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Assay Detail

CHEMBL4267041

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Binding
Inhibition of Plasmodium falciparum protein kinase G
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Plasmodium falciparum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

cGMP-dependent protein kinase (CHEMBL2169724)
Type SINGLE PROTEIN
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
IC50 17 8.29 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4285682 1 9.52
CHEMBL4288816 1 9.30
CHEMBL4288103 1 9.15
CHEMBL4286880 1 9.05
CHEMBL4279865 1 9.00
CHEMBL4286841 1 8.70
CHEMBL425949 1 8.52
CHEMBL4284547 1 8.22
CHEMBL190228 1 8.22
CHEMBL4283774 1 8.22
CHEMBL4287934 1 8.05
CHEMBL4282026 1 7.82
CHEMBL4281827 1 7.77
CHEMBL4295199 1 7.77
CHEMBL4280027 1 7.48
CHEMBL4294776 1 7.33
CHEMBL4291946 1 6.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4285682 IC50 = 0.3 nM 9.52
CHEMBL4288816 IC50 = 0.5 nM 9.30
CHEMBL4288103 IC50 = 0.7 nM 9.15
CHEMBL4286880 IC50 = 0.9 nM 9.05
CHEMBL4279865 IC50 = 1.0 nM 9.00
CHEMBL4286841 IC50 = 2.0 nM 8.70
CHEMBL425949 IC50 = 3.0 nM 8.52
CHEMBL4284547 IC50 = 6.0 nM 8.22
CHEMBL190228 IC50 = 6.0 nM 8.22
CHEMBL4283774 IC50 = 6.0 nM 8.22
CHEMBL4287934 IC50 = 9.0 nM 8.05
CHEMBL4282026 IC50 = 15.0 nM 7.82
CHEMBL4281827 IC50 = 17.0 nM 7.77
CHEMBL4295199 IC50 = 17.0 nM 7.77
CHEMBL4280027 IC50 = 33.0 nM 7.48
CHEMBL4294776 IC50 = 47.0 nM 7.33
CHEMBL4291946 IC50 = 149.0 nM 6.83