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Assay Detail

CHEMBL4028190

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

Binding
Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected insect cells using RHK-K(Ac)-AMC as substrate after 90 mins by fluorescence assay
27
Total Activities
27
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

(N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo.
Lee HY, Nepali K, Huang FI, Chang CY, Lai MJ, Li YH, Huang HL, Yang CR, Liou JP.
J Med Chem (2018) 61 : 905 -917
PubMed 29304284 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 7.89 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4104117 1 9.54
CHEMBL4095667 1 9.10
CHEMBL4063376 1 8.64
CHEMBL4091237 1 8.63
CHEMBL4098833 1 8.55
CHEMBL4079874 1 8.49
CHEMBL4085971 1 8.47
CHEMBL99 TRICHOSTATIN 1.0 1 8.45
CHEMBL4101436 1 8.45
CHEMBL4073165 1 8.37
CHEMBL2364628 RICOLINOSTAT 2.0 1 8.33
CHEMBL4068310 1 8.32
CHEMBL4083449 1 8.23
CHEMBL4093020 1 8.13
CHEMBL4080790 1 8.02
CHEMBL4064437 1 7.94
CHEMBL4082487 1 7.71
CHEMBL4083577 1 7.67
CHEMBL4060607 1 7.60
CHEMBL4069121 1 7.60
CHEMBL4096377 1 7.38
CHEMBL4065354 1 7.38
CHEMBL4073021 1 6.89
CHEMBL4088663 1 6.58
CHEMBL4061807 1 6.39
CHEMBL4060433 1 6.28
CHEMBL4093718 1 5.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4104117 IC50 = 0.291 nM 9.54
CHEMBL4095667 IC50 = 0.795 nM 9.10
CHEMBL4063376 IC50 = 2.31 nM 8.64
CHEMBL4091237 IC50 = 2.33 nM 8.63
CHEMBL4098833 IC50 = 2.83 nM 8.55
CHEMBL4079874 IC50 = 3.25 nM 8.49
CHEMBL4085971 IC50 = 3.35 nM 8.47
CHEMBL99 TRICHOSTATIN IC50 = 3.55 nM 8.45
CHEMBL4101436 IC50 = 3.56 nM 8.45
CHEMBL4073165 IC50 = 4.24 nM 8.37
CHEMBL2364628 RICOLINOSTAT IC50 = 4.7 nM 8.33
CHEMBL4068310 IC50 = 4.78 nM 8.32
CHEMBL4083449 IC50 = 5.89 nM 8.23
CHEMBL4093020 IC50 = 7.4 nM 8.13
CHEMBL4080790 IC50 = 9.48 nM 8.02
CHEMBL4064437 IC50 = 11.4 nM 7.94
CHEMBL4082487 IC50 = 19.6 nM 7.71
CHEMBL4083577 IC50 = 21.5 nM 7.67
CHEMBL4060607 IC50 = 25.3 nM 7.60
CHEMBL4069121 IC50 = 25.3 nM 7.60
CHEMBL4096377 IC50 = 41.7 nM 7.38
CHEMBL4065354 IC50 = 41.7 nM 7.38
CHEMBL4073021 IC50 = 129.0 nM 6.89
CHEMBL4088663 IC50 = 265.0 nM 6.58
CHEMBL4061807 IC50 = 403.0 nM 6.39
CHEMBL4060433 IC50 = 525.0 nM 6.28
CHEMBL4093718 IC50 = 1130.0 nM 5.95