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Assay Detail

CHEMBL5215554

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

Functional
Induction of HIV latency reactivation in Jurkat 2C4 cells assessed as reactivation of quiescent HIV provirus incubated for 15 mins in presence of 0.1 % normal human serum by Steady-Glo Luciferase Assay System
54
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Jurkat
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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
EC50 54 7.04 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5220926 1 8.22
CHEMBL5219825 1 8.15
CHEMBL5219294 1 8.10
CHEMBL5219875 1 8.00
CHEMBL5220360 1 7.96
CHEMBL5219409 1 7.77
CHEMBL5219739 1 7.72
CHEMBL5218854 1 7.62
CHEMBL5218553 1 7.62
CHEMBL5218693 1 7.58
CHEMBL5218537 1 7.58
CHEMBL5218556 1 7.57
CHEMBL5220254 1 7.52
CHEMBL5220233 1 7.50
CHEMBL5219115 1 7.47
CHEMBL5218651 1 7.46
CHEMBL5218586 1 7.43
CHEMBL5220278 1 7.41
CHEMBL5219634 1 7.38
CHEMBL5219422 1 7.30
CHEMBL5218926 1 7.29
CHEMBL5219006 1 7.22
CHEMBL5219490 1 7.21
CHEMBL5218918 1 7.21
CHEMBL5220616 1 7.19
CHEMBL5218767 1 7.07
CHEMBL5220715 1 7.04
CHEMBL5219039 1 7.03
CHEMBL5219359 1 7.01
CHEMBL4856631 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5220926 EC50 = 6.0 nM 8.22
CHEMBL5219825 EC50 = 7.0 nM 8.15
CHEMBL5219294 EC50 = 8.0 nM 8.10
CHEMBL5219875 EC50 = 10.0 nM 8.00
CHEMBL5220360 EC50 = 11.0 nM 7.96
CHEMBL5219409 EC50 = 17.0 nM 7.77
CHEMBL5219739 EC50 = 19.0 nM 7.72
CHEMBL5218854 EC50 = 24.0 nM 7.62
CHEMBL5218553 EC50 = 24.0 nM 7.62
CHEMBL5218693 EC50 = 26.0 nM 7.58
CHEMBL5218537 EC50 = 26.0 nM 7.58
CHEMBL5218556 EC50 = 27.0 nM 7.57
CHEMBL5220254 EC50 = 30.0 nM 7.52
CHEMBL5220233 EC50 = 32.0 nM 7.50
CHEMBL5219115 EC50 = 34.0 nM 7.47
CHEMBL5218651 EC50 = 35.0 nM 7.46
CHEMBL5218586 EC50 = 37.0 nM 7.43
CHEMBL5220278 EC50 = 39.0 nM 7.41
CHEMBL5219634 EC50 = 42.0 nM 7.38
CHEMBL5219422 EC50 = 50.0 nM 7.30
CHEMBL5218926 EC50 = 51.0 nM 7.29
CHEMBL5219006 EC50 = 60.0 nM 7.22
CHEMBL5219490 EC50 = 62.0 nM 7.21
CHEMBL5218918 EC50 = 61.0 nM 7.21
CHEMBL5220616 EC50 = 65.0 nM 7.19
CHEMBL5218767 EC50 = 85.0 nM 7.07
CHEMBL5220715 EC50 = 91.0 nM 7.04
CHEMBL5219039 EC50 = 93.0 nM 7.03
CHEMBL5219359 EC50 = 98.0 nM 7.01
CHEMBL4856631 EC50 = 100.0 nM 7.00
CHEMBL4862556 EC50 = 120.0 nM 6.92
CHEMBL5218535 EC50 = 120.0 nM 6.92
CHEMBL5220969 EC50 = 120.0 nM 6.92
CHEMBL5220720 EC50 = 130.0 nM 6.89
CHEMBL5220454 EC50 = 130.0 nM 6.89
CHEMBL5220844 EC50 = 140.0 nM 6.85
CHEMBL5219969 EC50 = 140.0 nM 6.85
CHEMBL5220408 EC50 = 160.0 nM 6.80
CHEMBL5219118 EC50 = 190.0 nM 6.72
CHEMBL5219338 EC50 = 210.0 nM 6.68
CHEMBL5219978 EC50 = 210.0 nM 6.68
CHEMBL5220815 EC50 = 220.0 nM 6.66
CHEMBL5221068 EC50 = 220.0 nM 6.66
CHEMBL4745088 EC50 = 250.0 nM 6.60
CHEMBL5218980 EC50 = 260.0 nM 6.58
CHEMBL5218487 EC50 = 280.0 nM 6.55
CHEMBL5220120 EC50 = 310.0 nM 6.51
CHEMBL5220576 EC50 = 480.0 nM 6.32
CHEMBL5219811 EC50 = 760.0 nM 6.12
CHEMBL5221097 EC50 = 970.0 nM 6.01