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Assay Detail

CHEMBL5158356

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

Binding
Competitive inhibition of N-terminal His-SUMO tagged zebra fish recombinant HDAC6 catalytic domain 2 transfected with pET28b(+) vector in Escherichia coli BL21 (DE3) RILP cells incubated for 10 mins followed by addition of FITC-M344 measured af ter 10 mins by fluorescence polarization assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Danio rerio
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 9 6.68 7.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2364628 RICOLINOSTAT 2.0 1 7.04
CHEMBL5202595 1 6.86
CHEMBL5177475 1 6.86
CHEMBL3693786 CITARINOSTAT 2.0 1 6.81
CHEMBL5192865 1 6.76
CHEMBL5179295 1 6.74
CHEMBL408513 BELINOSTAT 4.0 1 6.67
CHEMBL5199669 1 6.45
CHEMBL5195141 1 5.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2364628 RICOLINOSTAT IC50 = 90.2 nM 7.04
CHEMBL5202595 IC50 = 137.0 nM 6.86
CHEMBL5177475 IC50 = 139.0 nM 6.86
CHEMBL3693786 CITARINOSTAT IC50 = 154.0 nM 6.81
CHEMBL5192865 IC50 = 173.0 nM 6.76
CHEMBL5179295 IC50 = 182.0 nM 6.74
CHEMBL408513 BELINOSTAT IC50 = 213.0 nM 6.67
CHEMBL5199669 IC50 = 356.0 nM 6.45
CHEMBL5195141 IC50 = 1126.0 nM 5.95