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Assay Detail

CHEMBL828450

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

Binding
Inhibition of biotinylated lamin B peptide farnesylation by rat farnesyltransferase
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2095197)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Protein farnesyltransferase inhibitors exhibit potent antimalarial activity.
Nallan L, Bauer KD, Bendale P, Rivas K, Yokoyama K, Hornéy CP, Pendyala PR, Floyd D, Lombardo LJ, Williams DK, Hamilton A, Sebti S, Windsor WT, Weber PC, Buckner FS, Chakrabarti D, Gelb MH, Van Voorhis WC.
J Med Chem (2005) 48 : 3704 -3713
PubMed 15916422 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 8.20 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL181102 1 9.15
CHEMBL193034 1 9.10
CHEMBL182888 1 8.92
CHEMBL183536 1 8.92
CHEMBL194447 1 8.82
CHEMBL373337 1 8.74
CHEMBL365742 1 8.52
CHEMBL370298 1 8.49
CHEMBL191843 1 8.47
CHEMBL192244 1 8.42
CHEMBL192898 1 8.30
CHEMBL195168 1 8.22
CHEMBL195597 1 8.12
CHEMBL365549 1 8.00
CHEMBL372017 1 6.80
CHEMBL371408 1 6.36
CHEMBL193161 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL181102 IC50 = 0.7 nM 9.15
CHEMBL193034 IC50 = 0.8 nM 9.10
CHEMBL182888 IC50 = 1.2 nM 8.92
CHEMBL183536 IC50 = 1.2 nM 8.92
CHEMBL194447 IC50 = 1.5 nM 8.82
CHEMBL373337 IC50 = 1.8 nM 8.74
CHEMBL365742 IC50 = 3.0 nM 8.52
CHEMBL370298 IC50 = 3.2 nM 8.49
CHEMBL191843 IC50 = 3.4 nM 8.47
CHEMBL192244 IC50 = 3.8 nM 8.42
CHEMBL192898 IC50 = 5.0 nM 8.30
CHEMBL195168 IC50 = 6.0 nM 8.22
CHEMBL195597 IC50 = 7.6 nM 8.12
CHEMBL365549 IC50 = 10.0 nM 8.00
CHEMBL372017 IC50 = 160.0 nM 6.80
CHEMBL371408 IC50 = 440.0 nM 6.36
CHEMBL193161 IC50 = 1000.0 nM 6.00