Ki Summary

Reaction Details

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Target

Bromodomain-containing protein 4 [42-168]

Ligand

BDBM362673

Substrate/Competitor

n/a

Meas. Tech.

BRD4 AlphaScreen Assay

IC50

<25±n/a nM

Citation

Combs, AP; Sparks, RB Tricyclic heterocycles as bet protein inhibitors US Patent US10227359 Publication Date 3/12/2019

More Info.:

Get all data from this article, Assay Method

Bromodomain-containing protein 4 [42-168]

Name:

Bromodomain-containing protein 4 [42-168]

Synonyms:

BRD4 | BRD4 BD1 (aa 42-168) | BRD4_HUMAN | Bromodomain-containing protein 4 Bromo Domain 1 | HUNK1

Type:

Enzyme Catalytic Domain

Mol. Mass.:

15054.68

Organism:

Homo sapiens (Human)

Description:

O60885[42-168]

Residue:

127

Sequence:

STNPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKII
KTPMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKI
NELPTEE

BDBM362673

n/a

Name

BDBM362673

Synonyms:

(4S)-2-[4-(cyclobutylcarbonyl)piperazin-1- yl]-7-(3,5-dimethylisoxazol-4-yl)-4- pyridin-2-yl-4,5-dihydroimidazo[1,5,4- de][1,4]benzoxazine | US10227359, Example 28 | US10618910, Example 28 | US9834565, Example 28

Type

Small organic molecule

Emp. Form.

C28H30N6O3

Mol. Mass.

498.5762

SMILES

Cc1noc(C)c1-c1ccc2nc(N3CCN(CC3)C(=O)C3CCC3)n3[C@H](COc1c23)c1ccccn1 |wD:26.36,(.39,-5.61,;1.85,-6.08,;2.33,-7.55,;3.87,-7.55,;4.34,-6.08,;5.81,-5.61,;3.1,-5.18,;3.1,-3.64,;4.43,-2.87,;4.43,-1.33,;3.1,-.56,;2.53,.88,;.99,.88,;.22,2.21,;-1.32,2.21,;-2.09,3.55,;-1.32,4.88,;.22,4.88,;.99,3.55,;-2.09,6.21,;-1.32,7.55,;-3.63,6.21,;-4.72,5.12,;-5.81,6.21,;-4.72,7.3,;.43,-.56,;-.9,-1.33,;-.9,-2.87,;.43,-3.64,;1.76,-2.87,;1.76,-1.33,;-2.24,-.56,;-3.57,-1.33,;-4.91,-.56,;-4.91,.98,;-3.57,1.75,;-2.24,.98,)|

Structure