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Assay Detail

CHEMBL3381044

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Functional
Antiproliferative activity against human A2780 cells after 72 hrs
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A2780
Confidence 1 — Organism
Curated By Autocuration

Target

A2780 (CHEMBL614004)
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 25 5.37 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL252164 LUMINESPIB 2.0 1 9.00
CHEMBL3310151 1 5.81
CHEMBL3309998 1 5.67
CHEMBL3309997 1 5.67
CHEMBL3310003 1 5.44
CHEMBL3309988 1 5.30
CHEMBL3309995 1 5.22
CHEMBL3310152 1 5.19
CHEMBL3309990 1 5.18
CHEMBL3310155 1 5.16
CHEMBL3309999 1 5.09
CHEMBL3309269 1 5.09
CHEMBL3310001 1 5.08
CHEMBL3309989 1 5.05
CHEMBL3309991 1 5.04
CHEMBL3310000 1 5.04
CHEMBL3310002 1 5.04
CHEMBL3310156 1 5.04
CHEMBL3310004 1 5.02
CHEMBL3309985 1 5.00
CHEMBL3309993 1 4.96
CHEMBL3309994 1 4.96
CHEMBL3309996 1 -
CHEMBL3310153 1 -
CHEMBL3310154 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL252164 LUMINESPIB IC50 = 1.0 nM 9.00
CHEMBL3310151 IC50 = 1550.0 nM 5.81
CHEMBL3309998 IC50 = 2116.0 nM 5.67
CHEMBL3309997 IC50 = 2119.0 nM 5.67
CHEMBL3310003 IC50 = 3600.0 nM 5.44
CHEMBL3309988 IC50 = 5047.0 nM 5.30
CHEMBL3309995 IC50 = 5961.0 nM 5.22
CHEMBL3310152 IC50 = 6516.0 nM 5.19
CHEMBL3309990 IC50 = 6613.0 nM 5.18
CHEMBL3310155 IC50 = 6948.0 nM 5.16
CHEMBL3309999 IC50 = 8112.0 nM 5.09
CHEMBL3309269 IC50 = 8190.0 nM 5.09
CHEMBL3310001 IC50 = 8303.0 nM 5.08
CHEMBL3309989 IC50 = 8823.0 nM 5.05
CHEMBL3309991 IC50 = 9030.0 nM 5.04
CHEMBL3310000 IC50 = 9189.0 nM 5.04
CHEMBL3310002 IC50 = 9010.0 nM 5.04
CHEMBL3310156 IC50 = 9103.0 nM 5.04
CHEMBL3310004 IC50 = 9500.0 nM 5.02
CHEMBL3309985 IC50 = 10000.0 nM 5.00
CHEMBL3309993 IC50 = 11000.0 nM 4.96
CHEMBL3309994 IC50 = 11020.0 nM 4.96
CHEMBL3309996 IC50 > 10000.0 nM -
CHEMBL3310153 IC50 > 10000.0 nM -
CHEMBL3310154 IC50 > 10000.0 nM -