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Assay Detail

CHEMBL1019539

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Functional
Antiplasmodial activity against Plasmodium falciparum 3D7
17
Total Activities
17
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

QSAR study on tetrahydroquinoline analogues as plasmodium protein farnesyltransferase inhibitors: a comparison of rationales of malarial and mammalian enzyme inhibitory activities for selectivity.
Gupta MK, Prabhakar YS.
Eur J Med Chem (2008) 43 : 2751 -2767
PubMed 18329140 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.07 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL182888 1 8.30
CHEMBL183536 1 8.30
CHEMBL194447 1 8.30
CHEMBL193034 1 8.22
CHEMBL181102 1 8.16
CHEMBL192244 1 7.29
CHEMBL191843 1 7.26
CHEMBL373337 1 7.07
CHEMBL370298 1 7.00
CHEMBL365742 1 6.95
CHEMBL195168 1 5.57
CHEMBL371408 1 5.56
CHEMBL193161 1 5.52
CHEMBL365549 1 5.52
CHEMBL372017 1 -
CHEMBL233288 1 -
CHEMBL192898 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL182888 IC50 = 5.012 nM 8.30
CHEMBL183536 IC50 = 5.012 nM 8.30
CHEMBL194447 IC50 = 5.012 nM 8.30
CHEMBL193034 IC50 = 6.026 nM 8.22
CHEMBL181102 IC50 = 6.918 nM 8.16
CHEMBL192244 IC50 = 51.29 nM 7.29
CHEMBL191843 IC50 = 54.95 nM 7.26
CHEMBL373337 IC50 = 85.11 nM 7.07
CHEMBL370298 IC50 = 100.0 nM 7.00
CHEMBL365742 IC50 = 112.2 nM 6.95
CHEMBL195168 IC50 = 2691.53 nM 5.57
CHEMBL371408 IC50 = 2754.23 nM 5.56
CHEMBL193161 IC50 = 3019.95 nM 5.52
CHEMBL365549 IC50 = 3019.95 nM 5.52
CHEMBL372017 IC50 > 5011.87 nM -
CHEMBL233288 IC50 > 5011.87 nM -
CHEMBL192898 IC50 > 5011.87 nM -