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Assay Detail

CHEMBL1944297

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

Binding
Inhibition of Plasmodium falciparum DHFR assessed as oxidation of NADPH to NADP+ after 15 mins spectrophotometric assay
11
Total Activities
11
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

Design and synthesis of small molecular dual inhibitor of falcipain-2 and dihydrofolate reductase as antimalarial agent.
Huang H, Lu W, Li X, Cong X, Ma H, Liu X, Zhang Y, Che P, Ma R, Li H, Shen X, Jiang H, Huang J, Zhu J.
Bioorg Med Chem Lett (2012) 22 : 958 -962
PubMed 22192590 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.22 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL36 PYRIMETHAMINE 4.0 1 7.70
CHEMBL1939367 1 5.75
CHEMBL1939223 1 5.30
CHEMBL1939368 1 5.20
CHEMBL1939233 1 5.03
CHEMBL1939234 1 4.90
CHEMBL1939235 1 4.84
CHEMBL1939229 1 4.82
CHEMBL1939228 1 4.78
CHEMBL1939232 1 4.70
CHEMBL549325 1 4.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL36 PYRIMETHAMINE IC50 = 20.0 nM 7.70
CHEMBL1939367 IC50 = 1800.0 nM 5.75
CHEMBL1939223 IC50 = 5000.0 nM 5.30
CHEMBL1939368 IC50 = 6300.0 nM 5.20
CHEMBL1939233 IC50 = 9400.0 nM 5.03
CHEMBL1939234 IC50 = 12600.0 nM 4.90
CHEMBL1939235 IC50 = 14600.0 nM 4.84
CHEMBL1939229 IC50 = 15100.0 nM 4.82
CHEMBL1939228 IC50 = 16800.0 nM 4.78
CHEMBL1939232 IC50 = 19800.0 nM 4.70
CHEMBL549325 IC50 = 35500.0 nM 4.45