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2171349 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2171352 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2171356 | — | IC50 | > | 30000.0 | nM | - |