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Assay Detail

CHEMBL5217051

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

Binding
Inhibition of HDAC6 (unknown origin) measured by fluorescence based assay
28
Total Activities
28
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

Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template.
Li Z, Zhao C, He G, Wang Y, Wang Y, Ma X.
Bioorg Med Chem (2022) 73 : 117028 -117028
PubMed 36182802 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.25 8.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2018302 TUBASTATIN A 1 8.03
CHEMBL5219048 1 7.96
CHEMBL5218472 1 7.89
CHEMBL5220434 1 7.89
CHEMBL5218525 1 7.89
CHEMBL2364628 RICOLINOSTAT 2.0 1 7.77
CHEMBL5218764 1 7.57
CHEMBL5219798 1 7.57
CHEMBL5220934 1 7.55
CHEMBL5218454 1 7.50
CHEMBL5219657 1 7.44
CHEMBL98 VORINOSTAT 4.0 1 7.41
CHEMBL5220310 1 7.37
CHEMBL5220776 1 7.35
CHEMBL5218549 1 7.35
CHEMBL5221123 1 7.18
CHEMBL5219941 1 7.17
CHEMBL5218671 1 7.06
CHEMBL5221043 1 6.92
CHEMBL5219509 1 6.78
CHEMBL5219246 1 6.66
CHEMBL5219356 1 6.57
CHEMBL5218504 1 6.55
CHEMBL5218681 1 6.48
CHEMBL5220325 1 6.40
CHEMBL5220243 1 6.22
CHEMBL5219236 1 -
CHEMBL2216870 IDELALISIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2018302 TUBASTATIN A IC50 = 9.4 nM 8.03
CHEMBL5219048 IC50 = 11.0 nM 7.96
CHEMBL5218472 IC50 = 13.0 nM 7.89
CHEMBL5220434 IC50 = 13.0 nM 7.89
CHEMBL5218525 IC50 = 13.0 nM 7.89
CHEMBL2364628 RICOLINOSTAT IC50 = 17.0 nM 7.77
CHEMBL5218764 IC50 = 27.0 nM 7.57
CHEMBL5219798 IC50 = 27.0 nM 7.57
CHEMBL5220934 IC50 = 28.0 nM 7.55
CHEMBL5218454 IC50 = 32.0 nM 7.50
CHEMBL5219657 IC50 = 36.0 nM 7.44
CHEMBL98 VORINOSTAT IC50 = 39.0 nM 7.41
CHEMBL5220310 IC50 = 43.0 nM 7.37
CHEMBL5220776 IC50 = 45.0 nM 7.35
CHEMBL5218549 IC50 = 45.0 nM 7.35
CHEMBL5221123 IC50 = 66.0 nM 7.18
CHEMBL5219941 IC50 = 67.0 nM 7.17
CHEMBL5218671 IC50 = 87.0 nM 7.06
CHEMBL5221043 IC50 = 121.0 nM 6.92
CHEMBL5219509 IC50 = 168.0 nM 6.78
CHEMBL5219246 IC50 = 219.0 nM 6.66
CHEMBL5219356 IC50 = 267.0 nM 6.57
CHEMBL5218504 IC50 = 280.0 nM 6.55
CHEMBL5218681 IC50 = 331.0 nM 6.48
CHEMBL5220325 IC50 = 398.0 nM 6.40
CHEMBL5220243 IC50 = 604.0 nM 6.22
CHEMBL5219236 IC50 - -
CHEMBL2216870 IDELALISIB IC50 - -