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Assay Detail

CHEMBL3865059

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of recombinant Plasmodium falciparum PKG assessed as decrease in depletion of ATP by Kinase glo luciferase assay
4
Total Activities
4
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

5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents.
Huang W, Hulverson MA, Zhang Z, Choi R, Hart KJ, Kennedy M, Vidadala RSR, Maly DJ, Van Voorhis WC, Lindner SE, Fan E, Ojo KK.
Bioorg Med Chem Lett (2016) 26 : 5487 -5491
PubMed 27780638 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.63 5.65

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3109011 1 5.65
CHEMBL3770802 1 5.63
CHEMBL3108913 1 5.62
CHEMBL3108997 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3109011 IC50 = 2220.0 nM 5.65
CHEMBL3770802 IC50 = 2360.0 nM 5.63
CHEMBL3108913 IC50 = 2370.0 nM 5.62
CHEMBL3108997 IC50 = 2520.0 nM 5.60