Assay Detail
Functional
CHEMBL1046014
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Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 infected in African green monkey (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 | 6.79 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL403233 | MANZAMINE A | — | 1 | 8.10 |
| CHEMBL612054 | — | — | 1 | 7.96 |
| CHEMBL595533 | 8-N-HEXAMIDOMANZAMINE A | — | 1 | 7.50 |
| CHEMBL595621 | 6-CYCLOHEXAMIDOMANZAMINE A | — | 1 | 7.47 |
| CHEMBL595418 | 8-N-BUTAMIDOMANZAMINE A | — | 1 | 7.46 |
| CHEMBL269671 | ARTEMISININ | 3.0 | 1 | 7.34 |
| CHEMBL76 | CHLOROQUINE | 4.0 | 1 | 7.30 |
| CHEMBL608119 | 8-N-PENTAMIDOMANZAMINE A | — | 1 | 7.28 |
| CHEMBL608123 | 8-N-OCTAMIDOMANZAMINE A | — | 1 | 7.26 |
| CHEMBL595391 | 8-N-PROPAMIDOMANZAMINE A | — | 1 | 6.91 |
| CHEMBL608124 | — | — | 1 | 6.86 |
| CHEMBL607833 | 8-ISOBUTAMIDOMANZAMINE A | — | 1 | 6.80 |
| CHEMBL608121 | 8-PIVALAMIDOMANZAMINE A | — | 1 | 6.77 |
| CHEMBL595522 | 8-ACETAMIDOMANZAMINE A | — | 1 | 6.74 |
| CHEMBL595275 | — | — | 1 | 6.68 |
| CHEMBL608120 | 6-PIVALAMIDOANZAMINE A | — | 1 | 6.64 |
| CHEMBL595435 | 6-N-HEXAMIDOMANZAMINE A | — | 1 | 6.17 |
| CHEMBL608122 | 6-N-OCTAMIDOMANZAMINE A | — | 1 | 6.16 |
| CHEMBL595762 | 8-CYCLOHEXAMIDOMANZAMINE A | — | 1 | 6.02 |
| CHEMBL607832 | 6-ISOBUTAMIDOMANZAMINE A | — | 1 | 5.96 |
| CHEMBL595461 | 6-N-BUTAMIDOMANZAMINE A | — | 1 | 5.94 |
| CHEMBL595515 | 6-N-PROPAMIDOMANZAMINE A | — | 1 | 5.93 |
| CHEMBL595532 | 6-N-PENTAMIDOMANZAMINE A | — | 1 | 5.91 |
| CHEMBL595531 | 6-ACETAMIDOMANZAMINE A | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL403233 | MANZAMINE A | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL612054 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL595533 | 8-N-HEXAMIDOMANZAMINE A | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL595621 | 6-CYCLOHEXAMIDOMANZAMINE A | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL595418 | 8-N-BUTAMIDOMANZAMINE A | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL269671 | ARTEMISININ | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL76 | CHLOROQUINE | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL608119 | 8-N-PENTAMIDOMANZAMINE A | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL608123 | 8-N-OCTAMIDOMANZAMINE A | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL595391 | 8-N-PROPAMIDOMANZAMINE A | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL608124 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL607833 | 8-ISOBUTAMIDOMANZAMINE A | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL608121 | 8-PIVALAMIDOMANZAMINE A | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL595522 | 8-ACETAMIDOMANZAMINE A | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL595275 | — | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL608120 | 6-PIVALAMIDOANZAMINE A | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL595435 | 6-N-HEXAMIDOMANZAMINE A | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL608122 | 6-N-OCTAMIDOMANZAMINE A | IC50 | = | 696.0 | nM | 6.16 |
| CHEMBL595762 | 8-CYCLOHEXAMIDOMANZAMINE A | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL607832 | 6-ISOBUTAMIDOMANZAMINE A | IC50 | = | 1105.0 | nM | 5.96 |
| CHEMBL595461 | 6-N-BUTAMIDOMANZAMINE A | IC50 | = | 1152.0 | nM | 5.94 |
| CHEMBL595515 | 6-N-PROPAMIDOMANZAMINE A | IC50 | = | 1162.0 | nM | 5.93 |
| CHEMBL595532 | 6-N-PENTAMIDOMANZAMINE A | IC50 | = | 1235.0 | nM | 5.91 |
| CHEMBL595531 | 6-ACETAMIDOMANZAMINE A | IC50 | = | 1288.0 | nM | 5.89 |