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Assay Detail

CHEMBL4714060

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Binding
Inhibition of HSP90-alpha (unknown origin) expressed in Escherichia coli BL21 assessed as reduction in ATPase activity in presence of PEP, NADH and ATP by pyruvate kinase/lactic dehydrogenase based coupled enzyme assay
11
Total Activities
11
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

Discovering High Potent Hsp90 Inhibitors as Antinasopharyngeal Carcinoma Agents through Fragment Assembling Approach.
Xu M,Zhao C,Zhu B,Wang L,Zhou H,Yan D,Gu Q,Xu J
J Med Chem (2021) 64 : 2010 -2023
PubMed 33543615 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.64 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4741221 1 6.80
CHEMBL109480 TANESPIMYCIN 3.0 1 6.07
CHEMBL4777111 1 5.89
CHEMBL4748845 1 5.77
CHEMBL4759116 1 5.57
CHEMBL4777925 1 5.30
CHEMBL4777557 1 5.25
CHEMBL4778213 1 5.21
CHEMBL4745924 1 4.86
CHEMBL4746322 1 -
CHEMBL4760861 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4741221 IC50 = 160.0 nM 6.80
CHEMBL109480 TANESPIMYCIN IC50 = 850.0 nM 6.07
CHEMBL4777111 IC50 = 1300.0 nM 5.89
CHEMBL4748845 IC50 = 1700.0 nM 5.77
CHEMBL4759116 IC50 = 2700.0 nM 5.57
CHEMBL4777925 IC50 = 5000.0 nM 5.30
CHEMBL4777557 IC50 = 5600.0 nM 5.25
CHEMBL4778213 IC50 = 6200.0 nM 5.21
CHEMBL4745924 IC50 = 13700.0 nM 4.86
CHEMBL4746322 IC50 > 40000.0 nM -
CHEMBL4760861 IC50 > 40000.0 nM -