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Assay Detail

CHEMBL4051109

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Functional
Antiproliferative activity against human MX1 cells after 72 hrs by Cell Titer Glo assay
ChEMBL ↗
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MX1
Confidence 1 — Organism
Curated By Autocuration

Target

MX1 (CHEMBL613704) ↗
Type CELL-LINE
Organism Homo sapiens

Publication

Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors.
Wang L, Pratt JK, Soltwedel T, Sheppard GS, Fidanze SD, Liu D, Hasvold LA, Mantei RA, Holms JH, McClellan WJ, Wendt MD, Wada C, Frey R, Hansen TM, Hubbard R, Park CH, Li L, Magoc TJ, Albert DH, Lin X, Warder SE, Kovar P, Huang X, Wilcox D, Wang R, Rajaraman G, Petros AM, Hutchins CW, Panchal SC, Sun C, Elmore SW, Shen Y, Kati WM, McDaniel KF.
J Med Chem (2017) 60 : 3828 -3850
PubMed 28368119 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 39 7.14 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4068431 — — 1 8.38
CHEMBL4078875 — — 1 8.33
CHEMBL4099010 — — 1 8.25
CHEMBL4075776 — — 1 8.24
CHEMBL4073279 — — 1 8.24
CHEMBL4068991 — — 1 8.16
CHEMBL4090068 — — 1 8.00
CHEMBL4075567 — — 1 7.89
CHEMBL4094644 — — 1 7.80
CHEMBL4103153 — — 1 7.80
CHEMBL4063808 — — 1 7.80
CHEMBL4091597 — — 1 7.75
CHEMBL4089651 — — 1 7.72
CHEMBL4082889 — — 1 7.62
CHEMBL4077124 — — 1 7.62
CHEMBL4083186 — — 1 7.60
CHEMBL4093439 — — 1 7.52
CHEMBL4059680 — — 1 7.50
CHEMBL4075757 — — 1 7.48
CHEMBL4071697 — — 1 7.40
CHEMBL4099335 — — 1 7.33
CHEMBL4061006 — — 1 7.30
CHEMBL4101823 — — 1 7.28
CHEMBL4083819 — — 1 7.21
CHEMBL4078459 — — 1 6.92
CHEMBL4091093 — — 1 6.89
CHEMBL4102713 — — 1 6.85
CHEMBL4090979 — — 1 6.85
CHEMBL4072399 — — 1 6.60
CHEMBL4063083 — — 1 6.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4068431 — EC50 = 4.2 nM 8.38
CHEMBL4078875 — EC50 = 4.7 nM 8.33
CHEMBL4099010 — EC50 = 5.6 nM 8.25
CHEMBL4075776 — EC50 = 5.7 nM 8.24
CHEMBL4073279 — EC50 = 5.7 nM 8.24
CHEMBL4068991 — EC50 = 6.9 nM 8.16
CHEMBL4090068 — EC50 = 10.0 nM 8.00
CHEMBL4075567 — EC50 = 13.0 nM 7.89
CHEMBL4094644 — EC50 = 16.0 nM 7.80
CHEMBL4103153 — EC50 = 16.0 nM 7.80
CHEMBL4063808 — EC50 = 16.0 nM 7.80
CHEMBL4091597 — EC50 = 18.0 nM 7.75
CHEMBL4089651 — EC50 = 19.0 nM 7.72
CHEMBL4082889 — EC50 = 24.0 nM 7.62
CHEMBL4077124 — EC50 = 24.0 nM 7.62
CHEMBL4083186 — EC50 = 25.0 nM 7.60
CHEMBL4093439 — EC50 = 30.0 nM 7.52
CHEMBL4059680 — EC50 = 32.0 nM 7.50
CHEMBL4075757 — EC50 = 33.0 nM 7.48
CHEMBL4071697 — EC50 = 40.0 nM 7.40
CHEMBL4099335 — EC50 = 47.0 nM 7.33
CHEMBL4061006 — EC50 = 50.0 nM 7.30
CHEMBL4101823 — EC50 = 53.0 nM 7.28
CHEMBL4083819 — EC50 = 62.0 nM 7.21
CHEMBL4078459 — EC50 = 120.0 nM 6.92
CHEMBL4091093 — EC50 = 130.0 nM 6.89
CHEMBL4102713 — EC50 = 140.0 nM 6.85
CHEMBL4090979 — EC50 = 140.0 nM 6.85
CHEMBL4072399 — EC50 = 250.0 nM 6.60
CHEMBL4063083 — EC50 = 710.0 nM 6.15
CHEMBL4101187 — EC50 = 710.0 nM 6.15
CHEMBL4072862 — EC50 = 730.0 nM 6.14
CHEMBL4099746 — EC50 = 1300.0 nM 5.89
CHEMBL4070131 — EC50 = 1500.0 nM 5.82
CHEMBL4092002 — EC50 = 4300.0 nM 5.37
CHEMBL4061472 — EC50 = 4500.0 nM 5.35
CHEMBL4064267 — EC50 = 7200.0 nM 5.14
CHEMBL4083304 — EC50 = 13000.0 nM 4.89
CHEMBL4072714 — EC50 > 3000.0 nM -