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Assay Detail

CHEMBL4151773

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

Functional
Protection against cisplatin-induced toxicity in P3 mouse cochlear explants assessed as increase in outer hair cell count incubated for 24 hrs by phalloidin staining based confocal microscopy
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Tissue Spiral organ of cochlea
Confidence 1 — Organism
Curated By Intermediate

Target

Spiral organ of cochlea (CHEMBL4296537)
Type TISSUE
Organism Mus musculus

Publication

Development of Second-Generation CDK2 Inhibitors for the Prevention of Cisplatin-Induced Hearing Loss.
Hazlitt RA, Teitz T, Bonga JD, Fang J, Diao S, Iconaru L, Yang L, Goktug AN, Currier DG, Chen T, Rankovic Z, Min J, Zuo J.
J Med Chem (2018) 61 : 7700 -7709
PubMed 30091915 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 6.45 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL488436 AZD-5438 1.0 1 8.30
CHEMBL445813 AT-7519 2.0 1 7.60
CHEMBL457177 1 7.55
CHEMBL296586 KENPAULLONE 1 6.82
CHEMBL409450 6BIO 1 6.24
CHEMBL411491 1 6.00
CHEMBL1094304 OLOMOUCINE II 1 5.52
CHEMBL258805 SU-9516 1.0 1 5.22
CHEMBL4162724 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL488436 AZD-5438 EC50 = 5.0 nM 8.30
CHEMBL445813 AT-7519 EC50 = 25.0 nM 7.60
CHEMBL457177 EC50 = 28.0 nM 7.55
CHEMBL296586 KENPAULLONE EC50 = 150.0 nM 6.82
CHEMBL409450 6BIO EC50 = 570.0 nM 6.24
CHEMBL411491 EC50 = 1000.0 nM 6.00
CHEMBL1094304 OLOMOUCINE II EC50 = 3000.0 nM 5.52
CHEMBL258805 SU-9516 EC50 = 6000.0 nM 5.22
CHEMBL4162724 EC50 = 15000.0 nM 4.82