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Assay Detail

CHEMBL3224129

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

Binding
Inhibition of human GGTase1 in human Burkitt lymphoma (Daudi) cell supernatant using [3H]geranylgeranyl
12
Total Activities
12
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

Prenyltransferase Inhibitors: Treating Human Ailments from Cancer to Parasitic Infections.
Ochocki JD, Distefano MD.
Medchemcomm (2013) 4 : 476 -492
PubMed 25530833 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.49 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282103 1 8.30
CHEMBL3218390 GGTI-2418 1.0 1 8.02
CHEMBL3218391 1 7.68
CHEMBL3218393 1 7.30
CHEMBL54044 1 7.30
CHEMBL3218389 1 6.33
CHEMBL279433 L-778123 FREE BASE 1.0 1 -
CHEMBL3218388 1 -
CHEMBL289228 TIPIFARNIB 3.0 1 -
CHEMBL2171679 1 -
CHEMBL1738728 1 -
CHEMBL298734 LONAFARNIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282103 IC50 = 5.0 nM 8.30
CHEMBL3218390 GGTI-2418 IC50 = 9.5 nM 8.02
CHEMBL3218391 IC50 = 21.0 nM 7.68
CHEMBL3218393 IC50 = 50.0 nM 7.30
CHEMBL54044 IC50 = 50.0 nM 7.30
CHEMBL3218389 IC50 = 466.0 nM 6.33
CHEMBL279433 L-778123 FREE BASE IC50 = 98.0 nM -
CHEMBL3218388 IC50 > 1000.0 nM -
CHEMBL289228 TIPIFARNIB IC50 > 50000.0 nM -
CHEMBL2171679 IC50 > 99500.0 nM -
CHEMBL1738728 IC50 > 99500.0 nM -
CHEMBL298734 LONAFARNIB IC50 > 50000.0 nM -