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Assay Detail

CHEMBL656832

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

Functional
Compound was tested for the inhibition of COS cells in monkey.
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cercopithecidae
Cell Type COS-1
Confidence 1 — Organism
Curated By Expert

Target

COS-1 (CHEMBL614563)
Type CELL-LINE
Organism Chlorocebus aethiops

Publication

Structure-activity relationship of 3-substituted N-(pyridinylacetyl)-4- (8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene )- piperidine inhibitors of farnesyl-protein transferase: design and synthesis of in vivo active antitumor compounds.
Njoroge FG, Vibulbhan B, Rane DF, Bishop WR, Petrin J, Patton R, Bryant MS, Chen KJ, Nomeir AA, Lin CC, Liu M, King I, Chen J, Lee S, Yaremko B, Dell J, Lipari P, Malkowski M, Li Z, Catino J, Doll RJ, Girijavallabhan V, Ganguly AK.
J Med Chem (1997) 40 : 4290 -4301
PubMed 9435898 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.84 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41934 1 6.22
CHEMBL336219 1 6.10
CHEMBL289404 1 6.00
CHEMBL337204 1 6.00
CHEMBL63804 1 6.00
CHEMBL334635 1 6.00
CHEMBL428979 1 6.00
CHEMBL342686 1 5.51
CHEMBL337193 1 5.47
CHEMBL336824 1 5.46
CHEMBL335685 1 5.43
CHEMBL344691 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41934 IC50 = 600.0 nM 6.22
CHEMBL336219 IC50 = 800.0 nM 6.10
CHEMBL289404 IC50 = 1000.0 nM 6.00
CHEMBL337204 IC50 = 1000.0 nM 6.00
CHEMBL63804 IC50 = 1000.0 nM 6.00
CHEMBL334635 IC50 = 1000.0 nM 6.00
CHEMBL428979 IC50 = 1000.0 nM 6.00
CHEMBL342686 IC50 = 3100.0 nM 5.51
CHEMBL337193 IC50 = 3400.0 nM 5.47
CHEMBL336824 IC50 = 3500.0 nM 5.46
CHEMBL335685 IC50 = 3700.0 nM 5.43
CHEMBL344691 IC50 > 10000.0 nM -