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Assay Detail

CHEMBL5326944

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Functional
Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo assay
ChEMBL ↗
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type THP-1
Confidence 1 — Organism
Curated By Autocuration

Target

THP-1 (CHEMBL614245) ↗
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of novel, potent, and orally bioavailable HDACs inhibitors with LSD1 inhibitory activity for the treatment of solid tumors.
Duan Y, Yu T, Jin L, Zhang S, Shi X, Zhang Y, Zhou N, Xu Y, Lu W, Zhou H, Zhu H, Bai S, Hu K, Guan Y.
Eur J Med Chem (2023) 254 : 115367 -115367
PubMed 37086699 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 5.69 6.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5433364 — — 1 6.51
CHEMBL5434546 — — 1 6.36
CHEMBL5435925 — — 1 6.33
CHEMBL5440196 — — 1 6.11
CHEMBL5440032 — — 1 6.00
CHEMBL5406191 — — 1 5.97
CHEMBL5406759 — — 1 5.92
CHEMBL5436035 — — 1 5.91
CHEMBL5419295 — — 1 5.89
CHEMBL5406671 — — 1 5.86
CHEMBL5418093 — — 1 5.82
CHEMBL5428176 — — 1 5.82
CHEMBL5429412 — — 1 5.80
CHEMBL5435026 — — 1 5.80
CHEMBL5416264 — — 1 5.77
CHEMBL5413316 — — 1 5.76
CHEMBL5403862 — — 1 5.70
CHEMBL5437604 — — 1 5.67
CHEMBL5424948 — — 1 5.54
CHEMBL98 VORINOSTAT 4.0 1 5.54
CHEMBL5420493 — — 1 5.49
CHEMBL5401496 — — 1 5.47
CHEMBL5403602 — — 1 5.47
CHEMBL5399635 — — 1 5.46
CHEMBL5432401 — — 1 5.45
CHEMBL5407947 — — 1 5.43
CHEMBL5428924 — — 1 5.36
CHEMBL5407953 — — 1 5.28
CHEMBL5424227 — — 1 5.19
CHEMBL5420359 — — 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5433364 — IC50 = 310.0 nM 6.51
CHEMBL5434546 — IC50 = 440.0 nM 6.36
CHEMBL5435925 — IC50 = 470.0 nM 6.33
CHEMBL5440196 — IC50 = 770.0 nM 6.11
CHEMBL5440032 — IC50 = 990.0 nM 6.00
CHEMBL5406191 — IC50 = 1070.0 nM 5.97
CHEMBL5406759 — IC50 = 1190.0 nM 5.92
CHEMBL5436035 — IC50 = 1240.0 nM 5.91
CHEMBL5419295 — IC50 = 1280.0 nM 5.89
CHEMBL5406671 — IC50 = 1380.0 nM 5.86
CHEMBL5418093 — IC50 = 1510.0 nM 5.82
CHEMBL5428176 — IC50 = 1520.0 nM 5.82
CHEMBL5435026 — IC50 = 1590.0 nM 5.80
CHEMBL5429412 — IC50 = 1590.0 nM 5.80
CHEMBL5416264 — IC50 = 1710.0 nM 5.77
CHEMBL5413316 — IC50 = 1750.0 nM 5.76
CHEMBL5403862 — IC50 = 1980.0 nM 5.70
CHEMBL5437604 — IC50 = 2120.0 nM 5.67
CHEMBL5424948 — IC50 = 2890.0 nM 5.54
CHEMBL98 VORINOSTAT IC50 = 2900.0 nM 5.54
CHEMBL5420493 — IC50 = 3220.0 nM 5.49
CHEMBL5401496 — IC50 = 3420.0 nM 5.47
CHEMBL5403602 — IC50 = 3380.0 nM 5.47
CHEMBL5399635 — IC50 = 3470.0 nM 5.46
CHEMBL5432401 — IC50 = 3520.0 nM 5.45
CHEMBL5407947 — IC50 = 3670.0 nM 5.43
CHEMBL5428924 — IC50 = 4350.0 nM 5.36
CHEMBL5407953 — IC50 = 5200.0 nM 5.28
CHEMBL5424227 — IC50 = 6480.0 nM 5.19
CHEMBL5420359 — IC50 = 6870.0 nM 5.16
CHEMBL5424063 — IC50 = 8350.0 nM 5.08
CHEMBL5409400 — IC50 = 9570.0 nM 5.02
CHEMBL5412547 — IC50 > 10000.0 nM -
CHEMBL5429127 — IC50 > 10000.0 nM -
CHEMBL5419239 — IC50 - — -
CHEMBL5413744 — IC50 > 10000.0 nM -
CHEMBL5429228 — IC50 > 10000.0 nM -
CHEMBL5439488 — IC50 > 10000.0 nM -
CHEMBL5431560 — IC50 > 10000.0 nM -
CHEMBL5417682 — IC50 > 10000.0 nM -
CHEMBL5440160 — IC50 > 10000.0 nM -
CHEMBL3781751 IADADEMSTAT IC50 > 50000.0 nM -
CHEMBL5433627 — IC50 > 10000.0 nM -
CHEMBL5404035 — IC50 > 10000.0 nM -
CHEMBL5416658 — IC50 - — -
CHEMBL5426091 — IC50 - — -