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Assay Detail

CHEMBL686124

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

Binding
Inhibition of partially purified Geranylgeranyl transferase type I (GGTase-I) from human Burkitt lymphoma (Daudi) cells
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and synthesis of potent nonpeptidic farnesyltransferase inhibitors based on a terphenyl scaffold.
Ohkanda J, Lockman JW, Kothare MA, Qian Y, Blaskovich MA, Sebti SM, Hamilton AD.
J Med Chem (2002) 45 : 177 -188
PubMed 11754590 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 5.11 6.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55497 1 6.19
CHEMBL58822 1 5.62
CHEMBL55484 1 5.41
CHEMBL55639 1 5.36
CHEMBL55427 1 5.36
CHEMBL55893 1 5.30
CHEMBL299245 1 5.23
CHEMBL301433 1 5.16
CHEMBL292361 1 5.16
CHEMBL301667 1 4.46
CHEMBL417600 1 4.05
CHEMBL53732 1 4.00
CHEMBL55676 1 -
CHEMBL299489 1 -
CHEMBL292164 1 -
CHEMBL301842 1 -
CHEMBL55306 1 -
CHEMBL54366 1 -
CHEMBL56949 1 -
CHEMBL266005 1 -
CHEMBL293110 1 -
CHEMBL53999 1 -
CHEMBL55514 1 -
CHEMBL55527 1 -
CHEMBL298613 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55497 IC50 = 640.0 nM 6.19
CHEMBL58822 IC50 = 2400.0 nM 5.62
CHEMBL55484 IC50 = 3900.0 nM 5.41
CHEMBL55639 IC50 = 4400.0 nM 5.36
CHEMBL55427 IC50 = 4400.0 nM 5.36
CHEMBL55893 IC50 = 5000.0 nM 5.30
CHEMBL299245 IC50 = 5900.0 nM 5.23
CHEMBL301433 IC50 = 7000.0 nM 5.16
CHEMBL292361 IC50 = 6900.0 nM 5.16
CHEMBL301667 IC50 = 35000.0 nM 4.46
CHEMBL417600 IC50 = 90000.0 nM 4.05
CHEMBL53732 IC50 = 100000.0 nM 4.00
CHEMBL55676 IC50 > 10000.0 nM -
CHEMBL299489 IC50 > 10000.0 nM -
CHEMBL292164 IC50 > 100000.0 nM -
CHEMBL301842 IC50 > 10000.0 nM -
CHEMBL55306 IC50 > 10000.0 nM -
CHEMBL54366 IC50 > 10000.0 nM -
CHEMBL56949 IC50 > 10000.0 nM -
CHEMBL266005 IC50 > 10000.0 nM -
CHEMBL293110 IC50 > 10000.0 nM -
CHEMBL53999 IC50 > 10000.0 nM -
CHEMBL55514 IC50 > 10000.0 nM -
CHEMBL55527 IC50 > 100000.0 nM -
CHEMBL298613 IC50 > 10000.0 nM -