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Assay Detail

CHEMBL2161920

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

Binding
Inhibition of recombinant Plasmodium falciparum falcipain 2 incubated with compound for 10 mins before addition of Z-Phe-Arg-AMC substrate by fluorescence spectrophotometry
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Plasmodium falciparum
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Pyrido[1,2-a]pyrimidin-4-ones as antiplasmodial falcipain-2 inhibitors.
Mane UR, Li H, Huang J, Gupta RC, Nadkarni SS, Giridhar R, Naik PP, Yadav MR.
Bioorg Med Chem (2012) 20 : 6296 -6304
PubMed 23040894 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.11 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL374508 E-64 1 7.70
CHEMBL2158883 1 5.22
CHEMBL2158886 1 5.16
CHEMBL2158177 1 4.92
CHEMBL2158881 1 4.85
CHEMBL2158888 1 4.82
CHEMBL2158879 1 4.80
CHEMBL2158182 1 4.75
CHEMBL2158175 1 4.72
CHEMBL2158885 1 4.68
CHEMBL2158887 1 4.64
CHEMBL2158875 1 -
CHEMBL2158183 1 -
CHEMBL1424094 1 -
CHEMBL2158181 1 -
CHEMBL2158180 1 -
CHEMBL2158179 1 -
CHEMBL2158178 1 -
CHEMBL2158176 1 -
CHEMBL2158174 1 -
CHEMBL2158889 1 -
CHEMBL2158876 1 -
CHEMBL2158877 1 -
CHEMBL2158878 1 -
CHEMBL2158884 1 -
CHEMBL2158880 1 -
CHEMBL2158882 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL374508 E-64 IC50 = 20.0 nM 7.70
CHEMBL2158883 IC50 = 6000.0 nM 5.22
CHEMBL2158886 IC50 = 7000.0 nM 5.16
CHEMBL2158177 IC50 = 12000.0 nM 4.92
CHEMBL2158881 IC50 = 14000.0 nM 4.85
CHEMBL2158888 IC50 = 15000.0 nM 4.82
CHEMBL2158879 IC50 = 16000.0 nM 4.80
CHEMBL2158182 IC50 = 18000.0 nM 4.75
CHEMBL2158175 IC50 = 19000.0 nM 4.72
CHEMBL2158885 IC50 = 21000.0 nM 4.68
CHEMBL2158887 IC50 = 23000.0 nM 4.64
CHEMBL2158875 IC50 - -
CHEMBL2158183 IC50 - -
CHEMBL1424094 IC50 - -
CHEMBL2158181 IC50 - -
CHEMBL2158180 IC50 - -
CHEMBL2158179 IC50 - -
CHEMBL2158178 IC50 - -
CHEMBL2158176 IC50 - -
CHEMBL2158174 IC50 - -
CHEMBL2158889 IC50 - -
CHEMBL2158876 IC50 - -
CHEMBL2158877 IC50 - -
CHEMBL2158878 IC50 - -
CHEMBL2158884 IC50 - -
CHEMBL2158880 IC50 - -
CHEMBL2158882 IC50 - -