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Assay Detail

CHEMBL833504

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Binding
Inhibition of bovine Geranylgeranyltransferase
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Geranylgeranyl transferase type I (CHEMBL2096987)
Type PROTEIN COMPLEX
Organism Bos taurus

Publication

Synthesis and activity of 1-aryl-1'-imidazolyl methyl ethers as non-thiol farnesyltransferase inhibitors.
Li Q, Wang GT, Li T, Gwaltney SL, Woods KW, Claiborne A, Wang X, Gu W, Cohen J, Stoll VS, Hutchins C, Frost D, Rosenberg SH, Sham HL.
Bioorg Med Chem Lett (2004) 14 : 5371 -5376
PubMed 15454229 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 5.88 7.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL187254 1 7.06
CHEMBL184044 1 6.66
CHEMBL187128 1 6.62
CHEMBL184916 1 6.38
CHEMBL186617 1 6.25
CHEMBL187807 1 6.14
CHEMBL188127 1 6.09
CHEMBL184330 1 6.06
CHEMBL181748 1 6.00
CHEMBL289228 TIPIFARNIB 3.0 1 5.96
CHEMBL362881 1 5.89
CHEMBL186641 1 5.89
CHEMBL363524 1 5.85
CHEMBL182816 1 5.75
CHEMBL181442 1 5.68
CHEMBL362338 1 5.66
CHEMBL362519 1 5.64
CHEMBL184568 1 5.64
CHEMBL184537 1 5.47
CHEMBL187037 1 5.26
CHEMBL186906 1 5.17
CHEMBL186927 1 5.09
CHEMBL182810 1 5.07
CHEMBL365289 1 -
CHEMBL185416 1 -
CHEMBL184425 1 -
CHEMBL183953 1 -
CHEMBL186715 1 -
CHEMBL185053 1 -
CHEMBL185058 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL187254 IC50 = 87.0 nM 7.06
CHEMBL184044 IC50 = 220.0 nM 6.66
CHEMBL187128 IC50 = 240.0 nM 6.62
CHEMBL184916 IC50 = 420.0 nM 6.38
CHEMBL186617 IC50 = 565.0 nM 6.25
CHEMBL187807 IC50 = 730.0 nM 6.14
CHEMBL188127 IC50 = 810.0 nM 6.09
CHEMBL184330 IC50 = 870.0 nM 6.06
CHEMBL181748 IC50 = 990.0 nM 6.00
CHEMBL289228 TIPIFARNIB IC50 = 1100.0 nM 5.96
CHEMBL362881 IC50 = 1300.0 nM 5.89
CHEMBL186641 IC50 = 1300.0 nM 5.89
CHEMBL363524 IC50 = 1400.0 nM 5.85
CHEMBL182816 IC50 = 1800.0 nM 5.75
CHEMBL181442 IC50 = 2100.0 nM 5.68
CHEMBL362338 IC50 = 2200.0 nM 5.66
CHEMBL184568 IC50 = 2300.0 nM 5.64
CHEMBL362519 IC50 = 2300.0 nM 5.64
CHEMBL184537 IC50 = 3400.0 nM 5.47
CHEMBL187037 IC50 = 5500.0 nM 5.26
CHEMBL186906 IC50 = 6800.0 nM 5.17
CHEMBL186927 IC50 = 8200.0 nM 5.09
CHEMBL182810 IC50 = 8600.0 nM 5.07
CHEMBL182171 IC50 > 10000.0 nM -
CHEMBL183313 IC50 > 10000.0 nM -
CHEMBL365427 IC50 > 10000.0 nM -
CHEMBL362750 IC50 > 10000.0 nM -
CHEMBL185058 IC50 > 10000.0 nM -
CHEMBL185053 IC50 > 10000.0 nM -
CHEMBL186715 IC50 > 10000.0 nM -
CHEMBL183953 IC50 > 10000.0 nM -
CHEMBL184425 IC50 > 10000.0 nM -
CHEMBL185416 IC50 > 10000.0 nM -
CHEMBL365289 IC50 > 10000.0 nM -