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Assay Detail

CHEMBL3377300

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Functional
Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as inhibition of parasite growth after 72 hrs by parasite lactate dehydrogenase assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

Clofazimine analogs with antileishmanial and antiplasmodial activity.
Barteselli A, Casagrande M, Basilico N, Parapini S, Rusconi CM, Tonelli M, Boido V, Taramelli D, Sparatore F, Sparatore A.
Bioorg Med Chem (2015) 23 : 55 -65
PubMed 25497962 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.44 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3356383 1 7.20
CHEMBL3356379 1 6.96
CHEMBL3356394 1 6.75
CHEMBL3356392 1 6.68
CHEMBL3356387 1 6.68
CHEMBL3356384 1 6.62
CHEMBL3356382 1 6.57
CHEMBL3356391 1 6.57
CHEMBL3356386 1 6.57
CHEMBL3356395 1 6.55
CHEMBL3356377 1 6.54
CHEMBL3356389 1 6.47
CHEMBL3356393 1 6.46
CHEMBL76 CHLOROQUINE 4.0 1 6.44
CHEMBL3356388 1 6.41
CHEMBL3356385 1 6.40
CHEMBL3356375 1 6.36
CHEMBL3356378 1 6.35
CHEMBL3356390 1 6.24
CHEMBL3356376 1 6.12
CHEMBL3356380 1 6.09
CHEMBL3356381 1 6.02
CHEMBL1292 CLOFAZIMINE 4.0 1 5.15
CHEMBL267345 AMPHOTERICIN B 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3356383 IC50 = 63.0 nM 7.20
CHEMBL3356379 IC50 = 110.0 nM 6.96
CHEMBL3356394 IC50 = 180.0 nM 6.75
CHEMBL3356392 IC50 = 210.0 nM 6.68
CHEMBL3356387 IC50 = 210.0 nM 6.68
CHEMBL3356384 IC50 = 240.0 nM 6.62
CHEMBL3356382 IC50 = 270.0 nM 6.57
CHEMBL3356391 IC50 = 270.0 nM 6.57
CHEMBL3356386 IC50 = 270.0 nM 6.57
CHEMBL3356395 IC50 = 280.0 nM 6.55
CHEMBL3356377 IC50 = 290.0 nM 6.54
CHEMBL3356389 IC50 = 340.0 nM 6.47
CHEMBL3356393 IC50 = 350.0 nM 6.46
CHEMBL76 CHLOROQUINE IC50 = 360.0 nM 6.44
CHEMBL3356388 IC50 = 390.0 nM 6.41
CHEMBL3356385 IC50 = 400.0 nM 6.40
CHEMBL3356375 IC50 = 440.0 nM 6.36
CHEMBL3356378 IC50 = 450.0 nM 6.35
CHEMBL3356390 IC50 = 570.0 nM 6.24
CHEMBL3356376 IC50 = 750.0 nM 6.12
CHEMBL3356380 IC50 = 810.0 nM 6.09
CHEMBL3356381 IC50 = 960.0 nM 6.02
CHEMBL1292 CLOFAZIMINE IC50 = 7020.0 nM 5.15
CHEMBL267345 AMPHOTERICIN B IC50 - -