erythromycin [Ligand Id: 1456] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL532 (Akne-mycin, Aknemycin plus, A/t/s, Benzamycin, Bristamycin, C-solve-2, E-base, E-Base, E-glades, E-Glades, Emgel, E-mycin, E-Mycin, Eritromicina, Eryacne 2, Eryacne 4, Eryc, Eryc 125, Erycette, Eryc sprinkles, Eryderm, Erygel, Erymax, Erymax sprinkle, Erypar, Ery-tab, ERY-TAB, Erythra-derm, Erythro 200, Erythrocin, Erythromycin, Erythromycine, Erythromycin estolate impurity, free erythromycin-, Erythro-statin, Erythro-Statin, E-solve 2, Gallimycin, Ilotycin, Isotrexin, J01FA01, Kerymax, NSC-55929, Oftalmolosa cusi eritromicina, Paediathrocin, PCE, Pfizer-E, Retcin, Robimycin, Rommix 250 ec, Rommix 500 ec, R-p mycin, Sansac, Staticin, Stiemycin, Tiloryth, T-stat, Wyamycin, Zineryt)
  • aldehyde oxidase 1/Aldehyde oxidase in Human [ChEMBL: CHEMBL3257] [GtoPdb: 3186] [UniProtKB: Q06278]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
aldehyde oxidase 1/Aldehyde oxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3257] [GtoPdb: 3186] [UniProtKB: Q06278]
ChEMBL Inhibition of aldehyde oxidase in human liver cytosolic fraction using methyl-nicotinamide substrate incubated for 120 mins by HPLC analysis B 4.01 pIC50 96900 nM IC50 WO-2018198842-A1. Therapeutic agent for nonalcoholic fatty liver disease (2018)
CYP1B1/Cytochrome P450 1B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4878] [GtoPdb: 1320] [UniProtKB: Q16678]
ChEMBL Inhibition of CYP1B1 (unknown origin) expressed in Escherichia coli DH5alpha coexpressing human NADPH-P450 reductase using 7-Ethoxyresorufin as substrate up to 6 mins in presence of NADP+ by spectrofluorometric analysis B 4.4 pIC50 40000 nM IC50 Eur J Med Chem (2017) 135: 296-306 [PMID:28458135]
GroEL/GroES in Escherichia coli (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106139] [UniProtKB: Q548M1, Q7BGE6]
ChEMBL Inhibition of Escherichia coli GroEL expressed in Escherichia coliDH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured soluble pig heart MDH refolding by measuring MDH enzyme activity using sodium mesoxalate as substrate after 20 to 40 mins by malachite green dye based spectrometric analysis B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (2019) 29: 1106-1112 [PMID:30852084]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibitory concentration against IKr potassium channel B 4.41 pIC50 39000 nM IC50 Bioorg Med Chem Lett (2004) 14: 4771-4777 [PMID:15324906]
ChEMBL Inhibition of human ERG expressed in HEK cells B 7.41 pIC50 39 nM IC50 J Med Chem (2009) 52: 6851-6859 [PMID:19821563]
HSP60/HSP10 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106131] [UniProtKB: P10809, P61604]
ChEMBL Inhibition of human N-terminal octa-His-tagged HSP60 expressed in Escherichia coli Rosetta(DE3) pLysS/human HSP10 expressed in Escherichia coli Rosetta(DE3) assessed as reduction in HSP60/HSP10-mediated denatured MDH refolding by measuring MDH enzyme activity using sodium mesoxalate as substrate after 40 to 60 mins by malachite green dye based spectrometric analysis B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (2019) 29: 1106-1112 [PMID:30852084]
motilin receptor/Motilin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2203] [GtoPdb: 297] [UniProtKB: O43193]
ChEMBL In vitro binding affinity towards human motilin receptor B 4.43 pKi 37000 nM Ki J Med Chem (2004) 47: 1704-1708 [PMID:15027861]
GtoPdb - - 6.5 pIC50 - - - Science (1999) 284: 2184-8 [PMID:10381885];
J Pharmacol Exp Ther (2005) 313: 1397-405 [PMID:15764739]
ChEMBL Compound was tested for in vitro motilin receptor binding affinity after treatment with hydrochloric acid solution (pH 2.5) B 7.15 pIC50 70.79 nM IC50 Bioorg Med Chem Lett (1995) 5: 835-838
ChEMBL Compound was tested for in vitro motilin receptor binding affinity B 7.36 pIC50 43.65 nM IC50 Bioorg Med Chem Lett (1995) 5: 835-838
ChEMBL Agonist activity at motilin receptor F 6 pEC50 1000 nM EC50 Bioorg Med Chem (2010) 18: 7651-7658 [PMID:20869254]
ChEMBL Agonist activity at motilin receptor F 6 pEC50 1000 nM EC50 Bioorg Med Chem Lett (2011) 21: 3712-3714 [PMID:21570844]
ChEMBL Agonist activity at human recombinant motilin receptor expressed in HEK293 cells by FLIPR assay F 6.2 pEC50 630.96 nM EC50 Bioorg Med Chem Lett (2008) 18: 6429-6436 [PMID:19006669]
ChEMBL In vitro effective concentration towards human motilin receptor F 6.4 pEC50 400 nM EC50 J Med Chem (2004) 47: 1704-1708 [PMID:15027861]
ChEMBL Agonist activity at human recombinant motilin receptor expressed in CHO cells assessed as increase in intracellular calcium by FLIPR assay F 7.3 pEC50 50.12 nM EC50 J Med Chem (2009) 52: 1180-1189 [PMID:19191554]
ChEMBL Agonist activity at human recombinant motilin receptor expressed in CHO cells by FLIPR assay F 7.3 pEC50 50.12 nM EC50 Bioorg Med Chem Lett (2008) 18: 6429-6436 [PMID:19006669]
Motilin receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5306] [UniProtKB: A5A4K8]
ChEMBL Agonist activity at motilin receptor in rabbit smooth muscle assessed as maximal possible tissue contraction F 5.92 pEC50 1200 nM EC50 J Med Chem (2009) 52: 6851-6859 [PMID:19821563]
ChEMBL Agonist activity at motilin receptor in rabbit smooth muscle assessed as increase of muscle contraction F 5.92 pEC50 1200 nM EC50 Bioorg Med Chem Lett (2010) 20: 5658-5661 [PMID:20801039]
ChEMBL Agonist activity at motilin receptor in rabbit smooth muscle assessed as maximal possible tissue contraction F 5.92 pEC50 1200 nM EC50 Bioorg Med Chem Lett (2011) 21: 3712-3714 [PMID:21570844]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: increase in Vinblastine intracellular accumulation in MDR1-expressing LLC-PK1 cells F 4.42 pKi 37790 nM Ki Mol Pharmacol (2002) 61: 964-973 [PMID:11961113]
ChEMBL Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.3 pIC50 >50000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells F 4.3 pIC50 >50000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCEC F 4.37 pIC50 43000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
P-glycoprotein 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3467] [UniProtKB: P06795]
ChEMBL Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.46 pIC50 >35000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells F 4.46 pIC50 >35000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ABCB1/P-glycoprotein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447]
ChEMBL Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.3 pIC50 >50000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells F 4.37 pIC50 43000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimalarial activity against Plasmodium falciparum FCR 3TC after 48 hrs F 4.17 pIC50 68000 nM IC50 J Med Chem (2016) 59: 5587-5603 [PMID:26791529]
ChEMBL Antimalarial activity after 96 hrs against azithromycin-resistant Plasmodium falciparum 7G8 by [3H]hypoxanthine uptake F 4.4 pIC50 39500 nM IC50 J Biol Chem (2007) 282: 2494-2504 [PMID:17110371]
ChEMBL Antimalarial activity after 96hrs against Plasmodium falciparum 7G8 by [3H]hypoxanthine uptake F 4.46 pIC50 34700 nM IC50 J Biol Chem (2007) 282: 2494-2504 [PMID:17110371]
ChEMBL Antimalarial activity after 96 hrs against azithromycin-resistant Plasmodium falciparum Dd2 by [3H]hypoxanthine uptake F 4.69 pIC50 20300 nM IC50 J Biol Chem (2007) 282: 2494-2504 [PMID:17110371]
ChEMBL Antimicrobial activity against Plasmodium falciparum F 4.74 pIC50 18000 nM IC50 Bioorg Med Chem (2010) 18: 2225-2231 [PMID:20185316]
ChEMBL Antimalarial activity after 96 hrs against Plasmodium falciparum Dd2 by [3H]hypoxanthine uptake F 5.03 pIC50 9400 nM IC50 J Biol Chem (2007) 282: 2494-2504 [PMID:17110371]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]