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Assay Detail

CHEMBL832973

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Binding
Inhibitory concentration against activity of Hsp90 was determined by fluorescence polarization (FP) assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design.
Dymock BW, Barril X, Brough PA, Cansfield JE, Massey A, McDonald E, Hubbard RE, Surgenor A, Roughley SD, Webb P, Workman P, Wright L, Drysdale MJ.
J Med Chem (2005) 48 : 4212 -4215
PubMed 15974572 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.65 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL365617 1 7.60
CHEMBL424811 1 7.41
CHEMBL366215 1 7.28
CHEMBL364968 1 7.21
CHEMBL190182 1 7.16
CHEMBL365700 1 6.92
CHEMBL371380 1 6.82
CHEMBL191074 1 6.68
CHEMBL399530 1 6.55
CHEMBL426446 1 6.29
CHEMBL109480 TANESPIMYCIN 3.0 1 5.90
CHEMBL192894 1 5.36
CHEMBL188965 1 5.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL365617 IC50 = 25.0 nM 7.60
CHEMBL424811 IC50 = 39.0 nM 7.41
CHEMBL366215 IC50 = 53.0 nM 7.28
CHEMBL364968 IC50 = 62.0 nM 7.21
CHEMBL190182 IC50 = 70.0 nM 7.16
CHEMBL365700 IC50 = 120.0 nM 6.92
CHEMBL371380 IC50 = 150.0 nM 6.82
CHEMBL191074 IC50 = 210.0 nM 6.68
CHEMBL399530 IC50 = 280.0 nM 6.55
CHEMBL426446 IC50 = 510.0 nM 6.29
CHEMBL109480 TANESPIMYCIN IC50 = 1270.0 nM 5.90
CHEMBL192894 IC50 = 4400.0 nM 5.36
CHEMBL188965 IC50 = 4730.0 nM 5.33