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Assay Detail

CHEMBL754546

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

Functional
Growth inhibition (IC50) against Plasmodium falciparum wild-type TM4/8.2
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Plasmodium falciparum
Confidence 1 — Organism
Curated By Expert

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

Development of a lead inhibitor for the A16V+S108T mutant of dihydrofolate reductase from the cycloguanil-resistant strain (T9/94) of Plasmodium falciparum.
Yuthavong Y, Vilaivan T, Chareonsethakul N, Kamchonwongpaisan S, Sirawaraporn W, Quarrell R, Lowe G.
J Med Chem (2000) 43 : 2738 -2744
PubMed 10893311 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.41 7.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6741 1 7.51
CHEMBL93153 1 7.46
CHEMBL92047 1 7.40
CHEMBL7130 1 7.22
CHEMBL7004 1 7.19
CHEMBL93748 1 6.88
CHEMBL90461 1 6.88
CHEMBL443013 1 6.78
CHEMBL89959 1 6.56
CHEMBL7005 1 6.53
CHEMBL92182 1 6.33
CHEMBL6742 1 6.26
CHEMBL94281 1 6.20
CHEMBL264392 1 5.54
CHEMBL433204 1 5.54
CHEMBL90358 1 5.08
CHEMBL93001 1 5.01
CHEMBL92846 1 4.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6741 IC50 = 31.0 nM 7.51
CHEMBL93153 IC50 = 35.0 nM 7.46
CHEMBL92047 IC50 = 40.0 nM 7.40
CHEMBL7130 IC50 = 60.0 nM 7.22
CHEMBL7004 IC50 = 65.0 nM 7.19
CHEMBL93748 IC50 = 132.0 nM 6.88
CHEMBL90461 IC50 = 132.0 nM 6.88
CHEMBL443013 IC50 = 167.0 nM 6.78
CHEMBL89959 IC50 = 273.0 nM 6.56
CHEMBL7005 IC50 = 294.0 nM 6.53
CHEMBL92182 IC50 = 462.0 nM 6.33
CHEMBL6742 IC50 = 546.0 nM 6.26
CHEMBL94281 IC50 = 638.0 nM 6.20
CHEMBL264392 IC50 = 2908.0 nM 5.54
CHEMBL433204 IC50 = 2908.0 nM 5.54
CHEMBL90358 IC50 = 8223.0 nM 5.08
CHEMBL93001 IC50 = 9661.0 nM 5.01
CHEMBL92846 IC50 = 11632.0 nM 4.93