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Assay Detail

CHEMBL667608

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Binding
Compound was tested for its inhibition against dihydrofolate reductase enzyme of Plasmodium berghei
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Plasmodium berghei
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Bifunctional dihydrofolate reductase-thymidylate synthase (CHEMBL3963)
Type SINGLE PROTEIN
Organism Plasmodium berghei str. ANKA

Publication

2,4-Diamino-5-benzylpyrimidines as antibacterial agents. 4. 6-Substituted trimethoprim derivatives from phenolic Mannich intermediates. Application to the synthesis of trimethoprim and 3,5-dialkylbenzyl analogues.
Roth B, Aig E, Lane K, Rauckman BS.
J Med Chem (1980) 23 : 535 -541
PubMed 6991695 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.38 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL22 TRIMETHOPRIM 4.0 1 6.92
CHEMBL325533 1 6.47
CHEMBL339058 1 6.32
CHEMBL149353 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL22 TRIMETHOPRIM IC50 = 120.0 nM 6.92
CHEMBL325533 IC50 = 340.0 nM 6.47
CHEMBL339058 IC50 = 480.0 nM 6.32
CHEMBL149353 IC50 = 1500.0 nM 5.82