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Assay Detail

CHEMBL749433

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

Functional
Effective concentration against anchorage-independent growth of H-ras-transformed NIH3T3 cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type NIH3T3
Confidence 1 — Organism
Curated By Expert

Target

NIH3T3 (CHEMBL614822)
Type CELL-LINE
Organism Mus musculus

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
EC50 13 5.62 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL312598 1 6.72
CHEMBL75237 1 6.39
CHEMBL74363 1 6.30
CHEMBL73862 1 6.24
CHEMBL77419 1 6.00
CHEMBL306294 1 5.75
CHEMBL75677 1 5.70
CHEMBL310413 1 5.30
CHEMBL308724 1 5.30
CHEMBL309188 1 5.08
CHEMBL310863 1 4.82
CHEMBL311710 1 4.82
CHEMBL75804 1 4.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL312598 EC50 = 190.0 nM 6.72
CHEMBL75237 EC50 = 410.0 nM 6.39
CHEMBL74363 EC50 = 500.0 nM 6.30
CHEMBL73862 EC50 = 570.0 nM 6.24
CHEMBL77419 EC50 = 1000.0 nM 6.00
CHEMBL306294 EC50 = 1800.0 nM 5.75
CHEMBL75677 EC50 = 2000.0 nM 5.70
CHEMBL310413 EC50 = 5000.0 nM 5.30
CHEMBL308724 EC50 = 5000.0 nM 5.30
CHEMBL309188 EC50 = 8300.0 nM 5.08
CHEMBL310863 EC50 = 15000.0 nM 4.82
CHEMBL311710 EC50 = 15000.0 nM 4.82
CHEMBL75804 EC50 = 26000.0 nM 4.58