Reaction Details Report a problem with these data
Target
Bromodomain-containing protein 4 [44-166,Y139F]
Ligand
BDBM50365262
Substrate
n/a
Meas. Tech.
TR-FRET Competition Assay
pH
7.5±0
Temperature
277.15±0 K
Kd
61.3±16.5 nM
Citation
Jung, M; Philpott, M; Müller, S; Schulze, J; Badock, V; Eberspächer, U; Moosmayer, D; Bader, B; Schmees, N; Fernández-Montalván, A; Haendler, B Affinity map of bromodomain protein 4 (BRD4) interactions with the histone H4 tail and the small molecule inhibitor JQ1. J Biol Chem 289:9304-19 (2014) [PubMed] Article
More Info.:
Target
Name:
Bromodomain-containing protein 4 [44-166,Y139F]
Synonyms:
BRD4 | BRD4_HUMAN | Bromodomain protein 4 bromodomain 1 (BRD4 BD1 Y139F) | HUNK1
Type:
Protein
Mol. Mass.:
14594.28
Organism:
Homo sapiens (Human)
Description:
Human BRD4 BD1 (44-166 aa) Y139F mutant
Residue:
123
Sequence:
NPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIFNKPGDDIVLMAEALEKLFLQKINELPT
Inhibitor
Name:
BDBM50365262
Synonyms:
(+)-JQ1 | (S)-JQ1 (1) | CHEMBL1957266 | JQ1 | US10124009, Compound (S)-JQ1 | US10202360, Example JQ-1 | US10308662, Compound JQ-1 | US10407441, Compound (S)-JQ1 | US10617680, Example JQ-1 | US10881668, Compound JQ1 | US10925881, Name (S)-JQ1 | US11020380, Example JQ-1 | US11078188, Example (+)-JQ1 | US11279703, TABLE 6.180 | US11427593, Compound JQ1 | US11466034, Example (+)-JQ1 | US9320741, (S)-JQ1 | US9695172, JQ1
Type:
Small organic molecule
Emp. Form.:
C23H25ClN4O2S
Mol. Mass.:
456.988
SMILES:
Cc1nnc2[C@H](CC(=O)OC(C)(C)C)N=C(c3c(C)c(C)sc3-n12)c1ccc(Cl)cc1 |r,c:14|