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Assay Detail

CHEMBL839760

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

Binding
Displacement of 5 nM GM-BODIPY from mouse heat shock protein HSP90-alpha
ChEMBL ↗
54
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Heat shock protein HSP 90-alpha (CHEMBL4197) ↗
Type SINGLE PROTEIN
Organism Mus musculus

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 54 5.51 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL365159 — — 1 7.52
CHEMBL191635 — — 1 7.30
CHEMBL192145 — — 1 7.16
CHEMBL193282 — — 1 6.92
CHEMBL191786 — — 1 6.80
CHEMBL192647 — — 1 6.75
CHEMBL273986 — — 1 6.72
CHEMBL192062 — — 1 6.70
CHEMBL191268 — — 1 6.07
CHEMBL191241 — — 1 6.01
CHEMBL189537 — — 1 5.82
CHEMBL190518 — — 1 5.82
CHEMBL193259 — — 1 5.82
CHEMBL371570 — — 1 5.70
CHEMBL370247 — — 1 5.68
CHEMBL364450 — — 1 5.68
CHEMBL370092 — — 1 5.64
CHEMBL191920 — — 1 5.62
CHEMBL439852 — — 1 5.60
CHEMBL363860 — — 1 5.57
CHEMBL191601 — — 1 5.55
CHEMBL191641 — — 1 5.51
CHEMBL193056 — — 1 5.51
CHEMBL191668 — — 1 5.47
CHEMBL426086 — — 1 5.47
CHEMBL193672 — — 1 5.46
CHEMBL364456 — — 1 5.43
CHEMBL195869 — — 1 5.34
CHEMBL192649 — — 1 5.33
CHEMBL192937 — — 1 5.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL365159 — EC50 = 30.0 nM 7.52
CHEMBL191635 — EC50 = 50.0 nM 7.30
CHEMBL192145 — EC50 = 70.0 nM 7.16
CHEMBL193282 — EC50 = 120.0 nM 6.92
CHEMBL191786 — EC50 = 160.0 nM 6.80
CHEMBL192647 — EC50 = 180.0 nM 6.75
CHEMBL273986 — EC50 = 190.0 nM 6.72
CHEMBL192062 — EC50 = 200.0 nM 6.70
CHEMBL191268 — EC50 = 850.0 nM 6.07
CHEMBL191241 — EC50 = 970.0 nM 6.01
CHEMBL189537 — EC50 = 1500.0 nM 5.82
CHEMBL190518 — EC50 = 1500.0 nM 5.82
CHEMBL193259 — EC50 = 1500.0 nM 5.82
CHEMBL371570 — EC50 = 2000.0 nM 5.70
CHEMBL364450 — EC50 = 2100.0 nM 5.68
CHEMBL370247 — EC50 = 2100.0 nM 5.68
CHEMBL370092 — EC50 = 2300.0 nM 5.64
CHEMBL191920 — EC50 = 2400.0 nM 5.62
CHEMBL439852 — EC50 = 2500.0 nM 5.60
CHEMBL363860 — EC50 = 2700.0 nM 5.57
CHEMBL191601 — EC50 = 2800.0 nM 5.55
CHEMBL191641 — EC50 = 3100.0 nM 5.51
CHEMBL193056 — EC50 = 3100.0 nM 5.51
CHEMBL191668 — EC50 = 3400.0 nM 5.47
CHEMBL426086 — EC50 = 3400.0 nM 5.47
CHEMBL193672 — EC50 = 3500.0 nM 5.46
CHEMBL364456 — EC50 = 3700.0 nM 5.43
CHEMBL195869 — EC50 = 4600.0 nM 5.34
CHEMBL192649 — EC50 = 4700.0 nM 5.33
CHEMBL192937 — EC50 = 4800.0 nM 5.32
CHEMBL363196 — EC50 = 5000.0 nM 5.30
CHEMBL371372 — EC50 = 5600.0 nM 5.25
CHEMBL424824 — EC50 = 8600.0 nM 5.07
CHEMBL192480 — EC50 = 8500.0 nM 5.07
CHEMBL195096 — EC50 = 10600.0 nM 4.97
CHEMBL364239 — EC50 = 13400.0 nM 4.87
CHEMBL194716 — EC50 = 15400.0 nM 4.81
CHEMBL370286 — EC50 = 19100.0 nM 4.72
CHEMBL192013 — EC50 = 30400.0 nM 4.52
CHEMBL193892 — EC50 = 34900.0 nM 4.46
CHEMBL365118 — EC50 = 37500.0 nM 4.43
CHEMBL190439 — EC50 = 42200.0 nM 4.38
CHEMBL192761 — EC50 = 76500.0 nM 4.12
CHEMBL190438 — EC50 = 85100.0 nM 4.07
CHEMBL364272 — EC50 = 85100.0 nM 4.07
CHEMBL415775 — EC50 = 90700.0 nM 4.04
CHEMBL191835 — EC50 > 100000.0 nM -
CHEMBL364730 — EC50 > 100000.0 nM -
CHEMBL427169 — EC50 > 50000.0 nM -
CHEMBL362972 — EC50 > 50000.0 nM -