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Assay Detail

CHEMBL683643

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

Binding
Inhibition of bovine Geranylgeranyl transferase type I
10
Total Activities
10
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

N-Arylalkyl pseudopeptide inhibitors of farnesyltransferase.
deSolms SJ, Giuliani EA, Graham SL, Koblan KS, Kohl NE, Mosser SD, Oliff AI, Pompliano DL, Rands E, Scholz TH, Wiscount CM, Gibbs JB, Smith RL.
J Med Chem (1998) 41 : 2651 -2656
PubMed 9651171 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.31 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1790750 1 8.00
CHEMBL1790748 1 6.35
CHEMBL1790756 1 5.33
CHEMBL1790745 1 5.24
CHEMBL1790753 1 5.00
CHEMBL1790752 1 5.00
CHEMBL1790754 1 5.00
CHEMBL1790760 1 4.41
CHEMBL1790744 1 4.37
CHEMBL2052018 1 4.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1790750 IC50 = 10.0 nM 8.00
CHEMBL1790748 IC50 = 450.0 nM 6.35
CHEMBL1790756 IC50 = 4700.0 nM 5.33
CHEMBL1790745 IC50 = 5750.0 nM 5.24
CHEMBL1790753 IC50 = 10000.0 nM 5.00
CHEMBL1790752 IC50 = 10000.0 nM 5.00
CHEMBL1790754 IC50 = 10000.0 nM 5.00
CHEMBL1790760 IC50 = 39000.0 nM 4.41
CHEMBL1790744 IC50 = 43000.0 nM 4.37
CHEMBL2052018 IC50 = 45000.0 nM 4.35