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Assay Detail

CHEMBL991606

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Binding
Inhibition of Plasmodium falciparum plasmepsin-2
34
Total Activities
34
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

Plasmepsin II (CHEMBL4414)
Type SINGLE PROTEIN
Organism Plasmodium falciparum

Publication

Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin.
Hidaka K, Kimura T, Ruben AJ, Uemura T, Kamiya M, Kiso A, Okamoto T, Tsuchiya Y, Hayashi Y, Freire E, Kiso Y.
Bioorg Med Chem (2008) 16 : 10049 -10060
PubMed 18952439 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 7.58 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL231522 1 9.30
CHEMBL452345 1 8.40
CHEMBL503181 1 8.30
CHEMBL452725 1 8.22
CHEMBL449918 1 8.15
CHEMBL448977 1 8.05
CHEMBL509323 1 8.00
CHEMBL448365 1 8.00
CHEMBL448631 1 8.00
CHEMBL508668 1 8.00
CHEMBL509191 1 7.85
CHEMBL499762 1 7.72
CHEMBL504596 1 7.68
CHEMBL444759 1 7.68
CHEMBL466535 1 7.64
CHEMBL509473 1 7.64
CHEMBL501972 1 7.60
CHEMBL500010 1 7.60
CHEMBL507484 1 7.58
CHEMBL499956 1 7.55
CHEMBL442632 1 7.54
CHEMBL502445 1 7.52
CHEMBL508023 1 7.42
CHEMBL510300 1 7.41
CHEMBL453415 1 7.38
CHEMBL507473 1 7.26
CHEMBL508116 1 7.26
CHEMBL502985 1 6.95
CHEMBL448257 1 6.90
CHEMBL506609 1 6.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL231522 Ki = 0.5 nM 9.30
CHEMBL452345 Ki = 4.0 nM 8.40
CHEMBL503181 Ki = 5.0 nM 8.30
CHEMBL452725 Ki = 6.0 nM 8.22
CHEMBL449918 Ki = 7.0 nM 8.15
CHEMBL448977 Ki = 9.0 nM 8.05
CHEMBL509323 Ki = 10.0 nM 8.00
CHEMBL448365 Ki = 10.0 nM 8.00
CHEMBL448631 Ki = 10.0 nM 8.00
CHEMBL508668 Ki = 10.0 nM 8.00
CHEMBL509191 Ki = 14.0 nM 7.85
CHEMBL499762 Ki = 19.0 nM 7.72
CHEMBL504596 Ki = 21.0 nM 7.68
CHEMBL444759 Ki = 21.0 nM 7.68
CHEMBL509473 Ki = 23.0 nM 7.64
CHEMBL466535 Ki = 23.0 nM 7.64
CHEMBL500010 Ki = 25.0 nM 7.60
CHEMBL501972 Ki = 25.0 nM 7.60
CHEMBL507484 Ki = 26.0 nM 7.58
CHEMBL499956 Ki = 28.0 nM 7.55
CHEMBL442632 Ki = 29.0 nM 7.54
CHEMBL502445 Ki = 30.0 nM 7.52
CHEMBL508023 Ki = 38.0 nM 7.42
CHEMBL510300 Ki = 39.0 nM 7.41
CHEMBL453415 Ki = 42.0 nM 7.38
CHEMBL507473 Ki = 55.0 nM 7.26
CHEMBL508116 Ki = 55.0 nM 7.26
CHEMBL502985 Ki = 112.0 nM 6.95
CHEMBL448257 Ki = 126.0 nM 6.90
CHEMBL506609 Ki = 132.0 nM 6.88
CHEMBL509164 Ki = 145.0 nM 6.84
CHEMBL506575 Ki = 153.0 nM 6.82
CHEMBL453959 Ki = 479.0 nM 6.32
CHEMBL503590 Ki = 782.0 nM 6.11