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Assay Detail

CHEMBL2060799

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

Functional
Antimalarial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green fluorescence assay
22
Total Activities
22
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

Imidazolopiperazines: lead optimization of the second-generation antimalarial agents.
Nagle A, Wu T, Kuhen K, Gagaring K, Borboa R, Francek C, Chen Z, Plouffe D, Lin X, Caldwell C, Ek J, Skolnik S, Liu F, Wang J, Chang J, Li C, Liu B, Hollenbeck T, Tuntland T, Isbell J, Chuan T, Alper PB, Fischli C, Brun R, Lakshminarayana SB, Rottmann M, Diagana TT, Winzeler EA, Glynne R, Tully DC, Chatterjee AK.
J Med Chem (2012) 55 : 4244 -4273
PubMed 22524250 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 7.54 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2058838 1 8.40
CHEMBL2058827 1 8.40
CHEMBL2059066 1 8.30
CHEMBL2057225 1 8.30
CHEMBL2058833 GANAPLACIDE 2.0 1 8.22
CHEMBL2058834 1 8.22
CHEMBL2058839 1 8.15
CHEMBL2058837 1 8.05
CHEMBL2058844 1 7.89
CHEMBL1800836 1 7.64
CHEMBL2058828 1 7.62
CHEMBL2058832 1 7.62
CHEMBL1800137 1 7.60
CHEMBL2058829 1 7.54
CHEMBL2058843 1 7.19
CHEMBL2058836 1 7.12
CHEMBL2058835 1 6.96
CHEMBL2058842 1 6.87
CHEMBL2058840 1 6.75
CHEMBL2058831 1 6.70
CHEMBL2058830 1 6.33
CHEMBL2058841 1 5.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2058838 EC50 = 4.0 nM 8.40
CHEMBL2058827 EC50 = 4.0 nM 8.40
CHEMBL2059066 EC50 = 5.0 nM 8.30
CHEMBL2057225 EC50 = 5.0 nM 8.30
CHEMBL2058833 GANAPLACIDE EC50 = 6.0 nM 8.22
CHEMBL2058834 EC50 = 6.0 nM 8.22
CHEMBL2058839 EC50 = 7.0 nM 8.15
CHEMBL2058837 EC50 = 9.0 nM 8.05
CHEMBL2058844 EC50 = 13.0 nM 7.89
CHEMBL1800836 EC50 = 23.0 nM 7.64
CHEMBL2058828 EC50 = 24.0 nM 7.62
CHEMBL2058832 EC50 = 24.0 nM 7.62
CHEMBL1800137 EC50 = 25.0 nM 7.60
CHEMBL2058829 EC50 = 29.0 nM 7.54
CHEMBL2058843 EC50 = 65.0 nM 7.19
CHEMBL2058836 EC50 = 76.0 nM 7.12
CHEMBL2058835 EC50 = 111.0 nM 6.96
CHEMBL2058842 EC50 = 136.0 nM 6.87
CHEMBL2058840 EC50 = 178.0 nM 6.75
CHEMBL2058831 EC50 = 202.0 nM 6.70
CHEMBL2058830 EC50 = 470.0 nM 6.33
CHEMBL2058841 EC50 = 1168.0 nM 5.93