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Assay Detail

CHEMBL2160398

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Functional
Cytoprotective activity against glucotoxicity in Sprague-Dawley rat DRG neurons assessed as cell viability by calcein-AM assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type DRG neuron
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and evaluation of novologues as C-terminal Hsp90 inhibitors with cytoprotective activity against sensory neuron glucotoxicity.
Kusuma BR, Zhang L, Sundstrom T, Peterson LB, Dobrowsky RT, Blagg BS.
J Med Chem (2012) 55 : 5797 -5812
PubMed 22702513 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 7.08 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2159227 CEMDOMESPIB 2.0 1 7.89
CHEMBL2159239 1 7.74
CHEMBL2159231 1 6.73
CHEMBL460005 1 6.62
CHEMBL2159233 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2159227 CEMDOMESPIB EC50 = 13.0 nM 7.89
CHEMBL2159239 EC50 = 18.4 nM 7.74
CHEMBL2159231 EC50 = 187.7 nM 6.73
CHEMBL460005 EC50 = 240.2 nM 6.62
CHEMBL2159233 EC50 = 384.0 nM 6.42