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Assay Detail

CHEMBL882865

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

Binding
Inhibition constant against plasmepsin-1 of Plasmodium falciparum, 10 min using 3 uM of DABCYL-Glu-Arg-Nle-Phe-Le u-Ser-Phe-Pro-EDANS as substrate
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Plasmepsin I (CHEMBL4687)
Type SINGLE PROTEIN
Organism Plasmodium falciparum

Publication

Synthesis of malarial plasmepsin inhibitors and prediction of binding modes by molecular dynamics simulations.
Ersmark K, Nervall M, Hamelink E, Janka LK, Clemente JC, Dunn BM, Blackman MJ, Samuelsson B, Aqvist J, Hallberg A.
J Med Chem (2005) 48 : 6090 -6106
PubMed 16162010 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 6.92 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL372618 1 8.22
CHEMBL435119 1 8.05
CHEMBL370422 1 7.96
CHEMBL370424 1 7.72
CHEMBL366393 1 7.57
CHEMBL196614 1 7.51
CHEMBL371522 1 7.42
CHEMBL196062 1 6.91
CHEMBL177718 1 6.79
CHEMBL371256 1 6.70
CHEMBL196165 1 6.58
CHEMBL382274 1 6.16
CHEMBL196696 1 5.96
CHEMBL194415 1 5.80
CHEMBL410049 1 5.74
CHEMBL197463 1 5.70
CHEMBL198356 1 -
CHEMBL198767 1 -
CHEMBL373047 1 -
CHEMBL197834 1 -
CHEMBL381027 1 -
CHEMBL195004 1 -
CHEMBL196265 1 -
CHEMBL426999 1 -
CHEMBL198165 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL372618 Ki = 6.0 nM 8.22
CHEMBL435119 Ki = 9.0 nM 8.05
CHEMBL370422 Ki = 11.0 nM 7.96
CHEMBL370424 Ki = 19.0 nM 7.72
CHEMBL366393 Ki = 27.0 nM 7.57
CHEMBL196614 Ki = 31.0 nM 7.51
CHEMBL371522 Ki = 38.0 nM 7.42
CHEMBL196062 Ki = 124.0 nM 6.91
CHEMBL177718 Ki = 163.0 nM 6.79
CHEMBL371256 Ki = 198.0 nM 6.70
CHEMBL196165 Ki = 261.0 nM 6.58
CHEMBL382274 Ki = 698.0 nM 6.16
CHEMBL196696 Ki = 1090.0 nM 5.96
CHEMBL194415 Ki = 1600.0 nM 5.80
CHEMBL410049 Ki = 1837.0 nM 5.74
CHEMBL197463 Ki = 2000.0 nM 5.70
CHEMBL198356 Ki > 3000.0 nM -
CHEMBL198767 Ki > 3000.0 nM -
CHEMBL373047 Ki > 3000.0 nM -
CHEMBL197834 Ki > 3000.0 nM -
CHEMBL381027 Ki > 3000.0 nM -
CHEMBL195004 Ki > 3000.0 nM -
CHEMBL196265 Ki > 3000.0 nM -
CHEMBL426999 Ki > 3000.0 nM -
CHEMBL198165 Ki > 3000.0 nM -