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Assay Detail

CHEMBL1918874

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

Binding
Binding affinity to human Hsp90beta after overnight incubation by fluorescence polarization assay
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Heat shock protein HSP 90-beta (CHEMBL4303)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tricyclic series of heat shock protein 90 (Hsp90) inhibitors part I: discovery of tricyclic imidazo[4,5-c]pyridines as potent inhibitors of the Hsp90 molecular chaperone.
Vallée F, Carrez C, Pilorge F, Dupuy A, Parent A, Bertin L, Thompson F, Ferrari P, Fassy F, Lamberton A, Thomas A, Arrebola R, Guerif S, Rohaut A, Certal V, Ruxer JM, Gouyon T, Delorme C, Jouanen A, Dumas J, Grépin C, Combeau C, Goulaouic H, Dereu N, Mikol V, Mailliet P, Minoux H.
J Med Chem (2011) 54 : 7206 -7219
PubMed 21972823 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
K 2 - -
Kd 2 8.80 9.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1917878 2 9.46
CHEMBL109480 TANESPIMYCIN 3.0 2 8.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1917878 Kd = 0.35 nM 9.46
CHEMBL109480 TANESPIMYCIN Kd = 7.3 nM 8.14
CHEMBL1917878 K = 1.8 nM -
CHEMBL109480 TANESPIMYCIN K = 61.0 nM -