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Assay Detail

CHEMBL947922

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Binding
Inhibition of HDAC2
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Histone deacetylase 2 (CHEMBL1937)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Exploration of the internal cavity of histone deacetylase (HDAC) with selective HDAC1/HDAC2 inhibitors (SHI-1:2).
Methot JL, Chakravarty PK, Chenard M, Close J, Cruz JC, Dahlberg WK, Fleming J, Hamblett CL, Hamill JE, Harrington P, Harsch A, Heidebrecht R, Hughes B, Jung J, Kenific CM, Kral AM, Meinke PT, Middleton RE, Ozerova N, Sloman DL, Stanton MG, Szewczak AA, Tyagarajan S, Witter DJ, Secrist JP, Miller TA.
Bioorg Med Chem Lett (2008) 18 : 973 -978
PubMed 18182289 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.37 7.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL235842 1 7.31
CHEMBL269935 1 6.70
CHEMBL271949 1 6.44
CHEMBL437029 1 6.19
CHEMBL271741 1 6.11
CHEMBL405072 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL235842 IC50 = 49.0 nM 7.31
CHEMBL269935 IC50 = 200.0 nM 6.70
CHEMBL271949 IC50 = 360.0 nM 6.44
CHEMBL437029 IC50 = 640.0 nM 6.19
CHEMBL271741 IC50 = 780.0 nM 6.11
CHEMBL405072 IC50 = 3300.0 nM 5.48