Assay Detail
Binding
CHEMBL873882
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Topoisomerase I by cleavage complex formation in human HL-60 cells
55
Total Activities
55
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HL-60 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Plant antitumor agents. 30. Synthesis and structure activity of novel camptothecin analogs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 55 | 6.22 | 7.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL307794 | — | — | 1 | 7.57 |
| CHEMBL10741 | — | — | 1 | 7.42 |
| CHEMBL2114243 | — | — | 1 | 7.32 |
| CHEMBL90636 | — | — | 1 | 7.21 |
| CHEMBL52057 | — | — | 1 | 7.17 |
| CHEMBL90761 | — | — | 1 | 7.12 |
| CHEMBL2114244 | — | — | 1 | 7.07 |
| CHEMBL274070 | 9-AMINOCAMPTOTHECIN | 2.0 | 1 | 6.96 |
| CHEMBL273862 | HYDROXYCAMPTOTHECIN | 3.0 | 1 | 6.96 |
| CHEMBL90296 | — | — | 1 | 6.96 |
| CHEMBL91051 | — | — | 1 | 6.89 |
| CHEMBL102252 | — | — | 1 | 6.85 |
| CHEMBL2115019 | — | — | 1 | 6.85 |
| CHEMBL2114245 | — | — | 1 | 6.82 |
| CHEMBL90413 | — | — | 1 | 6.80 |
| CHEMBL91104 | — | — | 1 | 6.72 |
| CHEMBL329664 | — | — | 1 | 6.66 |
| CHEMBL540569 | — | — | 1 | 6.58 |
| CHEMBL2115014 | — | — | 1 | 6.52 |
| CHEMBL314950 | — | — | 1 | 6.43 |
| CHEMBL545250 | — | — | 1 | 6.37 |
| CHEMBL315269 | RS-9-Aminocamptothecin | — | 1 | 6.36 |
| CHEMBL89887 | — | — | 1 | 6.33 |
| CHEMBL90436 | — | — | 1 | 6.26 |
| CHEMBL558618 | — | — | 1 | 6.24 |
| CHEMBL2115022 | — | — | 1 | 6.19 |
| CHEMBL65 | CAMPTOTHECIN | -1.0 | 1 | 6.17 |
| CHEMBL2114241 | — | — | 1 | 6.08 |
| CHEMBL87791 | — | — | 1 | 6.06 |
| CHEMBL93068 | — | — | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL307794 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL10741 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2114243 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL90636 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL52057 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL90761 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL2114244 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL274070 | 9-AMINOCAMPTOTHECIN | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL273862 | HYDROXYCAMPTOTHECIN | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL90296 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL91051 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL102252 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2115019 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2114245 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL90413 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL91104 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL329664 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL540569 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL2115014 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL314950 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL545250 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL315269 | RS-9-Aminocamptothecin | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL89887 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL90436 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL558618 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL2115022 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL65 | CAMPTOTHECIN | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL2114241 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL87791 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL93068 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL84 | TOPOTECAN | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL93122 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL543849 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL276820 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL91945 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL10724 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL88912 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL91495 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL418951 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL328461 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL91017 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL2114242 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL91117 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL330072 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL539032 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL432949 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL164269 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL314025 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL88605 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL3350297 | — | IC50 | > | 30000.0 | nM | - |