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Assay Detail

CHEMBL896246

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

Binding
Inhibition of protein farnesyltransferase
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2094108)
Type PROTEIN COMPLEX
Organism Homo sapiens

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 19 7.97 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL428712 1 8.77
CHEMBL395222 1 8.59
CHEMBL365742 1 8.52
CHEMBL232104 1 8.49
CHEMBL191843 1 8.47
CHEMBL192244 1 8.42
CHEMBL234757 1 8.32
CHEMBL192898 1 8.30
CHEMBL232523 1 8.26
CHEMBL234151 1 8.19
CHEMBL231662 1 8.15
CHEMBL233742 1 8.12
CHEMBL394086 1 8.11
CHEMBL365549 1 8.00
CHEMBL394407 1 7.80
CHEMBL392237 1 7.60
CHEMBL234161 1 6.98
CHEMBL371408 1 6.36
CHEMBL193161 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL428712 IC50 = 1.7 nM 8.77
CHEMBL395222 IC50 = 2.6 nM 8.59
CHEMBL365742 IC50 = 3.0 nM 8.52
CHEMBL232104 IC50 = 3.2 nM 8.49
CHEMBL191843 IC50 = 3.4 nM 8.47
CHEMBL192244 IC50 = 3.8 nM 8.42
CHEMBL234757 IC50 = 4.8 nM 8.32
CHEMBL192898 IC50 = 5.0 nM 8.30
CHEMBL232523 IC50 = 5.5 nM 8.26
CHEMBL234151 IC50 = 6.5 nM 8.19
CHEMBL231662 IC50 = 7.0 nM 8.15
CHEMBL233742 IC50 = 7.5 nM 8.12
CHEMBL394086 IC50 = 7.8 nM 8.11
CHEMBL365549 IC50 = 10.0 nM 8.00
CHEMBL394407 IC50 = 16.0 nM 7.80
CHEMBL392237 IC50 = 25.0 nM 7.60
CHEMBL234161 IC50 = 105.0 nM 6.98
CHEMBL371408 IC50 = 440.0 nM 6.36
CHEMBL193161 IC50 = 1000.0 nM 6.00