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Assay Detail

CHEMBL685886

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

Binding
In vitro inhibition of geranylgeranyltransferase-1
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Geranylgeranyl transferase type I (CHEMBL2095164)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Aryl tetrahydropyridine inhibitors of farnesyltransferase: bioavailable analogues with improved cellular potency.
Gwaltney SL, O'Connor SJ, Nelson LT, Sullivan GM, Imade H, Wang W, Hasvold L, Li Q, Cohen J, Gu WZ, Tahir SK, Bauch J, Marsh K, Ng SC, Frost DJ, Zhang H, Muchmore S, Jakob CG, Stoll V, Hutchins C, Rosenberg SH, Sham HL.
Bioorg Med Chem Lett (2003) 13 : 1363 -1366
PubMed 12657283 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.73 6.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282161 1 6.27
CHEMBL280847 1 6.22
CHEMBL27677 1 5.89
CHEMBL29633 1 5.89
CHEMBL29503 1 5.85
CHEMBL284637 1 5.82
CHEMBL29980 1 5.80
CHEMBL282166 1 5.57
CHEMBL430073 1 5.40
CHEMBL30059 1 5.35
CHEMBL29499 1 5.00
CHEMBL29619 1 -
CHEMBL30118 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282161 IC50 = 540.0 nM 6.27
CHEMBL280847 IC50 = 600.0 nM 6.22
CHEMBL27677 IC50 = 1300.0 nM 5.89
CHEMBL29633 IC50 = 1300.0 nM 5.89
CHEMBL29503 IC50 = 1400.0 nM 5.85
CHEMBL284637 IC50 = 1500.0 nM 5.82
CHEMBL29980 IC50 = 1600.0 nM 5.80
CHEMBL282166 IC50 = 2700.0 nM 5.57
CHEMBL430073 IC50 = 4000.0 nM 5.40
CHEMBL30059 IC50 = 4500.0 nM 5.35
CHEMBL29499 IC50 = 10000.0 nM 5.00
CHEMBL29619 IC50 > 10000.0 nM -
CHEMBL30118 IC50 = 161000.0 nM -