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Assay Detail

CHEMBL4020218

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Functional
Antiproliferative activity against human MX1 cells after 72 hrs by Cell Titer Glo assay
32
Total Activities
32
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

Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.
McDaniel KF, Wang L, Soltwedel T, Fidanze SD, Hasvold LA, Liu D, Mantei RA, Pratt JK, Sheppard GS, Bui MH, Faivre EJ, Huang X, Li L, Lin X, Wang R, Warder SE, Wilcox D, Albert DH, Magoc TJ, Rajaraman G, Park CH, Hutchins CW, Shen JJ, Edalji RP, Sun CC, Martin R, Gao W, Wong S, Fang G, Elmore SW, Shen Y, Kati WM.
J Med Chem (2017) 60 : 8369 -8384
PubMed 28949521 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 32 7.20 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3933555 1 8.10
CHEMBL3987016 MIVEBRESIB 2.0 1 7.89
CHEMBL3898684 1 7.85
CHEMBL3948433 1 7.85
CHEMBL3970220 1 7.80
CHEMBL3933860 1 7.77
CHEMBL3911104 1 7.72
CHEMBL4098055 1 7.66
CHEMBL3901761 1 7.57
CHEMBL3974260 1 7.54
CHEMBL4059602 1 7.52
CHEMBL3904317 1 7.51
CHEMBL3942897 1 7.47
CHEMBL3889757 1 7.34
CHEMBL3928793 1 7.34
CHEMBL3973984 1 7.28
CHEMBL3980661 1 7.25
CHEMBL3898479 1 7.19
CHEMBL3926000 1 7.14
CHEMBL3963357 1 7.11
CHEMBL4060619 1 7.08
CHEMBL4061028 1 7.07
CHEMBL3964603 1 6.96
CHEMBL3914893 1 6.92
CHEMBL3967185 1 6.89
CHEMBL3919590 1 6.89
CHEMBL4089203 1 6.68
CHEMBL1957266 1 6.59
CHEMBL3980983 1 6.26
CHEMBL4082851 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3933555 EC50 = 7.9 nM 8.10
CHEMBL3987016 MIVEBRESIB EC50 = 13.0 nM 7.89
CHEMBL3898684 EC50 = 14.0 nM 7.85
CHEMBL3948433 EC50 = 14.0 nM 7.85
CHEMBL3970220 EC50 = 16.0 nM 7.80
CHEMBL3933860 EC50 = 17.0 nM 7.77
CHEMBL3911104 EC50 = 19.0 nM 7.72
CHEMBL4098055 EC50 = 22.0 nM 7.66
CHEMBL3901761 EC50 = 27.0 nM 7.57
CHEMBL3974260 EC50 = 29.0 nM 7.54
CHEMBL4059602 EC50 = 30.0 nM 7.52
CHEMBL3904317 EC50 = 31.0 nM 7.51
CHEMBL3942897 EC50 = 34.0 nM 7.47
CHEMBL3889757 EC50 = 46.0 nM 7.34
CHEMBL3928793 EC50 = 46.0 nM 7.34
CHEMBL3973984 EC50 = 52.0 nM 7.28
CHEMBL3980661 EC50 = 56.0 nM 7.25
CHEMBL3898479 EC50 = 65.0 nM 7.19
CHEMBL3926000 EC50 = 72.0 nM 7.14
CHEMBL3963357 EC50 = 77.0 nM 7.11
CHEMBL4060619 EC50 = 83.0 nM 7.08
CHEMBL4061028 EC50 = 86.0 nM 7.07
CHEMBL3964603 EC50 = 110.0 nM 6.96
CHEMBL3914893 EC50 = 120.0 nM 6.92
CHEMBL3967185 EC50 = 130.0 nM 6.89
CHEMBL3919590 EC50 = 130.0 nM 6.89
CHEMBL4089203 EC50 = 210.0 nM 6.68
CHEMBL1957266 EC50 = 254.0 nM 6.59
CHEMBL3980983 EC50 = 550.0 nM 6.26
CHEMBL4082851 EC50 = 2400.0 nM 5.62
CHEMBL4088769 EC50 = 4800.0 nM 5.32
CHEMBL4100828 EC50 > 5000.0 nM -