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Assay Detail

CHEMBL4346397

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Binding
Binding affinity to human BRD4 BD2 by isothermal calorimetry analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bromodomain-containing protein 4 (CHEMBL1163125)
Type SINGLE PROTEIN
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
Kd 1 6.87 6.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2393130 APABETALONE 3.0 1 6.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2393130 APABETALONE Kd = 135.0 nM 6.87