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Assay Detail

CHEMBL681672

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

Binding
In vitro inhibitory activity against Geranylgeranyl transferase in the geranylgeranylation of H-ras-CAIL protein
17
Total Activities
17
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 evaluation of hydroxyproline-derived isoprenyltransferase inhibitors.
O'Connell CE, Ackermann K, Rowell CA, Garcia AM, Lewis MD, Schwartz CE.
Bioorg Med Chem Lett (1999) 9 : 2095 -2100
PubMed 10450988 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.56 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL62387 1 9.00
CHEMBL305536 1 7.96
CHEMBL2092855 1 7.28
CHEMBL63366 1 7.05
CHEMBL65257 1 7.00
CHEMBL303414 1 6.96
CHEMBL67663 1 6.82
CHEMBL305584 1 6.77
CHEMBL307974 1 6.75
CHEMBL3349357 1 6.70
CHEMBL67174 1 6.68
CHEMBL432538 1 6.60
CHEMBL306018 1 6.24
CHEMBL303509 1 5.48
CHEMBL63663 1 5.10
CHEMBL2092731 1 4.96
CHEMBL3349310 1 4.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL62387 IC50 = 1.0 nM 9.00
CHEMBL305536 IC50 = 11.0 nM 7.96
CHEMBL2092855 IC50 = 53.0 nM 7.28
CHEMBL63366 IC50 = 89.0 nM 7.05
CHEMBL65257 IC50 = 100.0 nM 7.00
CHEMBL303414 IC50 = 110.0 nM 6.96
CHEMBL67663 IC50 = 150.0 nM 6.82
CHEMBL305584 IC50 = 170.0 nM 6.77
CHEMBL307974 IC50 = 180.0 nM 6.75
CHEMBL3349357 IC50 = 200.0 nM 6.70
CHEMBL67174 IC50 = 210.0 nM 6.68
CHEMBL432538 IC50 = 250.0 nM 6.60
CHEMBL306018 IC50 = 570.0 nM 6.24
CHEMBL303509 IC50 = 3300.0 nM 5.48
CHEMBL63663 IC50 = 8000.0 nM 5.10
CHEMBL2092731 IC50 = 11000.0 nM 4.96
CHEMBL3349310 IC50 = 67000.0 nM 4.17