Fused bi-heteroaryl substituted hydantoin compounds as TACE inhibitors
Copyright policy ) Ling Tong; Seong Heon Kim; Kristin Rosner; Wensheng Yu; Bandarpalle B. Shankar; Lei Chen; Dansu Li; +15 Authors
Ling Tong; Seong Heon Kim; Kristin Rosner; Wensheng Yu; Bandarpalle B. Shankar; Lei Chen; Dansu Li; Chaoyang Dai; Vinay Girijavallabhan; Janeta Popovici-Muller; Liping Yang; Guowei Zhou; Aneta Kosinski; M. Arshad Siddiqui; Neng-Yang Shih; Zhuyan Guo; Peter Orth; Shiying Chen; Daniel Lundell; Xiaoda Niu; Shelby Umland; Joseph A. Kozlowski;
Fused bi-heteroaryl substituted hydantoin compounds as TACE inhibitors
We have identified a series of hydantoin-derived TNF-a converting enzyme (TACE) inhibitors containing a pendant fused bi-heteroaryl group, which demonstrate sub-nanomolar potency (Ki), excellent activity in human whole blood assay, and improved DMPK profiles over prior series.
- Merck & Co. United States
- University of California, San Diego United States
Hydantoins, Haplorhini, ADAM17 Protein, Rats, Enzyme Activation, Structure-Activity Relationship, Dogs, ROC Curve, Area Under Curve, Animals, Humans, Protease Inhibitors, Half-Life
Hydantoins, Haplorhini, ADAM17 Protein, Rats, Enzyme Activation, Structure-Activity Relationship, Dogs, ROC Curve, Area Under Curve, Animals, Humans, Protease Inhibitors, Half-Life
citations This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).9 popularity This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.Top 10% influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).Average impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.Average
citations
Citations provided by BIP!
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
Citations provided by BIP!popularityPopularity provided by BIP!
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
Popularity provided by BIP! 9
Top 10%
Average
Average
