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Assay Detail

CHEMBL684169

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

Binding
In vitro inhibition of Geranylgeranyl transferase type I
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Development of highly potent inhibitors of Ras farnesyltransferase possessing cellular and in vivo activity.
Leftheris K, Kline T, Vite GD, Cho YH, Bhide RS, Patel DV, Patel MM, Schmidt RJ, Weller HN, Andahazy ML, Carboni JM, Gullo-Brown JL, Lee FY, Ricca C, Rose WC, Yan N, Barbacid M, Hunt JT, Meyers CA, Seizinger BR, Zahler R, Manne V.
J Med Chem (1996) 39 : 224 -236
PubMed 8568812 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.83 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL75804 1 8.89
CHEMBL74363 1 8.32
CHEMBL73862 1 7.85
CHEMBL311507 1 7.66
CHEMBL310413 1 6.96
CHEMBL75237 1 6.70
CHEMBL77419 1 6.40
CHEMBL75677 1 6.00
CHEMBL312598 1 5.85
CHEMBL308724 1 5.39
CHEMBL78855 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL75804 IC50 = 1.3 nM 8.89
CHEMBL74363 IC50 = 4.8 nM 8.32
CHEMBL73862 IC50 = 14.0 nM 7.85
CHEMBL311507 IC50 = 22.0 nM 7.66
CHEMBL310413 IC50 = 110.0 nM 6.96
CHEMBL75237 IC50 = 200.0 nM 6.70
CHEMBL77419 IC50 = 400.0 nM 6.40
CHEMBL75677 IC50 = 1000.0 nM 6.00
CHEMBL312598 IC50 = 1400.0 nM 5.85
CHEMBL308724 IC50 = 4100.0 nM 5.39
CHEMBL78855 IC50 = 8100.0 nM 5.09