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Assay Detail

CHEMBL940369

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

Binding
Inhibition of human HDAC1 expressed in mammalian cells
39
Total Activities
39
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 1 (CHEMBL325)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

SAR profiles of spirocyclic nicotinamide derived selective HDAC1/HDAC2 inhibitors (SHI-1:2).
Methot JL, Hamblett CL, Mampreian DM, Jung J, Harsch A, Szewczak AA, Dahlberg WK, Middleton RE, Hughes B, Fleming JC, Wang H, Kral AM, Ozerova N, Cruz JC, Haines B, Chenard M, Kenific CM, Secrist JP, Miller TA.
Bioorg Med Chem Lett (2008) 18 : 6104 -6109
PubMed 18951790 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 7.59 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL513250 1 8.22
CHEMBL486152 1 8.15
CHEMBL486770 1 8.10
CHEMBL471399 1 8.10
CHEMBL470582 1 8.10
CHEMBL513568 1 8.10
CHEMBL471414 1 8.05
CHEMBL511797 1 8.00
CHEMBL470791 1 7.96
CHEMBL471824 1 7.96
CHEMBL469950 1 7.96
CHEMBL472442 1 7.92
CHEMBL511984 1 7.89
CHEMBL470147 1 7.89
CHEMBL471220 1 7.89
CHEMBL470581 1 7.85
CHEMBL513027 1 7.80
CHEMBL471219 1 7.77
CHEMBL472261 1 7.77
CHEMBL472251 1 7.75
CHEMBL469514 1 7.68
CHEMBL472252 1 7.66
CHEMBL472443 1 7.64
CHEMBL471400 1 7.64
CHEMBL521193 1 7.57
CHEMBL470798 1 7.55
CHEMBL470148 1 7.54
CHEMBL470156 1 7.44
CHEMBL487346 1 7.41
CHEMBL255805 1 7.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL513250 IC50 = 6.0 nM 8.22
CHEMBL486152 IC50 = 7.0 nM 8.15
CHEMBL471399 IC50 = 8.0 nM 8.10
CHEMBL470582 IC50 = 8.0 nM 8.10
CHEMBL513568 IC50 = 8.0 nM 8.10
CHEMBL486770 IC50 = 8.0 nM 8.10
CHEMBL471414 IC50 = 9.0 nM 8.05
CHEMBL511797 IC50 = 10.0 nM 8.00
CHEMBL470791 IC50 = 11.0 nM 7.96
CHEMBL471824 IC50 = 11.0 nM 7.96
CHEMBL469950 IC50 = 11.0 nM 7.96
CHEMBL472442 IC50 = 12.0 nM 7.92
CHEMBL511984 IC50 = 13.0 nM 7.89
CHEMBL470147 IC50 = 13.0 nM 7.89
CHEMBL471220 IC50 = 13.0 nM 7.89
CHEMBL470581 IC50 = 14.0 nM 7.85
CHEMBL513027 IC50 = 16.0 nM 7.80
CHEMBL471219 IC50 = 17.0 nM 7.77
CHEMBL472261 IC50 = 17.0 nM 7.77
CHEMBL472251 IC50 = 18.0 nM 7.75
CHEMBL469514 IC50 = 21.0 nM 7.68
CHEMBL472252 IC50 = 22.0 nM 7.66
CHEMBL472443 IC50 = 23.0 nM 7.64
CHEMBL471400 IC50 = 23.0 nM 7.64
CHEMBL521193 IC50 = 27.0 nM 7.57
CHEMBL470798 IC50 = 28.0 nM 7.55
CHEMBL470148 IC50 = 29.0 nM 7.54
CHEMBL470156 IC50 = 36.0 nM 7.44
CHEMBL487346 IC50 = 39.0 nM 7.41
CHEMBL255805 IC50 = 48.0 nM 7.32
CHEMBL269935 IC50 = 58.0 nM 7.24
CHEMBL256440 IC50 = 65.0 nM 7.19
CHEMBL236902 IC50 = 79.0 nM 7.10
CHEMBL486738 IC50 = 89.0 nM 7.05
CHEMBL486737 IC50 = 120.0 nM 6.92
CHEMBL520050 IC50 = 130.0 nM 6.89
CHEMBL499776 IC50 = 160.0 nM 6.80
CHEMBL511625 IC50 = 230.0 nM 6.64
CHEMBL236678 IC50 = 2630.0 nM 5.58