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Assay Detail

CHEMBL5158338

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

Binding
Inhibition of full length human recombinant HDAC6 expressed in Sf9 baculovirus system using FAM-labeled acetylated peptide as substrate by measuring fluorescence intensity by EMSA method
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of HDAC6-Selective Inhibitor NN-390 with <i>in Vitro</i> Efficacy in Group 3 Medulloblastoma.
Nawar N, Bukhari S, Adile AA, Suk Y, Manaswiyoungkul P, Toutah K, Olaoye OO, Raouf YS, Sedighi A, Garcha HK, Hassan MM, Gwynne W, Israelian J, Radu TB, Geletu M, Abdeldayem A, Gawel JM, Cabral AD, Venugopal C, de Araujo ED, Singh SK, Gunning PT.
J Med Chem (2022) 65 : 3193 -3217
PubMed 35119267 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.82 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3693786 CITARINOSTAT 2.0 1 8.66
CHEMBL2364628 RICOLINOSTAT 2.0 1 8.59
CHEMBL5179295 1 8.37
CHEMBL98 VORINOSTAT 4.0 1 8.24
CHEMBL5177475 1 8.22
CHEMBL5192865 1 8.07
CHEMBL2179618 NEXTURASTAT A 1 7.91
CHEMBL4763401 1 7.85
CHEMBL5173782 1 7.79
CHEMBL5202595 1 7.61
CHEMBL5191960 1 7.56
CHEMBL5199669 1 7.30
CHEMBL5202970 1 7.30
CHEMBL5195141 1 6.92
CHEMBL5184540 1 6.84
CHEMBL5208971 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3693786 CITARINOSTAT IC50 = 2.21 nM 8.66
CHEMBL2364628 RICOLINOSTAT IC50 = 2.59 nM 8.59
CHEMBL5179295 IC50 = 4.32 nM 8.37
CHEMBL98 VORINOSTAT IC50 = 5.8 nM 8.24
CHEMBL5177475 IC50 = 6.0 nM 8.22
CHEMBL5192865 IC50 = 8.5 nM 8.07
CHEMBL2179618 NEXTURASTAT A IC50 = 12.4 nM 7.91
CHEMBL4763401 IC50 = 14.0 nM 7.85
CHEMBL5173782 IC50 = 16.2 nM 7.79
CHEMBL5202595 IC50 = 24.6 nM 7.61
CHEMBL5191960 IC50 = 27.8 nM 7.56
CHEMBL5199669 IC50 = 49.9 nM 7.30
CHEMBL5202970 IC50 = 50.4 nM 7.30
CHEMBL5195141 IC50 = 121.0 nM 6.92
CHEMBL5184540 IC50 = 143.0 nM 6.84
CHEMBL5208971 IC50 > 1000.0 nM -