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Assay Detail

CHEMBL829720

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Functional
Effective concentration against heat shock protein HSP90-alpha in SKBr3 cells
16
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type SKBr3
Confidence 9 — Direct single protein target
Curated By Expert

Target

Heat shock protein HSP 90-alpha (CHEMBL3880)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Evaluation of 8-arylsulfanyl, 8-arylsulfoxyl, and 8-arylsulfonyl adenine derivatives as inhibitors of the heat shock protein 90.
Llauger L, He H, Kim J, Aguirre J, Rosen N, Peters U, Davies P, Chiosis G.
J Med Chem (2005) 48 : 2892 -2905
PubMed 15828828 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 6.27 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL365159 1 7.70
CHEMBL191635 1 7.52
CHEMBL193282 1 7.05
CHEMBL192145 1 6.89
CHEMBL273986 1 6.80
CHEMBL112953 1 6.77
CHEMBL192062 1 6.51
CHEMBL192647 1 6.48
CHEMBL191786 1 6.33
CHEMBL349231 1 5.80
CHEMBL193259 1 5.70
CHEMBL161992 1 5.44
CHEMBL352683 2 5.44
CHEMBL190518 1 5.38
CHEMBL191668 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL365159 EC50 = 20.0 nM 7.70
CHEMBL191635 EC50 = 30.0 nM 7.52
CHEMBL193282 EC50 = 90.0 nM 7.05
CHEMBL192145 EC50 = 130.0 nM 6.89
CHEMBL273986 EC50 = 160.0 nM 6.80
CHEMBL112953 EC50 = 170.0 nM 6.77
CHEMBL192062 EC50 = 310.0 nM 6.51
CHEMBL192647 EC50 = 330.0 nM 6.48
CHEMBL191786 EC50 = 470.0 nM 6.33
CHEMBL349231 EC50 = 1600.0 nM 5.80
CHEMBL193259 EC50 = 2000.0 nM 5.70
CHEMBL161992 EC50 = 3600.0 nM 5.44
CHEMBL352683 EC50 = 3600.0 nM 5.44
CHEMBL190518 EC50 = 4200.0 nM 5.38
CHEMBL352683 EC50 = 5100.0 nM 5.29
CHEMBL191668 EC50 = 5300.0 nM 5.28