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Assay Detail

CHEMBL1260233

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity to wild type Plasmodium falciparum DHFR by competitive binding assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Plasmodium falciparum
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate.
Nzila A, Rottmann M, Chitnumsub P, Kiara SM, Kamchonwongpaisan S, Maneeruttanarungroj C, Taweechai S, Yeung BK, Goh A, Lakshminarayana SB, Zou B, Wong J, Ma NL, Weaver M, Keller TH, Dartois V, Wittlin S, Brun R, Yuthavong Y, Diagana TT.
Antimicrob Agents Chemother (2010) 54 : 2603 -2610
PubMed 20350951 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 9.19 9.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL138060 1 9.41
CHEMBL129788 1 9.30
CHEMBL36 PYRIMETHAMINE 4.0 1 9.23
CHEMBL747 CYCLOGUANIL 2.0 1 8.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL138060 Ki = 0.39 nM 9.41
CHEMBL129788 Ki = 0.5 nM 9.30
CHEMBL36 PYRIMETHAMINE Ki = 0.59 nM 9.23
CHEMBL747 CYCLOGUANIL Ki = 1.51 nM 8.82