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Assay Detail

CHEMBL5215550

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Binding
Inhibition of human full length FLAG-tagged HDAC2 expressed in baculovirus infected Sf9 cells using BML-KI104 as substrate preincubated for 3 hrs followed by substrate addition measured after 60 mins by modified FLUOR DE LYS assay
ChEMBL ↗
54
Total Activities
54
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 2 (CHEMBL1937) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Ethyl Ketone-Based Highly Selective HDACs 1, 2, 3 Inhibitors for HIV Latency Reactivation with Minimum Cellular Potency Serum Shift and Reduced hERG Activity.
Yu W, Liu J, Clausen D, Yu Y, Duffy JL, Wang M, Xu S, Deng L, Suzuki T, Chung CC, Myers RW, Klein DJ, Fells JI, Holloway MK, Wu J, Wu G, Howell BJ, Barnard RJO, Kozlowski J.
J Med Chem (2021) 64 : 4709 -4729
PubMed 33797924 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 54 8.42 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5220926 — — 1 9.40
CHEMBL5218854 — — 1 9.23
CHEMBL5218537 — — 1 9.22
CHEMBL5219115 — — 1 9.15
CHEMBL5220969 — — 1 9.15
CHEMBL5218918 — — 1 8.96
CHEMBL5218693 — — 1 8.96
CHEMBL5220278 — — 1 8.89
CHEMBL5218586 — — 1 8.85
CHEMBL5220233 — — 1 8.85
CHEMBL4856631 — — 1 8.80
CHEMBL5218767 — — 1 8.70
CHEMBL5220616 — — 1 8.70
CHEMBL5219359 — — 1 8.68
CHEMBL5220715 — — 1 8.66
CHEMBL5219634 — — 1 8.66
CHEMBL5220254 — — 1 8.66
CHEMBL5219039 — — 1 8.64
CHEMBL5219006 — — 1 8.64
CHEMBL5220454 — — 1 8.62
CHEMBL5219590 — — 1 8.60
CHEMBL5219739 — — 1 8.60
CHEMBL5218926 — — 1 8.51
CHEMBL5218535 — — 1 8.51
CHEMBL4862556 — — 1 8.49
CHEMBL5219490 — — 1 8.49
CHEMBL5219969 — — 1 8.48
CHEMBL5219422 — — 1 8.39
CHEMBL5220720 — — 1 8.38
CHEMBL5219338 — — 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5220926 — IC50 = 0.4 nM 9.40
CHEMBL5218854 — IC50 = 0.59 nM 9.23
CHEMBL5218537 — IC50 = 0.6 nM 9.22
CHEMBL5219115 — IC50 = 0.7 nM 9.15
CHEMBL5220969 — IC50 = 0.7 nM 9.15
CHEMBL5218918 — IC50 = 1.1 nM 8.96
CHEMBL5218693 — IC50 = 1.1 nM 8.96
CHEMBL5220278 — IC50 = 1.3 nM 8.89
CHEMBL5218586 — IC50 = 1.4 nM 8.85
CHEMBL5220233 — IC50 = 1.4 nM 8.85
CHEMBL4856631 — IC50 = 1.6 nM 8.80
CHEMBL5218767 — IC50 = 2.0 nM 8.70
CHEMBL5220616 — IC50 = 2.0 nM 8.70
CHEMBL5219359 — IC50 = 2.1 nM 8.68
CHEMBL5220254 — IC50 = 2.2 nM 8.66
CHEMBL5220715 — IC50 = 2.2 nM 8.66
CHEMBL5219634 — IC50 = 2.2 nM 8.66
CHEMBL5219039 — IC50 = 2.3 nM 8.64
CHEMBL5219006 — IC50 = 2.3 nM 8.64
CHEMBL5220454 — IC50 = 2.4 nM 8.62
CHEMBL5219590 — IC50 = 2.5 nM 8.60
CHEMBL5219739 — IC50 = 2.5 nM 8.60
CHEMBL5218926 — IC50 = 3.1 nM 8.51
CHEMBL5218535 — IC50 = 3.1 nM 8.51
CHEMBL5219490 — IC50 = 3.2 nM 8.49
CHEMBL4862556 — IC50 = 3.2 nM 8.49
CHEMBL5219969 — IC50 = 3.3 nM 8.48
CHEMBL5219422 — IC50 = 4.1 nM 8.39
CHEMBL5220720 — IC50 = 4.2 nM 8.38
CHEMBL5219338 — IC50 = 5.0 nM 8.30
CHEMBL5220408 — IC50 = 5.1 nM 8.29
CHEMBL5218980 — IC50 = 5.4 nM 8.27
CHEMBL4745088 — IC50 = 5.8 nM 8.24
CHEMBL5219978 — IC50 = 5.9 nM 8.23
CHEMBL5219241 — IC50 = 9.9 nM 8.00
CHEMBL5220815 — IC50 = 11.0 nM 7.96
CHEMBL5219118 — IC50 = 13.0 nM 7.89
CHEMBL5218651 — IC50 = 14.0 nM 7.85
CHEMBL5220576 — IC50 = 16.0 nM 7.80
CHEMBL5221068 — IC50 = 19.0 nM 7.72
CHEMBL5220120 — IC50 = 23.0 nM 7.64
CHEMBL5218487 — IC50 = 30.0 nM 7.52
CHEMBL5219074 — IC50 = 34.0 nM 7.47
CHEMBL5219811 — IC50 = 35.0 nM 7.46
CHEMBL5218749 — IC50 = 41.0 nM 7.39
CHEMBL5221097 — IC50 = 44.0 nM 7.36
CHEMBL5218556 — IC50 < 1.5 nM -
CHEMBL5218553 — IC50 < 1.5 nM -
CHEMBL5220360 — IC50 < 0.3 nM -
CHEMBL5219875 — IC50 < 0.3 nM -