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Assay Detail

CHEMBL4267042

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Functional
Antimalarial activity against Plasmodium falciparum after 48 hrs by microbeta scintillation counting-based [3H]-hypoxanthine incorporation assay
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 Intermediate

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG).
Tsagris DJ, Birchall K, Bouloc N, Large JM, Merritt A, Smiljanic-Hurley E, Wheldon M, Ansell KH, Kettleborough C, Whalley D, Stewart LB, Bowyer PW, Baker DA, Osborne SA.
Bioorg Med Chem Lett (2018) 28 : 3168 -3173
PubMed 30174152 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 6.52 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4285682 1 7.60
CHEMBL4288816 1 7.14
CHEMBL4294776 1 7.05
CHEMBL4288103 1 7.04
CHEMBL4286880 1 6.98
CHEMBL4286841 1 6.95
CHEMBL4283774 1 6.84
CHEMBL4279865 1 6.81
CHEMBL425949 1 6.40
CHEMBL190228 1 6.35
CHEMBL4284547 1 5.88
CHEMBL4282026 1 5.83
CHEMBL4287934 1 5.81
CHEMBL4281827 1 5.74
CHEMBL4280027 1 5.34
CHEMBL4291946 1 -
CHEMBL4295199 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4285682 EC50 = 25.0 nM 7.60
CHEMBL4288816 EC50 = 73.0 nM 7.14
CHEMBL4294776 EC50 = 90.0 nM 7.05
CHEMBL4288103 EC50 = 92.0 nM 7.04
CHEMBL4286880 EC50 = 105.0 nM 6.98
CHEMBL4286841 EC50 = 113.0 nM 6.95
CHEMBL4283774 EC50 = 144.0 nM 6.84
CHEMBL4279865 EC50 = 155.0 nM 6.81
CHEMBL425949 EC50 = 400.0 nM 6.40
CHEMBL190228 EC50 = 450.0 nM 6.35
CHEMBL4284547 EC50 = 1330.0 nM 5.88
CHEMBL4282026 EC50 = 1490.0 nM 5.83
CHEMBL4287934 EC50 = 1560.0 nM 5.81
CHEMBL4281827 EC50 = 1810.0 nM 5.74
CHEMBL4280027 EC50 = 4570.0 nM 5.34
CHEMBL4291946 EC50 - -
CHEMBL4295199 EC50 - -