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Assay Detail

CHEMBL5367105

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

Binding
Inhibition of HDAC6 (unknown origin)
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

Histone deacetylase 6 (CHEMBL1865)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of (S)-N<sup>1</sup>-(thiazol-2-yl) pyrrolidine-1,2-dicarboxamide derivatives targeting PI3Ka/HDAC6 for the treatment of cancer.
Zhang Y, Gao J, Wu J, Liu S, Zhang X, Lv X.
Bioorg Med Chem Lett (2023) 94 : 129462 -129462
PubMed 37652098 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.31 8.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5420057 1 8.01
CHEMBL98 VORINOSTAT 4.0 1 7.92
CHEMBL5439214 1 7.58
CHEMBL5418257 1 7.55
CHEMBL5406498 1 7.42
CHEMBL5438456 1 7.41
CHEMBL5400641 1 7.35
CHEMBL5422044 1 7.28
CHEMBL5410409 1 6.89
CHEMBL5410758 1 6.82
CHEMBL5435973 1 6.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5420057 IC50 = 9.8 nM 8.01
CHEMBL98 VORINOSTAT IC50 = 12.0 nM 7.92
CHEMBL5439214 IC50 = 26.0 nM 7.58
CHEMBL5418257 IC50 = 28.0 nM 7.55
CHEMBL5406498 IC50 = 38.0 nM 7.42
CHEMBL5438456 IC50 = 39.0 nM 7.41
CHEMBL5400641 IC50 = 45.0 nM 7.35
CHEMBL5422044 IC50 = 53.0 nM 7.28
CHEMBL5410409 IC50 = 130.0 nM 6.89
CHEMBL5410758 IC50 = 152.0 nM 6.82
CHEMBL5435973 IC50 = 680.0 nM 6.17