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Assay Detail

CHEMBL681414

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

Binding
Inhibition of bovine Farnesyltransferase in vitro.
21
Total Activities
21
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 (CHEMBL2095178)
Type PROTEIN COMPLEX
Organism Bos taurus

Publication

Imidazole-containing diarylether and diarylsulfone inhibitors of farnesyl-protein transferase.
Dinsmore CJ, Williams TM, O'Neill TJ, Liu D, Rands E, Culberson JC, Lobell RB, Koblan KS, Kohl NE, Gibbs JB, Oliff AI, Graham SL, Hartman GD.
Bioorg Med Chem Lett (1999) 9 : 3301 -3306
PubMed 10612589 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.70 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL113226 1 9.40
CHEMBL114086 1 9.35
CHEMBL112940 1 9.15
CHEMBL332495 1 9.10
CHEMBL109303 1 9.00
CHEMBL321241 1 8.59
CHEMBL112324 1 8.10
CHEMBL112956 1 8.10
CHEMBL112883 1 7.72
CHEMBL112079 1 7.38
CHEMBL325995 1 7.09
CHEMBL109418 1 7.03
CHEMBL326434 1 6.85
CHEMBL114025 1 6.63
CHEMBL321195 1 6.00
CHEMBL112490 1 5.89
CHEMBL110046 1 5.50
CHEMBL25734 1 -
CHEMBL109426 1 -
CHEMBL112190 1 -
CHEMBL113096 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL113226 IC50 = 0.4 nM 9.40
CHEMBL114086 IC50 = 0.45 nM 9.35
CHEMBL112940 IC50 = 0.7 nM 9.15
CHEMBL332495 IC50 = 0.8 nM 9.10
CHEMBL109303 IC50 = 1.0 nM 9.00
CHEMBL321241 IC50 = 2.6 nM 8.59
CHEMBL112324 IC50 = 8.0 nM 8.10
CHEMBL112956 IC50 = 8.0 nM 8.10
CHEMBL112883 IC50 = 19.0 nM 7.72
CHEMBL112079 IC50 = 42.0 nM 7.38
CHEMBL325995 IC50 = 81.0 nM 7.09
CHEMBL109418 IC50 = 93.0 nM 7.03
CHEMBL326434 IC50 = 140.0 nM 6.85
CHEMBL114025 IC50 = 232.0 nM 6.63
CHEMBL321195 IC50 = 1000.0 nM 6.00
CHEMBL112490 IC50 = 1300.0 nM 5.89
CHEMBL110046 IC50 = 3200.0 nM 5.50
CHEMBL25734 IC50 = 0.25 nM -
CHEMBL109426 IC50 > 100000.0 nM -
CHEMBL112190 IC50 > 100000.0 nM -
CHEMBL113096 IC50 > 100000.0 nM -