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Assay Detail

CHEMBL3381045

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

Functional
Induction of Her2 degradation in human BT474 cells assessed as inhibition of signal by immunocytochemistry
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type BT-474
Confidence 1 — Organism
Curated By Autocuration

Target

BT-474 (CHEMBL614529)
Type CELL-LINE
Organism Homo sapiens

Publication

Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.
Casale E, Amboldi N, Brasca MG, Caronni D, Colombo N, Dalvit C, Felder ER, Fogliatto G, Galvani A, Isacchi A, Polucci P, Riceputi L, Sola F, Visco C, Zuccotto F, Casuscelli F.
Bioorg Med Chem (2014) 22 : 4135 -4150
PubMed 24980703 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.79 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL252164 LUMINESPIB 2.0 1 8.00
CHEMBL3310151 1 5.69
CHEMBL3309997 1 5.59
CHEMBL3309998 1 5.54
CHEMBL3309990 1 5.17
CHEMBL3309995 1 4.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL252164 LUMINESPIB IC50 = 10.0 nM 8.00
CHEMBL3310151 IC50 = 2050.0 nM 5.69
CHEMBL3309997 IC50 = 2560.0 nM 5.59
CHEMBL3309998 IC50 = 2880.0 nM 5.54
CHEMBL3309990 IC50 = 6706.0 nM 5.17
CHEMBL3309995 IC50 = 18147.0 nM 4.74