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Assay Detail

CHEMBL718158

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

Functional
Inhibition of anchorage independent growth of H-Ras transformed Rat-1 cells.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type Rat1
Confidence 1 — Organism
Curated By Expert

Target

Rat1 (CHEMBL614630)
Type CELL-LINE
Organism Rattus norvegicus

Publication

Discovery and structure-activity relationships of imidazole-containing tetrahydrobenzodiazepine inhibitors of farnesyltransferase.
Ding CZ, Batorsky R, Bhide R, Chao HJ, Cho Y, Chong S, Gullo-Brown J, Guo P, Kim SH, Lee F, Leftheris K, Miller A, Mitt T, Patel M, Penhallow BA, Ricca C, Rose WC, Schmidt R, Slusarchyk WA, Vite G, Yan N, Manne V, Hunt JT.
J Med Chem (1999) 42 : 5241 -5253
PubMed 10602709 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 5.97 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL359140 1 6.96
CHEMBL430778 1 6.80
CHEMBL355971 1 6.70
CHEMBL148870 1 6.70
CHEMBL358056 1 6.52
CHEMBL148487 1 6.47
CHEMBL358499 1 6.26
CHEMBL151497 1 6.16
CHEMBL348452 1 6.05
CHEMBL359092 1 6.00
CHEMBL149923 1 5.80
CHEMBL341861 1 5.80
CHEMBL147502 1 5.62
CHEMBL150737 1 5.62
CHEMBL151813 1 5.52
CHEMBL356905 1 5.40
CHEMBL358680 1 5.22
CHEMBL151633 1 4.96
CHEMBL151978 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL359140 EC50 = 110.0 nM 6.96
CHEMBL430778 EC50 = 160.0 nM 6.80
CHEMBL355971 EC50 = 200.0 nM 6.70
CHEMBL148870 EC50 = 200.0 nM 6.70
CHEMBL358056 EC50 = 300.0 nM 6.52
CHEMBL148487 EC50 = 340.0 nM 6.47
CHEMBL358499 EC50 = 550.0 nM 6.26
CHEMBL151497 EC50 = 700.0 nM 6.16
CHEMBL348452 EC50 = 900.0 nM 6.05
CHEMBL359092 EC50 = 1000.0 nM 6.00
CHEMBL149923 EC50 = 1600.0 nM 5.80
CHEMBL341861 EC50 = 1600.0 nM 5.80
CHEMBL147502 EC50 = 2400.0 nM 5.62
CHEMBL150737 EC50 = 2400.0 nM 5.62
CHEMBL151813 EC50 = 3000.0 nM 5.52
CHEMBL356905 EC50 = 4000.0 nM 5.40
CHEMBL358680 EC50 = 6000.0 nM 5.22
CHEMBL151633 EC50 = 11000.0 nM 4.96
CHEMBL151978 EC50 = 12000.0 nM 4.92