PMID-sentid	Pub_year	Sent_text	compound_name	comp_offset	prot_official_name	organism	prot_offset
11160632-0	2001	A common mechanism for cystic fibrosis transmembrane conductance regulator protein activation by genistein and benzimidazolone analogs.	benzimidazolone	111-126	CF transmembrane conductance regulator	Homo sapiens	23-74
11160632-1	2001	We have investigated the mechanism of action of two benzimidazolone analogs (NS004 and NS1619) on DeltaF508-CFTR using both whole-cell and cell-attached patch-clamp techniques and compared their effects with those of genistein.	benzimidazolone	52-67	CF transmembrane conductance regulator	Homo sapiens	108-112
11160632-4	2001	From our studies with the double mutant DeltaF508/K1250A-CFTR, we conclude that benzimidazolone analogs and genistein rectify the DeltaF508-CFTR prolonged closed time independent of their effects on channel open time, since these agonists enhance DeltaF508/K1250A-CFTR activity by shortening the channel closed time.	benzimidazolone	80-95	CF transmembrane conductance regulator	Homo sapiens	57-61
11160632-4	2001	From our studies with the double mutant DeltaF508/K1250A-CFTR, we conclude that benzimidazolone analogs and genistein rectify the DeltaF508-CFTR prolonged closed time independent of their effects on channel open time, since these agonists enhance DeltaF508/K1250A-CFTR activity by shortening the channel closed time.	benzimidazolone	80-95	CF transmembrane conductance regulator	Homo sapiens	140-144
11160632-4	2001	From our studies with the double mutant DeltaF508/K1250A-CFTR, we conclude that benzimidazolone analogs and genistein rectify the DeltaF508-CFTR prolonged closed time independent of their effects on channel open time, since these agonists enhance DeltaF508/K1250A-CFTR activity by shortening the channel closed time.	benzimidazolone	80-95	CF transmembrane conductance regulator	Homo sapiens	140-144
11160649-5	2001	Structure activity studies with 30 benzimidazolone derivatives revealed that ethyl and hydrogen groups at the 1 and 3 nitrogen positions, respectively, were critical for the activation of hIK1 K+ channels and that other alkyl groups were not tolerated at these positions without some loss in potency.	benzimidazolone	35-50	IKAROS family zinc finger 1	Homo sapiens	188-192
9922378-14	1999	Compounds that increase the activity of CFTR include the alkylxanthines, phosphodiesterase inhibitors, phosphatase inhibitors, isoflavones and flavones, benzimidazolones, and psoralens.	benzimidazolone	153-169	CF transmembrane conductance regulator	Homo sapiens	40-44
10704921-10	2000	These results indicate that apical membrane insertion of Cl(-) channel-forming peptides such as C-K4-M2GlyR and direct activation of basolateral K(+) channels with benzimidazolones may coordinate the apical Cl(-) conductance and the basolateral K(+) conductance, thereby providing a pharmacological approach to modulating Cl(-) and fluid secretion by human epithelia deficient in cystic fibrosis transmembrane conductance regulator Cl(-) channels.	benzimidazolone	164-180	CF transmembrane conductance regulator	Homo sapiens	380-431
31889499-3	2020	OBJECTIVE: A novel class of hybrids having coumate and benzimidazolone scaffolds were designed to mimic BRCA1 protein, supressing the tumor activity of breast cancer cell.	benzimidazolone	55-70	BRCA1 DNA repair associated	Homo sapiens	104-109
7512555-5	1994	This work presents the properties of NS004, a substituted benzimidazolone, which is the first activator of normal and mutant CFTR-associated chloride channels to be described.	benzimidazolone	58-73	CF transmembrane conductance regulator	Homo sapiens	125-129
7984293-2	1994	Binding was inhibited by serotonin and by synthetic indoles, benzamides and benzimidazolones known to characterize the 5-HT4R in functional tests.	benzimidazolone	76-92	5-hydroxytryptamine receptor 4	Homo sapiens	119-125
32275432-0	2020	Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders.	benzimidazolone	77-92	B cell leukemia/lymphoma 6	Mus musculus	93-97
32275432-2	2020	Herein we report the discovery of a series of benzimidazolone inhibitors of the protein-protein interaction between BCL6 and its co-repressors.	benzimidazolone	46-61	B cell leukemia/lymphoma 6	Mus musculus	116-120
8944722-4	1996	In the present work, we evaluated the effects on Cl-secretion of other benzimidazolones, NS-004 and NS-1619, which have been shown to open cystic fibrosis transmembrane conductance regulator (CFTR) Cl- channels.	benzimidazolone	71-87	CF transmembrane conductance regulator	Homo sapiens	139-190
8944722-4	1996	In the present work, we evaluated the effects on Cl-secretion of other benzimidazolones, NS-004 and NS-1619, which have been shown to open cystic fibrosis transmembrane conductance regulator (CFTR) Cl- channels.	benzimidazolone	71-87	CF transmembrane conductance regulator	Homo sapiens	192-196
32588636-2	2020	In this work a new rearrangement of quinoxalinones with the participation of in situ generated 2-en-1-imine moiety of the substituent at C-3 makes it possible to construct two new heterocyclic systems, namely a benzimidazolone and a pyrrole, simultaneously under one-pot reaction conditions.	benzimidazolone	211-226	complement C3	Homo sapiens	137-140
30128074-4	2018	High-throughput screen lead 4 was optimized for potency and brain penetration to provide benzimidazolone 3, JNJ-55511118.1 Replacement of the benzimidazolone core in 3 with an oxindole mitigated reactive metabolite formation and led to the identification of 18 (GluA1/gamma-8 pIC50 = 9.7).	benzimidazolone	89-104	glutamate ionotropic receptor AMPA type subunit 1	Rattus norvegicus	262-267
30199635-5	2018	Herein we describe the synthesis and optimization of piperidine benzimidazolone MOR agonists that together display a wide range of bias (G/betaarr2).	benzimidazolone	64-79	opioid receptor, mu 1	Mus musculus	80-83
30199635-5	2018	Herein we describe the synthesis and optimization of piperidine benzimidazolone MOR agonists that together display a wide range of bias (G/betaarr2).	benzimidazolone	64-79	arrestin, beta 2	Mus musculus	139-147
27326325-2	2016	A selective benzimidazolone BRPF1 inhibitor showing micromolar activity in a cellular target engagement assay was recently described.	benzimidazolone	12-27	bromodomain and PHD finger containing 1	Homo sapiens	28-33
27061977-0	2016	Benzimidazolone bioisosteres of potent GluN2B selective NMDA receptor antagonists.	benzimidazolone	0-15	glutamate ionotropic receptor NMDA type subunit 2B	Homo sapiens	39-45
27061977-3	2016	Herein benzimidazolone bioisosteres of potent GluN2B antagonists 1-5 were designed and synthesized.	benzimidazolone	7-22	glutamate ionotropic receptor NMDA type subunit 2B	Homo sapiens	46-52
26476078-9	2015	Among the found hits, a benzimidazolone compound, CB-20903630, had low micromolar IC50 for growth inhibition of HCT116 cells and selectively induced senescence-associated beta-galactosidase activity in the entire treated cell population without cytotoxicity or apoptosis induction.	benzimidazolone	24-39	galactosidase beta 1	Homo sapiens	171-189
25974391-4	2016	Here we identified potent acetyl-lysine mimetic benzimidazolones TRIM24 bromodomain inhibitors.	benzimidazolone	48-64	tripartite motif containing 24	Homo sapiens	65-71
25590863-4	2015	In the present study, a series of novel pyrazole-benzimidazolone hybrids were designed, synthesized and evaluated as potent human HPPD inhibitors.	benzimidazolone	49-64	4-hydroxyphenylpyruvate dioxygenase	Homo sapiens	130-134
25590863-0	2015	Synthesis and bioevaluation of pyrazole-benzimidazolone hybrids as novel human 4-Hydroxyphenylpyruvate dioxygenase inhibitors.	benzimidazolone	40-55	4-hydroxyphenylpyruvate dioxygenase	Homo sapiens	79-114
22789708-4	2013	The finding of the benzimidazolone moiety as a tryptophan replacement in mdm2 is significant as it offers access to novel scaffolds with potentially higher selectivity and potency and improved biological activities.	benzimidazolone	19-34	MDM2 proto-oncogene	Homo sapiens	73-77
24909677-0	2014	Lead identification of benzimidazolone and azabenzimidazolone arylsulfonamides as CC-chemokine receptor 4 (CCR4) antagonists.	benzimidazolone	23-38	C-C motif chemokine receptor 4	Homo sapiens	82-105
24909677-0	2014	Lead identification of benzimidazolone and azabenzimidazolone arylsulfonamides as CC-chemokine receptor 4 (CCR4) antagonists.	benzimidazolone	23-38	C-C motif chemokine receptor 4	Homo sapiens	107-111
25466173-2	2014	Here, we found that addition of an alpha-methyl moiety within the PLD2-biased piperidinyl triazaspirone scaffold abolished PLD2 preference, while the incorporation of substituents onto the piperidine moiety of the PLD1-biased piperidinyl benzimidazolone, or replacement with a bioisosteric [3.3.0] core, generally retained PLD1 preference, but at diminished significance.	benzimidazolone	238-253	phospholipase D2	Homo sapiens	66-70
25466173-2	2014	Here, we found that addition of an alpha-methyl moiety within the PLD2-biased piperidinyl triazaspirone scaffold abolished PLD2 preference, while the incorporation of substituents onto the piperidine moiety of the PLD1-biased piperidinyl benzimidazolone, or replacement with a bioisosteric [3.3.0] core, generally retained PLD1 preference, but at diminished significance.	benzimidazolone	238-253	phospholipase D2	Homo sapiens	123-127
24050887-0	2013	Synthesis and SAR studies of benzimidazolone derivatives as histamine H3-receptor antagonists.	benzimidazolone	29-44	histamine receptor H3	Rattus norvegicus	60-81
24050887-1	2013	A novel series of benzimidazolone-containing histamine H3-receptor antagonists were prepared and their structure-activity relationship was explored.	benzimidazolone	18-33	histamine receptor H3	Rattus norvegicus	45-66
23083067-9	2013	Pretreating the apical membrane with amiloride, which inhibits ENaC, completely prevented the stimulating effects of benzimidazolones on I(SC).	benzimidazolone	117-133	sodium channel epithelial 1 subunit gamma	Rattus norvegicus	63-67
23352481-0	2013	Design, synthesis and structure-activity relationship of novel tricyclic benzimidazolone derivatives as potent 18 kDa translocator protein (TSPO) ligands.	benzimidazolone	73-88	translocator protein	Homo sapiens	118-138
23352481-0	2013	Design, synthesis and structure-activity relationship of novel tricyclic benzimidazolone derivatives as potent 18 kDa translocator protein (TSPO) ligands.	benzimidazolone	73-88	translocator protein	Homo sapiens	140-144
23083067-13	2013	The antagonist sensitivity of this effect suggests the benzimidazolones elicit this action by activating the highly selective ENaC currents.	benzimidazolone	55-71	sodium channel epithelial 1 subunit gamma	Rattus norvegicus	126-130
22070604-0	2011	Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor gamma (PPARgamma) modulators.	benzimidazolone	0-16	peroxisome proliferator activated receptor gamma	Homo sapiens	43-91
22070604-0	2011	Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor gamma (PPARgamma) modulators.	benzimidazolone	0-16	peroxisome proliferator activated receptor gamma	Homo sapiens	93-102
17010605-0	2006	Discovery and design of benzimidazolone based inhibitors of p38 MAP kinase.	benzimidazolone	24-39	mitogen-activated protein kinase 14	Homo sapiens	60-63
21733690-0	2011	Benzimidazolone as potent chymase inhibitor: modulation of reactive metabolite formation in the hydrophobic (P1) region.	benzimidazolone	0-15	chymase 1	Homo sapiens	26-33
21733690-1	2011	A new class of chymase inhibitor featuring a benzimidazolone core with an acid side chain and a P(1) hydrophobic moiety is described.	benzimidazolone	45-60	chymase 1	Homo sapiens	15-22
18947992-0	2008	Potent benzimidazolone-based CGRP receptor antagonists.	benzimidazolone	7-22	calcitonin related polypeptide alpha	Homo sapiens	29-33
18947992-1	2008	The previously disclosed spirohydantoin-based CGRP receptor antagonists were optimized for potency through modification of the benzimidazolone substituents.	benzimidazolone	127-142	calcitonin related polypeptide alpha	Homo sapiens	46-50
18440813-0	2008	The SAR studies of novel CB2 selective agonists, benzimidazolone derivatives.	benzimidazolone	49-64	cannabinoid receptor 2	Homo sapiens	25-28
18440813-1	2008	Benzimidazolone derivatives were discovered as novel CB2 selective agonists.	benzimidazolone	0-15	cannabinoid receptor 2	Homo sapiens	53-56
18155683-2	2008	In the first approach, di-N-glycosyl and mono-N-alkyl-N-glycosyl compounds were obtained by grafting C-6-activated glycosides onto benzimidazolone.	benzimidazolone	131-146	complement C6	Homo sapiens	101-104
19237285-0	2009	Benzimidazolone-based serotonin 5-HT1A or 5-HT7R ligands: synthesis and biological evaluation.	benzimidazolone	0-15	5-hydroxytryptamine receptor 1A	Homo sapiens	32-38
17010605-1	2006	A new class of benzimidazolone p38 MAP kinase inhibitors was discovered through high-throughput screening.	benzimidazolone	15-30	mitogen-activated protein kinase 14	Homo sapiens	31-34
16931005-0	2006	Potent benzimidazolone based human beta(3)-adrenergic receptor agonists.	benzimidazolone	7-22	adrenoceptor beta 3	Homo sapiens	35-62
16931005-1	2006	The synthesis and biological evaluation of a series of benzimidazolone beta(3) adrenergic receptor agonists are described.	benzimidazolone	55-70	adrenoceptor beta 3	Homo sapiens	71-98
12651632-0	2003	CFTR activation in human bronchial epithelial cells by novel benzoflavone and benzimidazolone compounds.	benzimidazolone	78-93	CF transmembrane conductance regulator	Homo sapiens	0-4
16134941-1	2005	Mimics of the benzimidazolone nucleus found in inhibitors of p38 kinase are proposed, and their theoretical potential as bioisosteres is described.	benzimidazolone	14-29	mitogen-activated protein kinase 14	Homo sapiens	61-64
15978807-3	2005	These findings prompted us to examine if there is a similar effect of the 6-aryl moieties on the PR functional activity for the benzimidazolone template.	benzimidazolone	128-143	progesterone receptor	Homo sapiens	97-99
15978807-5	2005	More interestingly, pyrrole-containing benzimidazolones 24-27 remained as PR antagonists in contrast to the PR agonist activity switch for oxindole and benzoxazinone scaffolds when a 5"-cyanopyrrol-2"-yl group was installed as a pendant aryl group.	benzimidazolone	39-55	progesterone receptor	Homo sapiens	74-76
15012994-0	2004	Benzimidazolone p38 inhibitors.	benzimidazolone	0-15	mitogen-activated protein kinase 14	Homo sapiens	16-19
15012994-1	2004	The synthesis and in vitro p38 alpha activity of a novel series of benzimidazolone inhibitors is described.	benzimidazolone	67-82	mitogen-activated protein kinase 14	Homo sapiens	27-36
15012994-2	2004	The p38 alpha SAR is consistent with a mode of binding wherein the benzimidazolone carbonyl serves as the H-bond acceptor to Met109 of p38 alpha in a manner analogous to the pyridine nitrogen of prototypical pyridylimidazole p38 inhibitors.	benzimidazolone	67-82	mitogen-activated protein kinase 14	Homo sapiens	4-13
15012994-2	2004	The p38 alpha SAR is consistent with a mode of binding wherein the benzimidazolone carbonyl serves as the H-bond acceptor to Met109 of p38 alpha in a manner analogous to the pyridine nitrogen of prototypical pyridylimidazole p38 inhibitors.	benzimidazolone	67-82	sarcosine dehydrogenase	Homo sapiens	14-17
15012994-2	2004	The p38 alpha SAR is consistent with a mode of binding wherein the benzimidazolone carbonyl serves as the H-bond acceptor to Met109 of p38 alpha in a manner analogous to the pyridine nitrogen of prototypical pyridylimidazole p38 inhibitors.	benzimidazolone	67-82	mitogen-activated protein kinase 14	Homo sapiens	135-144
15012994-2	2004	The p38 alpha SAR is consistent with a mode of binding wherein the benzimidazolone carbonyl serves as the H-bond acceptor to Met109 of p38 alpha in a manner analogous to the pyridine nitrogen of prototypical pyridylimidazole p38 inhibitors.	benzimidazolone	67-82	mitogen-activated protein kinase 14	Homo sapiens	4-7
12651632-2	2003	Short-circuit current (Isc) measurements were done on human bronchial epithelial cells to characterize the best flavone and benzimidazolone CFTR activators identified by lead-based combinatorial synthesis and high-throughput screening.	benzimidazolone	124-139	CF transmembrane conductance regulator	Homo sapiens	140-144
14502435-0	2003	Comparative pharmacology of the activity of wild-type and G551D mutated CFTR chloride channel: effect of the benzimidazolone derivative NS004.	benzimidazolone	109-124	cystic fibrosis transmembrane conductance regulator	Cricetulus griseus	72-76
14502435-1	2003	The pharmacological activation of the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel mutated at glycine 551 (G551D-CFTR) was studied in the presence of the benzimidazolone derivative NS004 and compared to that of wild-type (wt) CFTR.	benzimidazolone	185-200	cystic fibrosis transmembrane conductance regulator	Cricetulus griseus	38-89
14502435-1	2003	The pharmacological activation of the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel mutated at glycine 551 (G551D-CFTR) was studied in the presence of the benzimidazolone derivative NS004 and compared to that of wild-type (wt) CFTR.	benzimidazolone	185-200	cystic fibrosis transmembrane conductance regulator	Cricetulus griseus	91-95