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Assay Detail

CHEMBL4346336

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

Functional
Antiproliferative activity against human SKM1 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

SKM-1 (CHEMBL2366085)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of <i>N</i>-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1<i>H</i>-pyrrolo[2,3-<i>c</i>]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain.
Sheppard GS, Wang L, Fidanze SD, Hasvold LA, Liu D, Pratt JK, Park CH, Longenecker K, Qiu W, Torrent M, Kovar PJ, Bui M, Faivre E, Huang X, Lin X, Wilcox D, Zhang L, Shen Y, Albert DH, Magoc TJ, Rajaraman G, Kati WM, McDaniel KF.
J Med Chem (2020) 63 : 5585 -5623
PubMed 32324999 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 7.70 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4529861 1 8.77
CHEMBL4454614 1 8.60
CHEMBL4461291 1 8.59
CHEMBL4470856 1 8.48
CHEMBL4548794 1 8.48
CHEMBL4435166 1 8.46
CHEMBL4465299 1 8.38
CHEMBL4462804 1 8.28
CHEMBL4555714 1 8.21
CHEMBL4469571 1 8.21
CHEMBL3915707 1 8.18
CHEMBL4297454 ABBV-744 1.0 1 8.17
CHEMBL4455576 1 8.17
CHEMBL4471851 1 8.15
CHEMBL4539875 1 8.02
CHEMBL4434761 1 8.01
CHEMBL3964225 1 8.00
CHEMBL4452278 1 8.00
CHEMBL4483338 1 7.96
CHEMBL4467038 1 7.96
CHEMBL4552305 1 7.89
CHEMBL4461289 1 7.85
CHEMBL4589568 1 7.85
CHEMBL4442074 1 7.85
CHEMBL4449740 1 7.72
CHEMBL4564879 1 7.70
CHEMBL4555653 1 7.68
CHEMBL4443563 1 7.64
CHEMBL4586647 1 7.62
CHEMBL4587188 1 7.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4529861 IC50 = 1.7 nM 8.77
CHEMBL4454614 IC50 = 2.5 nM 8.60
CHEMBL4461291 IC50 = 2.6 nM 8.59
CHEMBL4470856 IC50 = 3.3 nM 8.48
CHEMBL4548794 IC50 = 3.3 nM 8.48
CHEMBL4435166 IC50 = 3.5 nM 8.46
CHEMBL4465299 IC50 = 4.2 nM 8.38
CHEMBL4462804 IC50 = 5.2 nM 8.28
CHEMBL4555714 IC50 = 6.2 nM 8.21
CHEMBL4469571 IC50 = 6.2 nM 8.21
CHEMBL3915707 IC50 = 6.6 nM 8.18
CHEMBL4297454 ABBV-744 IC50 = 6.7 nM 8.17
CHEMBL4455576 IC50 = 6.7 nM 8.17
CHEMBL4471851 IC50 = 7.0 nM 8.15
CHEMBL4539875 IC50 = 9.5 nM 8.02
CHEMBL4434761 IC50 = 9.8 nM 8.01
CHEMBL3964225 IC50 = 10.0 nM 8.00
CHEMBL4452278 IC50 = 10.0 nM 8.00
CHEMBL4483338 IC50 = 11.0 nM 7.96
CHEMBL4467038 IC50 = 11.0 nM 7.96
CHEMBL4552305 IC50 = 13.0 nM 7.89
CHEMBL4461289 IC50 = 14.0 nM 7.85
CHEMBL4589568 IC50 = 14.0 nM 7.85
CHEMBL4442074 IC50 = 14.0 nM 7.85
CHEMBL4449740 IC50 = 19.0 nM 7.72
CHEMBL4564879 IC50 = 20.0 nM 7.70
CHEMBL4555653 IC50 = 21.0 nM 7.68
CHEMBL4443563 IC50 = 23.0 nM 7.64
CHEMBL4586647 IC50 = 24.0 nM 7.62
CHEMBL4587188 IC50 = 24.0 nM 7.62
CHEMBL4455214 IC50 = 25.0 nM 7.60
CHEMBL4464739 IC50 = 26.0 nM 7.58
CHEMBL4547415 IC50 = 28.0 nM 7.55
CHEMBL4454597 IC50 = 31.0 nM 7.51
CHEMBL4560574 IC50 = 34.0 nM 7.47
CHEMBL4440089 IC50 = 37.0 nM 7.43
CHEMBL4466931 IC50 = 42.0 nM 7.38
CHEMBL4533567 IC50 = 50.0 nM 7.30
CHEMBL4590365 IC50 = 50.0 nM 7.30
CHEMBL4551285 IC50 = 56.0 nM 7.25
CHEMBL4554545 IC50 = 65.0 nM 7.19
CHEMBL4521111 IC50 = 66.0 nM 7.18
CHEMBL4568610 IC50 = 68.0 nM 7.17
CHEMBL4584480 IC50 = 80.0 nM 7.10
CHEMBL4548127 IC50 = 110.0 nM 6.96
CHEMBL4453740 IC50 = 150.0 nM 6.82
CHEMBL4452861 IC50 = 290.0 nM 6.54
CHEMBL4457805 IC50 = 1300.0 nM 5.89
CHEMBL4579396 IC50 = 3100.0 nM 5.51