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Assay Detail

CHEMBL833084

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

Functional
Inhibition of cellular reversion in H-ras transformed Rat-1 cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type Rat-1
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2095197)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors.
Lombardo LJ, Camuso A, Clark J, Fager K, Gullo-Brown J, Hunt JT, Inigo I, Kan D, Koplowitz B, Lee F, McGlinchey K, Qian L, Ricca C, Rovnyak G, Traeger S, Tokarski J, Williams DK, Wu LI, Zhao Y, Manne V, Bhide RS.
Bioorg Med Chem Lett (2005) 15 : 1895 -1899
PubMed 15780629 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.43 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183773 1 8.10
CHEMBL179598 1 8.00
CHEMBL360330 1 7.89
CHEMBL183536 1 7.52
CHEMBL181102 1 7.30
CHEMBL182813 1 7.22
CHEMBL439846 1 7.16
CHEMBL183217 1 7.00
CHEMBL183590 1 6.65
CHEMBL180411 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183773 IC50 = 8.0 nM 8.10
CHEMBL179598 IC50 = 10.0 nM 8.00
CHEMBL360330 IC50 = 13.0 nM 7.89
CHEMBL183536 IC50 = 30.0 nM 7.52
CHEMBL181102 IC50 = 50.0 nM 7.30
CHEMBL182813 IC50 = 60.0 nM 7.22
CHEMBL439846 IC50 = 70.0 nM 7.16
CHEMBL183217 IC50 = 100.0 nM 7.00
CHEMBL183590 IC50 = 225.0 nM 6.65
CHEMBL180411 IC50 < 20.0 nM -