PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 26141771-12 2015 The amides showed highly improved hERG (functional IC50 >30 muM) profile. Amides 4-10 ETS transcription factor ERG Homo sapiens 34-38 26804230-2 2016 Herein we describe our work to eliminate this hERG activity via alteration of the substituents on the benzoic amide functionality. Amides 110-115 ETS transcription factor ERG Homo sapiens 46-50 20570511-3 2010 These studies led to the discovery of amide 24 which showed good c-Met inhibitory potency, low affinity to hERG and favorable pharmacokinetic properties in rats. Amides 38-43 ETS transcription factor ERG Homo sapiens 107-111 24486132-1 2014 Discovery of CXCR3 antagonists substituted with heterocycles as amide surrogates: improved PK, hERG and metabolic profiles. Amides 64-69 ETS transcription factor ERG Homo sapiens 95-99 24412109-2 2014 Among the structurally modified compounds we designed, compounds 5 and 6, which incorporate amides in place of the original compound"s amines, most appreciably alleviated hERG toxicity while maintaining T-type calcium channel blocking activity. Amides 92-98 ETS transcription factor ERG Homo sapiens 171-175 21515049-2 2011 In continuation of our research in this area, macrocyclic amides and lactams were explored to reduce the risk of hERG liabilities. Amides 58-64 ETS transcription factor ERG Homo sapiens 113-117 20684603-2 2010 Further study revealed that by replacing the aryl substitution on the imidazole ring with a more polar carboxylic ester or amide, these compounds displayed not only increased DPP4 binding activity but also significantly reduced human ether-a-go-go related gene (hERG) and sodium channel inhibitory activities. Amides 123-128 ETS transcription factor ERG Homo sapiens 262-266 21414780-4 2011 Increasing the acidity of the amide proton by converting the benzamide in lead 1 to an anilide provided single digit nanomolar MCHR1 antagonists while replacing the dimethoxyphenyl ring of 1 with alkyl groups possessing increased polarity dramatically reduced the hERG inhibition. Amides 30-35 ETS transcription factor ERG Homo sapiens 264-268 34413963-2 2021 Among 46 analogues tested, compounds 21, 30, and 33 displayed high activities against asexual blood stage parasites (PfNF54 IC50 = 0.025-0.043 muM), whereas amide compound 46 additionally showed activity against late-stage gametocytes (stage IV/V; PfLG IC50 = 0.6 +- 0.1 muM) and 860-fold higher selectivity over hERG (46, SI = 43) compared to AST. Amides 157-162 ETS transcription factor ERG Homo sapiens 313-317 19821563-3 2009 As the substituent on the amide was increased in lipophilicity the potency and hERG inhibition increased, while polar groups lowered potency, without significantly impacting hERG inhibition. Amides 26-31 ETS transcription factor ERG Homo sapiens 79-83