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Assay Detail

CHEMBL750687

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

Functional
Inhibition of mammalian H-Ras processing in NIH 3T3 cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type NIH3T3
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2096912)
Type PROTEIN COMPLEX
Organism Mus musculus

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 10 6.08 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL138719 1 7.70
CHEMBL431828 1 6.70
CHEMBL54044 1 6.00
CHEMBL141513 1 5.30
CHEMBL349270 1 4.70
CHEMBL336266 1 -
CHEMBL344687 1 -
CHEMBL165159 1 -
CHEMBL433873 1 -
CHEMBL342449 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL138719 IC50 = 20.0 nM 7.70
CHEMBL431828 IC50 = 200.0 nM 6.70
CHEMBL54044 IC50 = 1000.0 nM 6.00
CHEMBL141513 IC50 = 5000.0 nM 5.30
CHEMBL349270 IC50 = 20000.0 nM 4.70
CHEMBL336266 IC50 > 100000.0 nM -
CHEMBL344687 IC50 > 100000.0 nM -
CHEMBL165159 IC50 > 100000.0 nM -
CHEMBL433873 IC50 > 100000.0 nM -
CHEMBL342449 IC50 > 100000.0 nM -