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Assay Detail

CHEMBL1015016

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

Binding
Binding affinity to human recombinant Hsp90alpha N-terminal domain by scintillation proximity assay
7
Total Activities
7
Compounds Tested
1
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-alpha (CHEMBL3880)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus.
Menzella HG, Tran TT, Carney JR, Lau-Wee J, Galazzo J, Reeves CD, Carreras C, Mukadam S, Eng S, Zhong Z, Timmermans PB, Murli S, Ashley GW.
J Med Chem (2009) 52 : 1518 -1521
PubMed 19231864 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 6.57 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL511618 1 7.30
CHEMBL383824 ALVESPIMYCIN 2.0 1 6.30
CHEMBL109480 TANESPIMYCIN 3.0 1 6.12
CHEMBL517853 1 -
CHEMBL469932 1 -
CHEMBL512489 1 -
CHEMBL511439 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL511618 Kd = 50.0 nM 7.30
CHEMBL383824 ALVESPIMYCIN Kd = 500.0 nM 6.30
CHEMBL109480 TANESPIMYCIN Kd = 760.0 nM 6.12
CHEMBL517853 Kd - -
CHEMBL469932 Kd - -
CHEMBL512489 Kd - -
CHEMBL511439 Kd - -