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Assay Detail

CHEMBL682098

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Binding
Inhibitory activity against human purified recombinant farnesyltransferase (hFT)
ChEMBL ↗
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2094108) ↗
Type PROTEIN COMPLEX
Organism Homo sapiens

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
IC50 43 5.35 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL151497 — — 1 6.50
CHEMBL356840 — — 1 6.47
CHEMBL358680 — — 1 6.34
CHEMBL151094 — — 1 6.32
CHEMBL151851 — — 1 6.23
CHEMBL147502 — — 1 6.22
CHEMBL347961 — — 1 6.16
CHEMBL149923 — — 1 6.14
CHEMBL357974 — — 1 6.08
CHEMBL424509 — — 1 5.96
CHEMBL356469 — — 1 5.92
CHEMBL148816 — — 1 5.89
CHEMBL348426 — — 1 5.89
CHEMBL151813 — — 1 5.55
CHEMBL151902 — — 1 5.50
CHEMBL348672 — — 1 5.00
CHEMBL355971 — — 1 4.81
CHEMBL148487 — — 1 4.74
CHEMBL342079 — — 1 4.68
CHEMBL430778 — — 1 4.62
CHEMBL151882 — — 1 4.57
CHEMBL359140 — — 1 4.55
CHEMBL358056 — — 1 4.54
CHEMBL347100 — — 1 4.47
CHEMBL356905 — — 1 4.45
CHEMBL358499 — — 1 4.24
CHEMBL348452 — — 1 4.04
CHEMBL341861 — — 1 4.02
CHEMBL151362 — — 1 -
CHEMBL149160 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL151497 — IC50 = 320.0 nM 6.50
CHEMBL356840 — IC50 = 340.0 nM 6.47
CHEMBL358680 — IC50 = 460.0 nM 6.34
CHEMBL151094 — IC50 = 480.0 nM 6.32
CHEMBL151851 — IC50 = 590.0 nM 6.23
CHEMBL147502 — IC50 = 600.0 nM 6.22
CHEMBL347961 — IC50 = 700.0 nM 6.16
CHEMBL149923 — IC50 = 720.0 nM 6.14
CHEMBL357974 — IC50 = 840.0 nM 6.08
CHEMBL424509 — IC50 = 1100.0 nM 5.96
CHEMBL356469 — IC50 = 1200.0 nM 5.92
CHEMBL348426 — IC50 = 1300.0 nM 5.89
CHEMBL148816 — IC50 = 1300.0 nM 5.89
CHEMBL151813 — IC50 = 2800.0 nM 5.55
CHEMBL151902 — IC50 = 3200.0 nM 5.50
CHEMBL348672 — IC50 = 10000.0 nM 5.00
CHEMBL355971 — IC50 = 15400.0 nM 4.81
CHEMBL148487 — IC50 = 18100.0 nM 4.74
CHEMBL342079 — IC50 = 21000.0 nM 4.68
CHEMBL430778 — IC50 = 24000.0 nM 4.62
CHEMBL151882 — IC50 = 27000.0 nM 4.57
CHEMBL359140 — IC50 = 28000.0 nM 4.55
CHEMBL358056 — IC50 = 28500.0 nM 4.54
CHEMBL347100 — IC50 = 34000.0 nM 4.47
CHEMBL356905 — IC50 = 35500.0 nM 4.45
CHEMBL358499 — IC50 = 58000.0 nM 4.24
CHEMBL348452 — IC50 = 91000.0 nM 4.04
CHEMBL341861 — IC50 = 95000.0 nM 4.02
CHEMBL356257 — IC50 = 2968000.0 nM -
CHEMBL348262 — IC50 = 186000.0 nM -
CHEMBL148870 — IC50 = 124000.0 nM -
CHEMBL359092 — IC50 = 145000.0 nM -
CHEMBL348237 — IC50 = 177000.0 nM -
CHEMBL149103 — IC50 = 168000.0 nM -
CHEMBL151633 — IC50 = 249000.0 nM -
CHEMBL148811 — IC50 = 1423000.0 nM -
CHEMBL151978 — IC50 = 350000.0 nM -
CHEMBL357714 — IC50 = 702000.0 nM -
CHEMBL121010 — IC50 = 228000.0 nM -
CHEMBL150690 — IC50 = 540000.0 nM -
CHEMBL150737 — IC50 = 1000000.0 nM -
CHEMBL149160 — IC50 = 205000.0 nM -
CHEMBL151362 — IC50 = 426000.0 nM -