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Assay Detail

CHEMBL682233

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Binding
Inhibition of mammalian Farnesyltransferase
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2094108)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity.
Ohkanda J, Lockman JW, Yokoyama K, Gelb MH, Croft SL, Kendrick H, Harrell MI, Feagin JE, Blaskovich MA, Sebti SM, Hamilton AD.
Bioorg Med Chem Lett (2001) 11 : 761 -764
PubMed 11277514 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.65 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54044 1 9.30
CHEMBL431828 1 9.00
CHEMBL141513 1 8.14
CHEMBL434997 1 7.39
CHEMBL349270 1 6.66
CHEMBL344687 1 6.58
CHEMBL433873 1 6.42
CHEMBL140126 1 6.19
CHEMBL343393 1 6.11
CHEMBL165159 1 5.52
CHEMBL336266 1 5.51
CHEMBL342449 1 5.22
CHEMBL138719 1 4.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54044 IC50 = 0.5 nM 9.30
CHEMBL431828 IC50 = 1.0 nM 9.00
CHEMBL141513 IC50 = 7.2 nM 8.14
CHEMBL434997 IC50 = 41.0 nM 7.39
CHEMBL349270 IC50 = 220.0 nM 6.66
CHEMBL344687 IC50 = 260.0 nM 6.58
CHEMBL433873 IC50 = 380.0 nM 6.42
CHEMBL140126 IC50 = 640.0 nM 6.19
CHEMBL343393 IC50 = 780.0 nM 6.11
CHEMBL165159 IC50 = 3000.0 nM 5.52
CHEMBL336266 IC50 = 3100.0 nM 5.51
CHEMBL342449 IC50 = 6000.0 nM 5.22
CHEMBL138719 IC50 = 34000.0 nM 4.47