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Assay Detail

CHEMBL4187413

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

Binding
Inhibition of HDAC6 (unknown origin) preincubated for 10 mins followed by Ac-Leu-GlyLys(Ac)-AMC substrate addition measured after 30 mins by fluorescence based assay
26
Total Activities
26
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

Design, synthesis and evaluate of novel dual FGFR1 and HDAC inhibitors bearing an indazole scaffold.
Liu J, Qian C, Zhu Y, Cai J, He Y, Li J, Wang T, Zhu H, Li Z, Li W, Hu L.
Bioorg Med Chem (2018) 26 : 747 -757
PubMed 29317150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 7.07 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2179618 NEXTURASTAT A 1 8.28
CHEMBL98 VORINOSTAT 4.0 1 8.06
CHEMBL4211463 1 7.48
CHEMBL4203874 1 7.47
CHEMBL4211477 1 7.42
CHEMBL4204972 1 7.40
CHEMBL4217830 1 7.39
CHEMBL4205573 1 7.24
CHEMBL4217618 1 7.23
CHEMBL4214775 1 7.19
CHEMBL4212669 1 7.19
CHEMBL4212219 1 7.16
CHEMBL4208584 1 7.11
CHEMBL4203741 1 7.01
CHEMBL4205375 1 6.99
CHEMBL4214652 1 6.88
CHEMBL4213207 1 6.83
CHEMBL4208276 1 6.80
CHEMBL4207699 1 6.75
CHEMBL4210396 1 6.66
CHEMBL4210899 1 6.62
CHEMBL4210578 1 6.60
CHEMBL4217088 1 6.55
CHEMBL4203935 1 6.53
CHEMBL4202659 1 6.46
CHEMBL4215505 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2179618 NEXTURASTAT A IC50 = 5.2 nM 8.28
CHEMBL98 VORINOSTAT IC50 = 8.8 nM 8.06
CHEMBL4211463 IC50 = 33.0 nM 7.48
CHEMBL4203874 IC50 = 34.0 nM 7.47
CHEMBL4211477 IC50 = 38.0 nM 7.42
CHEMBL4204972 IC50 = 40.0 nM 7.40
CHEMBL4217830 IC50 = 41.0 nM 7.39
CHEMBL4205573 IC50 = 58.0 nM 7.24
CHEMBL4217618 IC50 = 59.0 nM 7.23
CHEMBL4214775 IC50 = 65.0 nM 7.19
CHEMBL4212669 IC50 = 64.0 nM 7.19
CHEMBL4212219 IC50 = 69.0 nM 7.16
CHEMBL4208584 IC50 = 78.0 nM 7.11
CHEMBL4203741 IC50 = 98.0 nM 7.01
CHEMBL4205375 IC50 = 103.0 nM 6.99
CHEMBL4214652 IC50 = 132.0 nM 6.88
CHEMBL4213207 IC50 = 147.0 nM 6.83
CHEMBL4208276 IC50 = 157.0 nM 6.80
CHEMBL4207699 IC50 = 178.0 nM 6.75
CHEMBL4210396 IC50 = 218.0 nM 6.66
CHEMBL4210899 IC50 = 242.0 nM 6.62
CHEMBL4210578 IC50 = 250.0 nM 6.60
CHEMBL4217088 IC50 = 281.0 nM 6.55
CHEMBL4203935 IC50 = 293.0 nM 6.53
CHEMBL4202659 IC50 = 345.0 nM 6.46
CHEMBL4215505 IC50 = 385.0 nM 6.42