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Assay Detail

CHEMBL2014781

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

Functional
Antiplasmodial activity against Plasmodium falciparum Dd2 infected in human renal proximal tubule cells after 72 hrs by SYBR green assay
41
Total Activities
41
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

Optimization of Potent Inhibitors of P. falciparum Dihydroorotate Dehydrogenase for the Treatment of Malaria.
Skerlj RT, Bastos CM, Booker ML, Kramer ML, Barker RH, Celatka CA, O'Shea TJ, Munoz B, Sidhu AB, Cortese JF, Wittlin S, Papastogiannidis P, Angulo-Barturen I, Jimenez-Diaz MB, Sybertz E.
ACS Med Chem Lett (2011) 2 : 708 -713
PubMed 24900364 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 7.10 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2012961 1 8.40
CHEMBL2012955 1 8.22
CHEMBL2012953 1 8.22
CHEMBL2012957 1 8.15
CHEMBL2012966 1 8.10
CHEMBL1234899 1 8.05
CHEMBL2012958 1 8.00
CHEMBL2012965 1 7.92
CHEMBL2012962 1 7.89
CHEMBL2012960 1 7.77
CHEMBL2012963 1 7.75
CHEMBL2012943 1 7.66
CHEMBL2012951 1 7.58
CHEMBL2012948 1 7.55
CHEMBL2012947 1 7.28
CHEMBL2012964 1 7.22
CHEMBL2012945 1 7.13
CHEMBL2012824 1 7.05
CHEMBL2012949 1 7.02
CHEMBL2012956 1 6.99
CHEMBL2012950 1 6.96
CHEMBL2012829 1 6.96
CHEMBL2012952 1 6.95
CHEMBL2012954 1 6.95
CHEMBL2012944 1 6.89
CHEMBL2012821 1 6.82
CHEMBL2012959 1 6.80
CHEMBL2012830 1 6.75
CHEMBL2012946 1 6.54
CHEMBL2012820 1 6.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2012961 IC50 = 4.0 nM 8.40
CHEMBL2012955 IC50 = 6.0 nM 8.22
CHEMBL2012953 IC50 = 6.0 nM 8.22
CHEMBL2012957 IC50 = 7.0 nM 8.15
CHEMBL2012966 IC50 = 8.0 nM 8.10
CHEMBL1234899 IC50 = 9.0 nM 8.05
CHEMBL2012958 IC50 = 10.0 nM 8.00
CHEMBL2012965 IC50 = 12.0 nM 7.92
CHEMBL2012962 IC50 = 13.0 nM 7.89
CHEMBL2012960 IC50 = 17.0 nM 7.77
CHEMBL2012963 IC50 = 18.0 nM 7.75
CHEMBL2012943 IC50 = 22.0 nM 7.66
CHEMBL2012951 IC50 = 26.0 nM 7.58
CHEMBL2012948 IC50 = 28.0 nM 7.55
CHEMBL2012947 IC50 = 53.0 nM 7.28
CHEMBL2012964 IC50 = 60.0 nM 7.22
CHEMBL2012945 IC50 = 74.0 nM 7.13
CHEMBL2012824 IC50 = 90.0 nM 7.05
CHEMBL2012949 IC50 = 96.0 nM 7.02
CHEMBL2012956 IC50 = 102.0 nM 6.99
CHEMBL2012950 IC50 = 109.0 nM 6.96
CHEMBL2012829 IC50 = 110.0 nM 6.96
CHEMBL2012952 IC50 = 113.0 nM 6.95
CHEMBL2012954 IC50 = 113.0 nM 6.95
CHEMBL2012944 IC50 = 130.0 nM 6.89
CHEMBL2012821 IC50 = 150.0 nM 6.82
CHEMBL2012959 IC50 = 159.0 nM 6.80
CHEMBL2012830 IC50 = 180.0 nM 6.75
CHEMBL2012946 IC50 = 290.0 nM 6.54
CHEMBL2012820 IC50 = 420.0 nM 6.38
CHEMBL2012825 IC50 = 440.0 nM 6.36
CHEMBL2012831 IC50 = 630.0 nM 6.20
CHEMBL2012823 IC50 = 810.0 nM 6.09
CHEMBL2012822 IC50 = 1100.0 nM 5.96
CHEMBL2012941 IC50 = 1710.0 nM 5.77
CHEMBL2012827 IC50 = 5500.0 nM 5.26
CHEMBL2012826 IC50 = 7300.0 nM 5.14
CHEMBL2012819 IC50 > 30000.0 nM -
CHEMBL2012942 IC50 > 1000.0 nM -
CHEMBL2012940 IC50 > 5000.0 nM -
CHEMBL2012828 IC50 > 40000.0 nM -