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Assay Detail

CHEMBL5364103

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

Binding
Binding affinity to N-terminal His-tagged HDAC6 UBD (1109 to 1213 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) incubated for 10 mins using N-terminal FITC-labeled LRLRGG as substrate by fluorescence polarization assay
24
Total Activities
24
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 and Characterization of a Chemical Probe Targeting the Zinc-Finger Ubiquitin-Binding Domain of HDAC6.
Harding RJ, Franzoni I, Mann MK, Szewczyk MM, Mirabi B, Ferreira de Freitas R, Owens DDG, Ackloo S, Scheremetjew A, Juarez-Ornelas KA, Sanichar R, Baker RJ, Dank C, Brown PJ, Barsyte-Lovejoy D, Santhakumar V, Schapira M, Lautens M, Arrowsmith CH.
J Med Chem (2023) 66 : 10273 -10288
PubMed 37499118 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 24 5.75 7.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5410606 1 7.02
CHEMBL5428090 1 6.75
CHEMBL5426586 1 6.66
CHEMBL5406492 1 6.64
CHEMBL5402254 1 6.62
CHEMBL5402050 1 6.54
CHEMBL5409340 1 6.50
CHEMBL5409494 1 6.50
CHEMBL5427723 1 6.26
CHEMBL5430040 1 6.21
CHEMBL5412490 1 5.80
CHEMBL5424155 1 5.70
CHEMBL5401898 1 5.70
CHEMBL5437248 1 5.29
CHEMBL5412794 1 5.29
CHEMBL5431399 1 5.09
CHEMBL5439441 1 5.04
CHEMBL5401737 1 5.04
CHEMBL5410297 1 5.03
CHEMBL5433542 1 5.03
CHEMBL5393985 1 5.02
CHEMBL5430203 1 4.96
CHEMBL5420153 1 4.85
CHEMBL5426708 1 4.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5410606 Kd = 95.0 nM 7.02
CHEMBL5428090 Kd = 180.0 nM 6.75
CHEMBL5426586 Kd = 220.0 nM 6.66
CHEMBL5406492 Kd = 230.0 nM 6.64
CHEMBL5402254 Kd = 240.0 nM 6.62
CHEMBL5402050 Kd = 290.0 nM 6.54
CHEMBL5409340 Kd = 320.0 nM 6.50
CHEMBL5409494 Kd = 320.0 nM 6.50
CHEMBL5427723 Kd = 550.0 nM 6.26
CHEMBL5430040 Kd = 620.0 nM 6.21
CHEMBL5412490 Kd = 1600.0 nM 5.80
CHEMBL5424155 Kd = 2000.0 nM 5.70
CHEMBL5401898 Kd = 2000.0 nM 5.70
CHEMBL5437248 Kd = 5100.0 nM 5.29
CHEMBL5412794 Kd = 5100.0 nM 5.29
CHEMBL5431399 Kd = 8100.0 nM 5.09
CHEMBL5439441 Kd = 9100.0 nM 5.04
CHEMBL5401737 Kd = 9100.0 nM 5.04
CHEMBL5410297 Kd = 9300.0 nM 5.03
CHEMBL5433542 Kd = 9400.0 nM 5.03
CHEMBL5393985 Kd = 9600.0 nM 5.02
CHEMBL5430203 Kd = 11000.0 nM 4.96
CHEMBL5420153 Kd = 14000.0 nM 4.85
CHEMBL5426708 Kd = 33000.0 nM 4.48