Assay Detail
Functional
CHEMBL1046015
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in African green monkey (Cercopithecus aethiops) (Cercopithecus aethiops) Vero cells assessed as parasite LDH activity after 72 hrs
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Plasmodium falciparum |
| Cell Type | Vero |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Structure-activity relationship studies of manzamine A: amidation of positions 6 and 8 of the beta-carboline moiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.65 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL403233 | MANZAMINE A | — | 1 | 7.96 |
| CHEMBL612054 | — | — | 1 | 7.85 |
| CHEMBL269671 | ARTEMISININ | 3.0 | 1 | 7.55 |
| CHEMBL608123 | 8-N-OCTAMIDOMANZAMINE A | — | 1 | 7.37 |
| CHEMBL608119 | 8-N-PENTAMIDOMANZAMINE A | — | 1 | 7.31 |
| CHEMBL595621 | 6-CYCLOHEXAMIDOMANZAMINE A | — | 1 | 7.28 |
| CHEMBL595533 | 8-N-HEXAMIDOMANZAMINE A | — | 1 | 7.19 |
| CHEMBL595391 | 8-N-PROPAMIDOMANZAMINE A | — | 1 | 7.06 |
| CHEMBL595418 | 8-N-BUTAMIDOMANZAMINE A | — | 1 | 6.92 |
| CHEMBL608124 | — | — | 1 | 6.90 |
| CHEMBL607833 | 8-ISOBUTAMIDOMANZAMINE A | — | 1 | 6.69 |
| CHEMBL595522 | 8-ACETAMIDOMANZAMINE A | — | 1 | 6.64 |
| CHEMBL608121 | 8-PIVALAMIDOMANZAMINE A | — | 1 | 6.63 |
| CHEMBL595275 | — | — | 1 | 6.52 |
| CHEMBL608120 | 6-PIVALAMIDOANZAMINE A | — | 1 | 6.38 |
| CHEMBL76 | CHLOROQUINE | 4.0 | 1 | 6.32 |
| CHEMBL608122 | 6-N-OCTAMIDOMANZAMINE A | — | 1 | 6.12 |
| CHEMBL595435 | 6-N-HEXAMIDOMANZAMINE A | — | 1 | 6.11 |
| CHEMBL595762 | 8-CYCLOHEXAMIDOMANZAMINE A | — | 1 | 6.00 |
| CHEMBL595532 | 6-N-PENTAMIDOMANZAMINE A | — | 1 | 5.83 |
| CHEMBL607832 | 6-ISOBUTAMIDOMANZAMINE A | — | 1 | 5.81 |
| CHEMBL595461 | 6-N-BUTAMIDOMANZAMINE A | — | 1 | 5.72 |
| CHEMBL595515 | 6-N-PROPAMIDOMANZAMINE A | — | 1 | 5.71 |
| CHEMBL595531 | 6-ACETAMIDOMANZAMINE A | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL403233 | MANZAMINE A | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL612054 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL269671 | ARTEMISININ | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL608123 | 8-N-OCTAMIDOMANZAMINE A | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL608119 | 8-N-PENTAMIDOMANZAMINE A | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL595621 | 6-CYCLOHEXAMIDOMANZAMINE A | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL595533 | 8-N-HEXAMIDOMANZAMINE A | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL595391 | 8-N-PROPAMIDOMANZAMINE A | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL595418 | 8-N-BUTAMIDOMANZAMINE A | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL608124 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL607833 | 8-ISOBUTAMIDOMANZAMINE A | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL595522 | 8-ACETAMIDOMANZAMINE A | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL608121 | 8-PIVALAMIDOMANZAMINE A | IC50 | = | 232.0 | nM | 6.63 |
| CHEMBL595275 | — | IC50 | = | 302.0 | nM | 6.52 |
| CHEMBL608120 | 6-PIVALAMIDOANZAMINE A | IC50 | = | 417.0 | nM | 6.38 |
| CHEMBL76 | CHLOROQUINE | IC50 | = | 484.0 | nM | 6.32 |
| CHEMBL608122 | 6-N-OCTAMIDOMANZAMINE A | IC50 | = | 754.0 | nM | 6.12 |
| CHEMBL595435 | 6-N-HEXAMIDOMANZAMINE A | IC50 | = | 786.0 | nM | 6.11 |
| CHEMBL595762 | 8-CYCLOHEXAMIDOMANZAMINE A | IC50 | = | 995.0 | nM | 6.00 |
| CHEMBL595532 | 6-N-PENTAMIDOMANZAMINE A | IC50 | = | 1482.0 | nM | 5.83 |
| CHEMBL607832 | 6-ISOBUTAMIDOMANZAMINE A | IC50 | = | 1547.0 | nM | 5.81 |
| CHEMBL595461 | 6-N-BUTAMIDOMANZAMINE A | IC50 | = | 1894.0 | nM | 5.72 |
| CHEMBL595515 | 6-N-PROPAMIDOMANZAMINE A | IC50 | = | 1937.0 | nM | 5.71 |
| CHEMBL595531 | 6-ACETAMIDOMANZAMINE A | IC50 | = | 1982.0 | nM | 5.70 |