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Assay Detail

CHEMBL896243

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

Binding
Inhibition of Plasmodium falciparum protein farnesyltransferase by scintillation proximity assay
31
Total Activities
31
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

Second generation tetrahydroquinoline-based protein farnesyltransferase inhibitors as antimalarials.
Bendale P, Olepu S, Suryadevara PK, Bulbule V, Rivas K, Nallan L, Smart B, Yokoyama K, Ankala S, Pendyala PR, Floyd D, Lombardo LJ, Williams DK, Buckner FS, Chakrabarti D, Verlinde CL, Van Voorhis WC, Gelb MH.
J Med Chem (2007) 50 : 4585 -4605
PubMed 17722901 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 8.62 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL539862 1 9.54
CHEMBL183499 1 9.40
CHEMBL395222 1 9.30
CHEMBL232523 1 9.30
CHEMBL232104 1 9.24
CHEMBL394086 1 9.22
CHEMBL399827 1 9.22
CHEMBL393970 1 9.19
CHEMBL265603 1 9.12
CHEMBL429443 1 9.10
CHEMBL233743 1 9.05
CHEMBL233921 1 9.05
CHEMBL394085 1 8.92
CHEMBL392237 1 8.85
CHEMBL232122 1 8.70
CHEMBL233941 1 8.62
CHEMBL558175 1 8.57
CHEMBL234151 1 8.52
CHEMBL234561 1 8.30
CHEMBL394407 1 8.15
CHEMBL192898 1 8.10
CHEMBL233288 1 7.38
CHEMBL232877 1 6.10
CHEMBL234359 1 6.05
CHEMBL438670 1 -
CHEMBL233496 1 -
CHEMBL233712 1 -
CHEMBL233919 1 -
CHEMBL233819 1 -
CHEMBL233920 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL539862 IC50 = 0.29 nM 9.54
CHEMBL183499 IC50 = 0.4 nM 9.40
CHEMBL395222 IC50 = 0.5 nM 9.30
CHEMBL232523 IC50 = 0.5 nM 9.30
CHEMBL232104 IC50 = 0.58 nM 9.24
CHEMBL394086 IC50 = 0.6 nM 9.22
CHEMBL399827 IC50 = 0.6 nM 9.22
CHEMBL393970 IC50 = 0.65 nM 9.19
CHEMBL265603 IC50 = 0.75 nM 9.12
CHEMBL429443 IC50 = 0.8 nM 9.10
CHEMBL233743 IC50 = 0.9 nM 9.05
CHEMBL233921 IC50 = 0.9 nM 9.05
CHEMBL394085 IC50 = 1.2 nM 8.92
CHEMBL392237 IC50 = 1.4 nM 8.85
CHEMBL232122 IC50 = 2.0 nM 8.70
CHEMBL233941 IC50 = 2.4 nM 8.62
CHEMBL558175 IC50 = 2.7 nM 8.57
CHEMBL234151 IC50 = 3.0 nM 8.52
CHEMBL234561 IC50 = 5.0 nM 8.30
CHEMBL394407 IC50 = 7.0 nM 8.15
CHEMBL192898 IC50 = 8.0 nM 8.10
CHEMBL233288 IC50 = 42.0 nM 7.38
CHEMBL232877 IC50 = 800.0 nM 6.10
CHEMBL234359 IC50 = 900.0 nM 6.05
CHEMBL438670 IC50 > 50.0 nM -
CHEMBL233496 IC50 > 50.0 nM -
CHEMBL233712 IC50 > 50.0 nM -
CHEMBL233919 IC50 = - nM -
CHEMBL233819 IC50 = - nM -
CHEMBL233920 IC50 = - nM -
CHEMBL234129 IC50 = - nM -