GNE-886

Names

[ CAS No. ]:
2101957-05-3

[ Name ]:
GNE-886

[Synonym ]:
1H-Pyrrolo[2,3-c]pyridine-4-carboxamide, 6,7-dihydro-N-[1-[6-(3-methoxyphenyl)-4-pyrimidinyl]-4-piperidinyl]-N-methyl-7-oxo-6-(2-propen-1-yl)-
MFCD31556840
6-Allyl-N-{1-[6-(3-methoxyphenyl)-4-pyrimidinyl]-4-piperidinyl}-N-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-4-carboxamide

Biological Activity

[Description]:

GNE-886 is a potent and selective CECR2 bromodomain inhibitor with IC50 of 16 nM; shows a wide selectivity over the 40 bromodomains, >100-fold selectivity over BRD9, BRD7, TAF1(2), and BRD4(1); has a highly favorable measured kinetic solubility of 122 uM and is an appropriate in vitro tool compound for the CECR2 bromodomain.

[References]

References 1. Crawford TD, et al. ACS Med Chem Lett. 2017 Jun 1;8(7):737-741. View Related Products by Target Bromodomain

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
796.3±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₈H₃₀N₆O₃

[ Molecular Weight ]:
498.576

[ Flash Point ]:
435.4±32.9 °C

[ Exact Mass ]:
498.237946

[ LogP ]:
1.99

[ Vapour Pressure ]:
0.0±2.8 mmHg at 25°C

[ Index of Refraction ]:
1.675

Related Compounds

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