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Assay Detail

CHEMBL4157378

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

Binding
Inhibition of human N-terminal octa-His-tagged HSP60 expressed in Escherichia coli Rosetta(DE3) pLysS/human HSP10 expressed in Escherichia coli Rosetta(DE3) assessed as reduction in HSP60/HSP10-mediated denatured MDH refolding by measuring MDH enzyme activity using sodium mesoxalate as substrate after 40 to 60 mins by spectrometric analysis
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Intermediate

Target

HSP60/HSP10 (CHEMBL4106131)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Sulfonamido-2-arylbenzoxazole GroEL/ES Inhibitors as Potent Antibacterials against Methicillin-Resistant Staphylococcus aureus (MRSA).
Abdeen S, Kunkle T, Salim N, Ray AM, Mammadova N, Summers C, Stevens M, Ambrose AJ, Park Y, Schultz PG, Horwich AL, Hoang QQ, Chapman E, Johnson SM.
J Med Chem (2018) 61 : 7345 -7357
PubMed 30060666 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.10 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4161583 1 6.00
CHEMBL4167333 1 5.68
CHEMBL4169499 1 5.62
CHEMBL4160098 1 5.35
CHEMBL4166077 1 5.33
CHEMBL4176697 1 5.30
CHEMBL4162794 1 5.23
CHEMBL4161487 1 5.21
CHEMBL4168023 1 4.96
CHEMBL3955935 1 4.29
CHEMBL3970551 1 4.24
CHEMBL3975683 1 4.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4161583 IC50 = 1000.0 nM 6.00
CHEMBL4167333 IC50 = 2100.0 nM 5.68
CHEMBL4169499 IC50 = 2400.0 nM 5.62
CHEMBL4160098 IC50 = 4500.0 nM 5.35
CHEMBL4166077 IC50 = 4700.0 nM 5.33
CHEMBL4176697 IC50 = 5000.0 nM 5.30
CHEMBL4162794 IC50 = 5900.0 nM 5.23
CHEMBL4161487 IC50 = 6100.0 nM 5.21
CHEMBL4168023 IC50 = 11000.0 nM 4.96
CHEMBL3955935 IC50 = 51000.0 nM 4.29
CHEMBL3970551 IC50 = 58000.0 nM 4.24
CHEMBL3975683 IC50 = 96000.0 nM 4.02