L 755507: a benzenesulfonamide derivative; structure in first source
ID Source | ID |
---|---|
PubMed CID | 9829836 |
CHEMBL ID | 12998 |
SCHEMBL ID | 5165122 |
MeSH ID | M0291242 |
Synonym |
---|
NCGC00092331-01 |
cid 9829836 |
CHEMBL12998 , |
l-755507 |
4-(3-hexyl-ureido)-n-(4-{2-[(s)-2-hydroxy-3-(4-hydroxy-phenoxy)-propylamino]-ethyl}-phenyl)-benzenesulfonamide |
4-(3-hexyl-ureido)-n-(4-{2-[2-hydroxy-3-(4-hydroxy-phenoxy)-propylamino]-ethyl}-phenyl)-benzenesulfonamide |
bdbm50070156 |
(s)-4-(3-hexylureido)-n-(4-(2-(1-hydroxy-2-(4-hydroxyphenoxy)ethylamino)ethyl)phenyl)benzenesulfonamide |
(s)-4-(3-hexylureido)-n-(4-(2-(2-hydroxy-3-(4-hydroxyphenoxy)propylamino)ethyl)phenyl)benzenesulfonamide |
4-[[(hexylamino)carbonyl]amino]-n-[4-[2-[[(2s)-2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]phenyl]-benzenesulfonamide |
S7974 |
l755507 |
gtpl3931 |
l-755,507 |
l 755507 |
1-hexyl-3-[4-[[4-[2-[[(2s)-2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]phenyl]sulfamoyl]phenyl]urea |
SCHEMBL5165122 |
159182-43-1 |
CS-7782 |
AC-32762 |
AKOS024456983 |
3-hexyl-1-(4-{[4-(2-{[(2s)-2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino}ethyl)phenyl]sulfamoyl}phenyl)urea |
l755507, >=98% (hplc) |
J-009574 |
HY-19334 |
EX-A2397 |
HMS3677M07 |
CP-0074 |
Q27078423 |
HMS3413M07 |
HMS3886B21 |
CCG-270146 |
N13286 |
a selective beta3-adrenergic receptor partial agonist |
DTXSID901104874 |
4-[[(hexylamino)carbonyl]amino]-n-[4-[2-[[(2s)-2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]phenyl]benzenesulfonamide |
benzenesulfonamide, 4-[[(hexylamino)carbonyl]amino]-n-[4-[2-[[(2s)-2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]phenyl]- |
benzenesulfonamide, 4-[[(hexylamino)carbonyl]amino]-n-[4-[2-[[2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]phenyl]-, (s)- |
H3HB4MCV7G |
Excerpt | Reference | Relevance |
---|---|---|
" Oral bioavailability in dogs, 41% for L-749,372 and 47% for L-750,355, is improved relative to phenol analogs." | ( 3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties. Alvaro, RF; Candelore, MR; Cascieri, MA; Chiu, SH; Deng, L; Fisher, MH; Forrest, MJ; Hom, GJ; Hutchins, JE; Kao, J; MacIntyre, DE; Mathvink, RJ; McLoughlin, D; Miller, RR; Newbold, RC; Ok, HO; Olah, TV; Parmee, ER; Perkins, L; Stearns, RA; Strader, CD; Szumiloski, J; Tang, YS; Tota, L; Weber, AE, 1998) | 0.3 |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 22.3872 | 0.0040 | 23.8416 | 100.0000 | AID485290 |
Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 8.9125 | 0.1778 | 14.3909 | 39.8107 | AID2147 |
15-lipoxygenase, partial | Homo sapiens (human) | Potency | 7.9433 | 0.0126 | 10.6917 | 88.5700 | AID887 |
phosphopantetheinyl transferase | Bacillus subtilis | Potency | 25.1189 | 0.1413 | 37.9142 | 100.0000 | AID1490 |
Microtubule-associated protein tau | Homo sapiens (human) | Potency | 28.7968 | 0.1800 | 13.5574 | 39.8107 | AID1460; AID1468 |
thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 19.9526 | 0.0013 | 18.0743 | 39.8107 | AID926 |
glucocerebrosidase | Homo sapiens (human) | Potency | 7.9433 | 0.0126 | 8.1569 | 44.6684 | AID2101 |
Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 39.8107 | 0.5406 | 17.6392 | 96.1227 | AID2528 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 24.8033 | 0.0079 | 8.2332 | 1,122.0200 | AID2546; AID2551 |
cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 7.9433 | 0.0316 | 10.2792 | 39.8107 | AID884; AID885 |
lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 31.6228 | 0.0200 | 10.7869 | 31.6228 | AID912 |
Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 3.1623 | 0.3162 | 12.7657 | 31.6228 | AID881 |
Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 3.1623 | 0.0063 | 8.2350 | 39.8107 | AID881 |
Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1.0000 | 12.2248 | 31.6228 | AID885 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Beta-2 adrenergic receptor | Homo sapiens (human) | IC50 (µMol) | 1.5950 | 0.0002 | 0.9326 | 7.2000 | AID41178; AID41183 |
Beta-2 adrenergic receptor | Homo sapiens (human) | Ki | 0.1600 | 0.0000 | 0.6635 | 9.5499 | AID220780 |
Beta-1 adrenergic receptor | Homo sapiens (human) | IC50 (µMol) | 0.2000 | 0.0002 | 1.4681 | 9.0000 | AID40245 |
Beta-1 adrenergic receptor | Homo sapiens (human) | Ki | 0.5700 | 0.0001 | 1.3391 | 9.9840 | AID220776 |
Cruzipain | Trypanosoma cruzi | IC50 (µMol) | 36.0000 | 0.0002 | 2.0450 | 8.0000 | AID444614; AID444615 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Beta-2 adrenergic receptor | Homo sapiens (human) | EC50 (µMol) | 0.0200 | 0.0000 | 0.3111 | 10.0000 | AID220777 |
Gamma-aminobutyric acid receptor subunit alpha-1 | Bos taurus (cattle) | EC50 (µMol) | 0.0004 | 0.0004 | 0.2252 | 0.4500 | AID41667 |
Gamma-aminobutyric acid receptor subunit beta-1 | Bos taurus (cattle) | EC50 (µMol) | 0.0004 | 0.0004 | 0.2252 | 0.4500 | AID41667 |
Beta-1 adrenergic receptor | Homo sapiens (human) | EC50 (µMol) | 0.3300 | 0.0001 | 0.4914 | 6.0000 | AID220771 |
Gamma-aminobutyric acid receptor subunit alpha-2 | Bos taurus (cattle) | EC50 (µMol) | 0.0004 | 0.0004 | 0.2252 | 0.4500 | AID41667 |
Gamma-aminobutyric acid receptor subunit alpha-3 | Bos taurus (cattle) | EC50 (µMol) | 0.0004 | 0.0004 | 0.2252 | 0.4500 | AID41667 |
Beta-3 adrenergic receptor | Homo sapiens (human) | EC50 (µMol) | 0.0005 | 0.0001 | 0.4553 | 10.0000 | AID220781; AID41664; AID41667; AID41669; AID41779 |
Gamma-aminobutyric acid receptor subunit alpha-4 | Bos taurus (cattle) | EC50 (µMol) | 0.0004 | 0.0004 | 0.2252 | 0.4500 | AID41667 |
Gamma-aminobutyric acid receptor subunit gamma-2 | Bos taurus (cattle) | EC50 (µMol) | 0.0004 | 0.0004 | 0.2252 | 0.4500 | AID41667 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID444614 | Inhibition of Trypanosoma cruzi cruzain by quantitative high throughput screening | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1 | Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease. |
AID41664 | Binding affinity towards human Beta-3 adrenergic receptor | 1999 | Journal of medicinal chemistry, Jan-28, Volume: 42, Issue:2 | Pharmacological treatment of obesity: therapeutic strategies. |
AID220777 | Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors | 2001 | Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9 | (4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists. |
AID220776 | Inhibition of I-iodocyanopindolol binding to human beta 1 adrenergic receptors | 2001 | Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9 | (4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists. |
AID416746 | Inhibition of Escherichia coli AmpC assessed as induction of protein unfolding measured by trypsin mediated degradation of compound-AmpC enzyme complex at 100 uM after 4 hrs by gel electrophoresis | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Promiscuous aggregate-based inhibitors promote enzyme unfolding. |
AID220784 | Compound was tested for increased thermogenesis using beta-3 human transgenic mice | 2001 | Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9 | (4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists. |
AID41669 | Evaluated for its agonist activity against human Beta-3 adrenergic receptor | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16 | 3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties. |
AID220780 | Inhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptors | 2001 | Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9 | (4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists. |
AID13468 | Compound was evaluated for absorption of radioligand following oral administration to bile duct cannulated rat. | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16 | 3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties. |
AID41646 | Agonist activity towards human Beta-3 adrenergic receptor by adenylyl cyclase activation given as % of the maximal stimulation with isoproterenol | 1998 | Bioorganic & medicinal chemistry letters, May-05, Volume: 8, Issue:9 | Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist. |
AID444615 | Inhibition of Trypanosoma cruzi cruzain by Flexstation microplate spectrofluorimetry | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1 | Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease. |
AID444613 | Inhibition of Beta-lactamase AmpC by quantitative high throughput screening | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1 | Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease. |
AID41183 | In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol. | 1998 | Bioorganic & medicinal chemistry letters, May-05, Volume: 8, Issue:9 | Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist. |
AID41178 | Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol | 1998 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 8, Issue:21 | 3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists. |
AID220781 | In vitro increase in cAMP levels in Chinese hamster ovary cells expressing the human cloned beta 3 Adrenergic receptor. | 2001 | Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9 | (4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists. |
AID41667 | Agonism against Beta-3 adrenergic receptor | 1998 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 8, Issue:21 | 3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists. |
AID220771 | In vitro activity to increase cAMP levels in Chinese hamster ovary (CHO) cells expressing the cloned human beta 1 Adrenergic receptor | 2001 | Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9 | (4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists. |
AID41648 | Agonism of human beta-3 adrenergic receptor | 1998 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 8, Issue:21 | 3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists. |
AID40245 | In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol. | 1998 | Bioorganic & medicinal chemistry letters, May-05, Volume: 8, Issue:9 | Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist. |
AID41779 | Agonist activity towards human Beta-3 adrenergic receptor | 1998 | Bioorganic & medicinal chemistry letters, May-05, Volume: 8, Issue:9 | Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist. |
AID20859 | Oral bioavailability of the compound. | 1999 | Journal of medicinal chemistry, Jan-28, Volume: 42, Issue:2 | Pharmacological treatment of obesity: therapeutic strategies. |
AID9534 | Oral bioavailability in dog | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16 | 3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties. |
AID1346297 | Human beta3-adrenoceptor (Adrenoceptors) | 2010 | British journal of pharmacology, Jul, Volume: 160, Issue:5 | The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 7 (43.75) | 18.2507 |
2000's | 5 (31.25) | 29.6817 |
2010's | 4 (25.00) | 24.3611 |
2020's | 0 (0.00) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (16.62) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 0 (0.00%) | 5.53% |
Reviews | 1 (6.25%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 15 (93.75%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |