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Assay Detail

CHEMBL758323

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Functional
Inhibition of Plasmodium falciparum T9/94 mutant
19
Total Activities
19
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 19 6.30 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93153 1 7.72
CHEMBL13636 1 7.55
CHEMBL443013 1 6.82
CHEMBL93748 1 6.56
CHEMBL90461 1 6.56
CHEMBL7130 1 6.53
CHEMBL93001 1 6.51
CHEMBL92846 1 6.45
CHEMBL6742 1 6.35
CHEMBL92182 1 6.33
CHEMBL92047 1 6.31
CHEMBL89959 1 6.29
CHEMBL94281 1 6.14
CHEMBL7005 1 6.00
CHEMBL6741 1 5.56
CHEMBL264392 1 5.55
CHEMBL433204 1 5.55
CHEMBL90358 1 5.46
CHEMBL7004 1 5.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93153 IC50 = 19.0 nM 7.72
CHEMBL13636 IC50 = 28.0 nM 7.55
CHEMBL443013 IC50 = 152.0 nM 6.82
CHEMBL93748 IC50 = 277.0 nM 6.56
CHEMBL90461 IC50 = 277.0 nM 6.56
CHEMBL7130 IC50 = 298.0 nM 6.53
CHEMBL93001 IC50 = 312.0 nM 6.51
CHEMBL92846 IC50 = 356.0 nM 6.45
CHEMBL6742 IC50 = 445.0 nM 6.35
CHEMBL92182 IC50 = 464.0 nM 6.33
CHEMBL92047 IC50 = 486.0 nM 6.31
CHEMBL89959 IC50 = 517.0 nM 6.29
CHEMBL94281 IC50 = 725.0 nM 6.14
CHEMBL7005 IC50 = 1001.0 nM 6.00
CHEMBL6741 IC50 = 2759.0 nM 5.56
CHEMBL264392 IC50 = 2818.0 nM 5.55
CHEMBL433204 IC50 = 2818.0 nM 5.55
CHEMBL90358 IC50 = 3446.0 nM 5.46
CHEMBL7004 IC50 = 3617.0 nM 5.44