Assay Detail
Binding
CHEMBL5586208
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Inhibition of wild type Plasmodium falciparum DHFR expressed in Escherichia coli BL21(DE3) pLysS cells assessed as inhibition constant using DHF as substrate measured for 80 sec in presence of NADPH
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Plasmodium falciparum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Bifunctional dihydrofolate reductase-thymidylate synthase (CHEMBL1939) ↗| Type | SINGLE PROTEIN |
| Organism | Plasmodium falciparum K1 |
Publication
Novel flexible biphenyl <i>Pf</i>DHFR inhibitors with improved antimalarial activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 9.48 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5598041 | — | — | 1 | 9.80 |
| CHEMBL5596188 | — | — | 1 | 9.62 |
| CHEMBL5597152 | — | — | 1 | 9.62 |
| CHEMBL5597998 | — | — | 1 | 9.60 |
| CHEMBL5597854 | — | — | 1 | 9.59 |
| CHEMBL5597280 | — | — | 1 | 9.24 |
| CHEMBL5598010 | — | — | 1 | 9.22 |
| CHEMBL5590041 | — | — | 1 | 9.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5598041 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL5596188 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL5597152 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL5597998 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL5597854 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL5597280 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL5598010 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL5590041 | — | Ki | = | 0.67 | nM | 9.17 |