Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2176058

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

Binding
Inhibition of eIF4FA in human MDA-MB-231 cells transfected with c-myc- 5'-UTR-luciferase construct assessed as reduction in translation initiation incubated for 24 hrs by differential translation assay
38
Total Activities
38
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MDA-MB-231
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Eukaryotic initiation factor 4A-I (CHEMBL2052028)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthetic silvestrol analogues as potent and selective protein synthesis inhibitors.
Liu T, Nair SJ, Lescarbeau A, Belani J, Peluso S, Conley J, Tillotson B, O'Hearn P, Smith S, Slocum K, West K, Helble J, Douglas M, Bahadoor A, Ali J, McGovern K, Fritz C, Palombella VJ, Wylie A, Castro AC, Tremblay MR.
J Med Chem (2012) 55 : 8859 -8878
PubMed 23025805 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 37 8.23 9.70
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2170713 1 9.70
CHEMBL2170563 1 9.22
CHEMBL555196 SILVESTROL 1 9.10
CHEMBL2170562 1 9.10
CHEMBL2170556 1 9.05
CHEMBL2170714 1 9.00
CHEMBL2170555 1 9.00
CHEMBL2170703 1 8.92
CHEMBL2170559 1 8.70
CHEMBL2170725 1 8.52
CHEMBL2170718 1 8.52
CHEMBL2170722 1 8.52
CHEMBL2170560 1 8.52
CHEMBL2170561 1 8.52
CHEMBL2170557 1 8.40
CHEMBL2170558 1 8.30
CHEMBL2170724 1 8.00
CHEMBL394528 AGLAFOLIN 1 8.00
CHEMBL2170709 1 7.96
CHEMBL2169895 1 7.54
CHEMBL2170716 1 7.46
CHEMBL2170719 1 7.46
CHEMBL2170553 1 7.46
CHEMBL2170708 1 7.40
CHEMBL2170723 1 7.30
CHEMBL2170704 1 7.10
CHEMBL2170717 1 6.92
CHEMBL2170720 1 6.77
CHEMBL2170552 1 -
CHEMBL2170712 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2170713 EC50 = 0.2 nM 9.70
CHEMBL2170563 EC50 = 0.6 nM 9.22
CHEMBL2170562 EC50 = 0.8 nM 9.10
CHEMBL555196 SILVESTROL EC50 = 0.8 nM 9.10
CHEMBL2170556 EC50 = 0.9 nM 9.05
CHEMBL2170714 EC50 = 1.0 nM 9.00
CHEMBL2170555 EC50 = 1.0 nM 9.00
CHEMBL2170703 EC50 = 1.2 nM 8.92
CHEMBL2170559 EC50 = 2.0 nM 8.70
CHEMBL2170722 EC50 = 3.0 nM 8.52
CHEMBL2170561 EC50 = 3.0 nM 8.52
CHEMBL2170560 EC50 = 3.0 nM 8.52
CHEMBL2170718 EC50 = 3.0 nM 8.52
CHEMBL2170725 EC50 = 3.0 nM 8.52
CHEMBL2170557 EC50 = 4.0 nM 8.40
CHEMBL2170558 EC50 = 5.0 nM 8.30
CHEMBL2170724 EC50 = 10.0 nM 8.00
CHEMBL394528 AGLAFOLIN EC50 = 10.0 nM 8.00
CHEMBL2170709 EC50 = 11.0 nM 7.96
CHEMBL2169895 EC50 = 29.0 nM 7.54
CHEMBL2170719 EC50 = 35.0 nM 7.46
CHEMBL2170553 EC50 = 35.0 nM 7.46
CHEMBL2170716 EC50 = 35.0 nM 7.46
CHEMBL2170708 EC50 = 40.0 nM 7.40
CHEMBL2170723 EC50 = 50.0 nM 7.30
CHEMBL2170704 EC50 = 80.0 nM 7.10
CHEMBL2170717 EC50 = 120.0 nM 6.92
CHEMBL2170720 EC50 = 170.0 nM 6.77
CHEMBL2170554 EC50 > 5000.0 nM -
CHEMBL2170711 EC50 > 5000.0 nM -
CHEMBL2170707 EC50 > 5000.0 nM -
CHEMBL2170705 EC50 > 5000.0 nM -
CHEMBL2170710 EC50 > 2000.0 nM -
CHEMBL2170706 EC50 > 2000.0 nM -
CHEMBL2170721 EC50 > 2000.0 nM -
CHEMBL2170715 EC50 > 200.0 nM -
CHEMBL2170712 EC50 > 1000.0 nM -
CHEMBL2170552 Inhibition - % -