Target (1)
Compound (21)
Article Title (4)
Assay (8)
Hanessian, S; Sgarbi, PW Design and synthesis of mimics of S-adenosyl-L-homocysteine as potential inhibitors of erythromycin methyltransferases. Bioorg Med Chem Lett 10: 433 -7 (2000) Clark, MJ; Wright, T; Bertrand, PP; Bornstein, JC; Jenkinson, KM; Verlinden, M; Furness, JB Erythromycin derivatives ABT 229 and GM 611 act on motilin receptors in the rabbit duodenum. Clin Exp Pharmacol Physiol 26: 242 -5 (1999) Randolph, JT; Sauer, DR; Haviv, F; Nilius, AM; Greer, J Elimination of antibacterial activities of non-peptide luteinizing hormone-releasing hormone (LHRH) antagonists derived from erythromycin A. Bioorg Med Chem Lett 14: 1599 -602 (2004) Randolph, JT; Waid, P; Nichols, C; Sauer, D; Haviv, F; Diaz, G; Bammert, G; Besecke, LM; Segreti, JA; Mohning, KM; Bush, EN; Wegner, CD; Greer, J Nonpeptide luteinizing hormone-releasing hormone antagonists derived from erythromycin A: design, synthesis, and biological activity of cladinose replacement analogues. J Med Chem 47: 1085 -97 (2004)
ChEMBL_738360 (CHEMBL1743437) Mechanism based inhibition of human cytochrome P450 3A4 measured by N-demethylation of erythromycin ChEMBL_738390 (CHEMBL1743467) Mechanism based inhibition of human cytochrome P450 3A4 measured by testosterone 6-beta hydroxylation and erythromycin N-demethylation ChEMBL_738355 (CHEMBL1743432) Mechanism based inhibition of human cytochrome P450 3A4 measured by (14C)formaldehyde production from (N-methyl-14C)-erythromycin ChEMBL_738356 (CHEMBL1743433) Mechanism based inhibition of human cytochrome P450 3A4 measured by (14C)formaldehyde production from (N-methyl-14C)-erythromycin ChEMBL_1884204 (CHEMBL4385786) Inhibition of CYP3A4 in human liver microsomes using [14C]-erythromycin as substrate preincubated for 2 mins in presence of NADPH followed by substrate addition and measured after 5 mins by liquid scintillation counting method Biological Assay Example 6 The assay was based on a method published by Moody et al. (Xenobiotica 1999). The inhibition of cytochrome P450 3A4-isoenzyme catalysed N-demethylation of [N-methyl-14C]-Erythromycin by the test compound was assayed at 37° C with human recombinant cytochrome P450 3A4. Biological Assay Example 6 The assay was based on a method published by Moody et al. (Xenobiotica 1999). The inhibition of cytochrome P450 3A4-isoenzyme catalysed N-demethylation of [N-methyl-14C]-Erythromycin by the test compound was assayed at 37° C with human recombinant cytochrome P450 3A4. Surface Plasmon Resonance (SPR) (1) Screening of Macrolide and Cyclic Peptide Drugs by Taking SelH as a TargetA surface plasmon resonance (SPR) method was adopted to detect the interaction condition of a small molecule and a protein, so that the screening of drugs targeting SelH was carried out.1. Protein ImmobilizationPurified SelH was diluted into a 50 μg/mL protein solution by using 10 mM sodium acetate with a pH value of 5.5, the purified SelH was fixed onto a CM5 chip by an amino coupling method by using Biacore 8K (GE Healthcard, Sweden), and an RU value was recorded.2. Sample PreparationThe macrolide compound or cyclic peptide compound (the compounds specifically include carrimycin, isovalerylspiramycin I, spiramycin, carbomycin, azithromycin, erythromycin and thiostrepton) was dissolved in 100% DMSO to be prepared into solutions containing 5% DMSO of different concentrations (0, 31.25, 62.5, 125, 250 and 500 μM) by using a 1.05×PBS-P+ buffer solution (GE Healthcare, obtained by diluting 10×PBS-P+).3. Binding ExperimentA single-cycle kinetics method was adopted, the 1.05×PBS-P+ buffer solution containing 5% DMSO was used as a Running Buffer, different compounds of different concentrations flowed through the SelH fixed onto the chip, wherein the binding time was 120 s, and the change condition of the RU value was recorded. An equilibrium dissociation constant (KD) was calculated by using software in Biacore 8K so as to evaluate the binding affinity between the protein and the compounds.
MLS001074901 SMR000058868 BDBM96262 ERYTHROMYCIN ETHYLSUCCINATE cid_443953
Erythromycin A E-MYCIN E Erythromycin C Erycette Erymax T-Stat ERYTHROMYCIN ETHYLSUCCINATE ERYTHROMYCIN BDBM50344942 US20240118263, Compound Erythromycin CHEMBL532 Ilotycin
Erythromycin Estolate Erythromycin Propionate Lauryl Sulfate CHEBI:4846 BDBM50237591 Ilosone Erythromycin Lauryl Sulfate, Propionyl Propionyl Erythromycin Lauryl Sulfate
Erythromycin Estolate Erythromycin Propionate Lauryl Sulfate CHEBI:4846 Ilosone Erythromycin Lauryl Sulfate, Propionyl Propionyl Erythromycin Lauryl Sulfate BDBM50103515
BDBM181125 US9138393, Erythromycin
BDBM181792 US9144538, Erythromycin
Erythromycin Estolate BDBM31688
Erythromycin-B BDBM85998
ERYTHROMYCIN ESTOLATE BDBM50442912 Ilosone
Erythromycin A 6,9-enolether BDBM85846 CAS_33396-29-1 ME523 Erythromycin-A enol ether EM523
BDBM86686 Erythromycin A Enol Ether ME4
Erythromycin-B enol ether BDBM85993
BDBM86313 CAS_114-07-8 erythromycin-A NSC_12560
N-ethyl, N-Methyl Erythromycin-A BDBM85988
N-ethyl, N-methyl Erythromycin-A enol ether BDBM85989
3-Descladinosyl-11,12-dideoxy-6-O-methyl-3-oxo-12,11-(oxycarbonyl-(1-(([1,8]naphthyridin-4-yl)methyl)azetidin-3-yl)imino)-erythromycin A BDBM50299105 CHEMBL583091
3-Descladinosyl-11,12-dideoxy-6-Omethyl-3-oxo-12,11-(oxycarbonyl-(1-(1R-([1,8]naphthyridin-4-yl)-ethyl)azetidin-3-yl)imino)erythromycin A BDBM50299106 CHEMBL583093
BDBM50299104 3-Descladinosyl-11,12-dideoxy-6-O-methyl-3-oxo-12,11-(oxycarbonyl-(1-(([1,5]naphthyridin-4-yl)methyl)azetidin-3-yl)imino)-erythromycin A CHEMBL583090
3-Descladinosyl-11,12-dideoxy-6-O-methyl-3-oxo-12,11-(oxycarbonyl-(1-((3-hydroxy[1,8]naphthyridin-4-yl)methyl)azetidin-3-yl)imino)erythromycin A BDBM50299107 CHEMBL583298
BDBM50299108 3-Descladinosyl-11,12-dideoxy-6-O-methyl-3-oxo-12,11-(oxycarbonyl-(1-((3-hydroxy[1,5]naphthyridin-4-yl)methyl)azetidin-3-yl)imino)erythromycin A CHEMBL583299
BDBM50127141 Eryhtromycin A (3R,4S,5S,6R,7R,9R,11R,12R,13S,14R)-6-{[(2R,3S,4R,6S)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy}-14-ethyl-7,12,13-trihydroxy-4-{[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy}-3,5,7,9,11,13-hexamethyl-1-oxacyclotetradecane-2,10-dione erythromycin 11-(4-dimethylamino-3-hydroxy-6-methyltetrahydro-2H-2-pyranyloxy)-3-ethyl-4,5,10-trihydroxy-13-(5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-2-pyranyloxy)-4,6,8,10,12,14-hexamethyl-2-oxacyclotetradecane-1,7-dione erythromycin-A CHEMBL532